043854   SARMA B (Chemistry Dep, Royal Global Univ, Guwahati, Assam) : Survey of medicinal plants with potential antidiabetic activity used by villagers in lower Assam districts of North-East, India. Int J Herb Med 2020, 8(1), 01-6.

Diabetes is rapidly emerging as serious and major public health-care problem throughout the world. It is a complex and chronic illness. Apart from currently available different synthetic drugs, many herbal drugs have been recommended for the treatment of diabetic patients. An ethnobotanical study focused on medicinal utility of antidiabetic plants was carried out among the rural village peoples of few lower Assam districts, of North-East, India. A large number of medicinally important plant species are found to be present in the study area. Our survey has reported as many as 41 numbers of medicinal plant species belonging to 31 families. The most cited family was Moraceae, the most widely used plant part was the leaf and the most common mode of administration was juice. All these claims and findings need to be subjected to both phyto-and pharmaco-chemical investigations to assess the claimed activity with the aim of finding new potent antidiabetic drugs.

3 illus, 2 tables, 20 ref

043850   OGWUCHE C E, OGBU P, JOSHI R K (Chemistry Dep, Federal Univ of Petroleum Resources, Effurun, Delta, Nigeria) : Phytochemical antimicrobial and proximate analysis of the leaves of Mirabilis jalapa from Uvwie Delta state, Nigeria. Int J Herb Med 2020, 8(1), 39-45.

The leave extracts of Mirabilis jalapa collected from Uvwie local government were subjected to phytochemical screening, result show that the plant under study contains saponin, flavonoids, alkaloids, terpenoids, resins and phenols. Proximate analysis was carried out to determine ash content, crude protein, crude fibre, moisture content, lipid and nitrogen free extract. The result revealed the presence of high moisture content of 30 % and a low Lipid content of 3 %. The rest were obtained as follow; ash content 20 %, protein content 12.8 %, fibre content 8.22 % and nitrogen 25.98 %. Antimicrobial activity of Mirabilis jalapa leaf was tested on bacterial isolates from the standard laboratory. Bacterial isolates include Bacillus species, Pseudomonas, Micrococcus and E. coli. Five different concentrations (0.1, 0.2, 0.05, 0.025 and 0.012 (mg/ml)) of both the extracting solvents and the extracts were tested on the isolates. The results revealed that Mirabilis Jalapa is a strong antibiotic against E. coli, Bacillus and Pseudomonas but weak against Micrococcus.

17 tables, 12 ref

041954   SALAMA K F, OMAR E O M, ZAFAR M (Public Health Dep, Imamm Abdul Rehman Bin Faisal Univ, Dammam 34212, Saudi Arabia, Email: researchmubshir@outlook.com) : Assessment of BTX concentration around fuel station in eastern province kingdom of Saudi Arabia. Indian J Occup Environ Med 2020, 24(3), 163-7.

The aim of this study is to determine the benzene, toluene, and xylenes (BTX) concentration levels in and around fuel station and its expected health risks in the City of Dammam and Al-Khobar, Saudi Arabia. Forty fuel dispensing facilities were randomly selected on the basis of three different areas, residential, traffic intersection, and petrol pump locations (refueling stations). coconut shell charcoal cartridges were used for samples collection and portable Ambient Analyzer was used for measuring BTX (benzene, toluene, and xylenes) concentration. Results show that the average concentration of benzene, toluene, and xylenes level around fuel stations was 10.30, 4.09, and 2.47 ppm, respectively. All means of concentration values of BTX around residential, traffic intersection, and fuel stations are exceeding the limits of air quality standards values (P < 0.01). The mean concentration of BTX around residential area, side street, and direct street was benzene 8, 12.2, and 11.5 ppm, toluene 2.5, 5.95, and 3.37 ppm, and xylenes 2, 2.13, and 2.7 ppm. Hazard Quotient (HQ) was more than >1 which showed that carcinogenic probability has increased those exposed to this toxic chemical. Ambient concentration of BTX was high compare to neighboring residential area and 100 m from the fuel station which can negatively affect on health of several residences. The Environmental contamination associated with BTX in petrol fuel stations impulses the necessity of preventive programs to reduce further air quality deterioration and reduce the expected health risks.

2 illus, 5 tables, 29 ref

043843   KENDAGANNA P H , SHRUTHI G , KARUNAKAR P , PATIL S, KOLLUR S P, SRINIVASA C , SHIVAMALLU C (Biotechnology and Bioinformatics Dep, JSS Academy of Higher Education and Research, Mysuru, Karnataka, Email: chandans@jssuni.edu.in) : In Silico Study of Ceftazidime and Piperacillin Against Penicillin-Binding Protein 2, Beta-Lactamase (OXA-1 and SHV-28) of Klebsiella pneumoniae U25. Int J Green Pharm 2020, 14(4), 403-11.

To combat the action of beta-lactams, Klebsiella pneumoniae launches the enzymatic action by producing beta-lactamases to destruct the activity of ceftazidime and piperacillin. In our research, we want to know the action of ceftazidime and piperacillin on penicillin-binding protein2 (PBP2) and also does it have any interactions with beta-lactamases (OXA1 and SHV-28). Our idea is to prevent the action of beta-lactamases on ceftazidime and piperacillin. Hence, we have modified the beta-lactam core structures of ceftazidime and piperacillin and done the comparative docking interaction studies. K. pneumoniae U25 has been selected for the comparative docking analysis study with ceftazidime and piperacillin antibiotics by modifying its structures and targeting them against PBP2 and beta-lactamases (OXA-1 and SHV-28). Our docking analysis revealed that ceftazidime and modified ceftazidime are forming hydrogen bonds, but piperacillin and modified piperacillin are showing hydrophobic interactions with an active site serine residue (Ser316) of PBP2 responsible for the transpeptidase activity in K. pneumoniae U25. Protective action by beta-lactamases (OXA-1 and SHV-28) to K. pneumoniae U25 against beta-lactam antibiotics is also revealed through our study by docking interactions of Ser71 of OXA-1 and Ser66 of SHV-28 with the ceftazidime, modified ceftazidime, piperacillin, and modified piperacillin.

15 illus, 21 ref

043828   BENSATAL A , RAHMOUN D , ARDJA S A , CHEIKH M , KAHOUADJI A, BEKHIT M (Chemistry Dep, Djelfa Univ, Algeria, Email: matmatidz@gmail.com) : In vitro antilithiasic activity of saponins rich fraction from the leaves of Zizyphus lotus. Int J Green Pharm 2020, 14(3), 280-5.

A large number of medicinal plants have been used in Algeria since antiquity, which claims the efficient cure of urinary stone, one of these plants is the specie Zizyphus lotus (Family: Rhamnaceae). Leaves of this species are traditionally used for the treatment of many diseases. Nowadays, numerous clinical studies have provided reliable results on the effects of several hundred plants on several diseases such as the problem of urinary stones. The objective of this study is evaluated in vitro the activity antilithiasic of the extract saponins created fraction. Inhibition and dissolution of calcium oxalate (CaOx) were studied by the use of the techniques turbidimetric and gravimetric, using a ultraviolet–visible spectrophotometer and a precision balance. Qualitative secondary metabolites determination in the leaves of Z. lotus showed the presence of polyphenols, saponins, flavonoids, alkaloids, and tannins, and the yield of the fraction rich in saponins is equal to 1.41%. The absorbance decreased with the increase in the concentration of extract indicating that decreased the nucleation of CaOx particles with inhibition at 55.23 ± 1.23 %. The weight of CaOx crystal decreased with the increase in the concentration of saponins, and the extract at 100 % concentration possesses a maximum percentage of dissolution equal to 91.95 ± 0.72 %. This effect could be attributed to Ca²⁺ chelation by the compounds that exist in this fraction. This study indicates that extract can be considered as feasible natural products to improve the efficiency of CaOx inhibition and dissolution.

3 illus, 2 tables, 30 ref

043824   NAIDU M A , THIRUMALAI T , ARUMUGAM G (Biochemistry Dep, Kanchi Shri Krishna Coll of Arts and Science, Kanchipuram - 631 551, Tamil Nadu, Email: bioaru.g@gmail.com) : Biosynthesis of silver nanoparticles using Ailanthus excelsa leaf extract and their antibacterial activity. Int J Green Pharm 2020, 14(3), 247-56.

The objective of the study was to evaluate the antibacterial activity of silver nanoparticles (AgNP) synthesized from Ailanthus excelsa against human pathogens. Ultraviolet-visible (UV-Vis) spectrophotometry and transmission electron microscopy (TEM) were performed to confirm the formation and stability of AgNPs. Antibacterial activities of the synthesized AgNPs were determined using the agar well diffusion assay method. UV-Vis spectrum of the aqueous medium containing AgNPs showed an absorption peak at around 425 nm for the yellow to brown colored AgNPs synthesized from 10 to 3 (M) silver nitrate and the fixed volume fraction (ƒ = 0.2) aqueous leaf extract. TEM showed the formation of AgNPs with a size ranging from 15 to 25 nm. The X-ray diffraction patterns of AgNPs synthesized from leaf extract of A. excelsa clearly illustrates that the AgNPs were synthesized. The formed AgNPs showed good antibacterial activity against human pathogens. A. excelsa plant extract solution is potent for the green and eco-friendly synthesis of silver (Ag) nanoparticles, which provides efficient research applications.

