Drug Metabolism and Bioanalysis Letters - Volume 16, Issue 2, 2023

Objective: The inhibitory and stimulatory effects of several compounds, including steroid hormones and azole antifungal agents, on cortisol 6β-hydroxylation activity by cytochrome P450 (CYP) 3A4, polymorphically expressed CYP3A5, and fetal CYP3A7 were compared with those on testosterone 6β-hydroxylation to clarify the catalytic properties of the predominant forms of the human CYP3A subfamily. Methods: 6β-H Read More

Background: Natural products constitute a unique source of chemical compounds with multi-target potential for the treatment of complex human disorders. Phytochemicals are pure phytoconstituents of plants, mainly responsible for their therapeutic potential and pharmacological activities. Natural products isolated from medicinal plants have been used as a lead source of drug. Norisoboldine is an important isoquinoline alka Read More

Psoriasis is a complex autoimmune skin condition with a significant genetic component. It causes skin inflammation and is characterized by flaky, silvery reddish spots that can worsen with age. This condition results from an impaired immunological response of T-cells and affects 2-5% of the global population. The severity of the illness determines the choice of treatment. Topical treatments are commonly used to treat psorias Read More

Background: Oral bioavailability (F), which is evaluated by permeability and solubility, is one of the key parameters in drug discovery. Currently, Caco-2 and Ussing chamber are both used in the study of intestinal permeability of drugs at different stages of drug development. However, comparative research between the Ussing chamber and Caco-2 for predicting the intestinal availability data (Faæ#151;Fg) in humans h Read More

Objective: This work describes a simplified, 96-well plate method for determining the blood-to-plasma concentration ratio (BP ratio) for small molecules.Methods: The need for calibration curves was eliminated using a matrix-matching approach in which blood samples were mixed with blank plasma and plasma samples were mixed with blank blood. As a result, both blood- and plasma-origin samples shared an equivalen Read More

Background: Saccharolactone is used as a β-glucuronidase inhibitor in in vitro microsomal and recombinant uridine diphosphoglucuronosyl transferases (rUGTs) incubations to enhance glucuronide pathway and, thereby, formation of glucuronide metabolites. We investigated its effect on CYP mediated metabolism of drugs (compound-174, phenacetin and quinidine) using human liver microsomes (HLM) supplemented with Read More

Background: Desidustat (DES) belongs to a new category of drugs, i.e., Hypoxia-Inducible Factor (HIF) propyl hydroxylase inhibitor, and is used for the treatment of anemia in chronic kidney disease. However, no method has yet been reported in the literature for the estimation of drugs.Objective: The objective of the study is to develop a simple, precise, and accurate method for determining DES in bulk and pharm Read More

Background: Worldwide, it is projected that 285 million individuals have diabetes, and by 2030, this number is expected to climb to 438 million. About 90% of cases of diabetes mellitus are type 2 (T2DM). Insulin sensitizers, such as metformin and thiazolidinediones; insulin secretagogues, such as sulfonylureas and glinides; dipeptidyl peptidase 4 (DPP-4) inhibitors; glucosidase inhibitors, or oral combination therapy are curr Read More