ROSE K V S , JOSEPH A
043587 ROSE K V S , JOSEPH A (Marine Biology Dep, Cochin Univ of Science and Technology, Cochin, Kerala) : Effects of an organophosphate insecticide, chlorpyrifos on the survival of Macrobrachium rosenbergii at various life stages. Int J Ecol Environ Sci 2020, 2(4), 67-76.
The present study investigated the acute toxicity of an organophosphate insecticide, chlorpyrifos used in the paddy fields of Kuttanad, a part of the Vembanad wetland system which is a Ramsar site of international importance in the state of Kerala, India, to various life stages of Macrobrachium rosenbergii, a commercially important and indigenous prawn of Kuttanad. LC50 values were determined using the observations made on the mortality of prawns exposed to 5 different concentrations between the No Observable Effect Concentration (NOEC) and Lowest Observable Effect Concentration (LOEC) of chlorpyrifos. The LC50 values for 24, 48, 72 and 96 h was determined by probit analysis using SPSS, based on which safe concentrations were calculated using Hart’s formula. The study revealed the 96 h LC50 concentrations as 0.00041, 0.022 and 0.038 ppm and safe concentrations as 0.0001, 0.004 and 0.008 ppm for post-larvae, juvenile and adult, respectively of M. rosenbergii. The results revealed that the application of chlorpyrifos in the paddy fields of Kuttanad poses a threat to the existence of the species in its homeland, as the field application concentration (0.0025 ppm) of chlorpyrifos is higher than the safe concentration determined for post-larvae.
4 illus, 1 table, 80 ref
ALKHARSANN N H, AL-KAABI S J
046685 ALKHARSANN N H, AL-KAABI S J (Biology Dep, Kufa Univ, Najaf, Iraq, Email: noorh.alkhrsain@gmail.com) : Evaluation of the level of CXCL10 in patients with parainfluenza virus type III (HPIV3). Med Legal Update 2020, 20(1), 10.37506/v20/i1/2020/mlu/194362.
Acute respiratory illness could be caused by Human parainfluenza viruses (PIVs) in children, the old, and immunocompromised patients. The frequent and common cause of pneumonia and bronchiolitis is PIV3, whilst the upper respiratory tract illness and croup are frequently caused by PIV1 and PIV2. However, this study aimed to highlight a group of patients with type III influenza virus. 29 sample took from people suffering from upper and lower respiratory diseases as well as 27 conrol sample to assessing the level of a type of cellular motility in their catheter, cimclin cxcl10 by the use of ELISA. The study also showed that there were no significant differences between Male Injury Rate Now as well as an inverse relationship between the level of cimokin cxcl10 and age. Moreovere, this study showed an increase in the level of cimcin cxcl10 in the case of HPIV infection compared with the control group.
4 illus, 2 tables, 22 ref
MOSHFEGHI H, HAGHGOO R, SADEGHI R, NIAKAN M, REZVANI M B
041733 MOSHFEGHI H, HAGHGOO R, SADEGHI R, NIAKAN M, REZVANI M B (Periodontics Dep, Shahed Univ, Tehran, 1417755351, Iran, Email: sadeghi@shahed.ac.ir) : Antibacterial activity of a glass ionomer containing silver nanoparticles against Streptococcus mutans and Streptococcus sanguinis. Indian J Dent Res 2020, 31(4), 589-92.
Nano‑sized metal particles exhibit special biological, chemical, and physical properties. The aim of this study was to evaluate the effect of incorporating silver nanoparticles into a resin‑modified glass ionomer (GI) on its antimicrobial property. Antibacterial action of GI samples containing 0, 40, 80 ppm silver nanoparticles against standard strains of Streptococcus sanguinis and Streptococcus mutans were assessed by agar diffusion and direct contact tests. Data were analyzed using analysis of variance and Duncan test (P < 0.05). Agar diffusion test showed no bacterial inhibition zone, but direct contact test exhibited significant antimicrobial activity against S. sanguinis and S. mutans in resin containing 80 ppm of nanosilver. Incorporation of a certain amount of silver nanoparticles into GI can increase its antimicrobial activity compared to the original material.
1 illus, 22 ref
SHANMUGARAJ G B, RAO A K
041715 SHANMUGARAJ G B, RAO A K (Microbiology Dep, Meenakshi Ammal Dental Coll, Chennai - 600 095, Tamil Nadu, Email: arthikrao82@gmail.com) : A study to assess the microbial profile and index of microbial air contamination in dental operatories. Indian J Dent Res 2020, 31(3), 465-9.
Microbial contamination of air in dental operatory is an important source of infection. In this study, passive air sampling using settle plates was used as an effective method to assess the microbial profile and index of microbial air contamination (IMA) in dental operatories. To assess the microbial profile and index of microbial air contamination (IMA) in dental operatories. This study design was a experimental cum diagnosis study and was conducted in four outpatient dental operatories in a self‑financing dental college using stratified random sampling technique. Twenty air samples were collected by leaving blood agar plates open for 1 h, 1 m above the floor and 1 m from the wall. After incubation at 37°C for 48 h, colonies were counted to assess the number of colony‑forming units (CFUs) per plate. The number of CFU is the IMA. The evaluation of aerobic bacterial and fungal profiles of representative colonies was done by standard microbiological methods. Independent sample ‘t’ test was applied for this study. All air samples collected near the dental treatment unit showed more contamination than the ambient air. As per the IMA classes, the IMA near the dental treatment unit ranged from fair to poor. IMA of ambient air in all the four operatories was within the acceptable values. The most common microorganism isolated was Staphylococcus species. Passive air sampling is one of the effective ways of quantifying airborne bacteria as used in the present study. Air microbial level evaluation is a step towards cross‑infection prevention.
3 illus, 4 tables, 15 ref
ANNADURAI B , KENNEDY Z J , UTHANDI S
043517 ANNADURAI B , KENNEDY Z J , UTHANDI S (Agricultural Microbiology Dep, Tamil Nadu Agricultural Univ, Coimbatore, Tamil Nadu) : Drought tolerant Rhizobium sp. VRE1 induced osmotic stress tolerance, seed germination and seedling vigor in blackgram (Vigna mungo L.). Int J Ecol Environ Sci 2020, 2(3), 37-42.
In the present study, we evaluated the mechanism of osmotic stress-resilient nodule endophytic Rhizobium sp. VRE1 grown in simulated osmotic stress conditions. The results showed that Rhizobium sp. VRE1 tolerated up to -0.73 MPa and produced a detectable amount of IAA (2.0µg mL-1 ). A significant increase in the concentration of total free amino acids, proline, and total soluble sugar content due to inoculation of Rhizobium sp. VRE1 was observed moisture stressed conditions. However, the protein content had reportedly higher under non - stress condition (19.04 mg g-1 dry weight) but decreased under stress condition due to inoculation of Rhizobium sp. VRE1 (7.20 mg g-1 DW). Blackgram seeds biotized with Rhizobium sp. VRE1 showed germination efficiency of 60 % and vigor index of 1190 under induced moisture stress (-0.49MPa). Rhizobium sp. VRE1 produced higher levels of EPS (62.12 mg) under drought stress compared to non- stressed (11.37 mg). Hence, the study suggests the scope of enhancing the yield potential and fitness of blackgram by bio-augmenting Rhizobium sp. VRE1 as a biofertilizer for sustainable pulse production in rice fallow and rain-fed areas.
2 illus, 2 tables, 33 ref
MALI P Y, GOYAL S
041691 MALI P Y, GOYAL S (Pharmacology Dep, Mandsaur Univ, Madhya Pradesh - 458 001, Email: pymali2008@rediffmail.com) : Assessment of anti-proliferative effect of extract fractions of euphorbia neriifolia leaves in human prostate adenocarcinoma du-145 cells. Indian J Pharm Sci 2020, 82(5), 912-7.
Euphorbia neriifolia Linn. Sp. Pl. (451.1753) belonging to family Euphorbiaceae has several ethnomedicinal uses. To authenticate these uses scientifically, we have assessed anti-proliferative effect of extract fractions of Euphorbia neriifolia leaves in human prostate adenocarcinoma DU-145 cells by 3-[4,5-dimethylthiazol2-yl]-2,5-diphenyl tetrazolium bromide cell proliferation assay. 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyl tetrazolium bromide cell proliferation assay was used for assessment anti-proliferative effect of extract fractions of Euphorbia neriifolia leaves in human prostate adenocarcinoma DU-145 and normal (Vero) cells. The cells were treated with series of concentrations of extract fractions (4.12-1000 μg/ml) for 48 h. Doxorubicin was considered as standard anti-cancer drug. In order to inhibition concentration and Selectivity Index results, extract fractions have been classified into 05 categories as described by Prayog et al. No extract fraction (EN1 to EN6) of Euphorbia neriifolia leaves was found in first 02 categories at the tested concentrations. Only doxorubicin standard drug sample was found in second category. It can be concluded that no other cells studies were documented yet on isolates and extract fractions of Euphorbia neriifolia by in vitro methods except murine B16F10 melanoma cells. Therefore, there is a need to carry forward these studies at higher concentrations of extract fractions (EN1 to EN6) in same and other adenocarcinoma cells. It can also be study by using other in vivo allograft and xenograft experimental models to confirm anti-proliferative or anti-cancer effects of these extract fractions.
1 illus, 1 table, 37 ref
NARENDRAN K, JAYALAKSHMI S, NIVEDHITHA M S, SARVANAN A, GANESAN S A, SUKUMAR E
041690 NARENDRAN K, JAYALAKSHMI S, NIVEDHITHA M S, SARVANAN A, GANESAN S A, SUKUMAR E (Research and Development Dep, Saveetha Institute of Medical and Technical Sciences (SIMATS), Chennai - 602 105, Email: drsuku3@gmail.com) : Synthesis, characterization, free radical scavenging and cytotoxic activities of phenylvilangin, a substituted dimer of embelin. Indian J Pharm Sci 2020, 82(5), 909-12.
Plants contain a wide variety of secondary metabolites that are used either as drugs or lead compounds in the synthesis of interesting chemicals that show promise in drug discovery. Quinones and their derivatives are one such group of specialized compounds that exhibit amazing biological properties. In this study, a benzoquinone derivative phenylvilangin has been synthesized from the naturally occurring embelin and its structure was confirmed by Infrared Spectroscopy, Proton Nuclear Magnetic Resonance, Carbon-13 nuclear magnetic resonance, Distortionless enhancement by polarization transfer and mass spectral analysis. Phenylvilangin has been screened for free radical scavenging and cytotoxic by in vitro methods wherein it exhibited significant activities suggesting that it could be a compatible material for further investigation to develop as a potential drug candidate. On comparison of the above bifunctional activities of phenylvilangin with those of the parent quinone embelin and another derivative vilangin, it has been found that phenylvilangin possessed better potential than the other two compounds.
2 illus, 2 tables, 9 ref
AL-KAFAJY M
046678 AL-KAFAJY M (Microbiology Dep, Thi-Qar Univ, Nasiriyah, Iraq, Email: minen2006@gmail.com) : Breast cancer risk trends of Iraqi women. Med Legal Update 2020, 20(1), 10.37506/v20/i1/2020/mlu/194355.