9 illus, 30 ref

043820   BHATT S, ANJALY C T G, SHLINI P (Biochemistry Dep, Mount Carmel Coll, Bengaluru - 560 052, Karnataka, Email: shlinip1@gmail.com) : Molecular and pharmacokinetic properties of the histidine decarboxylase inhibitors from clove. Int J Green Pharm 2020, 14(2), 202-14.

Histidine decarboxylase is widely distributed in the gastrointestinal mucosa, mast cells, cerebrospinal fluid, bone marrow, and certain actively growing tumors. This enzyme has been studied till date of various organisms, but the mechanism of action had not been understood. In the present study, the inhibitory activity of flavonoids on purified histidine decarboxylase enzyme from bacterial source using a methanolic extract of clove was examined. Phytochemical screening of methanolic extract of clove was performed for the presence of various bioactive constituents. Further, the purification of flavonoids present in the spice extract was carried out by thin-layer chromatography (TLC) and high-performance liquid chromatography (HPLC) to isolate and identify the different flavonoids present in methanolic extract of clove. The inhibition of the enzyme was studied by checking the activity of an enzyme in the presence of varying concentrations of inhibitor. Dixon plot was plotted to determine the concentration of the inhibitor at which it inhibits the enzyme. Phytochemical screening of the clove extract revealed the presence of flavonoids in maximum in comparison to the other constituents. TLC and HPLC were carried out, which indicated the presence of ellagic acid, gallic acid, kaempferol, and quercetin in the methanolic extracts of the clove sample. The concentration of the clove extract in inhibiting the enzyme was found to be 0.9 µmoles from Dixon plot. All the components identified in HPLC quantification were subjected to software’s like Molinspiration and SwissADME to study the molecular properties, drug-likeness, and pharmacokinetics. In the present study, histidine decarboxylase and the various medical aspects in which the enzyme plays a role and where the function of the enzyme can be altered to treat the disease is highlighted to dictate their ability to be a promising lead compound. 

15 illus, 8 tables, 36 ref

043818   RAO T N , PATRUDU T B , RAO M V B , GANESH K (Chemistry Dep, GITAM Univ, Hyderabad Campus, Telangana, Email: patrudupath@gmail.com) : Determination and quantification of imiquimod and its related impurities from bulk drug production by high-performance liquid chromatography. Int J Green Pharm 2020, 14(2), 186-94.

A simple, selective, precise, and inexpensive reversed-phase high-performance liquid chromatography method has been developed and validated for the determination of imiquimod and related impurities such as 4-Chloro-1-isobutyl-1H-imidazo[4,5-c] quinoline, 1-isobutyl-1,5-dihydro-imidazo[4,5-c] quinolin-4-one, 1-isobutyl-4-methoxy-1H-imidazo[4,5-c] quinoline, and N-(1-isobutyl-1H-imidazo[4,5-c]quinolin-4-yl)- hydroxylamine-O-sulfonic acid. The method was followed using spectrophotometric detection at 260 nm with a Phenomenex Luna-RP-C18 column (250 × 4.6 mm, 5 µm) at a flow rate of 1.0 mL/min. The mobile phase consisted of deionized water spiked with 1 % H₃ PO₄ (Solvent A) and acetonitrile (Solvent B). Imiquimod and the common four impurities were eluted at different time intervals from 10 to 20 min. The developed method was validated in terms of system suitability, specificity, precision, linearity, accuracy, limit of detection, and limit of quantification. The mobile phase composition of 1 % v/v H₃ PO₄ in water: acetonitrile (90:10 v/v), showed good separation and resolution. Therefore, the proposed analytical procedure could be useful for regular monitoring, pharma manufacturing labs, and research scholars.

4 illus, 11 tables, 20 ref

046728   AHMED A A, AL-TIMIMI R J, ABDULRASOL E A (Chemistry and Biochemistry Dep, Al-Nahrin Univ, Baghdad, Iraq) : Study the role of selenium in the p-selectin and e-cadherin serum levels in women with preeclampsia. Med Legal Update 2020, 20(1), 10.37506/v20/i1/2020/mlu/194404.

Preeclampsia (PE) is characterized by endothelial dysfunction with vasoconstriction due to cell adhesion molecules or mediators released by defective placentation. Platelet selectin (P-selectin) and epithelial cadherin (E-cadherin) are the cell adhesion molecules, is elevated in many inflammatory conditions including PE. To investigate if P-selectin and E-cadherin levels can be used as a marker for adverse outcomes in pregnancy complicated with PE. This study involved 90 pregnant women in their third trimester of pregnancy divided into2 group: Group A: involves 45 pregnant women with PE. Group B: involve 45 healthy pregnant women and normal fetal growth (Control group). The results show there were a high significant increase in the mean values of P-selectin with high increase in the mean values of E-cadherin in PE group when compared to control group. ROC curve shows sensitivity and specificity and false positive rate for predication of PE by P-selectin and E-cadherin in control and patients groups, and the maximum accuracy for the P-selectin and E-cadherin in discrimination between control and PE patients groups. There is an inverse relationship between cell adhesion molecules and selenium in PE compared with normal pregnancy. High level of serum P-selectin and E-cadherin are associated with the presence PE, which provide additional information for predicting of PE and preventing its complications and for better understanding pathogenesis of PE.

4 illus, 17 ref

043734   MOHAMMEDI H, MECHERARA-IDJERI S, HASSANI A (Organic Chemistry Dep, Sciences and Technology Houari Boumediene Univ, Bab Ezzouar, Algeria) : Variability in essential oil composition, antioxidant and antimicrobial activities of Ruta montana L. collected from different geographical regions in Algeria. J Essent Oil Res 2020, 32(1), 88–101.

Essential oils of Algerian Ruta montana collected from seven different regions characterized by diverse climatic conditions were investigated for their chemical components, oil yield diversity, antioxidant and antibacterial activities. The lowest (0.38 %) and the highest (1.45 %) yields in essential oils were observed in samples from Tizi ouzou and Djelfa, respectively. GC-MS and ¹³C-NMR analyses allowed the identification of forty components representing 87.8–99.2 % of the total oils. The main components were 2-undecanone (27.2–81.7 %), 2-nonanone (1.9–39.5 %) and 2-nonanyl acetate (tr – 24.8 %). Based on cluster analysis, two groups were determined, including high 2-undecanone and high 2-undecanone/2-nonanone/2-nonanol acetate groups. Antioxidant activity was evaluated by DPPH and reducing power assays. Samples from M’sila and Djelfa (semi-arid regions) presented the highest antioxidant activity (IC₅₀ = 49.6 ± 2.7 and 50.2 ± 3.3 mg/L, respectively). Antimicrobial activity was tested against eight microbial strains using the agar disc diffusion method. Overall, moderate activity was observed (inhibition zones' diameters ≤18 mm). This variation confirmed the impact of the climatic conditions on yield and chemical composition of essential oils as well as their biological activities.

7 illus, 5 tables, 52 ref

043732   HAMIDA N B, MARTÍNEZ-DÍAZ R A, HELA M, MSAADA K, OUERGHI Z, ANDRES M F, GONZALEZ-COLOMA A (Tunis El Manar Univ, Tunis, Tunisia) : Effect of salinity on the antiparasitic activity of hyssop essential oil. J Essent Oil Res 2020, 32(1), 69–78.

The present work reports the effect of salt treatment on Hyssopus officinalis growth, essential oil (EO) yield and composition and the antiparasitic effects of the oil against the plant (Phytomonas davidi and Meloidogyne javanica) and human (Trypanosoma cruzi) parasites. Our results showed that salinity decreased plant growth and EO yield of hydroponically cultivated plants of H. officinalis with increasing NaCl levels. Salinity also induced changes in the chemical composition of treated hyssop EOs, decreasing the monoterpene and increasing the sesquiterpene groups. The oxygenated monoterpenes, represented primarily by isopinocamphone and pinocarvone, were the major chemical class. The EOs from treated H. officinalis showed moderate antiparasitic effects against T. cruzi, independent of the salt treatment, stronger salt-dependent effects on P. davidi and also a high salt-dependent nematicidal activity against M. javanica. Therefore, a moderate salt treatment reduced plant growth and EO yield but increased its biocidal effects on plant parasites (P. davidi and M. javanica).

3 illus, 3 tables, 79 ref

043731   KUMAR A, KAMAL A, SINGH S, PADALIA R C, TADON S, CHAUHAN A, SAIKIA D, VERMA R S (Molecular Bioprospection Dep, CSIR-Central Institute of Medicinal and Aromatic Plants (CIMAP), Lucknow) : Chemical composition, antimicrobial activity, kinetics and mechanism of action of Himalayan-thyme (Thymus linearis Benth.). J Essent Oil Res 2020, 32(1), 59–68.

In this study, antimicrobial activity of the essential oil (EO) and extracts of Himalayan-thyme (Thymus linearis Benth.) was evaluated against nine pathogenic microbial strains using disc diffusion and microdilution broth assays. The chemical composition of the EO was determined by gas chromatography-flame ionisation detector (GC-FID) and gas chromatography-mass spectrometry (GC-MS). The molecular mechanism of action of the EO was investigated against three pathogenic bacteria (Staphylococcus aureus, Staphylococcus epidermidis and Enterococcus faecalis) and three fungal strains (Candida albicans, Candida glabrata, and Candida tropicalis) using the assays of protein leakage, and DNA and RNA leakage through the membrane. Major components of the EO were thymol (54.9 %), γ-terpinene (16.6 %) and p- cymene (5.2 %). The EO showed broadspectrum potent antibacterial and antifungal activity (MIC 240–990 µg/mL) against test strains. The EO damaged cell membranes and altered cell membrane permeability of test microorganisms. The EO showed a time- and dose-dependent bactericidal and fungicidal effect. It could act as a promising antimicrobial agent due to its short killing time.

