Pharmacokinetic and Toxicological Characteristics of Tripterigium Glycosides and Their Derivatives.

Pharmacokinetic and Toxicological Characteristics of Tripterigium Glycosides and Their Derivatives. Curr Drug Metab. 2018 Mar 02;: Authors: Du X, Nyagblordzro M, An L, Gao X, Du L, Wang Y, Ondieki G, Kikete S, He X Abstract Tripterigium wilfordii glycosides (TWG) demonstrate paramount bioactive effectiveness in the management of many autoimmune diseases, such as rheumatoid arthritis, psoriasis, and nephrotic syndrome. However, its side effects on the hepatic, nephrotic, reproductive, and cardiovascular systems have limited its immense therapeutic potentials. Triptolide (TP) and Celastrol (CL), the leading bioactive as well as toxic constituents of TWG, have been widely studied. These studies have documented the key mechanisms that trigger the toxic reactions and the precautionary measures that could prevent and reduce such reactions. It has been reported that reactive oxygen species (ROS) generation, mitochondrial respiratory chain inhibition, cauda epididymis sperm structure disruption, and metabolizing enzyme inhibition are the leading factors of the toxic reactions. The bioactive effects and toxicities of TWG are closely related to its metabolic profiles. It has been confirmed that TP and CL inhibit Cytochrome P450 (CYP) and the transporters. This paper reviews and summarizes the pharmacokinetic and toxicological parameters of TWG, some mitigative interventions and several implications of its pharmacokinetic characteristics. Antio...
Source: Current Drug Metabolism - Category: Drugs & Pharmacology Authors: Tags: Curr Drug Metab Source Type: research