Breast cancer (BC) are one of the significant prevalence malignances among Iraqi women, which ranked as the number one cancer documented in all provinces. Although there is a rising incidence in the frequencies of BC, there were not enough studies conducted on the incidence’s frequencies over the Iraqi women in Thi-Qar provinces. It is well-known that incidence rates are informative. Analysis of tendencies would advantage in planning and organizing programs for control cancers incidence. The objective of the following study is to calculate the risk of BC using updated data from the cancer registries in the Iraqi health ministry and document its tendencies that released in different periods. : Data on incidence rates of BC were obtained from cancer registries of Iraq for the period between 2009 and 2015. Annual percent change in incidence and risk in terms of one in the number of women likely to develop cancer was estimated for both cancers’ types in five cities in Thi-Qar province. The incidence of BC ages group (45-49), (50-54) and (60-64) were significantly increased, while the age group (15-19) were significantly decreased. On the other hand, the higher increase in the incidence of BC in 2015 was reported to be 84 and 29 cases in Al-Nassiriya and Al-Shatra cities, respectively. Al-Refaey region recorded a decline in the incidence of BC, which is contrary to the observation in other cities, which showed an increase in breast cancer. On the other hand, the north side of the city which known to be more contaminated with pollution has higher incidence rate.
2 tables, 7 ref
SOWMYA B H, USHA ANANDHI D
041655 SOWMYA B H, USHA ANANDHI D (Zoology Dep, Bangalore Univ, Jnanabharathi, Bangalore - 560 056, Email: sowmyaarasu7@gmail.com) : Quantification of total phenolics, flavonoids and evaluation of in vitro free radical scavenging activities in Psidium guajava L. Indian J Pharm Sci 2020, 82(4), 578-85.
The present study was undertaken to quantify total phenolics and flavonoids and investigate in vitro free radical scavenging activities of leaf extracts of two varieties of Psidium guajava L. viz., Lalit and Allahabad safeda. Leaf extracts of Lalit and Allahabad safeda were prepared by Soxhlet extraction and ethanol extracts were used for in vitro assays. Total phenolic and flavonoid contents, 2,2-azinobis(3-ethylbenzothiazoline-6-sulfonic acid), 2,2-diphenyl-1-picrylhydrazyl, nitric oxide and super oxide free radical scavenging activities were determined at 100, 200, 300, 400, 500, 600 and 700 µg/ ml concentrations of Lalit and Allahabad safeda leaf extracts. Results indicated the presence of higher phenolic and flavonoid contents in the leaf extract of Lalit compared to that of Allahabad safeda. The leaf extracts of Lalit and Allahabad safeda showed dose-dependent increase in 2,2-azino -bis(3-ethylbenzothiazoline-6-sulfonic acid), 2,2-diphenyl-1-picrylhydrazyl and nitric oxide radical scavenging activities and a decrease in super oxide radical scavenging activities. However, Lalit showed higher free radical scavenging activity compared to that of Allahabad safeda. Further, the IC50 values of Psidium guajava for DPPH, 2,2-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid), nitric oxide and super oxide free radicals were 229.56, 503.07, 430.40, 07 and 377.96 µg/ml, respectively. In addition, the IC50 values of Allahabad safeda for 2,2-diphenyl-1-picrylhydrazyl, 2,2-azino-bis(3-ethylbenzothiazoline6-sulfonic acid), nitric oxide and super oxide free radicals were, 270.24, 543.63, 469.99 and 515.50 µg/ml, respectively. This study clearly demonstrated antioxidant activity in both the extracts of Lalit and Allahabad safeda. The better antioxidant activity of Lalit extract could be due to the presence of higher phenolic content compared to Allahabad safeda.
4 illus, 32 ref
MANURUNG B, HASAIRIN A, DAULAE A H
045274 MANURUNG B, HASAIRIN A, DAULAE A H (Biology Dep, Negeri Medan Univ, Medan- 202 21, Indonesia, Email: binarimanurung@unimed.ac.id) : Molecular analysis of rice green leafhopper, Nephotettix virescens (Distant) from Samosir Island-Indonesia using mitochondrial COI gene. J Ent Res 2020, 44(2), 183-8.
Present study is aimed to identify and analyse the genetic character of N. virescens and also its phylogeny to related species based on mt COI or DNA barcoding. The steps of this genetic analysis are leafhopper sample catching in rice field, DNA extraction, DNA amplification, product purification and DNA sequencing. Primer COI AB 976528 has been used in mtCOI-DNA amplification step. The research result showed that mtCOI-DNA fragment of N. virecens has length 677-681 bp. This mtCOI-DNA gene sequence was dominated by A and T bases with concentration 69.59 %, whereas CG content was 30.39 %. The concentration average of T (U), C, A and G nucleotides in the mtCOI gene sequence were 37.83, 15.96, 31.76 and 14.43 %, respectively. Based on molecular phylogeny analysis, green leafhopper N. virescens Samosir populations was similar (98.60 %) into green leafhopper N. virescens populations originated from Bangladesh. Identification of N. virescens based on this mtCOI-DNA gene sequence confirmed the identification result based on its morphological characters.
1 illus, 3 tables, 34 ref
SUDIARTI T, WINARIANI
046673 SUDIARTI T, WINARIANI (Pulmonology and Respiration Dep, Airlangga Univ, Surabaya- 60285, Indonesia, Email: winarianiwina@gmail.com) : Correlation of nitric oxide (NO) sputum level and lung physiology of indoor parking attendant. Med Legal Update 2020, 20(1), 10.37506/v20/i1/2020/mlu/194350.
Air contamination inside the building causes respiratory inflammation and increases NO sputum levels that cause changes in parking staffs’ lung physiology. To analyze the correlation between NO sputum level and lung physiology of indoor parking attendant. This research was conducted at the Toserba oceans in Tasikmalaya West Java, Indonesia with a sample of 40 people. Twenty indoor parking attendants as an exposed group and 20 administrative officers as a control group. Sputum NO and lung physiology were examined in both groups. The measurement of NO sputum level was using Griess method and lung physiology was by spirometry of brand of Fukuda. The mean of NO sputum level in the exposed group was 4689.75 ± 6778.452 and in the control group was 485.25 ± 307, the mean of NO level was obtained a significant difference between exposed group and control group (p = 0.009). The results of lung physiology examination in both exposure and control group from % FEV1,% FEV1 / FVC showed significant differences (p 0.05). The result of the Pearson correlation test showed a strong positive correlation between NO sputum level and lung physiology of indoor parking attendant (r = 0.461 with p <0.041). There was a correlation between NO sputum level and lung physiology of indoor parking attendant.
2 tables, 17 ref
HONG H, BAATAR D, SUKHBAATAR O, YANG S H, HWANG S G
041640 HONG H, BAATAR D, SUKHBAATAR O, YANG S H, HWANG S G (Animal Life and Environmental Science Dep, Hankyong National Univ, Anseong City 456-749, Korea, Email: sghwang@hknu.ac.kr) : Mongolian Chelidonium majus suppresses metastatic potential of hepatocellular carcinoma cells through TIMP up-regulation and MMP down-regulation. Indian J Pharm Sci 2020, 82(3), 456-64.
In this study, the antimetastatic effect of Chelidonium majus ethanol extract on hepatocellular carcinoma in vitro was investigated. The viability of SK-Hep1 and normal liver cells was determined using a cell counting kit-8 assay. Wound healing assays were performed to investigate SK-Hep1 cell migration and various metastatic characteristics including adhesion, aggregation and invasion were also measured using these cells. Furthermore, the proteolytic activity of extracellular matrix metalloproteinase-9 was measured using gelatin zymography. Expression levels of matrix metalloproteinase-2, matrix metalloproteinase-9, membrane type 1-matrix metalloproteinase and tissue inhibitor of metalloproteinase-1 were measured using reverse transcription-polymerase chain reaction and Western blotting. Chelidonium majus ethanol extract significantly inhibited the proliferation of SK-Hep1 hepatocellular carcinoma cells in a dosedependent manner. Moreover, metastatic characteristics including adhesion, migration, aggregation and invasion were significantly suppressed by Chelidonium majus ethanol extract treatment. Further, this preparation downregulated the expression of matrix metalloproteinase-2, matrix metalloproteinase-9 and membrane type 1-matrix metalloproteinase, but upregulated tissue inhibitor of metalloproteinase-1 and tissue inhibitor of metalloproteinase-2, in a dose-dependent manner. Additionally, the proteolytic activity of matrix metalloproteinase-9 was greatly diminished with 400 µg/ml of Chelidonium majus ethanol extract. Taken together, it was suggested that Chelidonium majus ethanol extract might exert an antimetastatic effect on hepatocellular carcinoma cells by inhibiting proliferation, adhesion, migration, aggregation and invasion through the downregulation of matrix metalloproteinases and upregulation of tissue inhibitor of metalloproteinases. Thus, this extract could represent a promising therapeutic agent for this disease.
7 illus, 1 table, 35 ref
PANDEY P, KIRAN U V
045269 PANDEY P, KIRAN U V (Human Development and Family Studies Dep, Babasaheb Bhimrao Ambedkar Univ, Lucknow– 226 025, Uttar Pradesh, Email: druvkiran@gmail.com) : Postural discomfort and musculoskeletal disorders among painters - An analytical study. J Ecophysiol Occup Health 2020, 20(3&4), 203-8.
The current investigation was to examine the intensity of body discomfort and various musculoskeletal disorders experienced by painter community due to their occupational habitat. A questionnaire was developed systematically with high competence with the current standard, which includes general profile sheet, occupational profile sheet and a modified Kromers body discomfort scale (Kroemer et al., 1987). These tools were used to gather information from the respondents. A sample of fifty two male painters aged between 19-75 years were interviewed randomly and mined various socio-demographic, socio-economic and health information. Data on occupational history, accidents, and leisure time activities were also collected. This paper focused on the intensity of pain due to prolonged standing and other postures during painting activities. The prevalence of occupational health hazards has been reported to be high among painter community in India. The study revealed that the painters were engaged in rigorous hand-intensive jobs for many years, this subsistence activity led to rigorous and permanent discomforts in different parts of their body as an occupational health hazards. From the findings of the study, it can be concluded that painters faced many occupational health hazards. The current study focused on musculoskeletal disorder and uncertainties due to the nature of high risk associated painting jobs. The study revealed that the painter’s communities were highly susceptible to musculoskeletal disorders, especially severe leg pain. Most of the interviewed painters were highly concerned about high risk areas (activities on scaffoldings). So for safeguarding the painter communities from high potential professional, physical and physiological health risk, the government must entrust contractors for providing standard and modernized safe working environment, safeguarding tools and risk incentives.
3 illus, 5 tables, 16 ref
HUSSEIN A A, BABAN R S, HUSSEIN A G, MOHAMMED S H
046667 HUSSEIN A A, BABAN R S, HUSSEIN A G, MOHAMMED S H (Biochemistry Laboratory, Baghdad, Iraq) : Prostate health index in a sample of Iraqi patients with prostate cancer and benign prostatic hyperplasia. Med Legal Update 2020, 20(1), 10.37506/v20/i1/2020/mlu/194344.
