Posted by admin on Aug 31, 2023 in |
Rosuvastatin is a widely used lipid-lowering medication that belongs to the class of “Statins” whereas Teneligiptin is a novel potent drug that belongs to the class of “DPP-4 inhibitors” which is used for the treatment of Type 2 Diabetes mellitus. The FDA recently approved the combination of these two drugs in 2021 since it proved to be highly effective for treating dyslipidemia associated with Type 2 Diabetes mellitus. Forced degradation studies have been performed on Rosuvastatin and Teneligliptin separately using various analytical techniques such as RP-HPLC, UV, RP-UFLC, RP-UPLC, UHPLC, HPTLC and TLC. Characterization of the degradation products generated during various stress conditions is also performed using various sophisticated techniques such as UPLC, LC/MS/MS, NMR, and FT-IR. These degradants can cause many adverse effects, such as carcinogenicity, mutagenicity, neurotoxicity, hepatotoxicity, skin sensitization, respiratory sensitization, etc. So, identifying and characterizing these degradation products will be very useful for their metabolic studies and in-silico toxicity assessment. In-silico toxicity studies are very helpful in predicting the toxic potential of these degradants, and...
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Posted by admin on Aug 31, 2023 in |
Tuberculosis (TB) is caused by a bacterium called Mycobacterium tuberculosis, identified as a global health emergency by the world health organization. The development of drug-resistance stains due to spontaneous gene mutation has been a major boost to research in the pathogenicity and biochemistry of Mtb. To combat drug resistance to tuberculosis, new drugs and methodologies are emerging. Since, starting itself mycobacterium complex cell wall has been a choice for widely selected targets for anti-TB drugs. Peptidoglycan, arabinogalactan, and mycolic acid are the basic layers supporting cell growth. The current work investigates virtual screening for optimal small molecule inhibitors targeted against selected mycolic acid targets (β-keto acyl ACP synthase, enoyl acyl ACP-reductase and Polyketide synthase 13). A small library of 485 compounds was designed and docked into a selected target core to identify the potential inhibitor. The designed compounds were subjected to docking studies using Glide (Schrodinger). InhA was the most suitable mycolic acid inhibitor target for the designed compounds. Further, the effectiveness of the study was evaluated by comparing the...
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Posted by admin on Aug 31, 2023 in |
Pan-genome analysis can identify the core genome, which is the total number of genes present in all strains of a bacterial species. Further essential genes can be identified in this core set of genes which gives us a minimal number of genes required for the survival of the bacteria. This set of genes can be analyzed to develop new antimicrobial agents against pathogenic, multidrug-resistant bacteria such as Listeria monocytogenes which causes several primary and secondary infections in humans. Pan-genome analysis of 38 strains of Listeria monocytogenes was performed to estimate 2331 genes in core genome, 1056 genes in the dispensable genome, and 152 genes in the strain-specific genome. Essentiality analysis of 2331 core genome proteins predicted 965 essential core-genome families (ECGFs). Furthermore, the identification of host non-homologous proteins using BLASTP with the Homo sapiens proteome resulted in 485 non-homologous essential core-genome families (NH-ECGFs). These putative proteins can be analyzed to identify novel drug targets that could generate broad-spectrum, safe and effective therapeutic agents against Listeria monocytogenes infections in...
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Posted by admin on Aug 31, 2023 in |
Medicinal plants belong to the Labiatae family, commonly known as the mint family. This family comprises the Anisomeles malabarica, which contain biologically important phytochemicals. Focus on solvent extraction of selected medicinal plant parts and its phytochemical analysis gives an insight for herbal drug discovery. A heat continuous percolation experiment was conducted for 24 hours using three different solvents, namely ethanol, methanol, and chloroform using the Soxhlet apparatus. The phytochemical examination of Anisomeles malabarica leaf extracts by the three solvents revealed that the extracts are abundant in alkaloids, saponins, tannins, flavonoids, and glycosides, all of which have been linked to the pharmacological effects of the plant. In the current study, derivatization procedures were employed to analyze both polar and non-polar compound present in the solvent extracts. Based on the GC-MS analysis, large amounts of carboxylic acids, which contain both saturated and unsaturated fatty acids, hydrocarbons, including alkanes and alkenes are responsible for the oily quality of all three extracts. According to analysis, the majority of polar molecules, such as alcohols,...
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Posted by admin on Aug 31, 2023 in |
Drug resistance in bacterial strains has often been detected in the last two decades and is increasing yearly. Novel survival mechanisms and over-the-counter antibiotic availability (OTC) complicated this issue, especially in relation to the Asian continent. Resistance to drug/antibiotic is multifactorial viz, plasmid encoding drug resistance, pumping the drug out by pumping mechanism from the bacterial cell, degradation of antibiotic by using enzymes such as β-lactamases, carbapenemase and others. Bacterial drug resistance is a global threat, and the discovery of novel antibiotics to address this challenge has not kept pace. Critical appraisal and drug development timelines in clinical phases made the task costly and tedious. Global pharmaceutical companies have withdrawn their attention, and only a limited number of companies are doing research and development in this field. The present review discusses the current scenario worldwide and introduces one health plan’s role in terms of the discovery of novel drugs and increased drug...
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