Posted by admin on Jun 30, 2021 in |
In the present research worked aims to increase the antimicrobial activity of quinoxaline thiosemicarbazide derivatives by substitution of some acetophenones and their antimicrobial evaluation against various antimicrobial strains with molecular docking studies. Lead molecule (1E, 4E)-1-(7-chloro-3-isopropylquinoxalin-2(1H)-ylidene) thiosemicarbazide was synthesized and condensed with various substituted acetophenones to synthesize derivatives. All derivatives were characterized by IR., NMR & Mass spectroscopy. The synthesized derivatives were evaluated in-vitro for antibacterial and antifungal activities against various strains using the agar dilution method. Molecular docking studies of the derivatives (Va – Vg) were performed against E. coli DNA gyrase B and Topoisomerase IV to find out essential binding sites against target protein PDB: 1AJ6 and 1S14, respectively. Among all these compounds,Vf and Vg were found to exhibit more potent activity against Gram –Ve, Gram +Ve bacterial and fungal strains at MIC 0.19 µg/ml, 0.39µg/ml, and 0.78 µg/ml, respectively. The docking studies of all the compounds exhibit potent binding energy, but the compound Vg exhibit interactive binding energy -8.1 and -7.5 kcal/mol to the active pockets...
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Posted by admin on Jun 30, 2021 in |
Rivastigmine is used for the treatment of mild to moderate dementia of the Alzheimer’s type. Transdermal delivery of Rivastigmine is preferable to improve gastrointestinal tolerability. A novel transdermal system with zero-order release kinetics was developed following a hybrid technique in a combination of the micro reservoir and adhesive dispersion system. The transdermal system was prepared by incorporating rivastigmine in adhesive matrix layer in which rivastigmine-loaded microspheres were dispersed. Microspheres were prepared by spray drying using poly-e-caprolactone and maltodextrin (1:1 ratio) as carriers in various drug: polymer ratios. Microspheres with1:2 drug: polymer ratio (A1) showed desired particle size, yield, assay and in-vitro drug release and were found to be suitable for designing the transdermal system. A1 was dispersed into silicon adhesive layer during the preparation of the patch with a calculated amount of rivastigmine. Transdermal patch with 18 mg rivastigmine was optimized by evaluating ratios of adhesive matrix and microsphere content following DOE where 13 formulations were evaluated for various physical and chemical properties. 5 among 13 formulations were found...
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Posted by admin on Jun 30, 2021 in |
The unripe fruit of Meyna spinosa / Laxiflora is used for the treatment of diabetes by traditional healers. The effect of the aqueous extract of the fruit is investigated on the normal and elevated blood glucose level of the experimental animal rats. The blood glucose level of the rats is elevated with the administration of I.P streptozotocin. The estimation of the blood glucose level is done by using a kit based on the glucose oxidase method. The rat has a blood glucose level above 280mg/dl is considered for the normal and anti-hyperglycemic study. The doses of the extract are selected as 200, 300mg/kg, and the route of administration is oral. The effect of the extract on the normal and elevated glucose level of the rat is compared with that of the standard drugs- glibenclamide and metformin. The effect of the extract on normal blood glucose level is not significant when compared with that of glibenclamide, whereas the effect of the extract on elevated blood glucose level is significant when...
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Posted by admin on Jun 30, 2021 in |
Background and Objectives: Cyanobacteria are rich in various bioactive compounds. This study aims to screen the antimicrobial activity of sub-aerial Cyanobacteria isolated from sub-aerial habitats (Old monuments and building facades). Materials and Methods: Crude aqueous and organic extracts were screened for phytochemical constituents and tested for their antimicrobial efficacy against human pathogens. The crude extract that showed better antimicrobial activities were further fractionated by column chromatography and purified by TLC. The active bands were scraped out separately and concentrated in vacuo to isolate pure compounds. Each purified compounds dissolved in respective solvents, assayed for antimicrobial activities were further characterised through FTIR and LC-MS. Results: The results indicated the presence of many secondary metabolites. Of the isolated purified compounds, the compounds from three species, viz. Scytonema hyalinum, Tolypothrix rechingeri, and Fischerella species exhibited antimicrobial activities, whereas others showed antibacterial activity. The FTIR spectra revealed the peaks of carboxylic acid, alkaloids, and phenolic compounds. The chemical compounds were identified as 1,3-dihydroxycyclohexane [Lyngbya kuetzingiana], 4-(4-hydroxyphenyl) butanoic acid [Nostoc linckia], octahydro-1H-indole-2-carboxylic acid [Scytonema...
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Posted by admin on Jun 30, 2021 in |
Linalool is the first ingredient to synthesize many other substances of higher value for the pharmaceutical and fragrance industry; therefore, finding sources of essential oils containing Linalool is an important and necessary task. The purpose of this study is to investigate Linalool of plants containing essential oil in Vietnam to extract Linalool sources for the pharmaceutical and fragrance industry. By the method of fresh sampling of essential oil plants in Vietnam, essential oils are extracted by steam distillation and then analyze on high-resolution chromatography (HRGC) to search for Linalool sources. We have found that some areas with a lot of plants containing high Linalool content grow concentrated wild in forests as Coriandrum sativum Linn., Homalomena occulta (Lour.) Schoot, Cinnamomum parthenoxylon Meissn, and some of them can be planned to cultivate the essential oil source to obtain Linalool for the pharmaceutical and aromatic industry. During the survey, we discovered and made a list of 21 plants with essential oil containing Linalool in...
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