Background
Understanding the mechanisms, activated and inhibited pathways as well as other molecular targets involved in existing and emerging disease conditions provides useful insights into their proper diagnosis and treatment and aids drug discovery, development and production. G protein-coupled receptors (GPCRs) are one of the most important classes of targets for small-molecule drug discovery. Of all drug targets, GPCRs are the most studied, undoubtedly because of their pharmacological tractability and role in the pathophysiology as well as the pathogenesis of human diseases.
Main body of the abstract
GPCRs are regarded as the largest target class of the “druggable genome” representing approximately 19% of the currently available drug targets. They have long played a prominent role in drug discovery, such that as of this writing, 481 drugs (about 34% of all FDA-approved drugs) act on GPCRs. More than 320 therapeutic agents are currently under clinical trials, of which a significant percentage targets novel GPCRs. GPCRs are implicated in a wide variety of diseases including CNS disorders, inflammatory diseases such as rheumatoid arthritis and Crohn’s disease, as well as metabolic disease and cancer. The non-olfactory human GPCRs yet to be clinically explored or tried are endowed with perhaps a huge untapped potential drug discovery especially in the field of immunology and genetics.
Short conclusion
This review discusses the recent advances in the molecular pharmacology and future opportunities for targeting GPCRs with a view to drug development.
The inhibition of acetylcholinesterase plays a vital role in the treatment of Alzheimer disease. This study aimed to explore the acetylcholinesterase inhibition potential of Phyllanthus amarus and its phytoconstituents through an in vitro and in silico approach. The in vitro acetylcholinesterase inhibitory activity of P amarus was carried out, followed by the molecular docking studies of its phytoconstituents. The top-ranked molecules identified through molecular docking were subjected to molecular dynamics simulation (MDS) and density functional theory (DFT) studies. The results obtained revealed the methanolic extract of P amarus as a potent acetylcholinesterase inhibitor, while amarosterol A, hinokinin, β-sitosterol, stigmasterol and ellagic acid were identified as potential acetylcholinesterase inhibitors. The MDS and DFT results are in agreement with those obtained from the docking studies. Our findings suggest further studies on the hit molecules.
Background: Ficus exasperata (Vahl) from the family Moraceae is a herb of ethnobotanical importance with antimicrobial properties. The past studies have been on the phytochemistry and pharmacological activities of the plant, but there is a need to formulate this valuable herb into tablet dosage form to offer standardisation.Aim: The aim of this study was to assess the antimicrobial activity of F. exasperata leaf extract (extract) and formulate it into herbal tablet dosage form.Setting: The experiments were performed at the laboratories of the Faculty of Pharmacy, University of Ibadan, Ibadan, Nigeria.Methods: The extract was obtained by maceration and assessed for antimicrobial activity using agar cup diffusion method. Tablets were prepared by direct compression using Avicel®, Lactose and Emcompress® at a drug–diluent ratio of 1:4 and 1:9. The flow properties of the powder mixtures were determined using compressibility index, Hausner’s ratio, angle of repose and density measurements. The mechanical properties of the tablets were assessed using crushing strength (CS), friability (FR) and the crushing strength–friability ratio (CSFR) and release properties with disintegration times (DT), disintegration efficiency ratio and dissolution times. Analyses were carried out using two-way analysis of variance on Prism 5.0.Results: The results showed that the extract had concentration-dependent antimicrobial activity. The flow properties of the powder mixtures were in the rank order of Avicel® Lactose Emcompress®. Tablet CS and CSFR increased, whilst FR decreased with increase in compression force and diluent concentration. All tablets passed the DT test. The ranking of dissolution times was Avicel® Lactose Emcompress® no diluent.Conclusion: Ficus exasperata extract demonstrated antimicrobial properties dependent on type of organism and extract concentration. The herbal tablets have acceptable mechanical and release parameters, which varied with diluent type, drug–diluent ratio and compression pressure.
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