Sesquiterpene Derivatives from Tripterygium wilfordii

Tripterygium wilfordii Hook. f. (Celastraceae) is a traditional Chinese medicine distributed in the southern part of China, the roots of which has been used to treat cancer and inflammation. Recently, a traditional Chinese medicine preparation derived from a water/chloroform extract of the roots of T. wilfordii (the so-called “total multi-glycoside”) has been employed in the clinical treatment of rheumatoid arthritis, skin disorders, male-fertility control, and other inflammatory and autoimmune diseases. On the basis of the significant pharmacological activities of T. wilfordii, many chemical investigations have been conducted to expound the bioactive substance. As a result, hundreds of compounds have been obtained from the roots of T. wilfordii, including sesquiterpenes, diterpenes, triterpenes, and lignans. Compared with the investigations of the roots of T. wilfordii, few chemical and bioactive studies have been conducted on the leaves. In order to promote the sustainable utilization of T. wilfordii, we performed extensive chemical and bioactive investigations on the ethanolic extract of the leaves of T. wilfordii. After the separation of the EtOAc extract of T. wilfordii by silica gel, MPLC, and preparative HPLC, twelve new dihydroagarofuran sesquiterpene polyol esters triptersinine A-L (1–12), together with eight known sesquiterpene pyridine alkaloids peritassine A (13), wilfordinine A (14), hypoglaunine A (15), hypoglaunine E (16), wilfordinine E (17), euonine (18), wilfortrine (19), and euonymine (20) were obtained. Their structures were determined by spectroscopic analyses.

Acknowledgements: This research program is supported by the National Key Technology R&D Program of the Ministry of Science and Technology of China (Nos. 2009BA173B03, 2011BAI01B05).