Posted by admin on Oct 31, 2020 in |
A series of 2-cyclopropylimidazo [2,1-b] [1,3,4] thiadiazole derivatives 5(a-i) have been synthesized by reacting 5-cyclopropyl-1,3,4-thiadiazol-2-amine (3) and an appropriate 2-bromo-1,2-(substituted aryl) ethanones 4(a-i). Structures of these compounds were recognized by IR, 1H NMR, 13C NMR spectroscopy and Mass spectrometry. Hypoxia-inducible factor (HIF) has been identified as an important cancer drug target. HIF transcription complex, which is activated by low oxygen tension, controls a diverse range of cellular processes, including angiogenesis and erythropoiesis. Here we analyzed the capacity of synthesized molecules to inhibit hypoxia-inducible factor prolyl hydroxylase (PHD2) in-silico as well as an in-vitro assay. Four compounds were granted NSC code at National Cancer Institute (NCI), USA, for anticancer activity at a single high dose (10-5 M) in full NCI 60 cell panel. Among the compounds tested,2-Cyclopropyl-6-(4-methoxyphenyl)-5-phenylimidazo[2,1-b][1,3,4]thiadiazole 5a (NSC D-754956/1) was found to be the most active candidate of the series at five dose level screening with a degree of selectivity toward leukemic cancer cell...
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Posted by admin on Oct 31, 2020 in |
The aim of the study was to determine the biologically active fractions of methanol extracts of mature leaves of Pogostemon benghalensis (burm. f.) Kuntze and Perilla frutescens L. Britton. The methanol extract was broadly fractionated sequentially in hexane, chloroform, acetone, ethyl acetate, and methanol. Activity index was recorded higher in methanol broad fractions of both of the plants. Broad fractions of both of the plants recorded a higher Proportion Index against E. coli (1.00). An increasing trend was recorded in the case of total phenol and flavonoid content with an increase in concentration from 1 mg/ml to 5 mg/ml. In case of Pogostemon benghalensis (Burm.f.) Kuntze, antioxidant inhibition of ascorbic acid against DPPH and ABTS are (98.28 ± 1.03% and 96.22 ± 2.01% respectively) which is higher than the crude extract (81.43 ± 0.09% and 72.32 ± 0.01% respectively) at 500 µl of the sample at 1mg/ml of concentration. TLC Spots from hexane and chloroform broad fraction recorded antibacterial inhibition against B. subtilis. Rf values of TLC spots from...
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Posted by admin on Oct 31, 2020 in |
Clarithromycin is a lipophilic and poorly water-soluble macrolide antibiotic which belongs to class II of the biopharmaceutics classification system. Its oral absorption and related bioavailability are dissolution rate-limited and relatively low. Subsequently, the formulation of oral clarithromycin delivery systems poses a huge challenge to the formulation scientist. Utilization of self – micro emulsifying drug delivery system technology, with the intent of enhancing oral bioavailability of clarithromycin was designed as this study’s principal objective. Following successful screening studies involving solubility, compatibility and phase evaluations, series of clarithromycin – loaded self – micro emulsifying drug delivery system formulations were developed. Formulations were subjected to optimization and characterization analyses, from which formulation C2A with compositions (% w/w) of olive oil 5%, Tween 80: ethanol (4:1) 94.42%, clarithromycin 0.5% and aspartame 0.08% was optimized. The optimized/ test formulation was subjected to stability, in-vitro drug release, and pharmacokinetic analyses. Estimated parameters included a droplet size of 16.30 ± 3.31 nm, polydispersity index of 0.203 ± 0.11, and zeta potential of -2.01 ± 1.56 millivolts....
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Posted by admin on Oct 31, 2020 in |
Cinnamaldehyde is the aldehyde that gives cinnamon its flavour and odour. It occurs naturally in the bark of cinnamon tree (Cinnamomum zeylanicum), a common Indian spice. The essential oil of cinnamon bark contains about 90% of cinnamaldehyde. It exists as a yellow oily liquid with a cinnamon odor and sweet taste and is traditionally known to have many medicinal properties, although the mechanism of action is not completely understood. Macrophages are one of the most important cells of the immune system and play important role in influencing the inflammation cascade process. The current study aimed towards understanding the role of this medicinal plant product on genes of the inflammatory pathways, especially in the context of macrophages. For this purpose, the effects of Cinnamaldehyde were studied on the macrophage cell line J774A.1. Our studies indicate that treatment of these cells with various concentrations of Cinnamaldehyde alters levels of the pro-inflammatory cytokine, IL-12. Further studies are required to get a better understanding of the molecular mechanisms by which Cinnamaldehyde may be...
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Posted by admin on Oct 31, 2020 in |
Free radicals are unstable molecules that are formed during normal cell metabolism through chemical changes that take place in a cell. This causes damage to cellular components such as cells, proteins, and DNA, or the cell membrane. Free radicals play a role in a complex interplay of different mechanisms in both normal agings, neurodegenerative, and other diseases. Aqueous and methanolic solvent extracts of pulp (without seed), pericarp, leaf, and seed of Aegle marmelos were subjected to phytochemical screening tests, quantitative determination of total phenol content (TPC), total flavonoid content (TFC), total flavonol content (TF) and in-vitro antioxidant activities such as DPPH, hydrogen Peroxide (H2O2), reducing power assay (RPA), ferric ion reducing antioxidant power (FRAP), ABTS and phosphomolybdenum total antioxidant assay (PM) by using standard procedures for the detection. The aqueous extract of pulp was found to possess maximum TPC (23.88±0.91mg GAE/g), TFC (63±0.25mg QE/g) and TF (13.30±0.53mg QE/g) values for methanolic leaf extract, respectively. The lower EC50 values were observed for DPPH assay for aqueous extract of seed is 160.117±1.62...
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