There is widespread of PSA using as a Prostate Cancer biomarker (threshold of 4ng/ml), but there is no single PSA value that avoids missing serious cancers at a treatable phase, avoids false-positives and unnecessary prostate biopsies. The evaluation of the clinical significant of [-2]proPSA and the Prostate Health Index(PHI) in diagnosis of Prostate Cancer was done in this research to enhance the correct prediction of the prostate cancer. The aim, of this study is to improve the method of testing by using newer PSA biomarkers in the subject sera for evaluating the diagnostic significance of [-2]proPSA and Prostate Health Index (PHI) in the detect of prostate cancer in early stages. A case-control research comprising 54 patients over 50 years old age having Prostate Cancer and Benign Prostatic Hyperplasia recruited from Iraqi urological clinics unit and AL-Amal National Hospital for Cancer Management during the period from July 2018 to March 2019. There was a significantly high difference (P<0.001) of serumPSA,P2PSA and PHI levels among all the study groups. The cut-off values of [-2]proPSA and Prostate Health Index (PHI) based on the ROC curve results in current study were >322 pg/ml and >578 respectively for Prostate cancer patients , while their values range between 322-89 pg/ml,and 578-209 respectively for BPH patients, and<89 pg/ml and <209 for apparently healthy men respectively, the area under curve(AUC) of (P2PSAg) and PHI were 0.968,0.960 for PCa group against noncancerous group respectively, 0.85 and 0.796 for BPH group against control group respectively. Their levels show significant increase in PCa patients in comparison with noncancerous group and in BPH patients when compared with control group.
3 illus, 3 tables, 15 ref
KUMAR P, SINGH P
041635 KUMAR P, SINGH P (Zoology Dep, Banaras Hindu Univ, Varanasi - 221 005, Email: poonom@gmail.com) : Withania somnifera ameliorates aluminium chloride-induced testicular toxicity and impaired fertility in Mus musculus. Indian J Pharm Sci 2020, 82(3), 398-408.
The present study was planned to evaluate the effectiveness of Withania somnifera against aluminium chloride-induced testicular toxicity and impaired fertility. Swiss mice were divided into 6 groups of 12 each. Mice of group I served as control while that of group II were administered with AlCl3 (100 mg/kg/ day) for 30 consecutive days. Animals of group III were administered with AlCl3 (100 mg/kg/day) for 30 consecutive days followed by sacrificing the animals 42 days after withdrawal of the treatment. Mice of groups IV, V and VI were administered with Withania somnifera (200 mg/kg/day) only, AlCl3 (100 mg/ kg/day) along with Withania somnifera (100 mg/kg/day) and AlCl3 (100 mg/kg/day) along with Withania somnifera (200 mg/kg/day), respectively, for 30 consecutive days. AlCl3 -induced noticeable alterations in the body weight, testicular weight, histoarchitechture of the testis, aluminium accumulation, level of LPO, activities of antioxidant enzymes, functional markers, concentration of cholesterol, level of serum testosterone and mating ability were restored markedly in the mice co-administered with either 100 or 200 mg/kg/day AlCl3. These findings thus revealed the ameliorating potential of Withania somnifera against aluminium chloride-induced testicular toxicity and impaired fertility.
7 illus, 3 tables, 59 ref
KUMAR N, ARADHYE S, YADAV S , SINGH V A
043453 KUMAR N, ARADHYE S, YADAV S , SINGH V A (Microbiology Dep, Government Medical Coll for Women, Khanpur Kalan, Sonipat, Haryana, Email: drsaritayadavmicrobiology@gmail. com) : Prevalence and antibiotic susceptibility pattern of clinically isolated New Delhi metallo-β-lactamaseproducing Klebsiella spp.. Int Dent Med J Adv Res 2020, 6, 1–3.
New Delhi metallo-β-lactamase (NDM-1) encoding carbapenem resistance, in Gram-negative bacteria, is very common in Indian subcontinent that results in treatment failure, increased health-care cost, and high mortality rate. The present study was conducted to determine the prevalence and susceptibility pattern of NDM-1-producing Klebsiella spp. A total of 3265 clinical samples were processed for the isolation of carbapenemase-producing Klebsiella spp. and antibiotic susceptibility testing. Sixty-one (12.2 %) NDM-1 producers were isolated from 502 Klebsiella species. All the NDM-1 producers were resistant to nearly all routine antibiotics. NDM-1 gene encoding carbapenemase-producing bacteria were found to be resistant to nearly all routine antibiotics. The sample-wise distribution and susceptibility pattern of NDM1-producing Klebsiella spp. will help clinicians for better treatment management and to develop effective hospital infection control policies.
2 tables, 12 ref
EJDER N, EKSI S, YAZICI Z, BERIS F, MAKBUL S, UZUNOK B
041626 EJDER N, EKSI S, YAZICI Z, BERIS F, MAKBUL S, UZUNOK B (Medical Microbiology Dep, Recep Tayyip Erdogan Univ, Rize, Turkey, Email: saliha.eksi@erdogan.edu.tr.com) : Antiproliferative effect of Ornithogalum balansae on human cancer cell lines. Indian J Pharm Sci 2020, 82(2), 321-8.
The purpose of this study was to investigate the antiproliferative effect of the methanol and ethyl acetate extracts of Ornithogalum balansae flower and bulb against normal ARPE-19 cell line and cancer cell lines, A549, CRL-2923, HT-29 and HeLa. The cytotoxic activities of the extracts were determined using cell viability, deoxyribonucleic acid fragmentation and caspase-3 activity tests. Flower and bulb extracts exhibited dose-dependent antiproliferative effects on non-transformed and transformed cells, with greater growth inhibition in A549 lung cancer cells at lower concentrations. The IC50 values of the flower extracts against A549 cells were 1.5±0.153 and 2.2±0.503 µg/ml, and of the bulb extracts were 1.8±0.220 and 1.56±0.106 µg/ml, respectively. Against ARPE-19 cell line the IC50 values were 22.5±6.466 and 25±2.887 µg/ml for flower and 14±4.726 and 12.5±3.182 µg/ml for bulb extracts, respectively. In addition, it was observed that at concentrations ≤3.12 µg/ml there were statistically significant differences between ARPE19 and transformed A549 cell lines (p <0.05). Finding caspase-3 activity of the methanol flower extract in A549 indicated apoptotic effects in those cells. These results showed that Ornithogalum balansae extracts could exhibit antitumor activity particularly on the A549 lung cancer cell line, a resistant cell line. Further investigations of the composition of the extracts are required to identify the effective components with antiproliferative activity, particularly on A549, the human alveolar adenocarcinoma cancer cell line. This study revealed that extracts of Ornithogalum balansae possessed considerable antiproliferative activity against A549 cells.
3 illus, 1 table, 29 ref
SHUKLA A H, SHAH P J, DEDHIYA P P, VYAS B A, SHAH S A
041625 SHUKLA A H, SHAH P J, DEDHIYA P P, VYAS B A, SHAH S A (Maliba Pharmacy Coll, Bardoli, Gujarat - 394 350, Email: praful.dedhiya@utu.ac.in) : Development and validation of a HPTLC method for rivaroxaban in human plasma for a pharmacokinetic study. Indian J Pharm Sci 2020, 82(2), 315-20.
The present study is concerned with the development and validation of a bioanalytical method for estimation of rivaroxaban in human plasma using high performance thin layer chromatography. The chromatographic separation was achieved on pre-coated silica gel 60F254 thin layer chromatography plate using toluene:ethylacetate:methanol (6:3:1, % v/v/v) as a mobile phase. Detection was carried out at 284 nm. A compact spot was obtained with an Rf value of 0.44±0.02. The linearity was found over the concentration range of 25-125 ng/band in human plasma. The relative standard deviation for repeatability of sample application and sample measurement was 0.60 and 1.65 %, respectively. The relative standard deviation for intraday and interday precisions was in the range of 1.37 to 1.85 % and 1.03 to 2.77 %, respectively. The limit of quantitation was 8.00 ng/band and the limit of detection was 2.64 ng/band. Percent recovery of rivaroxaban was in the range of 66.95-69.03%. This method was applied to a pharmacokinetic study of rivaroxaban. The Cmax and tmax for test and marketed formulation were found to be 63.83 and 47.3 ng/ ml and 3 and 4 h respectively. The area under the curve0-t for test and marketed formulation were found to be 290 and 219.0 ng/ml. h, respectively. The t1/2 for test and marketed formulation was found to be 6.87 and 6.64 h.
4 illus, 6 tables, 18 ref
KUMAR S P, GIRIJA A S S, PRIYADHARSINI J V
041623 KUMAR S P, GIRIJA A S S, PRIYADHARSINI J V (Microbiology Dep, Saveetha Univ, Chennai - 600 077, Email: smilinejames25@gmail.com) : Targeting NM23-H1-mediated inhibition of tumour metastasis in viral hepatitis with bioactive compounds from Ganoderma lucidum: A computational study. Indian J Pharm Sci 2020, 82(2), 300-5.
The aim of the present study is to evaluate the role of phytoconstituents of Ganoderma lucidum in the interactions with non-metastatic clone 23, isoform H1. 3D structure of non-metastatic clone 23, isoform H1 was retrieved from the PDB data bank with further optimization of both the protein and ligands. In silico binding potential of the selected ligands with non-metastatic clone 23, isoform H1 was determined using the Auto Dock Tool 2.0 and visualized with Bio via discovery studio visualizing tool to assess the molecular binding properties of the ligands with non-metastatic clone 23, isoform H1 by molinspiration calculations and further assessment of drug likeliness. Ganoderic acid H appeared to possess promising binding with non-metastatic clone 23, isoform H1 with least binding energy of –8.87 Kcal/mol forming 5 hydrogen bond interactions followed by ganoderic acid T and A. The findings of this study thus provide theoretical evidence for ganoderic acid derivatives from Ganoderma lucidum to possess promising binding to non-metastatic clone 23, isoform H1 suggesting it as a target to arrest tumour metastasis with further in vivo validation.
4 illus, 2 tables, 20 ref
NAYAKA S, BHAT M P, CHAKRABORTY B, PALLAVI S S, AIRODAGI D, MUTHURAJ R, HALASWAMY H M, DHANYAKUMARA S B, SHASHIRAJ K N, KUPANESHI C
041619 NAYAKA S, BHAT M P, CHAKRABORTY B, PALLAVI S S, AIRODAGI D, MUTHURAJ R, HALASWAMY H M, DHANYAKUMARA S B, SHASHIRAJ K N, KUPANESHI C (Studies in Botany Dep, Karnatak Univ, Dharwad - 580 003, Email: sreenivasankud@gmail.com) : Seed extract-mediated synthesis of silver nanoparticles from Putranjiva roxburghii wall., phytochemical characterization, antibacterial activity and anticancer activity against MCF-7 Cell Line. Indian J Pharm Sci 2020, 82(2), 260-9.