3 illus, 2 tables, 41 ref

043730   RAHALI N, YOUNSI F, BOUSSAID M, MESSAOUD C (Biology Dep, Carthage Univ, Tunis Cedex, Tunisia, Email: chok.messaoud@yahoo.f) : Chemical variability of Hertia cheirifolia (L.) Kuntze essential oils and incidence on antioxidant and anticholinesterase activities. J Essent Oil Res 2020, 32(1), 48–58.

The essential oils of Hertia cheirifolia, collected from different bioclimatic zones of Tunisia, were analyzed by GC-MS and GC-FID. The major compounds were α-pinene (17.51–60.31 %), germacrene D (6.14–19.18 %), unknown drimenin isomer (9.39–32.39 %) and drimenin (0.46–33.61 %). The essential oil composition varied significantly between populations. The chemical differentiation among populations occurs regardless their eco-geographic appurtenances. The species essential oils exhibited antioxidant and antiacetylcholinesterase activities. However, the level of activity varied between populations. The highest scavenging activity characterized the essential oils of the species collected from Sousse and Zaghouan (22.26 and 21.35 mg TE/gEO). Essential oils from Sousse possessed the uppermost inhibition of β-carotene bleaching (37.82 mg BHT equivalent/gEO). Essential oils from Sousse and Makthar exhibited the highest reducing capacity (162.05 and 171.80 µmol Fe²⁺/gEO). Essential oils from Siliana possessed the highest chelating ability (17.55 mg EDTA equivalent/gEO). Those from Siliana and Sousse exhibited the highest antiacetylcholinesterase activity (3.03 and 2.91 mg donepezil/gEO).

3 illus, 5 tables, 46 ref

043728   SILVA K L C D, SILVA M M C D, MORAES M M D, CAMARA C A G D, SANTOS M L D, FAGG C W (Química Dep, Federal Rural de Pernambuco Univ, Recife, PE, Brazil) : Chemical composition and acaricidal activity of essential oils from two species of the genus Bauhinia that occur in the Cerrado biome in Brazil. J Essent Oil Res 2020, 32(1), 23–31.

Essential oils from the leaves of Bauhinia rufa and B. dumosa collected from the Cerrado biome in central Brazil were obtained by hydrodistillation and analyzed using GC and GC/MS. Both oils had a predominance of sesquiterpenes (B. rufa: 95.3 ± 0.5 %; B. dumosa: 97.2 ± 1.1 %). β-Caryophyllene (15.8 ± 0.5 %), epi-α-cadinol (12.8 ± 0.4 %), γ-muurolene (12.2 ± 0.4 %) and α-cadinol (10.0 ± 0.5 %) were identified as the major constituents of the B. rufa oil, whereas germacrene B (37.6 ± 1.2 %) and (E)- nerolidol (29.1 ± 0.6 %) were the major constituents of the B. dumosa oil. Both oils were toxic to Tetranychus urticae by fumigation (B. rufa: LC50 = 2.76 µL/L of air; B. dumosa: LC50 = 0.97 µL/L of air) and residual contact (B. rufa: LC50 = 30.46 µL/mL; B. dumosa: LC50 = 16.44 µL/mL). The results of the twochoice method revealed that the oils affect the behavior of the mite, interfering in its feeding and egglaying preferences.

3 illus, 2 tables, 34 ref

043727   JARAMILLO-COLORADOA B E , STASHENKOB E E, WINTERHALTER P (Cartagena Univ, Cartagena, Colombia) : Fractionation of four colombian essential oils by countercurrent chromatography and evaluation of their antioxidant activity. J Essential Oil Res 2020, 32(1), 12–22.

High-speed countercurrent chromatography (HSCCC) is widely used for isolation of biologically active compounds of plant extracts and essential oils (EOs) in preparative scale. The objective of this work was the prefractionation of EOs from Lippia alba, Aloysia citriodora, Lantana armata and Xylopia aromatica by HSCCC and the evaluation of the antioxidant activity in vitro of their EOs and fractions. The antioxidant capacity was determined by two different in vitro assays: 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical and 2,2ʹ-Azinobis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical cation. EOs and their fractions showed a low-moderate ability to trap the radical cation ABTS+ and DPPH radical.

4 illus, 4 tables, 43 ref

043726   TIETBOHL L A C , MELLO C B, SILVA L R , DOLABELLA I B, FRANCO T C , ENRÍQUEZ J J S , SANTOS M G , FERNANDESF C P , MACHADOA F P , MEXAS R (Federal Fluminense Univ, Niterói, RJ, Brazil, Email: msgonzalez@id.uff.br) : Green insecticide against chagas disease: effects of essential oil from Myrciaria floribunda (Myrtaceae) on the development of Rhodnius prolixus nymphs. J Essent Oil Res 2020, 32(1), 1–11.

The main strategy of interrupting Trypanossoma cruzi transmission is to control the vector populations. Studies of new agents with activity against these vectors have a priority interest. This study evaluated the insecticidal activity of the essential oil of Myrciaria floribunda against nymphs of R. prolixus. M. floribunda was collected in Jurubatiba Sandbank (southeastern Brazil). Leaves were extracted by hydrodistillation and the essential oil analyzed by mass spectrometry and flame ionization gas chromatography. The pure essential oil at various dilutions or purified 1,8-cineole was topically applied to R. prolixus. Sesquiterpenes were the main group detected followed by monoterpenes. M. floribunda essential oil, but not 1,8-cineole, significantly increased mortality and disrupted metamorphosis. Overaged nymphs and juvenoid-like insects were also observed. Our data indicate the special metabolites in the essential oil of M. floribunda as promising candidates for studying insecticidal activity and for use as environmentally friendly control compounds to Chagas disease vectors.

3 illus, 5 tables, 73 ref

046721   DAYEKH S H, HAMZAH M I, ATEAAI J A (Chemistry and Biochemistry Dep, AL- Nahrain Univ, Baghdad, Iraq) : Evaluation of salusin β in patients with prediabetes and type 2 diabetes mellitus. Med Legal Update 2020, 20(1), 10.37506/v20/i1/2020/mlu/194397.

Type 2 Diabetes mellitus is a group of metabolic disease characterized by increase blood glucose level (hyperglycemia) resulting from either defect in insulin production by pancreas or increase insulin resistance that lead to decrease insulin effect in the body. prediabetes It is stage before diabetes mellitus including impaired fasting glucose (IFG)where the fasting glucose level (6.1-7.O mmol/L) and impaired glucose tolerance (IGT after glucose load) glucose level (7.8-11 mmol/L).(salusin-β) It is a newly glass of peptide it is synthesized in many body tissues, like (skeletal muscle, human vascular smooth muscle cells, and endothelial muscle) it have important role in Diabetes pathogenesis it has been reported to involve in vascular inflammation and the relation between salusin β and diabetes through endothelial injury, salusin β increase inflammation in diabetes. It have essential role in pathological endothelial dysfunction. Method: by using ELISA kit, we measured serum level of salusin β in 30 patients with prediabetes and 30 patients with type 2 DM compare with 30 healthy volunteers enlisted as normal controls. Result: serum salusin β level in patient with type 2 DM were significantly higher than prediabetes group and normal subjects. Salusin β in prediabetes group no significant higher than in healthy control subjects. Conclusion: Serum Salusin β level in patients with type 2 DM are expressed at significantly high levels were no difference in Salusin β level of prediabetes group and normal control subjects.

2 illus, 3 tables, 8 ref

041728   PRIBADI N, ROSSELLE V R, ZUBAIDAH N, WIDJIASTUTI I (Conservative Dentistry Dep, Airlangga Univ, Surabaya 60132, Indonesia, Email: nirawati?p@fkg.unair.ac.id) : The solubility and water sorption properties of a combination of Ca(OH)₂ and propolis when used as pulp capping material. Indian J Dent Res 2020, 31(4), 557-61.

Calcium hydroxide [Ca(OH)₂ ] is a material used during pulp capping treatment, despite being readily soluble in both water and acid. In contrast, propolis constitutes a nontoxic resin which is not easily dissolved in water. Therefore, a combination of Ca(OH)2 and propolis is assumed to be capable of increasing the mechanical properties of Ca(OH)₂ and to diffuse into the dentinal tubules. This research aimed to reveal the solubility and water sorption ability of a combination of Ca(OH)₂ and propolis as pulp capping material. The samples comprised 18 Ca(OH)₂ and Ca(OH)₂ ‑propolis chips, 15 mm × 1 mm in dimension, all of which were stored in an incubator for 24 h at 37°C. Each sample was then divided into two groups: one dissolved in 50 mL of artificial saliva for 24 h at 37°C and another for 7 days before being weighed, dried, incubated, and weighed for a second time. The result of the reduction in mass divided by the volume of the samples was considered to constitute the level of solubility and water sorption. The difference between the solubility and water sorption ability was analyzed using an independent t‑test with significant difference <0.05. The solubility of Ca(OH)₂ ‑propolis is lower than that of Ca(OH)₂ after immersion for 1 day (P = 0.001) and 7 days (P = 0.000). The water sorption ability of Ca(OH)₂ ‑propolis is no different than that of Ca(OH)₂ after immersion for 1 day (P = 0.088) and 7 days (P = 0.635). However, the water sorption ability of Ca(OH)₂ ‑propolis after 1‑day immersion is higher than immersion for 7 days (P = 0.012). The solubility Ca(OH)₂ ‑propolis is lower than that of Ca(OH)₂, but its water sorption is higher than that of Ca(OH)₂ .

