title: Immunosuppressant discovery from Tripterygium wilfordii Hook f: the novel triptolide analog (5R)-5-hydroxytriptolide (LLDT-8).
abstract: The Chinese traditional herb Tripterygium wilfordii Hook f (TwHF) has been widely used in the treatment of autoimmune and inflammatory diseases. Over the past few decades, great efforts have been made to explore modern preparations of TwHF with higher efficacy, solubility, and lower toxicity. In this study, we reviewed several examples both of naturally occurring compounds and their derivatives in TwHF, and summarized the preclinical evaluations with regard to autoimmune and inflammatory diseases. All of the candidate compounds described herein have been or are currently in clinical trials. Although some studies encountered problems, the data still provided valuable references for future studies. (5R)-5-hydroxytriptolide (LLDT-8, Leitengshu) is a novel triptolide derivative with potent immunosuppressive and anti-inflammatory activities developed at Shanghai Institute of Materia Medica. Indeed, a Phase I clinical trial for this compound has been completed in rheumatoid arthritis patients. The results will provide the basis for the further exploration of this ancient herb and encourage the research and development of valuable traditional Chinese medicine.
authors.affiliation: Laboratory of Immunopharmacology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, China.
authors.forename: Wei
authors.initials: W
authors.lastname: Tang
authors.forename: Jian-ping
authors.initials: JP
authors.lastname: Zuo
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D001172:Arthritis, Rheumatoid / Q000188:drug therapy / Q000503:physiopathology; D001327:Autoimmune Diseases / Q000188:drug therapy / Q000503:physiopathology; D004224:Diterpenes / Q000302:isolation & purification / Q000494:pharmacology*; D015195:Drug Design; D004365:Drugs, Chinese Herbal / Q000494:pharmacology; D006801:Humans; D007166:Immunosuppressive Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D007249:Inflammation / Q000188:drug therapy / Q000503:physiopathology; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology; D012995:Solubility; D029757:Tripterygium / Q000737:chemistry*
chemical_list: C509074:5-hydroxytriptolide; D000893:Anti-Inflammatory Agents; D004224:Diterpenes; D004365:Drugs, Chinese Herbal; D007166:Immunosuppressive Agents; D010936:Plant Extracts