The present study was focused on the green synthesis of silver nanoparticles using the aqueous extract of Putranjiva roxburghii seed and investigation of antibacterial activity of the nanoparticles. Further, the synthesized silver nanoparticles were tested on human breast cancer cell line the potential tumour suppressing property for antitumour activity. The seed extract was investigated for the presence of secondary metabolites and the formation of silver nanoparticles was indicated by a colour change from pale yellow to brown. The synthesis of the silver nanoparticles was ascertained with UV/Vis spectroscopy, atomic force microscopy, X-ray powder diffraction, energy dispersive X-ray analysis, Fourier Transform infrared spectroscopy and transmission electron microscopy. Antibacterial and anticancer activity of the synthesized silver nanoparticles was tested using agar well diffusion and 96 well plate mean transit time cell proliferation assay methods, respectively. The results showed that silver nanoparticles were spherical, 13- 69 nm in size with a maximum absorption peak at 371 nm. These silver nanoparticles showed considerable antibacterial effects on Staphylococcus aureus, Streptococcus pneumoniae and Enterococcus faecalis except on Escherichia coli. The cytotoxic effect of the silver nanoparticles was tested on human breast cancer cell line. The decrease in % viability of the human breast cancer cell line cells was observed at 12.5 to 200 µg/µl concentration with an IC50 of 72.32 µg/ml. It is an easy, inexpensive and eco-friendly approach for the biosynthesis of silver nanoparticles from Putranjiva roxburghii seed extract and the nanoparticles exhibited antibacterial activity and a potential to be used against human breast cancer.
11 illus, 2 tables, 39 ref
DEL FANTE Z, DI FAZIO N, QUATTROCCHI A, FAZIO V, DE MATTEIS A, ARCANGELI M, LA RUSSA R
046657 DEL FANTE Z, DI FAZIO N, QUATTROCCHI A, FAZIO V, DE MATTEIS A, ARCANGELI M, LA RUSSA R (Anatomical Dep, Sapienza Univ of Rome, Viale Regina Elena- 336 00161, Roma, Email: zoe.delfante@uniroma1.it) : The importance of post-mortem computed tomography (PMCT) as a complementary diagnostic technique to traditional autopsy in a case of asphyxia related-death. Med Legal Update 2020, 20(1), 10.37506/v20/i1/2020/mlu/194334.
Although asphyxia related-death is a common occurrence in forensic setting, traditional autopsy with neck dissection is not always sufficient to gain information about potential injuries of the deep structures of the neck. In this case a 40 years-old white female was found unresponsive on the floor of her living room, in supine position with a widespread brownish area on her neck. A preliminary PMCT examination showed a fracture line within the hyoid bone. This finding was confirmed by the autopsy, which revealed soft tissue’s haemorrhage of the sternocleidomastoid and sternohyoid muscles and a fracture of the right horn of the hyoid bone. A 3D reconstruction of the event showed the aggressor standing behind the victim while holding his arm around her neck. Our study demonstrates that, PMCT represent an effective aid to traditional examination techniques in order to visualize fractures. The former always requires to be associated with autoptic examination.
3 illus, 20 ref
FAN L Y, LIN Q, YANG N Y, CHEN L H
041608 FAN L Y, LIN Q, YANG N Y, CHEN L H (Nanjing Univ of Chinese Medicine, Nanjing 210023, China, Email: nianyunyang@hotmail.com) : Analgesic effects of the essential oil from Cinnamomum camphora against nitroglycerin-induced migraine in mice. Indian J Pharm Sci 2020, 82(1), 166-70.
This investigation was aimed to study the analgesic effect of the essential oil of Cinnamomum camphora leaves on migraine mouse model induced by nitroglycerin and its possible mechanism. The chemical constituents of essential oil of camphor leaves were analyzed by gas chromatography-mass spectrometry and the main compounds identified in essential oil were nerolidol and (E)-α-atlantone. The number of head scratching was recorded in the developed animal model. The contents of nitric oxide, inducible nitric oxide synthase and neuronal nitric oxide synthase in the serum and brain tissue of the mice were measured. The expression level of nuclear factor-kappa B of brain tissue was investigated using the Western blotting assay. Essential oil intervention significantly reduced the scratching number and decreased the levels of nitric oxide, inducible nitric oxide synthase, and nuclear factor-kappa B compared to the untreated group. Essential oil of camphor leaves has significant analgesic action on migraine by inhibiting the nuclear factor-kappa B/inducible nitric oxide synthase/nitric oxide pathway.
3 illus, 3 tables, 26 ref
KOTA P, SERU G, PANDA J, SAHU P K, PALLA M S
041605 KOTA P, SERU G, PANDA J, SAHU P K, PALLA M S (Pharmacognosy Dep, Raghu Coll of Pharmacy, Visakhapatnam - 531 162, Email: pharma.padmaja@gmail.com) : The pharmacognostic profile and biological potential of traditional medicinal shrub Hibiscus hiritus l. Indian J Pharm Sci 2020, 82(1), 139-48.
The proposed study has largely focused on two distinct lines of investigation. In the first approach, efforts have been made to evaluate macroscopic and microscopic pharmacognostic characteristics of Hibiscus hiritus L. In the second approach, the pharmacological potential of the whole plant extract was explored for in vitro antioxidant, antimicrobial and in vivo antiinflammatory activity. The extract and dry powdered plant material were screened for phytochemical constituents and other physiochemical parameters. Various microscopic characteristics of fresh leaves and stem of the plant (paradermal and T.S) were extensively evaluated. Methanol extract of the whole plant was used for pharmacological screening. Antioxidant potential of the extract was evaluated using the 1,1-diphenyl-2-picryl-hydrazil and hydroxyl radical scavenging assay using ascorbic acid as the standard. Antimicrobial property was evaluated using cup plate method against Staphylococcus aureus, Bacillus subtilis, Proteus vulgaris, Escherichia coli, Aspergillus niger and Candida albicans. Antiinflammatory potential was evaluated in the rat carrageenan-induced paw edema model. The IC50 values obtained in the antioxidant assay were, 42±0.06 and 2.8±1.64 % in the 1,1-diphenyl-2-picryl-hydrazil and hydroxyl radical scavenging assay, respectively. Inhibitory activity was observed against Staphylococcus aureus (14±0.15 mm), Bacillus subtilis (14±0.13 mm) and Escherichia coli (14±0.16 mm). The study also revealed significant and dose-dependent antiinflammatory activity in the carrageenan-induced rat paw edema model. The present study explored the pharmacognostic features and the pharmacological potential of Hibiscus hiritus to provide evidence for the traditional therapeutic use of the plant as an antibacterial, antioxidant and antiinflammatory agent.
7 illus, 6 tables, 25 ref
SAHOO J, KSHIRODA P, SARANGI N, ROUT S K, PAIDESETTY S K
041603 SAHOO J, KSHIRODA P, SARANGI N, ROUT S K, PAIDESETTY S K ( Pharmaceutical Chemistry Dep, Siksha ‘O’ Anusandhan (Deemed to be Univ), Bhubaneswar - 751 030, Email: sairampaidesetty@gmail.com) : In silico investigation and biological evaluation of synthesized sulfamethoxazole derivatives. Indian J Pharm Sci 2020, 82(1), 123-130.
A series of 4-[4-(substitutedaryl/heteroaryldiazenyl]-N-(5-methylisoxazol-3-yl)benzene sulphonamide derivatives (4a-4f) were designed and synthesized coupling a mixture of diazotized sulfamethoxazole with six different phenolic and enolic compounds in an in situ reaction. The structural environment of synthesis of each molecule was confirmed by Fourier-transform infrared spectroscopy, proton nuclear magnetic resonance and elemental analysis. These derivatives were further screened in various biological assays in vivo for analgesic and antiinflammatory activities and in vitro for antioxidant and antimicrobial activities. When tested for analgesic activity at a dose of 50 mg/kg, compounds 4-((2-hydroxynaphthalen1-yl)diazenyl)-N-(5-methylisoxazol-3-yl)benzene sulphonamide (4d) and 4-((4-hydroxy-5-isopropyl-2- methylphenyl)diazenyl)-N-(5-methylisoxazol-3- yl)benzene sulphonamide (4f) showed 58.33 and 57.76 % of pain inhibition, respectively. These two molecules also exhibited significant antioxidant activity at 10 and 50 µg/µl. The compound 4-[(4-hydroxy-2-oxo-2H-chromen-3-yl)diazenyl]-N-(5-methylisoxazol3-yl)benzene sulphonamide (4a) exhibited antibacterial activity against Staphylococcus aureus resistance, Candida albicans and DescriptionCryptococcus neoformans at a concentration of 31.25 µg/ml. The analgesic action of these synthesised analogues was predicted in molecular docking experiments with a specific target protein, cyclooxgenase-2 of Mus musculus and results indicated all tested compounds to exhibit good binding interaction with the active site amino acid of the target enzyme.
3 illus, 3 tables, 15 ref
GURJAR V K, PAL D, MAZUMDER A, MAZUMDER R
041595 GURJAR V K, PAL D, MAZUMDER A, MAZUMDER R (Pharmaceutical Sciences Dep, Guru Ghasidas Vishwavidyalaya (A Central Univ), Koni, Bilaspur - 495 009, Email: drdilip2003@yahoo.co.in) : Synthesis, biological evaluation and molecular docking studies of novel 1,8-naphthyridine-3-carboxylic acid derivatives as potential antimicrobial agents (part-1). Indian J Pharm Sci 2020, 82(1), 41-53.
Synthesis and investigation of antimicrobial activity of 6 novel 1,8-naphthyridine-3-carboxylic acid derivatives are presented. Among the derivatives, compounds 4a–5b2 showed a broad-spectrum antimicrobial activity against all reference Gram-positive, Gram-negative bacteria and fungi. These compounds exhibited remarkable bactericidal activity against Staphylococcus and Bacillus sps. The tested substances 4a–5b2 were found also found to be active against Escherichia coli, Salmonella and Shigella sps. The chlorine substituted compounds 4a and 5a2 were found to be the most active towards the tested microorganisms. Compounds 4a–5b2 were found to be fungicidal against Candida sp. with a MIC values in the range of 400-2000 μg/ml. Docking studies of these compounds with Salmonella typhi OmpF complexed with ciprofloxacin using PDB-4KRA revealed that the compounds acted as covalent crosslinker on the DNA gyrase B of the former and intercalate the latter both with higher C score values. Thus, the antibacterial activity against tested strains suggested 1,8-naphthyridine-3-carboxylic acid derivatives warrant further evaluation as potential novel antiinfective agents. The antifungal activity of these compounds was comparable to that of griseofulvin. The drug-likeness data of synthesized compounds made them promising leads for the future development as antifungal agents.
3 illus, 7 tables, 36 ref
HASSAN A B, AL-MSAID H L F, AL-DUJAILI A N G, JAFFAT H S
046647 HASSAN A B, AL-MSAID H L F, AL-DUJAILI A N G, JAFFAT H S (Biology Dep, Kufa Univ, Al-Najaf, Iraq, Email: adhraa.alshabawy@uokufa.edu.iq) : Measurement of lipid profile in fasting persons. Med Legal Update 2020, 20(1), 10.37506/v20/i1/2020/mlu/194324.
This study was performed within the DM center in Al-Sadder Teaching Hospital in Al-Najaf province to see the impact of not having breakfast for males in relation with Diabetes Mellitus sort two and supermolecule Profile. This study includes (25) male that not having breakfast , and (5) male that thought to be management cluster. (The results show important increase (P≤0.05) in abstinence glucose, cholesterin, acylglycerol, LDL, lipoprotein and high-density lipoprotein in comparison with management group).
1 table, 28 ref
KHABIROV A, KHAZIAKHMETOV F, KUZNETSOV V, TAGIROV H, REBEZOV M, ANDREYEVA A, BASHAROV A, YESSIMBEKOV Z, AYAZ M
041577 KHABIROV A, KHAZIAKHMETOV F, KUZNETSOV V, TAGIROV H, REBEZOV M, ANDREYEVA A, BASHAROV A, YESSIMBEKOV Z, AYAZ M (Pharmacy Dep, Malakand Univ, Khyber Pakhtunkhwa-18800, Pakistan, Email: ayazuop@gmail.com) : Effect of normosil probiotic supplementation on the growth performance and blood parameters of broiler chickens. Indian J Pharm Edu Res 2020, 54(4), 1046-55.