2 illus, 28 ref

041684   ALVES E, NAZARETH C, PEREIRA S (Pharmaceutical Chemistry Dep, PES’s Rajaram and Tarabai Bandekar Coll of Pharmacy, Farmagudi, Goa - 403 401, Email: celinanaz@yahoo.com) : Development and validation of a novel UV spectrophotometric method for simultaneous analysis of amlodipine, indapamide and perindopril. Indian J Pharm Sci 2020, 82(5), 843-50.

A simple, accurate, precise and economical ultraviolet spectrophotometric method has been developed for the simultaneous estimation of amlodipine, perindopril and indapamide. The developed method was based on determination of the three drugs using ultraviolet absorbance correction method. The three wavelengths chosen were 365 nm for amlodipine (as absorbances due to other two drugs were nil at this wavelength), 245 nm for indapamide (corrected for absorbance due to amlodipine) and 204 nm for perindopril (corrected for absorbances due to amlodipine and indapamide) with water as diluent. The Beer Lambert’s range for the three drugs was 10-60 µg/ml, 5-20 µg/ml and 10-100 µg/ml for amlodipine, indapamide and perindopril respectively, with correlation coefficient (r²) of ≥0.999. The developed method was validated as per International Conference on Harmonisation guidelines and was found to be accurate, precise, sensitive and robust. The percentage assay results were within acceptable limits. Hence the developed method can be successfully used for the routine analysis of amlodipine, perindopril and indapamide in bulk and in combination.

4 illus, 12 tables, 16 ref

041680   RAO M T, RAO Y S, RATNA J V, KUMARI P V K (Vignan Institute of Pharmaceutical Technology, Duvvada, Visakhapatnam - 530 049, Email: thrinadh_81@rediffmail.com) : Characterization and ex vivo studies of nanoparticle incorporated transdermal patch of itraconazole. Indian J Pharm Sci 2020, 82(5), 809-18.

Itraconazole, an antifungal drug possess poor solubility, gastrointestinal irritation and first pass effect. Hence in the present work it was initially made as nanoparticles to facilitate absorption and at later stage nanoparticles loaded transdermal patches were developed using promising nanoparticles. Nanoparticles were prepared with Eudragit RL 100 by solvent displacement technique. Formulations F1 to F9 were prepared by using different concentrations of Eudragit RL 100 and polyvinyl alcohol and evaluated for drug content, drug release, entrapment efficiency and mean particle size. The selected formulation was lyophilized to incorporate these formed nanoparticles into transdermal patch by varying concentrations of hydroxy propyl methyl cellulose K100M, polyvinyl alcohol and polyethylene glycol 400. The obtained patches were evaluated for thickness, tensile strength, folding endurance, moisture absorption and moisture content and the drug release showed biphasic release. All the formulations followed first order kinetics, diffusion controlled and fickian release. Flux (ex vivo) studies on rat skin of optimized formulation have high flux of 63.24 µg/cm² /h compared with pure drug, prepared itraconazole ointment 39.15 µg/cm² /h and prepared itraconazole gel 40.01 µg/cm² /h. The permeability of itraconazole nanoparticle loaded transdermal patch showed 2.63 folds enhancement compared to pure drug. Scanning electron microscopes clearly showed the drug loaded nanoparticle embedment in polymeric transdermal patch. Formulated nanoparticle loaded itraconazole transdermal patch can be successfully used as a carrier for enhancing transdermal permeation and the bioavailability.

8 illus, 6 tables, 37 ref

041675   PALIWAL S, PANDEY K, PAWAR S, JOSHI H, BISHT N (Graphic Era Hill Univ, Nainital - 263 156, Uttarakhand, Email: soniapaliwal49@gmail.com) : A review on carbon nanotubes: As a nano carrier drug delivery system. Indian J Pharm Sci 2020, 82(5), 766-72.

Carbon nanotubes were discovered in 1991, Sumio Iijima gives the theory of carbon nanotubes which is made up of carbon allotrope graphene having brilliant electrical, mechanical, optical and synthetic properties, pulling in extensive enthusiasm for their application in different fields including drug conveyance and malignancy treatment. Malignancy is one of the most testing sicknesses of present day times since its treatment includes recognizing ordinary sound cells from influenced cells. Here, carbon nanotubes assume a significant job since marvels, for example, electronic paramagnetic resonance, permit carbon nanotubes to recognize typical cells from influenced ones, the Holy Grail in malignancy treatment. Significant work has been done on carbon nanotubes as medication conveyance frameworks throughout the most recent 20 y. Not with standing, worries over specific issues, for example, biocompatibility and poisonousness have been raised and warrant broad exploration in this field. For the preparation of Single-walled carbon nanotubes and Multi-walled carbon nanotubes arc discharge, laser ablation and chemical vapor deposition method of preparation are used. By the process of acid treatment, magnetic purification and size exclusion chromatography carbon nanotubes impurities are removed out. Because of hydrophobic nature of carbon nanotubes, Covalent and non-covalent functionalization are done for the surface modification. Cytotoxic of carbon nanotubes have a beneficial effect in cancer treatment. Drug released from carbon nanotubes by using various stimulants such as electric, magnetic field and changes in pH.

3 illus, 1 table, 34 ref

041661   SINGH A, BAGHEL U S, SINHA M, ASHAWAT M S (Pharmaceutical Sciences Dep, Guru Nanak Dev Univ, Amritsar, Punjab – 143 005, Email: atampanesar@gmail.com) : Quantitative analysis of rosuvastatin calcium in bulk and solid pharmaceutical dosage forms using green and rapid fourier-transform infrared spectroscopic method. Indian J Pharm Sci 2020, 82(4), 632-9.

A fast, inexpensive and direct quantitative Fourier-Transform Infrared Spectroscopic method was established for rosuvastatin calcium for analysis in bulk and solid pharmaceutical dosage forms. Content of rosuvastatin calcium was directly analysed without any solvent extraction by this method. Absorption mode was used on KBr pallets for acquisition of Fourier-Transform Infrared spectra. The method was validated against prescribed parameters as per International Council for Harmonisation guidelines. Range of linearity range was found to be 5-20 % w/w in KBr pellet method. Proposed method was successfully applied for the determination of rosuvastatin in solid pharmaceutical dosage forms (tablets). The results suggest that the method is precise, accurate and reproducible. Due to its simplicity, cost effectiveness and less time taking, this method can be employed for routine estimation of rosuvastatin calcium in solid dosage forms in pharmaceutical industry.

5 illus, 4 tables, 69 ref

041657   AL-NIMRY S S, ALTANNI B M, HADDAD R H (Pharmaceutical Technology Dep, Jordan Univ of Science and Technology, P. O. Box 3030-Irbid-22110, Jordan, Email: ssnimry@just.edu.jo) : RP-HPLC method for estimating norethindrone in plasma and tissues following administration of a controlled release nanoparticulate liquid formulation. Indian J Pharm Sci 2020, 82(4), 593-600.

The purpose of this investigation was to develop and validate a simple reversed phase-high-performance liquid chromatography method coupled with UV detector estimating norethindrone in plasma and tissues. A Thermo Scientific C18 column (250×4.6 mm ID, 5 µm pore size) and a mobile phase consisting of deionized water:acetonitrile (60:40, v/v) were used. The flow was isocratic at a rate of 1.3 ml/min and the wavelength of detection was 245 nm. Estradiol was used as internal standard. Validation of linearity, accuracy and precision, limits of detection and quantification, specificity and recovery was carried out according to the International Conference of Harmonization guidelines. The method was used in estimating the bioavailability of a controlled release nanoparticulate liquid formulation, administered to dogs. It was also used estimating adhesion potential of the same formulation to the GIT of mice. The method was simple and only liquid-liquid extraction was used in case of plasma samples. However, sample preparation was more complex in the case of tissue samples. It was linear in the range studied, accurate and precise. It was specific and the excipients used in preparing the formulation did not interfere with the method. The recovery was high and consistent. The bioavailability of the drug was enhanced after the administration of the nanoparticulate liquid formulation as compared to unformulated drug. The formulation adhered to the stomach and intestines for 48 h. After 48 h the concentration reached undetectable levels. In conclusion, a simple, linear, accurate and precise reversed phase-high-performance liquid chromatography method coupled with UV detection was developed, validated, and used successfully for the determination of norethindrone in plasma and adhesion to GIT tissues. The cost of the analysis was expected to be low sine the extraction procedure was simple and no radiolabeled internal standard was useds.

5 illus, 6 tables, 20 ref

041656   SINGH M, PRASAD D N, AGNIHOTRI S (IKG Punjab Technical Univ, Jalandhar-144 603, Email: mandeepchadha7@gmail.com) : Synthesis and biological evaluation of novel triazolyl-acridine derivatives as cytotoxic agents. Indian J Pharm Sci 2020, 82(4), 586-92.

