Current Drug Metabolism - Volume 22, Issue 3, 2021

Background: The roots of Polygonum multiflorum (PM) are a well-known traditional Chinese medicine, widely used to treat a variety of conditions in Southeast Asia, South Korea, Japan and other countries. It is known that Polygoni Multiflori Radix Praeparata (PMRP) may enhance the efficacy and reduce the toxicity of PM. However, reports of adverse reactions, such as hepatotoxicity, caused by PM or PMRP, have continuously app Read More

Background: Catalpol, an iridoid glycoside, is one of the richest bioactive components present in Rehmannia glutinosa. More and more metabolites of drugs have exhibited various pharmacological effects, thus providing guidance for clinical application. However, few researches have paid attention to the metabolism of catalpol. Objective: This study aimed to establish a rapid and effective method to identify catalpol metab Read More

Background: Vitexin is a natural flavonoid compound with multiple pharmacological activities and is extracted from the leaves and seeds of Vitex negundo L. var. cannabifolia (Sieb. et Zucc.) Hand.-Mazz. However, the metabolite characterization of this component remains insufficient. Objective: To establish a rapid profiling and identification method for vitexin metabolites in rat urine, plasma and faeces after oral admin Read More

Background: Neuropathic pain (NP) is an egregious problem worldwide. Due to the side-effects of oral drugs, drugs delivered directly to the affected area of pain are preferred. Objective: Capsaicin, a chemical compound isolated from chili peppers, is used as an analgesic in topical ointments and dermal patches to alleviate pain. Objective of the study is to review the application and functionality of topical capsaicin i Read More

Aims: Base dissociation constants of 30 model chemicals were investigated to constitute potential determinant factors predicting the contributions of flavin-containing monooxygenases (FMOs). Background: The contributions of FMOs to the metabolic elimination of new drug candidates could be underestimated under certain experimental conditions during drug development. Objective: A method for predicting metabolic sites and Read More

Background: Pharmacokinetic and pharmacodynamic assessment of ester-containing drugs can be impacted by hydrolysis of the drugs in plasma samples post blood collection. The impact is different in the plasma of different species. Objective: This study evaluated the stability of a prodrug, ketoprofen methylester (KME), in commercially purchased and freshly collected plasma of mouse, rat, dog, cat, pig, sheep, cattle and h Read More

Background: Shenqi Jiangtang Granule (SJG), a classical prescription of traditional Chinese medicine, is widely used to treat diabetes and its complications. Although, the clinical efficacy of SJG, is sufficient, the pharmacokinetic behavior of various substances in the plasma of SJG is unknown. Objective: The aim of this study was to investigate the plasma pharmacokinetics during absorption of SJG after oral administra Read More

Background: Praziquantel (PZQ), which possesses an asymmetric center, is classified as a pyrazinoisoquinoline and has been the mainstay in the treatment of schistosomiasis since 1980. PZQ undergoes a pronounced first-pass metabolism in the liver through the CYP450 system which could be mediated by nuclear receptors. Objective: The purpose of this study was to investigate the possible different induction effects of CYP Read More

Aims: To study the effects of blood glucose regulating compounds on human and rat sulfotransferases (SULTs) expressions. Background: Phase-II enzymes, sulfotransferases catalyze the sulfuryl-group-transfer to endogenous/exogenous compounds. The alteration of expressions of SULTs may have influence on the sulfation of its substrate and other biomolecules. Objectives: The influence of the altered biotransformation might Read More