This study was aimed to investigate the effects of probiotic “Normosil” containing a mixture of living cultures of Lactobacillus and Enterococcus strains at a concentration of 1×106 and 1×107 CFU/mL was assessed. Effect of Normosil on the growth performance, hematological and biochemical factors of Arbor Acres broilers from a day-old to 42-day old (n= 175, 1 control + 4 experimental groups) daily and periodically. Results showed that Normosil (1×106 CFU/mL) had a relatively better growth performance and showed an increase in the average daily growth by 10.6 %-13.0 % compared to control. In comparison to control, broilers provided with daily and periodic dose of Normosil showed an increase in the level of blood erythrocytes by 5.6 % and 14.1 % after 21 days, respectively; and an increase in hemoglobin, glucose, total protein, albumin, sodium, potassium and calcium by 4.9 % and 10.9 %,12.3 % and 17.4 %,0.5 % and 5.7 %, 3.7 % and 14.4 %, 2.1 % and 5.0, 17.0 % and 33.3 % and 7.7 % and 21.2 % (p<0.05), respectively after 42 days of growth. Nutrient digestibility in context to organic matter, raw protein, raw fat and nitrogen-free extractive compounds in broilers fed with periodic and daily doses of Normosil (106 CFU/mL) was higher than in control by 4.4 %-6.6 %, 2.5 %-6.2, 1.6 %-5.5 % and 8.2 %-12.2 %, respectively. Compared to control, the femoral muscles had a higher protein content of 6.0 % and 15.7 % (experimental groups III and IV); low carcass fatness by 8.1 % (group IV); and low content of connective tissue. This study suggests the potential benefits of Normosil supplementation for improving the growth and quality of broilers.
5 tables, 15 ref
BHAKYASHREE K, KANNABIRAN K
041555 BHAKYASHREE K, KANNABIRAN K (Biomedical Sciences Dep, Vellore Institute of Technology, Vellore - 632 014, Tamil Nadu, Email: kkb@vit.ac.in) : Pharmaceutical and biotechnological importance of actinobacterial products. Indian J Pharm Edu Res 2020, 54(4), 858-64.
Many compounds produced by marine microbes possess significant pharmaceutical applications. Actinobacteria are one among the microbes producing a variety of antibiotics. Apart from antibiotics, it also produces many novel enzymes and important pharmaceutical products. Actinobacteria serves as a reservoir of antibiotics and novel chemical compounds and it contributes 80% of antibiotics available in the market. It was continuously been explored for novel bioactive compounds and new chemical entities. Many of them are more promising against microbial pathogens and even drug resistant pathogens. Apart from antibiotics, many enzymes are also produced by actinobacteria. The usage of enzymes in diverse pharmaceutical and biotechnological industries is gaining momentum and moreover, there is a growing demand for the discovery of novel metabolites and enzymes to fulfill the requirement of pharmaceutical industry. Apart from all these products actinobacteria also produces biosurfactants. Members of actinobactaerial genera have been extensively used in the removal of toxic dyes and other toxic pollutants. In this review, the up to date information available on the pharmaceutical and biotechnological uses of actinobacterial products and the scope for screening of actinobacterial genome for production of novel compounds for pharmaceutical applications have been discussed.
1 illus, 3 tables, 78 ref
VENKATESH K , JENOVA I , SHEEBA D J , KARTHIKEYAN S
043361 VENKATESH K , JENOVA I , SHEEBA D J , KARTHIKEYAN S (Physics Dep, Madras Christian Coll, Chennai, Tamil Nadu) : Conductivity studies of cellulose acetate-sodium nitrate polymer system. Int J Chem Sci 2020, 4(3), 21-4.
The effect of sodium nitrate (NaNO3) salt on the conductivity of polymer system based on the bio polymer cellulose acetate (CA) has been analysed in this study. The films were prepared by solution casting technique. The sample (CA: NaNO3) with the weight ratio of (0.6:0.4) gram exhibited the highest room temperature conductivity of the order 10-6 Scm-1 . Dielectric measurements were made using ac impedance analyser in the frequency range of 10 Hz–4 MHz. It was observed that the ionic conductivity increased with the increase in salt concentration as well as temperature. The conductivity–temperature relationship was found to obey Arrhenius rule. The activation energy is calculated for the highest conducting sample.
6 illus, 2 tables, 24 ref
KUMAR S, AGHARA J C, MANOJ A, ALEX A T, MATHEW A J, JOESPH A
041545 KUMAR S, AGHARA J C, MANOJ A, ALEX A T, MATHEW A J, JOESPH A (Pharmaceutical Chemistry Dep, Manipal Coll of Pharmaceutical Sciences, Manipal - 576 104, Karnataka, Email: alex.joseph@manipal.edu) : Novel quinolone substituted imidazol-5(4h)-ones as anti-inflammatory, anticancer agents: Synthesis, biological screening and molecular docking studies. Indian J Pharm Edu Res 2020, 54(3), 771-80.
Quinolones and imidazolones are important heterocyclic moieties which have been reported to possess potent anti-inflammatory and anticancer properties. The activity of these compounds were related to inhibition of nuclear factor-kappaB (NFκB) which is one of the important targets studied for designing of anti-inflammatory and antitumor drugs. Further, hybrid pharmacophore approach is used in the present study for designing potent molecules. Aim of the study is to synthesis a series of quinolone substituted imidazolones and evaluation of their anti-inflammatory and anticancer activity. Quinolone substituted imidazolones were synthesized by aminolysis of 7-amino-4-methyl-quinoline-2(1H)-one with substituted oxazolones afforded quinolone substituted imidazolones. Structures of synthesized compounds were characterized by spectral techniques and were evaluated for anti-inflammatory activity by carrageenan-induced rat paw oedema test. Differences between control and treatment groups were tested using one way analysis of variance followed by Tukey’s test. Anticancer activity was assessed by evaluating the cytotoxicity of compounds on BT-549 and HeLa, human cancer cell lines by MTT assay. Compounds 3-fluorobenzylidene substituted imidazolonyl quinolone (F3) and 4-phenoxybenzylidene substituted imidazolonyl quinolone (F12) were the most cytotoxic compounds against BT-549 and HeLa cell lines. While 2-chlorobenzylidene substituted imidazolonyl quinolone (F4) and 4-chlorobenzylidene substituted imidazolonyl quinolone (F5) exhibited the highest anti-inflammatory activity. Most of the test compounds exhibited statistically significant inhibition of paw oedema volume when compared to that of control. Molecular docking studies revealed that combination of two pharmacophores was crucial for binding of quinolone substituted imidazol-5(4H)-ones on NF-κB with good correlation between docking score and biological activity.
1 illus, 3 tables, 28 ref
REDDY G J, REDDY K B, REDDY G V S
041544 REDDY G J, REDDY K B, REDDY G V S (Pharmacology Dep, S V Univ, Tirupati - 517 502, Andhra Pradesh, Email: jyothi.reddy992@gmail.com) : In vivo anti-diabetic and anti-hyperlipidemic activities of ethyl acetate/methanol fractions of feronia elephantum fruit in type 2 diabetic rats: via α-amylase and ppar-γ by using in silico approach. Indian J Pharm Edu Res 2020, 54(3), 761-70.
Obesity and overweight, together with physical inactivity, are projected to cause a huge proportion of the global diabetes burden. Natural products play a key role in the discovery of novel therapeutic agents. The present study aimed to elucidate in silico and in vivo anti-diabetic and anti-hyperlipidemic potential of Ethyl acetate (EFE) and ethyl acetate:methanol (EMFE) fractions of F. elephantum fruit in diabetic rats. Male Sprague-Dawley rats were induced type 2 diabetes by high fat diet (HFD) for a period of 2 weeks and then injected intraperitoneally with Streptozotocin (STZ, 35 mg/ kg b.w). Significant antihyperglycemia was displayed in rats treated with EFE and EMFE in OGTT in normal rats. Daily oral treatment with EFE and EMFE each at 100 and 200 mg/kg b.w for 5 weeks resulted in significant reduction in plasma glucose levels and HbA1c, increased plasma insulin levels, normalised lipid profile and liver function parameters in HFD and STZ model. In addition, degenerative histopathological changes were found to be normalized. Molecular docking studies revealed strong binding efficacy of the active constituents of the extract viz., 22,23-dihydrostigmasterol, tocopherol and campesterol with α-amylase enzyme and PPAR-γ. These results suggest a promising anti-diabetic and anti-hyperlipidemic effect of Feronia elephantum fruit without apparent toxic effects.
5 illus, 4 tables, 39 ref
MUNDUGARU R, SHARMA S, SIVANESAN S, THANGARAJAN R , NAIK P R, RAJU N, ALFARHAN A, RAJAGOPAL R, ALMUNQEDHI B
041541 MUNDUGARU R, SHARMA S, SIVANESAN S, THANGARAJAN R , NAIK P R, RAJU N, ALFARHAN A, RAJAGOPAL R, ALMUNQEDHI B (Pharmacology Dep, DM Wayanad Institute of Medical Sciences, Wayanad, Kerala, Email: ravisdm13@gmail.com) : Neuroprotective effect of Vanda roxburghii extract in endothelin-1 (et-1) induced hippocampal ischemic damage and ameliorate cognitive deficit. Indian J Pharm Edu Res 2020, 54(3), 740-9.
The concept of neuroprotection gaining considerable interest in search for novel therapy that has potential to preserve brain tissues and improve cognitive functions in ischemic brain damage. In the present study we evaluated the neuroprotective efficacy of hydro alcoholic extract of Vanda roxburghii in experimental models of ischemic hippocampal injury in rats. Ischemic hippocampal injury was induced by single intra-hippocampal injection of Endothelin-1 (80μM) using stereotaxic instrument. Following ischemic hippocampal damage, hydro alcoholic extract of Vanda roxburghii (HAVR) (200 and 400mg/kg) was administered orally, once in a day for 14 consecutive days. The Morris water maze, Actophotometer and Open field behavioral test results showed significant cognitive deficit after ischemic hippocampal damage, however the repeated administration of HAVR at higher dose level for 14 consecutive days attenuated the cognitive deficits to a significant level. The histopathological examination of CA1 and CA3 regions of hippocampus revealed the loss of normal pyramidal cells and degenerative changes with shrunken, hyperdensed soma with pyknotic nuclei, however HAVR treatment at both dose levels significantly attenuated the observed qualitative changes. HAVR treatment showed significant anti-oxidant properties by inhibiting lipid peroxidation in ischemic condition as well as restoration of glutathione peroxidase enzymes to significant level. The study concludes that V. roxburghii extract and its constituents have neuroprotective potentials in ischemic hippocampal injury.
5 illus, 400 ref
BANSODE P V, PATIL K S, HAJARE A A
041537 BANSODE P V, PATIL K S, HAJARE A A (Pharmaceutics Dep, Bharati Vidyapeeth Coll of Pharmacy, Kolhapur, Maharashtra, Email: ashok.hajare@bharatividyapeeth.edu) : Bioactivity guided antidiabetic formulation development of Tridax procumbens linn leaves. Indian J Pharm Edu Res 2020, 54(3), 705-13.