Novel triazolyl-acridine compounds were synthesized in 4 series of 9-(2-(substituted phenyl-1H1,2,3-triazol-1-yl)ethoxy)acridine, 9-(3-(4-(2-substituted phenyl)-1H-1,2,3-triazol-1-yl)propoxy) acridine, N-(2-(4 substituted phenyl-1H-1,2,3-triazol-1-yl)ethyl)acridin-9-amine and N-(3- (4-(substituted phenyl)-1H-1,2,3-triazol-1-yl)propyl)acridin-9-amine using appropriate synthetic procedures and screened for cytotoxic activity. The structures of all synthesized compounds were confirmed by Fourier-transform infrared spectroscopy, proton nuclear magnetic resonance and mass spectroscopy and these compounds were assayed in vitro for cytotoxic activity against MCF-7 (human breast adenocarcinoma cell line) and HT-29 (human colon adenocarcinoma cell line) cells. Tested compounds showed better cytotoxic activities in terms of IC₅₀ value against MCF-7 and HT-29 cells. Methyl substituted compound MPP-9 exhibited excellent sensitivity with IC₅₀ value 1 and 2 µM, against MCF-7 and HT-29, respectively. Unsubstituted MPP-1 and chloro-substituted MPP-2 and MPP-5 also exhibited good IC₅₀ value ranges from 2-4 µM against both cell lines. These compounds were active at micro molar concentrations. Data study revealed that synthesized compounds are promising leads for future as cytotoxic agents.

2 illus, 2 tables, 25 ref

041654   PRAKASH V, KUMARI A, KAUR H, KUMAR M, GUPTA S, BALA R (Chemistry Dep, M.M. Univ, Haryana - 134 007, Email: vinitprakash@gmail.com) : Chemical constituents and biological activities of genus Picrorhiza: An update. Indian J Pharm Sci 2020, 82(4), 562-77.

This review article on Picrorhiza genus comprehensively summarized the characterization, morphology, distribution, traditional uses, chemical constituents and biological activities of isolated individual constituents as well as plant extracts. It belongs to the Scrophulariaceae family, a small genera with two species, which are mainly found in Western and Eastern Himalayas at an altitude of 3000-5200 m. It has been used traditionally to cure many diseases like asthma, arthritis, cancer, diabetes, diarrhea, dyspepsia, fever, gastrointestinal problems, jaundice, urinary disorders. Its phytochemical analysis reported the presence of glycosides, aromatic esters, bis-iridoid, phenyl propenoids, alcoholic compounds and fatty acids. Chemical constituents of the genus Picrorhiza and its crude extracts with various solvents exhibit biological activities such as antimicrobial, anticancer, antiasthmatic, antidiabetic effects.

1 illus, 4 tables, 123 ref

041633   TATIPAMULA V B, POLIMATI H, GOPAIAH K V, BABU A K, VANTAKU S, RAO P R, KILLARI K N (Andhra Univ, Visakhapatnam - 530 003, Email: kishorenaidu.killari@gmail.com) : Bioactive metabolites from manglicolous lichen Ramalina leiodea (Nyl.) Nyl.. Indian J Pharm Sci 2020, 82(2), 379-84.

The chemical investigation of acetone extract of manglicolous lichen Ramalina leiodea yielded three known metabolites, methyl 2,6-dihydroxy-4-methyl benzoate (1), haematommic acid (2) and ethyl haematommate (3), which are reported for the first time in this species. The acetone extract and the metabolites (1-3) were screened for antioxidant activity in α,α-diphenyl-β-picrylhydrazyl, 2,2’-azino-bis(3-ethylbenzothiazoline6-sulphonic acid) and superoxide free radical assays, for antiinflammatory activity in pretein denaturation assay and for anticancer activity in sulforhodamine B assay on lung, head and neck, and cervical cancer cells. The results showed that compounds 2 and 3 depicted inhibitory profiles against 2,2’-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid) free radical with an IC₅₀ of 40.0 and 40.5 µg/ml, respectively and caused protein denaturation with an IC₅₀ of 435 and 403 µg/ml, respectively. Furthermore, compounds 2 and 3 exhibited a significant degree of specificity against cervical, head and neck, and lung cancer cells, while these compounds showed little toxicity against normal human mammary epithelial cell line. In summary the manglicolous lichen Ramalina leiodea possessed free radical scavenging, antiinflammatory, and anticancer activities and the main metabolites responsible for these activities could be compounds 2 and 3.

4 illus, 29 ref

041630   XIAO Q, LU Y, CHEN X (Macau Univ, Macau, China, Email: xpchen@um.edu.mo) : Oleanolic acid induces apoptosis and necrosis in LO2 cells. Indian J Pharm Sci 2020, 82(2), 361-8.

This study mainly focused on the evaluation of cytotoxicity of oleanolic acid on normal human hepatic cells. Normal human hepatic cells were exposed to different concentrations of oleanolic acid and the results demonstrated that oleanolic acid induced cell death in a concentration- and time-dependent manner in LO2 cells. Low concentration of oleanolic acid (40 μM) induced apoptosis. Cleavage of caspase 3/7/9 and decrease of mitochondrial membrane potential was detected in normal human hepatic cells. While high concentration of oleanolic acid (80 μM) caused necrosis without producing cleavage of caspase 3/7/9 or DNA fragmentation. Both flow cytometry and PI staining detected necrotic cells. In addition, both low and high concentrations of oleanolic acid had no effect on the generation of intracellular reactive oxygen species. Present data showed that oleanolic acid could induce apoptosis and necrosis in normal human hepatic cells. Oleanolic acid might be a potential hepatotoxin at high dosage.

5 illus, 31 ref

041628   GUPTA S D, SUBRAHMANYAM C V S, GOWRISHANKAR N L, RAGHAVENDRA N M (Pharmaceutical Chemistry Dep, Gokaraju Rangaraju Coll of Pharmacy, Hyderabad - 500 090, Email: sayanduttagupta1@rediffmail.com) : Conserved water molecule-dependent docking strategy and atom-based 3D QSAR studies to design heat shock protein 90 inhibitors. Indian J Pharm Sci 2020, 82(2), 341-55.

In this study a methodology was described to recognize the conserved water molecules required for efficient binding of ligands with heat shock protein. Subsequently, a substantiated procedure for the determination of an effective docking methodology was generated using various programs of Schrodinger and SYBYL softwares. In order to identify the essential structural features responsible for heat shock protein inhibitions, an atom based 3D-quantitative structure-activity relationship model with an excellent surmising ability in both external and internal validation was established. The results of 3D-quantitative structure-activity relationship and docking studies correlated well with each other. A combined analysis of docking results and quantitative structure-activity relationship analysis indicates: The key amino acids and water molecules in the active pocket of heat shock protein. The important structural requirement in ligands that will lead to enhanced biological activity. The results provide a set of simple and effective guidelines for rationally designing new heat shock protein inhibitors prior to their synthesis.

10 illus, 4 tables, 38 ref

041620   ZHANG P, JIE H, LIU J, ZHANG X-Y, ZHANG W, LIU M, WANG Y, WANG Y-F, HUANG W, LIU Z (Jinan Univ, Guangdong Province, China, Email: tliuzh@jnu.edu.cn) : Studies on substituted thienopyridine carbonitriles as src inhibitors using a comprehensive in silico method. Indian J Pharm Sci 2020, 82(2), 270-81.

To explore the structural requirements and inhibitory mechanism of Src inhibitors, the comparative molecular field analysis, comparative molecular similarity indices analysis and three-dimensional quantitative structure-activity relationship and molecular docking of 45 substituted thienopyridine carbonitriles as tyrosine kinase pp60src inhibitors was conducted. Three three-dimensional quantitative structure-activity relationship models showed high predictabilities with cross-validated correlation coefficient and predictive correlation coefficient values of 0.793 and 0.887 for comparative molecular field analysis and 0.624 and 0.793 for comparative molecular similarity indices analysis, respectively. Docking results indicated that 4 compounds with high inhibitory activity penetrated into the active pocket of tyrosine kinase pp60src and formed stable hydrogen bonds with the binding pocket of tyrosine kinase pp60src. Leu273, Lys295, Thr338, Asp348, and Ser345 of tyrosine kinase pp60src are important residues. The results could be of great value in designing novel substituted thienopyridine carbonitriles with more potent Src kinase inhibitory activity.

7 illus, 4 tables, 21 ref

041618   MADHURI G, NAGARAJU R, KILLARI K N (Pharmaceutics Dep, Rao’s Coll of Pharmacy, Nellore - 524 320, Email: g_madhuri3@yahoo.com) : Enhancement of the physicochemical properties of poorly soluble lovastatin by co-crystallization techniques - in vivo studies. Indian J Pharm Sci 2020, 82(2), 249-59.

To overcome the poor solubility and low bioavailability of lovastatin co-crystallization was attempted. Lovastatin co-crystals were prepared with selected co-former gallic acid by co-grinding method. Characterization was carried out through X-ray diffraction, Fourier Transform infra-red spectroscopy, differential scanning colorimetry and scanning electron microscopy. The Fourier-transform infrared spectroscopy results showed that a hydrogen bond was formed between lovastatin and gallic acid to yield a co-crystal. Micrometric properties, solubility, dissolution studies, pre-compression and post-compression properties were evaluated. Lovastatin co-crystals were formulated into conventional tablets. In vivo and stability studies were performed. Pharmacokinetic parameters and dynamic studies of the formulation were statistically analysed and a value of p<0.05 was considered to be significant. Thus physicochemical properties and bioavailability of lovastatin was improved through co-crystallization.

