Posted by admin on Nov 30, 2022 in |
Hyperlipidemia is a term that encompasses various genetic and acquired disorders that describe elevated lipid levels within the human body. The present study aims to design newer potent PCSK9 Inhibitors to treat hyperlipidemia. In the current study, pharmacophoric features like one hydrogen bond acceptor, one hydrogen bond donor, and one aromatic ring were used to construct a virtual library of ligands. A virtual library consists of 150 ligands containing substituted heterocycles like Imidazole, Thiazole, Oxadiazole, thiadiazole, oxazole, Benzthiazole, Amino triazole, Benzoxazole, Pyrimidine, and Pyrrole. The binding mechanism of newly designed ligands with target enzyme PCSK9 was studied using Autodock 4.2.6. Docking studies show that Lig7, Lig15, Lig34, Lig49, and Lig103 were highly active hits, and nearly 90 designed ligands were found to moderately inhibit PCSK9 enzyme, which is proven to be effective hits. When all the 150designed ligands were further subjected to drug-likeliness properties using software like Molinspiration, Osiris property Explorer all ligands were found to possess drug-likeliness...
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Posted by admin on Nov 30, 2022 in |
SMEDDS are formulated to improve the oral bioavailability of lipophilic drugs. It is an isotropic mixture of compounds like oil, surfactant, co-surfactant, and drug having the unique ability to form fine o/w micro-emulsion by agitation and diluted with GI fluid. Its liquid formulation technique enhanced the absorption and bioavailability of poorly water-soluble drugs but also had a few drawbacks like long time period stability issues and storage conditions. Some special techniques convert the liquid form into solid dosage form to overcome these problems. The present paper gives exhaustive information about formulation design by screening excipients. We study the selection and solubility of excipients, its preparation and characterization, and the mechanism by which bioavailability can be improved. This discussion is useful for a better understanding of SMEDDS for its recent advancements, marketed formulation, and patents on SMEDDS. The poorly water-soluble drugs having dissolution rate absorption limited can be effectively formulated in the form of SMEDDS causing a stable plasma profile. The plasma levels of the poorly aqueous soluble medicament show...
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Posted by admin on Nov 30, 2022 in |
Cutaneous wound healing starts with an acute inflammatory phase marked by secretion of pro-inflammatory mediators that enhance infiltration of leukocytes with a peak in the first 24 to 48 h. This resolves to enable the continuation of other phases in series, namely, the proliferative, re-epithelialization, vascularisation, and tissue remodelling phases. The study uses a mechanical device, for the first time, to create a mechanical cutaneous wound in adult Zebrafish to simulate mammalian cutaneous wound. Topical application of 0.5% ointment of a fraction from hexane leaf extract of Vernonia arborea, accelerated wound healing in the developed model. The phytocompound in the fraction modulates the inflammation kinetics, increasing initial inflammation at 24 hrs by expediting neutrophil infiltration, three folds more than the untreated model. The resolution of inflammation was rapid in the experimental group after 3 dpw compared to the untreated control resulting in speedy proliferation and migration of keratinocytes and three times faster wound closure, measuring up to 92.3% as compared to 95.3% in the positive control group. The fraction...
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Posted by admin on Nov 30, 2022 in |
Bryophytes are the closest modern relatives of the predecessors to the earliest terrestrial plants and have shown to be brilliant chemists since they have long been a favorite treatment among tribal peoples all over the world, who use its pharmacological characteristics to treat a wide range of ailments. As bryophytes’ Phytochemistry contains a diverse range of biologically active compounds such as lipids, proteins, steroids, organic acids, alcohols, aliphatic and aromatic compounds, polyphenols, terpenoids, acetogenins and phenylquinones, it’s no surprise that substances derived from these ancestral plants are widely used as antitumor, antipyretic, insecticidal and antimicrobial agents. The present investigation has been an attempt to evaluate the antifungal potential of two ethnic botanically important liverworts, Plagiochasma appendiculatum, and Pellia endiviifolia. The methanolic extract was tested against two fungal species, Candida albicans MTCC 1637 and Aspergillus niger MTCC 1235. In-vitro antifungal activity was evaluated by disc diffusion method, which revealed inhibition of Candida albicans MTCC 1637 and Aspergillus niger MTCC 1235 growth. Plagiochasma appendiculatum proved to be more effective against both...
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Posted by admin on Nov 30, 2022 in |
Severe viral infections like Covid-19 are emerging now a day and are the common causes of human illness and death. Presently, we have a limited availability of antiviral chemotherapeutic agents to prevent and treat these infections, so it is the need of an hour to develop potential antiviral drugs against various harmful and fatal viral infections. A large quantity of research has been performed on 1,2,3 triazole and their derivatives, which has proved the promising antiviral activity of this heterocyclic nucleus. Among nitrogen-containing heterocyclic compounds, 1, 2, 3-triazoles are privileged structure motifs and received great attention in academics and industry. Even though absent in nature, 1, 2, 3-triazoles have found broad applications in drug discovery, organic synthesis, polymer chemistry, supramolecular chemistry, bioconjugation, chemical biology, fluorescent imaging, and materials science. 1, 2, 3 triazole nucleus is one of the most important and well-known heterocycle which is a common and integral skeleton of a variety of medicinal compounds like antidepressant, antihistaminic, antioxidant, antitubercular, anti-Parkinson, antineoplastic, antihypertensive, antimalarial, local anaesthetic, antianxiety, antiobesity...
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