Diabetes mellitus is a global health problem as it is one of the complex disease and main causes of premature illness and death. The present study was focused to scientifically overcome bioavailability drawbacks of Tridax procumbens Linn. and improve its medicinal use of for the treatment diabetes by formulating it into microemulsion from. In this study oil in water microemulsion of Tridax procumbens Linn leaves extract was prepared using olive oil, Tween 80 and propylene glycol for oral delivery. Phytochemical screening of Tridax procumbens Linn. leaves extract was carried out to isolate flavonoids by column chromatography. The o/w microemulsion of whole extract was prepared by water titration method followed by its evaluation for various physical tests and thermodynamic stability. The optimized formulation was tested for drug release in vitro and antidiabetic activity by in vivo study. Tridax procumbens Linn. leaves extract isolated for the active moiety showed antidiabetic action in rats. The optimized Tridax procumbens Linn. extract microemulsion showed an average particle size 292.4 nm. There was approximately 1.4 fold increase in drug release from microemulsion compared to marketed tablet formulation. At the end of seven days after oral administration of microemulsion a significant reduction in blood glucose level was observed. The optimized microemulsion was thermodynamically stable. The enhanced bioavailability of flavonoids in microemulsion proves the traditional claim with regard to Tridax procumbens Linn. for its antidiabetic activity.
4 illus, 4 tables, 19 ref
MESTRY M, RANE M, BAJAJ A
041531 MESTRY M, RANE M, BAJAJ A (Pharmaceutics Dep, SVKM's Dr. Bhanuben Nanavati Coll of Pharmacy, Mumbai - 400 056, Maharashtra, Email: meenal.rane@bncp.ac.in) : Commiphora mukul and quercetin loaded liposphere gel: Potential treatment for psoriasis. Indian J Pharm Edu Res 2020, 54(3), 654-67.
Psoriasis is a chronic autoimmune skin disorder characterized by thick skin patches, which are typically red, scaly and itchy. Topical drug delivery is backbone in mild and moderate psoriasis as well as useful complementary therapy to systemic therapy in severe conditions. The attempt was made to formulate, optimized and evaluate novel liposhpere based drug delivery system containing anti-psoriatic herbal drug such as Commiphora mukul and Quercetin for treatment of psoriasis. Liposphere were prepared separately for both the drugs by using Precirol ATO 5, Phosphotidylcholine, poloxamer 338. Physicochemical characteristics of the liposphere such as, particle size, drug encapsulation efficiency were determined. Also, drug release and in vitro skin permeability were evaluated using Franz diffusion cells. The results showed that the maximum encapsulation efficiency was 83 % and 81.77 % for Commiphora mukul and Quercetin loaded liposphere respectively. In vitro study was observed that F1 liposphere gel attributed 89.28 % release in 1440 min (24 hr) and F2 conventional cream batch attributed 80.24 % release in 540 min (9 hr). As per the result it was observed that liposphere gel gives more sustained release as compared to conventional cream. The results substantiate that liposphere gel containing combination of Commiphora mukul and Quercetin can be an efficacious for the treatment of psoriasis.
12 illus, 7 tables, 48 ref
VERMA V, KAUSHIK D
041529 VERMA V, KAUSHIK D (Pharmaceutics Dep, Hindu Coll of Pharmacy, Sonipat, Haryana, Email: dineshkoushik07@yahoo.com) : Mupirocin mounted copper nanoparticle offered augmented drug delivery against resistant bacteria. Indian J Pharm Edu Res 2020, 54(3), 637-46.
In present investigation, mupirocin coupled copper nanoparticles were synthesized to overwhelm drug resistance in Staphylococcus aureus, responsible for dermal skin infections. Mupirocin (Anclaima Pvt. Ltd. India), copper sulphate (Thermo Fisher Scientific, India), Tri sodium citrate (Nice chemicals, India) Copper nanoparticles were produced by size reduction method by using Copper Sulphate and Tri sodium citrate. CuNPs were merged into gel base of carbopol which was formed by hot method. Carbapol gel shows no phase separation. The particle size of CuNPs was found to be 413.0± 30.2nm. The % EE was found to be 65.2 %. On description unilamellar, sphere-shaped vesicles with soft surface were detected under transmission electron microscopy. XRD of CuNPs was found out crystalline in nature. The zeta potential of nanoparticle shows less aggregation of particle with - 15.1 ± 3.69 mV value. The amount of copper content was measured 5.9 microgram/10 mg of nanoparticles. In vitro release study of Cu NPs shows 96.5 % release of drug and show effective antibacterial activity against Staphylococcus aureus. Mupirocin copper nanoparticles were produced and show excellent antibacterial activity upon S. aureus.
16 illus, 4 tables, 41 ref
PANDA S
041528 PANDA S (Centurion Univ of Technology and Management, R.Sitapur, Odisha - 761 211, Email: subhraraj4u@gmail.com) : Molecular interaction of polymer dextran in sodium hydroxide through evaluation of thermo acoustic parameters. Indian J Pharm Edu Res 2020, 54(3), 630-6.
To find out the molecular interaction of solute dextran of different concentration with sodium hydroxide as a solvent. Dextran of molecular weight 70000 dalton and aqueous 1(N) Sodium hydroxide. To Measure the density by specific gravity bottle, Viscosity by Ostwald’s viscometer and ultrasonic velocity through ultrasonic interferometer of the solution and to calculate the thermo acoustical parameters using the measured parameters. Ultrasonic wave propagation affects the physical properties of the medium and hence furnishes information on the physics of liquid and solution. I have used the measured parameters, like ultrasonic velocity, density, viscosity and evaluated parameters to understand the solute-solute and solute-solvent interactions in the solution containing dextran with sodium hydroxide. The effect of frequency on thermo acoustical parameters had been studied. From the above studies, the nature of forces between molecules such as hydrogen bonds, charge transfer complexes, breaking of hydrogen bonds and complexes had been interpreted. Intermolecular forces (electrostatic forces between charged particles of a permanent dipole and an induced dipole molecules) are weak. Structural characteristics of the components arising from geometrical fitting of one molecules in to another due to the difference in shape and size of the molecules. In the present study ultrasonic velocity (U), viscosity (η) and density (ρ) have been measured at temperature 308 K in the solution of sodium hydroxide with polymer dextran in the concentration range 0.1% to 1 % at four different frequencies i.e. 1 MHz, 5 MHz, 9 MHz and 12 MHz using ultrasonic interferometer. The measured values of ultrasonic velocity (U), viscosity (η) and density (ρ) have been used to calculate the thermoacoustic parameters namely free volume (Vf), internal pressure (i), attenuation coefficient /absorption coefficient (α), Rao’s constant (R) and Wada’s constant (W) etc, These acoustical parameters are highly essential in studying various types of molecular interactions in liquid solution and provide qualitative information regarding the physical nature and quality of the molecular interaction in binary mixture dextran 1(N) sodium hydroxide. The molecular interactions like electrostriction, acceptor-donor association, dipole-dipole association and hydrogen bonding have been analyzed based on these parameters. Molecular interactions provide an understanding of the fundamental problems concerned with the mechanism of chemical and biochemical catalysis and the paths of the chemical reaction.
12 illus, 4 tables, 12 ref
SAROJ S, RAJPUT S
041524 SAROJ S, RAJPUT S (Pharmaceutical Quality Assurance Dep, Baroda Univ, Vadodara - 390 002, Gujarat, Email: sjrajput@gmail.com) : Bioavailability and dissolution rate enhancement of an anticancer drug bicalutamide by encapsulation into mesoporous silica nanoparticles: Effects of amine functionalization and caco-2 cell permeability study. Indian J Pharm Edu Res 2020, 54(3), 589-601.
The present study was undertaken with the aim of dissolution rate and Bioavailability enhancement of anticancer drug Bicalutamide (BIC) via encapsulation into mesoporous silica nanoparticles (MSNs). The bare (MCM-41) and surface decorated MSNs were subjected to thorough characterization pre and post drug loading by Fourier transform infrared spectroscopy, Nitrogen sorption analysis, Differential Scanning Calorimetry, Thermogravimetric analysis, Small angle and wide angle X-ray diffraction, Scanning electron microscopy and Transmission electron microscopy. Introduction of Nitrogen post functionalization was confirmed by the elemental analysis. Synthesized MSNs were surface decorated with amine groups (AMN-MSN) and in-depth study of effect of functionalization and food on dissolution kinetics was done. Developed MSNs and AMN-MSNs were thoroughly characterized pre and post BIC loading. In vitro intestinal permeability study was performed to determine the apparent permeability of synthesized MSNs. The formulations were also investigated for their in vivo behaviour by oral administration to male Swiss albino mice and various pharmacokinetic parameters calculated. A significant increase in permeability was obtained the dissolution rate and bioavailability were found to be 3.12 and 2.71 times enhanced in MCM-41 as comparison to the BIC suspension. Thus, MSNs could serve as an effective platform for delivering of various anti-cancer drugs and enhancing their efficiency.
10 illus, 8 tables, 21 ref
HOODA T, SHARMA S, GOYAL N
041511 HOODA T, SHARMA S, GOYAL N (Uttarakhand Technical Univ, Rohtak - 124 001, Haryana, Email: tanujhooda2010@gmail.com) : Synthesis, in-silico designing, SAR and microbiological evaluation of novel amide derivatives of 1-(4-Nitrophenyl)-2-(3-methylbenzo[b] thiophen-6-yl)-1H-benzo[d]imidazole-5-carboxylic acid. Indian J Pharm Edu Res 2020, 54(2), 471-83.
Due to this increasing predicament of antibiotic confrontation, the lot of distinct antibiotics available is dwindling and there are only smatterings of new antibiotics in the drug development channel. Therefore, an intense necessitate for new antimicrobial drugs. In current study, we have synthesized the new derivatives with the help of molecular docking studies and investigated antimicrobial activities. By focusing the enzymes i.e. aminoacyl-tRNA synthetase (AaRS) and tyrosyl-tRNA synthetase, new amides of 2-(3-methylbenzo[b]thiophen-6-yl)-1-(4-nitrophenyl)-1H-benzo[d]imidazole-5-carboxylic acid were synthesized and inhibition by docking study precedence to antimicrobial action. Studies were accomplished on a designed library of amide derivatives with the help of docking softwares i.e. AutoDock Vina 4.2 and Schrodinger’s maestro package against crystal structure of enzymes (PDB ID: 1wny.PDBQT and1jil.PDBQT). Based upon their dock score, superlative 23 focused amide derivatives of 2-(3-methylbenzo[b]thiophen-6-yl)- 1-(4-nitrophenyl)-1H-benzo[d]imidazole-5-carboxylic acid were synthesized and further investigated for in vitro antimicrobial. Among the library, superlative compounds C-1, C-10 and C-19 having tremendous dock score by AutoDock Vina/Schrodinger’s maestro against 1wny.PDBQT:1jil.PDBQT-9.0:-9.9/ -5.144:-5.328,-9.2:-9.4/ -5.007:- 5.369, -9.0:-9.6/ -5.184:-5.264 as compared to standard drug dock score -10.2:- 10.6/-5.847:-5.895.C-1, C-10 and C-19 derivatives also exhibited good MIC against six representative micro-organisms as compared to standard by tube dilution method. In-vitro results revealed that a large number of synthesized compounds having good antimicrobial activity and dock score can be used for in vivo studies for future. In-silico studies and in vitro results comply with each other.