7 illus, 7 tables, 27 ref

041617   SHI J, YAO W, PANG S (Osteoarthroplasty Dep, Cangzhou Hospital of Integrated TCM-WM, Hebei Province, 061001, China, Email: shijingrenjie@sina.com) : Morin attenuates interleukin-1β-induced inflammatory response in primary rat chondrocytes by suppressing the overproduction of nitric oxide and matrix metalloproteinases. Indian J Pharm Sci 2020, 82(2), 242-8.

The present investigation was aimed to evaluate the antiosteoarthritic effect of morin in isolated primary rat chondrocytes in the presence of interleukin-1β. Results obtained showed that morin effectively attenuated in vitro the production of inflammatory mediators, nitric oxide and prostaglandin E2. Moreover, morin also significantly decreased the levels of matrix metalloproteinases. Furthermore, in monosodium iodoacetateinduced osteoarthritis in mice, it was found that morin at 25 and 50 mg/kg, significantly reduced the heat hyperalgesia and increased the spontaneous motility in mice on days 7, 14, and 21. Besides, morin also significantly reduced the level of proinflammatory cytokines in the serum of osteoarthritic mice. Collectively, these findings demonstrated that morin could be a potential chondroprotective that could be used in the treatment of osteoarthritis.

5 tables, 43 ref

041604   BUYUK N I, ARAYICI P P, DERMAN S, MUSTAFAEVA Z, YUCEL S (Bioengineering Dep, Yildiz Technical Univ, Davutpasa Street, Istanbul, Email: yuce.sevil@gmail.com) : Synthesis of chitosan nanoparticles for controlled release of amiodarone. Indian J Pharm Sci 2020, 82(1), 131-8.

This work is based on a natural polymer chitosan used in a nanoparticulate drug delivery system for the controlled release of amiodarone along with β-cyclodextrin. Amiodarone-loaded chitosan nanoparticles were prepared using the ionic gelation method aided by sonication. Amiodarone loading on chitosan nanoparticles was done under optimum conditions. For particle characterization; zeta-sizer, UV/Vis, Fourier-transform infrared spectroscopy, X-ray powder diffraction, differential scanning calorimeter and scanning electron microscope techniques were used. In vitro drug release studies of amiodaroneloaded chitosan nanoparticles were performed using the dialysis diffusion technique. Drug loading and release values were determined using UV/Vis spectroscopy. Amiodarone encapsulated in nanoparticles was completely released at the end of 14 days. About 38 % was released at the end of day 1, 44 % released at the end of day 3, 50 % released at the end of day 5 followed slow release. Amiodarone-loaded chitosan nanoparticles could serve as a model for controlled delivery of many antiarrhythmic drugs.

7 illus, 2 tables, 54 ref

041602   TANDON N, GUPTA R, GUPTA N (Lovely Professional Univ, Phagwara - 144 411, Email: tandonnitin12004@gmail.com) : Interactions of ceftiofur sodium with H2-receptor antagonist. Indian J Pharm Sci 2020, 82(1), 114-22.

The purpose of this study was to examine the possible drug-drug interactions between ceftiofur sodium and famotidine on co-administration. These studies were carried out at normal as well as elevated temperature at pH corresponding to blood pH of 7.4. Spectrophotometric method was used to study the dissolution of each drug individually and in the presence of the other drug. Change in the rate of dissolution of ceftiofur sodium in the presence of cimetidine as compared to the rate of dissolution in the absence of cimetidine supported the possible interactions between the two drugs.

2 illus, 8 tables, 20 ref

041600   PORNPITCHANARONG C, SAHATSAPAN N, ROJANARATA T, OPANASOPIT P, NGAWHIRUNPAT T, PATROJANASOPHON P (Silpakorn Univ, Nakhon Pathom, 73000, Thailand, Email: patrojanasophon_p@su.ac.th) : Curcumin-incorporated thiolated chitosan/alginate nanocarriers: physicochemical properties and release mechanism. Indian J Pharm Sci 2020, 82(1), 97-103.

This study was aimed to develop thiolated chitosan/alginate nanoparticles for curcumin delivery. The nanoparticles were prepared from thiolated chitosan and sodium alginate using an ionic gelation technique. The concentrations of thiolated chitosan and alginate used to form the nanoparticles were optimal at 0.05 and 0.025 % w/v, respectively. Curcumin was incorporated into the nanoparticles by entrapment during nanoparticle preparation. The thiol content of the synthesized thiolated chitosan as well as the particle size, size distribution, surface charge, loading efficiency, loading capacity and drug release characteristics of the curcumin-loaded thiolated chitosan/alginate nanoparticles were investigated. Nano-sized particles ranging from 291-435 nm were obtained. The blank nanoparticles exhibited the smallest size and positive surface charge. Incorporation of curcumin into the nanoparticles resulted in a slightly bigger particle size and the surface charge became negative. After drug loading, the particle size was changed to 435 nm with the technique used. Sustained release of curcumin was observed from the nanoparticles. Kinetics of curcumin release fitted well with the zero-order model. Curcumin incorporated nanoparticles were successfully prepared with desirable physicochemical properties. Moreover, sustained release of curcumin from the nanoparticles with zero-order kinetic was obtained. Therefore, these nanoparticles may prove to be favourable carriers for curcumin delivery.

7 illus, 1 table, 25 ref

041593   GANJI L V, AGRAWAL P N (Pharmaceutical Chemistry Dep, Prin. K. M. Kundnani Coll of Pharmacy, Colaba, Mumbai-400 005, Email: ganjilata@gmail.com) : Design, synthesis and antiinflammatory evaluation of 5(6)-(un)-substituted-1H-benzimidazol-2-ylthioacetylpiperazine derivatives. Indian J Pharm Sci 2020, 82(1), 21-31.

Benzimidazole-2-thione derivatives are known to possess broad spectrum of biological activities, and the most prominent being the antiinflammatory activity. The synthesis of these compounds involve three steps, William’s reaction of 5(6)-(un)-substituted-1H-benzimidazol-2-thiols with chloroacetic acid in presence of sodium hydroxide and refluxing, which was further reacted with acetic anhydride in pyridine medium on a steam bath followed by hydrolysis with a N-mono substituted piperazine in ethanol medium under reflux conditions to get 5(6)-(un)-substituted(1H-benzimidazol-2-yl-thio)acetyl piperazine derivatives. Molecular docking experiments were carried out against cox-2 enzyme using GOLD software 5.1.0. Docking studies revealed important binding interactions of synthesized derivatives with cox-2 enzyme indicating nonselective interactions, which were in agreement with the in vivo antiinflammatory activity. Absorption, distribution, metabolism, and excretion properties of the synthesized derivatives were determined by QikProp. These derivatives were tested in the carrageenan-induced rat paw oedema model to determine the antiinflammatory activity.

6 illus, 4 tables, 25 ref

041588   SANDHALA D, LANKALAPALLI S (GITAM Institute of Pharmacy, Visakhapatnam - 530 045, Andhra Pradesh, Email: deepthi.sandela@gmail.com) : New method for the in vivo estimation of fluvastatin and its application for pharmacokinetic studies in rabbit. Indian J Pharm Edu Res 2020, 54(4), 1153-8.

The study was aimed to conduct a pharmacokinetic evaluation of Fluvastatin in rabbit plasma using a sensitive HPLC method. The plasma samples were assayed by Waters alliance e-2695 HPLC instrument using symmetry C₁₈ column (150x4.6mm, 3.5 µ) under isocratic condition. Here the buffer was 0.1 % ortho phosphoric acid. Mobile phase used was acetonitrile and 0.1 % ortho phosphoric acid in 50:50 v/v with a flow rate of 1 ml/min. The eluent was monitored at 224 nm for measurement of Fluvastatin. The calibration curve was linear over the concentration range of 5-200 ng/ml of Fuvastatin. The application denotes all the parameters of system suitability, specificity, linearity and accuracy are in good agreement with USFDA guidelines and applied effectively for the investigation of pharmacokinetic studies in rabbit.

5 illus, 3 tables, 27 ref

041586   YANG Y, XU J, CAO G (Guangdong Pharmaceutical Univ, Guangdong, China, Email: cg@gdpu.edu.cn) : An in-depth study of the concept of chirality in organic and pharmaceutical chemistry: Using crystal structure data with 3D visualization software. Indian J Pharm Edu Res 2020, 54(4), 1133-43.

Chirality is an essential feature of life and a universal phenomenon in nature, chirality in chemistry and biochemistry is closely related to biological, spectroscopic and physical properties. The concept of chirality also has important applications in pharmaceutical chemistry. This article aims to introduce how crystal structure data can be used in 3D visualization software to deepen students’ understanding of the concept of chirality in organic and pharmaceutical chemistry. Many crystal data examples are used to introduce chiral compounds and the absolute configuration of chiral factor, such as chiral atoms, axial chirality, planar chirality, spiral chirality and supramolecular chirality, the concrete teaching method is to import the crystal data into the visualization software, rotate it to the appropriate position, then labelled as the absolute configuration. The students were asked to do a set of chiral exercises based on crystal structure data. The effectiveness of this teaching method is judged by classroom test feedback. We successfully established and applied a chiral teaching method based on crystal structure data. The test scores of students using this method were higher than those who had not used it before. This method can help students better understand the concept of chirality, improve the teaching quality and test scores and also lay a foundation for the application of chemistry database in teaching.

