Posted by admin on Sep 30, 2021 in |
Indibulin (N-(pyridin-4-yl)-[1-(4-chlorbenzyl)-indol-3-yl]-glyoxyl-amid; ZIO-301 or D-24851) is a novel synthetic, orally active anti-mitotic agent that binds tubulin, destabilizes microtubulin polymerization, and arrests tumor cell growth at the G2/M phase. Its tubulin binding site is distinct from that of other microtubulin inhibitors such as taxanes, colchicines, and vinca alkaloids. Many researchers were motivated by this achievement of vinblastine and vincristine (vinca alkaloids) and developed the indole-based new anticancer chemical entities. Indole containing anticancer molecules has shown their anticancer properties through the diverse mechanism of action. The majority of the synthetic indoles have a structural analogy to natural anticancer products (vinca alkaloids or combretastatin) and exhibited anticancer activity through tubulin interactions. The indole ring system is an essential part of many tubulin inhibitors identified in recent years. The Substituted 2-Phenyl-1H-Indol-3yl Glyoxylamidewere was computationally designed and energy minimized. All the designed compounds show zero violations of the rule of 5, which indicates drug-likeness properties and good bioavailability. Among these, several aryl/ heteroaryl substituted indolylglyoxyamides have shown good inhibition towards tubulin...
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Posted by admin on Sep 30, 2021 in |
The goal of the research is to analyze the antiparkinsonian activity of hydroalcoholic extract of the stems of Capparis Decidua (HECD). Themost common neurodegenerative condition which stand second is Parkinson. It is reported by dopaminergic neuron loss in the striatum’s substantia nigra & dopamine loss (DA). Capparis Decidua plant is used as anti-inflammatory, laxative, anti-diabetic, anthelmintic, antibacterial, astringent, digestive and for so many other traditional use, we used this research to scientifically verify Parkinson behaviour using suitable animal models. In mice, using haloperidol (1 mg/kg i.p) catalepsy was induced. Bromocriptine (2.5 mg/kg) and HECD were administered orally to the treatment group at the dose of 100 mg/kg, 200 mg/kg, and 300 mg/kg. Bar tests for catalepsy, motor coordination tests by rotarod, and locomotor activity by actophotometer were performed to evaluate behavioural changes. Dopamine and catalase assay were also carried out to assess biochemical parameters. Using standard as ascorbic acid in UV visible spectrophotometer, evaluation of antioxidant activity by DPPH radical scavenging method were performed. The outcome of our work...
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Posted by admin on Sep 30, 2021 in |
Covid-2019: The pandemic that shook the entire world. There is no sarcasm if one says there will be a Pre and Post- COVID-19 world. Worldwide, millions of cases have been identified, and heaps have died. So many nations worldwide have issued a lockdown to stop the coronavirus’s unfolding, which triggered giant financial fallout. Like each and every incident has two dimensions, Covid-19 possesses both positive and negative aspects. This unfortunate pandemic’s positive aspect has been a fortunate scenario for many sectors, including pharmaceutical scientists all over the world, who are striving their best to discover antibodies that can fight the novel coronavirus. This review article mainly aims to study how this deadly pandemic has become a fortunate scenario for pharmaceutical scientists based on the data gathered (sources: websites, web blogs, reports on the internet study, newspapers, etc.). But there are some positive aspects, such as reducing pollution, reducing traffic accidents, and recognizing the importance of sanitation, hygiene, and social distancing. This pandemic revealed that there is a need to...
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Posted by admin on Sep 30, 2021 in |
The recommended doses of antacids by some manufacturers are in ranges. However, dosing decisions on antacids should be based on acid-neutralizing capacities (ANCs). This study evaluated the ANCs of different doses of antacids. Twenty-two antacids (3 granular, 5 tablet and 14 suspension formulations) were evaluated for their ANCs at half, minimum, and double their recommended adult doses. All the products complied with the minimum ANC recommendation (5 mEq/dose), although ANCs were significantly different from each other (p < 0.0001). The ANC range for minimum recommended doses for all products was 12.417−38.817 mEq. There were no significant differences in ANCs (p = 0.1662) based on dosage form. A dose-dependent effect was observed when minimum recommended doses were halved or doubled, with significant differences in ANCs at each dose level (p < 0.0001). The ANC range for doubled doses was 19.817-71.133 mEq. The ANCs at half-doses (7.583−20.417 mEq) were also compliant with the regulatory requirement. The findings show that doses smaller than recommended amounts could be indicated for mild hyperacidity conditions,...
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Posted by admin on Sep 30, 2021 in |
To evaluate the antibacterial activity, pharmacokinetics and molecular interaction of the compounds from Ricinus communis` leaf extract. Antibacterial activity was assessed by using the micro-dilution method. The chemical constituents of the methanolic leaf extract were assessed by using gas chromatography-mass spectrophotometry (GC-MS). The drug-like and toxicity properties of the phytocompounds were predicted by SwissADME and ADMET lab tools. AutoDock Vina was employed to investigate the binding strength of the ligand-receptor complexes. The extract displayed antibacterial activity with the lowest minimum inhibitory concentration of 1.56 mg/mL on Bacillus spizizenii (ATCC 6633). The GC-MS showed volatile compounds, namely hexadecanoic acid, methyl ester (0.62%), tridecanoic acid (0.76%), pentafluoro propionic acid, nonyl ester (0.85%), 10-octadecanoic acid, methyl ester (2.93%) and cis-vaccenic acid (94.84%). The compounds did not inhibit isomers of cytochrome P450 (CPY) (CYP 2D6 and CYP 3A4). They were all predicted to have drug-like properties as they adhered to the Lipinski Ro5. The compounds did not show to induce any hepatotoxic effects. The compounds revealed the docking scores in the range of...
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