9 illus, 3 tables, 30 ref
JAYAKAR V, LOKAPUR V, SHANTARAM M
046594 JAYAKAR V, LOKAPUR V, SHANTARAM M (Studies and Research in Biochemistry Dep, Jnana Kaveri PG Centre, Chikka Aluvara Kodagu- 571 232, Email: manjula59@gmail.com) : Identification of the volatile bioactive compounds by GC-MS analysis from the leaf extracts of Garcinia cambogia and Garcinia indica. Med Plants 2020, 12(4), 580-90.
Natural compounds originally derived from plants are historically considered a useful source of potential therapeutic agents, and are known to play essential roles in human diseases. The aim of the current study was to investigate the presence of bioactive compounds in hexane and methanol extracts of Garcinia cambogia and G. indica plant leaves. Both plant leaves were collected, shade dried, made into fine powder and extracted with organic solvents using Soxhlet extractor. The extracts were then analysed for the presence of phytochemicals by gas chromatography-mass spectrometry (GC-MS). The mass spectrum of the chromatography was matched with NIST and WILEY libraries. The GC-MS analysis revealed the presence of 11 and 17 bioactive compounds from the hexane and methanol extracts of G. cambogia respectively. Likewise, G. indica showed 14 compounds each from hexane and methanol extracts. The potent medicinal property within the plant extracts is due to the secondary metabolites present in the plant, which are identified by GCMS. The present investigation revealed preliminary information on bioactive components present in G. cambogia and G. indica leaf extracts, which can open a big platform for pharmacological companies to formulate various drugs from Garcinia species.
8 illus, 5 tables, 36 ref
BINDU G, DEVI V R, RAVI KUMAR B S, RAVI KIRAN S
046593 BINDU G, DEVI V R, RAVI KUMAR B S, RAVI KIRAN S (Biochemistry Dep, Aurora’s Degree & PG Coll, Hyderabad- 500 020, Email: srksuripeddi@gmail.com) : Chemical composition and in vitro potential activity on glucose metabolism and cytotoxicity of leaves of Erythroxylum monogynum Roxb.. Med Plants 2020, 12(4), 568-79.
The aim of this study was to screen extracts from the leaves and stems of Erythroxylum monogynum for in vitro antidiabetic activity by assessing the α-amylase and α-glucosidase inhibition activities. The bioassay guided fractionation of the petroleum ether extracts of leaves followed by AgNO3 -TLC, GC-MS, NMR and Mass spectrometry led to the identification of two new sterols, 4-methyl ergosta-7, 23-dien-3β-ol and 4-methyl ergosta-7, 24 (28)-dien-3β-ol. The 4- methyl ergosta-7, 23-dien-3β-ol and 4-methyl ergosta-7, 24 (28)-dien-3β-ol showed marked α-amylase and α-glucosidase inhibitory activities with IC50 of 41.52 & 56.42 and 45.47 & 61.71 mg/ml respectively. The essential oils from leaves and stems were obtained by hydrodistillation and the chemical composition was determined by GC and GC-MS. The three monoterpene alcohols, isofenchol, isopulegol and isothujanol were isolated by preparative GC and their enzymes inhibition was evaluated. Both the oils and monoterpene alcohols demonstrated excellent inhibition of α-amylase and α-glucosidase activities with IC50 < 100 mg/ml. Subsequently all the isolated compounds and essential oils were subjected to cytotoxicity using MTT assay wherein, all the compounds presented low level of toxicity at all concentrations tested. The results showed remarkable α-amylase and α-glucosidase inhibitory activity of oils and all the compounds with low toxicity suggesting for exploration as an alternative to the conventional hypoglycemic agents.
10 illus, 4 tables, 32 ref
SINGH M, PRASHAR Y
041505 SINGH M, PRASHAR Y (Pharmacology Dep, Rayat Institute of Pharmacy, Nawanshahr - 144 533, Punjab, Email: yashprashar@gmail.com) : Cerebral cortex and hippocampal protection mediated by Callistemon viminalis in aluminium chloride induced alzheimer’s disease. Indian J Pharm Edu Res 2020, 54(2), 422-31.
The study was carried out to evaluate the neuroprotective effect of methanol extract of Callistemon viminalis in aluminium chloride induced dementia of alzheimer’s type in mice. Swiss albino mice of either sex were divided into 5 groups: vehicle control; AlCl3 + normal saline; AlCl3 + rivastigmine; AlCl3+ extract (50 mg/kg; p.o); AlCl3 + extract (100 mg/kg; p.o). The following parameters were analyzed in all groups: a) Behavioral parameters- morris water maze test, b) Biochemical parametersAchE level, GSH level, SOD level, catalase level and nitrite level. Histopathological studyHippocampus and cerebral cortex region of mice brain. The presence of various phytoconstituents like betulinic acid, ursolic acid, β-sitosterol and lupeol reported through TLC, have a potent role as antioxidant and also known to improve blood flow as well as reduce plaque formation which proves that the extract of this plant can be used in alzheimer. Oral administration of MECV caused significant (p<0.01) decrease in escape latency time and significant (p<0.01) increase in total time in a dose dependent manner as compared to the aluminium chloride treated group. Additionally, post treatment with MECV (50mg/kg and 100 mg/kg) showed significant (p<0.01) decrease in AchE and nitrite level and significant (p<0.01) increase in the GSH, catalase and SOD level in mice brain. The histopathology of hippocampus and cerebral cortex of mice brain showed that the toxicity induced by the aluminium chloride was markedly reduced by the MECV. The normal histoarchitecture pattern of the hippocampus and cerebral cortex was also preserved. The evidence regarding the presence of phytoconstituents and analytical studies confirming their presence, along with preclinical studies on mice with conclusive results in treatment of Alzheimer shown by the extract concludes that the extract exhibits neuroprotective effect.
9 illus, 5 tables, 30 ref
FADHOLLY A, ANSORI A N M, PROBONINGRAT A, NUGRAHA A P, ISKANDAR R P D, RANTAM F A, SUDJARWO S A
041504 FADHOLLY A, ANSORI A N M, PROBONINGRAT A, NUGRAHA A P, ISKANDAR R P D, RANTAM F A, SUDJARWO S A (Pharmacology Dep, Airlangga Univ, Jawa Timur 60115, Indonesia, Email: ags158@yahoo.com) : Apoptosis of HeLa cells via caspase-3 expression induced by chitosan-based nanoparticles of Annona squamosa leaf extract: In vitro study. Indian J Pharm Edu Res 2020, 54(2), 416-21.
Annona squamosa is reported has a significant cytotoxic activity in some cancer cells. Thus, this study aim to investigate Annona squamosa leaf extract induced by chitosan nanoparticles (nano-ASLE) to enhance their biological activity as anticancer agent on HeLa cells. Nano-ASLE (50, 100, 200, 400 µg/mL in DMSO) given on HeLa cells to determined IC50 value by MTT assay. Then, it was devided into three groups as follow IC50, 2IC50, 4IC50 continued with analysis of caspase-3 expression. The present study demonstrated that nano-ASLE can surpress HeLa cells proliferation with the IC50 value of 344.48 µg/mL and rapid enhancement of caspase-3 activity has the mean score of 65.3 cell expression and the lowest score shows 45.3 cell expression. Nano-ASLE lead to HeLa cell death via the mitochondrial pathway on caspase-3 expression. In addition, the further studies are needed to obtain the loading efficiency, release of drug concentration and in vivo study of nano-ASLE to suppress HeLa cells.
4 illus, 22 ref
CINAR I, GULAPOGLU M, SULEYMAN H
041502 CINAR I, GULAPOGLU M, SULEYMAN H (Pharmacology Dep, Erzincan Binali Y?ld?r?m, Kampusu - 25030, Erzincan, TURKEY, Email: halis.suleyman@gmail.com) : Biochemical investigation of the protective effect of thiamine pyrophosphate on methotrexate-induced gastrotoxicity in rats. Indian J Pharm Edu Res 2020, 54(2), 397-402.
The aim of the study is to investigate the protective effect of thiamine pyrophosphate on methotrexate- induced gastrotoxicity biochemically in rats and to compare it with thiamine. Rats were divided into four groups as sham (SG), thiamine+ methotrexate (TAMTX), thiamine pyrophosphate+methotrexate (TPMTX) and Methotrexate (MTX) groups. 5 mg/kg methotrexate was administrated to 24 hrfasted rat groups by oral gastric tube except sham rats. 20 mg/kg thiamine was injected to TAMTX group and 20 mg/kg thiamine pyrophosphate was injected to TPMTX group i.p. 5 min before the methotrexate administration. Equal amount distilled water was injected i.p. to SG and MTX groups. 6 hr after the methotrexate administration, the rats were sacrificed with high dose thiopental anesthesia (50 mg/kg). The stomachs of the rats were extracted and MDA, MPO, GSH and SOD analyzes were performed. Biochemical results were evaluated by comparing among groups. While tGSH and MDA levels and MPO and SOD activities were 4.2±0.6, 10.0±0.9, 7.4±0.8, 5.2±0.9 µmol/g in MTX group, these parameters were 11.0±1.0, 3.4±0.4, 3.3±0.5, 13.2±1.1 µmol/g in SG group in the gastric tissue. These parameters were measured as 4.8±0.8, 8.7±0.8, 5.9±0.5, 6.1±0.8 µmol/g in TAMTX group and 10.8±0.8, 4.0±0.5, 3.6±0.4, 10.5±0.9 µmol/g in TPMTX group. The results showed that thiamine pyrophosphate prevented methotrexate induced oxidative damage in the gastric tissue, but thiamine could not prevent.
1 illus, 2 tables, 26 ref
RAI N, BAL T, SWAIN S
041501 RAI N, BAL T, SWAIN S (Pharmaceutical Sciences and Technology Dep, Birla Institute of Technology, Ranchi - 835 215, Jharkhand, Email: trishna.bal@gmail.com) : In vitro evaluations of biodegradable polyacrylamide grafted moringa bark gum graft copolymer (mog-gpaam) as biomedical and controlled drug delivery device synthesized by microwave accelerated free radical synthesis. Indian J Pharm Edu Res 2020, 54(2), 385-96.
The present work is based on preparation of different grades of Moringa Bark Gum (MOG) with Acrylamide (AM) with varying amount of AM (monomer) and APS (redox initiator) using microwave accelerated free radical reaction. In the current work, the Moringa bark gum grafted with acrylamide graft copolymer was tested for tissue engineered polymeric scaffold as well as controlled drug delivery system using metronidazole as a model drug. The microwave radiation process was used along with redox initiator for the graft copolymerization process and the optimization of the grades was done using % grafting efficiency, intrinsic viscosity. Moreover, the optimized grade GF4 was analyzed with FTIR as well as NMR proving efficient grafting has resulted along with TGA, OCA and XRD. The grade GF4 showed 95 % drug release for 24 hours with only 1 % hemolysis proving non-toxic and SEM images evidence its biodegradability thereby making the grade GF4 suitable for controlled release as well as tissue engineered scaffold. The results indicated that the optimized grade GF4 can be utilized as biodegradable polymer having applications in controlled delivery of drugs as well as scaffold for cell proliferation in wound healing and burn therapies.