19 illus, 1 table, 43 ref

041573   MOHAN R, SINGH S, KUMAR G, SRIVASTAVA M (Phytochemistry Div, CSIR-National Botanical Research Institute, Lucknow - 226 001, Uttar Pradesh, Email: m.srivastava@nbri.res.in) : Evaluation of gelling behavior of natural gums and their formulation prospects. Indian J Pharm Edu Res 2020, 54(4), 1016-23.

Gums and polymers can be found abundantly in the nature from various plants, microbial and marine sources. Their physical and functional characteristics can be customized according to its application in product development. The purpose of this study is to determine the potentiality of natural gums obtained from plant based sources in development of gel formulation and its comparison with the commercially used polymers viz. Carbapol 934, Carboxy Methyl Cellulose, Xanthan, Sodium Alginate. Gel formulations of varying ranges of polymeric concentrations were prepared and evaluated for its pharmaceutical parameters like pH, viscosity, homogeneity, tensile strength and antimicrobial activity. The analysis of the developed gel formulations indicated that formulations developed using Guar gum possess much better gelling behavior i.e. viscosity and muco-adhesiveness then other selected gums and is more closer to its synthetic counterpart like Carbopol 934. Thus natural gum provides a comparatively broader range of characteristics and eco-friendly approach which enhances its applicability in formulation development. This research work rationalizes the importance of natural gums as gelling agents in development of pharmaceutical dosage forms, cosmetic products and nutraceutical formulations.

5 illus, 3 tables, 20 ref

041572   VERMA C P S, VERMA S, ASHAWAT M S, PANDIT V (Pharmaceutics Dep, Laureate Institute of Pharmacy, Jawlamukhi, Himachal Pradesh, Email: vinay2121@gmail.com) : Development of solid dispersions of clopidogrel using innate excipient: Synergistic antiplatelet activity. Indian J Pharm Edu Res 2020, 54(4), 1007-15.

The present study encompasses on formulation and evaluation of solid dispersion of Clopidogrel, Class II drug-using pectin extracted from mango peel. Pectin was extracted from full-grown mango peel grown in the Kangra region. Solid dispersions were prepared using kneading, hot fusion method and solvent wetting method and the solvent wetting method were gauged and optimized. The prepared solid dispersions were subjected to solubility analysis and selected optimized formulation was further subjected to DSC, PXRD, in-vitro Dissolution and in-vitro antiplatelet activity. The in-vitro release studies are subjected to mathematical data analysis using DD Solver 1.0 version. Extracted pectin from mango peel was light brown in color and soluble in water. The screened carriers PVPK30 and extracted pectin showed the enhanced solubility of pure drug. The pectin was further selected for the formulation of solid dispersions by three different methods. The solvent wetting method has given expected results and the formulation SD6 containing drug: pectin ratio 1:2 was selected and evaluated. The in-vitro release has shown 91.2 % in 60 min with a mean dissolution time of 14.64 min and dissolution efficiency of 0.691 %. The formulation SD6 has shown 87.1 ±1.8 % antiplatelet activities whereas pure drug has shown 71.9 ±2.1 % indicating enhanced activity. It was concluded that the pectin extracted from ripened mango peels can be a suitable carrier for the formulation of solid dispersion of clopidogrel which not only enhances the solubility but also resulted in the enhanced antiplatelet activity.

5 illus, 4 tables, 20 ref

041569   SHIVAKUMAR H N, SOMASEKHAR V, ROY A (Pharmaceutical Chemistry Dep, KLE Coll of Pharmacy, Bengaluru - 560 010, Karnataka, Email: vanitasom@gmail.com) : Preparation and characterization of directly compressible spherical agglomerates of etoricoxib. Indian J Pharm Edu Res 2020, 54(4), 983-90.

The current work contemplates formulation of spherical agglomerates of Etoricoxib, with a view to improve the flow properties, solubility and dissolution rate. Spherical agglomerates of etoricoxib were produced employing quasi emulsion solvent diffusion method using hydrophilic polymers like PVP K30 and PEG 6000. IR spectroscopy and Scanning Electron Microscopy along with physicochemical evaluations were used to characterize the agglomerates. The optical microscopic studies indicated that the agglomerates were spherical in shape and varied in size from 1203.9 ± 126μm to 1297.2 ±164.2μm. The technique was found to enhance the aqueous solubility of the drug from 1.45 μg/ml to 8.26±0.05 μg/ml and the dissolution in 60 min from 39.57 % to 82.88 %. Etoricoxib tablets prepared using spherical agglomerates with PVP K30 and PEG 6000 displayed dissolution of 82.88 % and 76.89 % respectively that were considerably higher than conventional etoricoxib tablets. From the dissolution profile and % cumulative release from formulations it was concluded that Spherical Agglomeration technique substantially improves the flow properties, aqueous solubility and rate of dissolution of etoricoxib.

2 illus, 3 tables, 20 ref

041566   GADAD A P, PATIL A S, SINGH Y, DANDAGI P M, BOLMAL U B, BASU A (Pharmaceutics Dep, KLES Coll of Pharmacy, Belagavi - 590 010, Karnataka, Email: archupharma@gmail.com) : Development and evaluation of flurbiprofen loaded transethosomes to improve transdermal delivery. Indian J Pharm Edu Res 2020, 54(4), 954-62.

Flurbiprofen is prescribed for the symptomatic management of arthritis. Its oral administration leads to gastrointestinal damage and it has a short elimination halflife requiring multiple dosing. Transdermal drug delivery of flurbiprofen is an alternative route to bypass the stratum corneum layer of the skin. Nano-vesicular carriers can be used to overcome this problem as it increases the permeability and skin deposition of the drug and reduces dosing frequency. Flurbiprofen loaded Transethosomes has been formulated by Thin-film hydration using Span 80 and Tween 80 as edge activators, Soyaphosphotidylcholine and varying percentage of ethanol. The vesicles were further characterized to study the effect of the type and concentration of edge activator and ethanol percentage on various parameters such as, particles size, polydispersity index, deformability index, entrapment efficiency and in-vitro drug release. A formulation having the least particle size, highest deformability index and best ex-vivo profile was optimized. The optimized formulation was dispersed in a gelling agent and evaluated for pH, drug content and compared with marketed formulation for ex-vivo permeation and skin deposition. Formulation containing Tween 80 in the ratio of 95:05 (Soyaphosphotidylcholine: Edge Activator) and having the highest ethanol percentage was optimized. On comparison with the marketed gel it was revealed that the optimized gel formulation containing higher concentration of Tween 80 had better ex-vivo profile and skin deposition. The formulated transethosomes may serve as potential carrier for effective management of arthritis.

5 illus, 3 tables, 24 ref

041561   SITUMORANG M, PURBA J, SILABAN R (Chemistry Dep, Negeri Medan Univ, North Sumatera, Indonesia, Email: msitumorang@ unimed.ac.id) : Implementation of an innovative learning resource with project to facilitate active learning to improve students’ performance on chemistry. Indian J Pharm Edu Res 2020, 54(4), 905-14.

The provision of suitable and comprehensive learning resources concedes to be an effective strategy to create a serviceable learning process to achieve the competencies needed by students. This research aims to provide an innovative learning resource with projects to facilitate active learning to improve student performance in chemistry. This research conducted by developing of chemistry learning package through the integration of projects, media and multimedia into learning materials, followed by standardization and implementation for chemistry teaching. A section of an innovative learning resource with projects on the topic of Alkanes Compounds has been successfully developed. It also has been validated and standardized by experts and is considered appropriate for the teaching needs of undergraduate Chemistry and Pharmacy students. The implementation of a learning resource has proven to be beneficial in helping students to learn organic chemistry. The research findings authenticated that the developed learning resource effectively facilitates active learning in improving student performance on chemistry. The facilities available in the learning resources are sufficient to guide the students to carry out project assignments. The students are very enthusiastic about learning chemistry and their learning styles have changed to become independent learners. The developed learning resource discovered to be effective in building the skills and knowledge in chemistry. Students’ performance is classified as very good, where the average score successively obtained for skills is 89.18±2.86, the project report portfolio is 87.76±3.48 and the formative exam is 85.84±4.46. An innovative learning resource has succeeded in facilitating students’ active learning, making learning more enjoyable and ultimately increasing their knowledge and skills to meet the competencies needed in the field of chemistry. The learning resource model developed in this study could be adopted in other subjects to facilitate active learning and to achieve the competencies needed by scientists and pharmacists.

1 illus, 5 tables, 61 ref

041560   SAVITA J T, BHARAT V D, AVINASH B B, MEETA N J (Pharmaceutical Chemistry Dep, St John Institute of Pharmacy and Research, Palghar - 401 404, Maharashtra, Email: bharatpg@gmail.com) : An approach to the evaluation of program outcomes and consideration of activities beyond curriculum for improvement of program outcome attainment. Indian J Pharm Edu Res 2020, 54(4), 896-904.

Current global scenario demands outcome based education to develop graduates with universal acceptability. Program Outcomes (POs) laid by NBA (Table 1) are the assessable components indicative of graduate potential to demonstrate competencies to practice at appropriate levels. Program Outcomes (PO) can be defined and calculated by assessment of various Course Outcomes (CO) which can further be evaluated from Learning Outcomes (LOs). Blooms Taxonomy classifies LOs into the cognitive, affective and psychomotor domains based on their level of complexity. Each LO maps to CO and hence contributes to PO. The direct and indirect assessment tools can be used to obtain course outcome attainment level. Performance at the prerequisite subject and attainment of the outcomes for previous year are the factors determining defined CO attainment. The attainment of Program Outcomes POs is an indicator of the graduate’s potential to demonstrate competencies and practice at appropriate levels. POs are derived from the Graduate Attributes (GA) specified by the National Board of Accreditation (NBA). Curriculum designed by University is not enough for a graduate to achieve the desired level of PO attainment. PO attainment is calculated by considering co-curricular and extracurricular activities in addition to the curriculum specified by the affiliating University for a programmer. GA like Pharmacy Knowledge, Thinking Abilities, Planning Abilities, Professional Identity, Environment and Sustainability, Pharmacist and Society are achieved through regular curricular activities whereas other GA like Leadership Skills, Ethics, Communication and Life Long Learning can be better attained through participation in extracurricular and co-curricular activities. This paper describes a module for defining and calculating attainment of Program Outcomes. It also demonstrates how of Activities beyond Curriculum for improvement of Program Outcome attainment.

15 tables, 6 ref

043364   MICHAEL O S , SUCCESS M , BARIYAA W T , CYPRIAN I (Biochemistry Dep, Nigeria Univ, Nsukka Nigeria) : Production of lipase using Cucummeropsis Mannii obtain from south Eastern Nigeria. Int J Chem Sci 2020, 4(3), 33-7.

Lipase has attracted a lot of attention in recent years because of its diverse biotechnological applications, like biopolymer synthesis, biodiesel production, treatment of fat-containing waste effluents, enantiopure synthesis of pharmaceuticals and nutraceutical agents, have been established successfully. Lipase occurs widely in nature, but plant lipase, is significant because of its unique substrate selectivity/specificity. However new lipases with properties amenable for application in specific industrial process are being sought by the researchers. In this work, a penicillium strain was isolated that showed lipase production from endosperm tissues of decaying seeds of Cucummeropsis mannii obtained from the regular Ogige market in Nsukka metropolis, Enugu state. The optimization studies resulted to an increase in enzyme activity: the strain produces lipase in an inexpensive inorganic medium at highest when ammonium sulphate is used as a source of nitrogen when compared with lipase activity on other sources of inorganic nitrogen. Lipase production known to be induced when lipids such as vegetable oils (triacyiglycerides) are included in the medium as carbon sources. The potential to induce lipase production is dependent on the type of oil used. The inclusion of olive oil in medium showed that lipase extract from Cucumeropsis mannii had its highest enzyme activity when it is used as a carbon source when compared to other sources of carbon like palm kernel oil, groundnut oil, soyabean oil and sunflower oil. Further studies on the lipase activity from Cucumeropsis mannii also showed that the lipase produced from it was highest at pH 8.0, which meant that the lipase is best produced at an optimum medium pH of 8.0.

3 illus, 13 ref

043363   BEKELE B, HAILE A (Chemistry Dep, Bonga Univ, Bonga, Ethiopia) : Extraction, isolation and characterization of the stem bark of Combretum paniculatum occurring in South West Ethiopia. Int J Chem Sci 2020, 4(3), 29-32.

Combretum paniculatum has been used widely in ethnomedicine in the treatment of leprosy, chronic diarrhea, dysentery, flatulence, vomiting, colic, enlarges spleen and liver in Ethiopia and tropical African country. However, despite its use in traditional medicine, to date, there appears to have been no chemical or biological studies published on the stem bark part of the plant species. Phytochemical screening tests of the methanol extract of the stem bark revealed the presence of steroids, alkaloids, terpenoids, phenols, flavonoids, saponins, tannins, glycosides and the absence of anthraquinones and coumarines. Silica gel chromatographic separation of the methanol extract gave Apigenin-7-O-β-D-glycoside (CPB) for the first time from the stem bark of C. paniculatum. A complete characterization of the isolated compound was done with the help of spectroscopic techniques.

2 illus, 2 tables, 14 ref

043360   ZADE M B (Chemistry Dep, Azad Coll Ausa Dist. Latur, Maharastra) : Determination of iron content in neglected leafy vegetables sonchusarvensis and portulaca oleraceae by colorimertrically. Int J Chem Sci 2020, 4(3), 19-20.

Iron is one of the important nutrients for good health and Vigour. It is needed for the formation of the Hemoglobin which carries oxygen from the lungs to the body cells. Vegetables are richer in iron than fruits. Most of the iron for our body requirements can be obtained from green leafy vegetables and nutritional anemia can be easily cured by green leafy vegetables. Iron is an essential part of Red Blood Corpuscles and is an essential element in the body. Its best sources are Sonchus arvensis and portulaca Oleraceae.

1 table, 11 ref

041547   KUTUBUDDIN S T, SURESH S S, BALIRAM K R, AIKATERINI L (Pharmaceutical Sciences Dep, Rashtrasant Tukadoji Maharaj Nagpur Univ, Nagpur - 440 033, Maharashtra, Email: drkakde@yahoo.com) : Development and validation of stability indicating method for estimation of buparvaquone by forced degradation studies. Indian J Pharm Edu Res 2020, 54(3), 790-7.

A lucid, rapid and precise stability-indicating method was developed by using HPLC for the estimation of Buparvaquone in bulk as well as pharmaceutical dosage form by forced degradation studies. Princeton C₁₈ column (4.6 × 150 mm, 5µ) and mobile phase containing 1 % glacial acetic acid and acetonitrile in the proportion of 5:95 v/v was used throughout the study. The flow rate was 0.9 ml/m and the detecting wavelength was kept as 251 nm using the PDA detector. The retention time of Buparvaquone was found to be at 8.6 ± 0.5 m. The method developed was validated, as stated in ICH Q2 (R1) guidelines. It was found to be linear within concentration ranging from 2-20 µg/ml having a correlation coefficient 0.999 and other parameters are also under permissible limits. Buparvaquone was exposed to different stress conditions like acidic, basic, neutral, thermal, peroxide and also photolytic. Amongst all, the drug was found to be more degraded under basic as well as peroxide conditions.

4 illus, 10 tables, 12 ref

043359   LEHA M A , MONIHARAPON T , RETRAUBUN A S , SIMANJUNTAK P (Pattimura Univ, Kampus Poka, Ambon, Indonesia) : Phytochemicals analysis, and inhibitor enzyme a-glucosidase activity of teripang (Stichopus hermanii). Int J Chem Sci 2020, 4(3), 15-8.

Isolation, purification and identification of the ethanol extract of sea cucumber (Stichopus hermanii) originating from the area of Seira Island, Ambon Indonesia has been done. Extraction was carried out by maceration of dried sea cucumbers with 96 % ethanol (after cleaning, drying, smoked, and cut into small pieces). Ethanol extract was fractionated by column chromatography (SiO₂, CHCl₃ - MeOH = 10: 1 ~ 2: 1) gave 4 fractions (Fr. I ~ Fr. IV). GC-MS analysis for fraction III which resulting in -glucosidase enzyme inhibition of 131.52 ppm consisting of compounds fatty acids and monosacharides.

2 illus, 2 tables, 16 ref

043358   KARNA R K (Chemistry Dep, R.B. Jalan Bela Coll, Darbhanga, Bihar) : Synthetic studies of quinoxaline derivatives. Int J Chem Sci 2020, 4(3), 12-4.

In this paper, 2-ethyl-4(3H)-3, 1-benzoxazinone (1) was synthesized from acetylation with simultaneous cyclization of anthranilic acid and acetyl chloride. Compound 1 was treated with hydrazine hydrate to yield 3-amino-2-ethyl-4(3H)- quinazolinone (2). Reaction of compound 2 with aromatic aldehydes/ketones resulted Schiff bases 3-6. All newly synthesized compounds were characterized using different methods of spectroscopy such as IR, 1H-NMR and 13C-NMR.

1 table, 20 ref

041546   KIRUBAVATHY S J, CHITRA S (Chemistry Dep, PSGR Krishnammal Coll for Women, Coimbatore - 641 004, Tamil Nadu, Email: drjonekiruba@gmail.com) : Synthesis, characterization, biological and photoluminescence study of co(ii) complexes of fused heterocyclic ring systems. Indian J Pharm Edu Res 2020, 54(3), 781-9.

To synthesize and characterize the transition metal complexes of fused heteroccylic ring systems. Many of the fused ring heterocyclic compounds were found to be biologically active in the literature like anti-microbial, anti-cancer, anti-inflammatory, antioxidant and so on. The present work focus on the synthesis of the biologically active compounds. Synthesis of the ligands and the complexes are done using the standard procedures in earlier reports. Melting points were found using open glass capillaries on a Raaga melting point apparatus and are uncorrected. The percentage of C, H, N , infra-red and UV-Visible spectra of the compounds were recorded using Elementar Vario EL III CHN analyser, Shimadzu spectrophotometer (4000-400 cm^-1) and Elico SL 159 UV-Vis spectrophotometer respectively. The anti-microbial activity of the compounds was carried out by well diffusion method. The anti-cancer activity of the compounds were carried out for the MCF-7 cell line (breast Cancer) using MTT assay. Structural elucidation of newly synthesized Co(II) metal complexes of fused heterocyclic ring systems were done using various spectral techniques like FT-IR, ¹H-NMR, Electronic and TGA-DTA studies. The anti-microbial activity of the prepared complexes and the DNA Cleavage studies were screened for various test pathogens and explained. The photoluminescence property of the fused heterocyclic ligand and their complexes were studied and compared. Fluorescence enhancement is observed in these complexes which is contradictory to the normal Fluorescence quenching phenomena by added organic derivatives, paved way for photochemical applications.

4 illus, 14 ref