11 illus, 7 tables, 36 ref
KHAN S, GANGANE P S, MAHAPATRA D K, MAHAJAN N M
041484 KHAN S, GANGANE P S, MAHAPATRA D K, MAHAJAN N M (Pharmaceutics Dep, Dadasaheb Balpande Coll of Pharmacy, Nagpur - 440 037, Maharashtra, Email: p.gangane@gmail.com) : Natural and synthetic polymers assisted development of lurasidone hydrochloride intranasal mucoadhesive microspheres. Indian J Pharm Edu Res 2020, 54(1), 213-22.
To avoid the first-pass metabolism of the drug (lurasidone HCl) and further improving its contact time with the nasal mucosa, intranasal mucoadhesive microspheres were developed by using natural (chitosan) and synthetic (Eudragit L 100) polymers by spray-drying method. The study aims to enhance the systemic drug absorption via the nasal membrane and to further evaluate the effect of polymers on the drug release profile. The microspheres of each polymer were prepared in three different ratios with one blank batch, where the effect of concentration of polymer was assessed with all six formulations with respect to change in particle size and entrapment efficiency. The prepared microspheres were assessed for the essential parameters such as particle size, production yield, entrapment efficiency and histopathological study. The excipients-drug substance compatibility was assessed and their associative behavior was comprehensively studied by Differential Scanning Calorimetry (DSC), X-ray Diffraction (XRD) and Scanning Electron Microscopy (SEM). The particle size analysis also revealed that all the formulations had particle size in the range of 10-15 μm which is suitable for intranasal administration. The optimized batch of chitosan microspheres (CH-2) and optimized batch of Eudragit L 100 microspheres (EU-1) formulations showed maximum drug loading of 68.3 % and 74.9 % whereas the cumulative drug release was found to be 76.36 % and 80.18 %, respectively. From the obtained results, it was concluded that the study showed a satisfactory attempt to formulate mucoadhesive microspheres with improved absorption rate and contact time of drug with nasal mucosa.
7 illus, 1 table, 31 ref
BORSE V A, GANGUDE A B, DEORE A B
041483 BORSE V A, GANGUDE A B, DEORE A B (K. B. H. S. S. T’s. Institute of Pharmacy, Nashik - 423 105, Maharashtra, Email: vishwanathborse7@gmail.com) : Formulation and evaluation of antibacterial topical gel of doxycycline hyclate, neem oil and tea tree oil. Indian J Pharm Edu Res 2020, 54(1), 206-12.
To formulate novel topical antibacterial gel containing Doxycycline Hyclate, Tea tree oil and Neem oil to evaluate their antibacterial activity. Formulation excipients were selected using Drug-excipients compatibility study. Prepared gel was subjected to various evaluation parameters like pH, viscosity, spreadability, homogeneity, drug content uniformity, in-vitro drug diffusion and antibacterial activity. Prepared topical gel of doxycycline Hyclate was shown pH range 5.3±0.010 to 6.7±0.015, viscosity range 386±28.70 to 680±50.40 cp, spreadability range 18.14±0.98 to 28.13±2.18 g.cm/s and homogeneous. Prepared gel was shown uniformity in drug content which ranges from 94.41±0.61 to 97.44±0.69 %, zone of inhibition ranges 13.66±1.69 to 32.00±1.63 mm for Staphylococcus aureus, 04.00±1.63 to 12.33±0.94 mm for Pseudomonas aeruginosa and 11.66±0.94 to 33.33±1.24 mm for Propionibacterium acne. Prepared gel formulations were shown the negligible amount of drug diffusion, not more than 3.22±0.04 % was shown the non-fickian type of diffusion through the egg membrane. Formulation F8 was shown better antibacterial activity as compared to its other formulations. As the concentration of neem oil and tea tree oil was increased from 0.5 to 3 % and 0.5 to 2 % respectively in the gel, antibacterial activity was synergistically improved against Staphylococcus aureous, Pseudomonas aeruginosa and Propionibacterium acne. The prepared gel formulation was found useful for topical application due to its negligible diffusion, good spreadability, neutral pH, low viscosity and no irritation on human skin.
4 tables, 24 ref
KHAN D, MOHAMMED M, UPAGANLAWAR A, UPASANI C D, UNE H D
041477 KHAN D, MOHAMMED M, UPAGANLAWAR A, UPASANI C D, UNE H D (Y. B. Chavan Coll of Pharmacy, Aurangabad - 431 001, Maharashtra, Email: hemantdune@rediffmail.com) : Ameliorative potential of Allium cepa lam. leaves on diabetes induced and chronic constriction injury induced neuropathic pain in experimental rats. Indian J Pharm Edu Res 2020, 54(1), 143-9.
Neuropathy can be induced in rats by peripheral injuries, depending on compression of complete or a section of sciatic nerve and chemically by Streptozotocin (STZ). In the present study neuropathic pain were induced in rats by two methods, chronic constriction injury (surgical model) and STZ (40mg/kg/i.p.) induced diabetes (drug induced model). In both the models, behavioural as well as markers of oxidative stress were studied. Behavioural parameters were tested using vonfrey hair and Randall Selitto analgesiometer whereas biochemical parameter includes glycosylated haemoglobin and markers of oxidative stress. The study was further supported by histopathology of sciatic nerve. Flavonoid rich extract of Allium cepa Lam. leaves was administered at three different doses viz. 25, 50 and 100mg/kg/p.o to the rats with neuropathic pain. Both the models of neuropathic pain showed significant alteration in behavioural as well as oxidative stress parameters. Treatment of Allium cepa leaves extract showed dose dependent improvement in behavioural and biochemical parameters towards normal (p value <0.001, <0.05 and <0.01). The altered histopathological changes in sciatic nerve were also significantly improved as compared to rats with neuropathic pain. The neuroprotective effects of the Allium cepa leaves extract is a virtue of its strong antioxidant activity.
3 illus, 1 table, 26 ref
DARBAR S, SAHA S, PRAMANIK K, CHATTOPADHYAY A
041476 DARBAR S, SAHA S, PRAMANIK K, CHATTOPADHYAY A (Jadavpur Univ, Kolkata - 700 032, West Bengal, Email: atischatterjee@gmail.com) : Preliminary assessment of acute and 28-day repeated dose oral toxicity of a newly developed herbal mixture on experimental animal. Indian J Pharm Edu Res 2020, 54(1), 135-42.
Toxicity is an expression of being poisonous, indicating the state of adverse effects led by the interaction between toxicants and cells. The present study was designed to evaluate the acute oral toxicity study and 28 days repeated toxicity study of Herbal Mixture (HM) according to OECD guidelines. In acute oral toxicity study, Herbal mixture was administered at 2000mg/kg orally and animals were observed for toxic signs at 30 min, 1, 2 and 4 hr and thereafter once a day for the next 14 days. In repeated dose-28-day toxicity study, the animals were divided into four groups of 6 animals each. Group-1 animals served as a control. Group II Animals received low dose of test drug 100 mg/kg (orally). Group III animals received middle dose of test drug 200 mg/kg (orally) once daily for 28 days respectively. Group IV animals received high dose of test drug 400 mg/kg (orally) once daily for 28 days respectively. The study results showed that neither the acute toxicity study of herbal mixture at the dose level of 2000mg/kg nor the repeated dose study did not produce any toxic sign or mortality during study. In repeated dose toxicity study, no significant changes were observed in the haematological and biochemical parameters, relative organ weight, gross necropsy and histopathological examination with herbal mixture treatment. The results of the present study suggest that LD50 of newly developed Herbal Mixture (HM)>2000mg/kg and the mixture is completely safe and non-toxic for therapy.
5 illus, 5 tables, 14 ref
GOYAL A, GARABADU D
041475 GOYAL A, GARABADU D (Pharmacology Dep, GLA Univ, Mathura, Uttar Pradesh, Email: debapriya.garabadu@gla.ac.in) : Bilateral ovariectomy decreases the levels of cyclic nucleotides and nuclear phosphorylated estrogen receptor-alpha in memory-sensitive rat brain regions. Indian J Pharm Edu Res 2020, 54(1), 125-34.
The level of phosphorylated Estrogen Receptor alpha (ERα) in the nucleus was investigated in different memory-sensitive brain regions of estrogendeficient female rats. Further, the levels of cyclic nucleotides were estimated in those brain regions to draw a possible correlation with phosphorylated ERα signaling. Bilateral ovariectomy was performed on the first day of the experimental schedule of 60 days. Behavioural analysis was performed and various biochemical parameters were assessed in discrete brain regions of rat. Ovariectomy caused a significant deterioration in learning and memory of the animals in terms of increase in transfer latency, decrease in time spent and percentage of total distance traveled in the target quadrant in Morris Water Maze (MWM) test protocol. Further, ovariectomy reduced the spontaneous alteration behavior of the rats in the Y-maze test. There was a significant increase in cholinergic dysfunction in respect of decrease in the activity of choline acetyltransferase and level of acetylcholine and an increase in the activity of acetylcholinesterase in rat hippocampus, pre-frontal cortex and amygdala. Subsequently, ovariectomy significantly reduced the extent of phosphorylation and translocation of ERα in such rat brain regions. Moreover, ovariectomy caused a decrease in the levels of cyclic nucleotides such as cAMP and cGMP in these rat brain regions. Additionally, there was a significant positive correlation between the ratio of cyclic nucleotides (cGMP/cAMP) and nuclear p-ERα in all brain regions of these ovariectomized animals. The cyclic nucleotides could be a potential and alternate target to promote the phosphorylated ERα receptor-mediated mechanism during memory formation in estrogen deficiency condition.
8 illus, 39 ref
ABDOON I H, PARVEEN B, OSMAN B, MOHAMED M S, OSMAN W J A, AHMAD S
041472 ABDOON I H, PARVEEN B, OSMAN B, MOHAMED M S, OSMAN W J A, AHMAD S (School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi, Email: sahmad_jh@yahoo.co.in) : Immunomodulatory potential of Leptadenia arborea in immune-challenged rats. Indian J Pharm Edu Res 2020, 54(1), 101-7.
Plant-based remedies play a crucial role as powerful health aid worldwide. In recent years, the usage of complementary and alternative medicines has grown rapidly. The objective of the present study was to evaluate the immunomodulatory effects of methanolic extract of Leptadenia arborea leaves in BCG-immunized rats. L. arborea extract suspended in 1 % carboxymethyl cellulose (CMC) was administered in three doses viz 50, 100 and 200 mg/kg, p.o. All animals were challenged with 0.05 ml BCG, sc on day 0. Levamisole (18 mg/kg body weight; p.o.) was used as a positive control group. L. arborea extract exhibited a significant dose- and time-dependent increase in the plasma levels of IFN-γ and TGF-β. On day 14, plant's extract significantly increased TNF-α level at dose 200 mg/kg. Moreover, L. arborea extract elicited an inhibitory effect on IL-10 levels that was significantly observed at dose 200 mg/kg of the plant extract. LD50 value was calculated to be 15.5 g/kg body weight and the extract didn't display any behavioral changes or clinical signs after 12 hr of treatment. L. arborea methanol extract showed immunostimulatory effects through elevation of IFN-γ and thereby activation of cell-mediated immunity.
3 illus, 2 tables, 39 ref