Research On The Chemical Constituents And Bioactivities Of Zanthoxylum Echinocarpum Hemsl.and A Fungus Of Xylaria

Zanthoxylum echinocarpum Hemsl.,a vine of the family Rutaceae and Zanthoxylum,is mainly distributed in Hubei,Hunan,Guangdong,Guangxi,Guizhou and so on.It is commonly found in jungles at 200-1000 meters above sea level.The root bark of Z.echinocarpum is used to treat rheumatoid arthritis（RA）by the Tujia residents of western Hubei.Few investigations have been made on the pharmacological activity and chemical composition of Z.echinocarpum.Thus,the purpose of this research was to clarify the chemical composition of Z.echinocarpum and provide evidences for its further clinical application.A study on the 95% ethanol extract of the root bark of Z.echinocarpum led to the isolation of 59 compounds.Their structures were identified by extensive spectroscopic methods,modified Mosher ester analysis,X-ray diffraction and so on.17 simple coumarins and dihydrocoumarins were elucidated as new compounds.Among the known compounds,compounds 26,29,30,36,38,30,40,41,42,43,45,46,47,48,50,51,52,54 and 58 were separated for the first time in the genus.Xylaria is a member of the family of Xylariaceae.More than 300 species of Xylaria have been discovered worldwide,which are a great source of cytochalasins,alkaloids,polyketides,terpenoids and so on.A fungus of Xylaria,named Xylaria sp.DO1801,was isolated from the root of Damnacanthus officinarum.Its chemical composition was investigated.9 cytochalasins,including a new one（60）,were isolated from the ethyl acetate extract of the Xylaria sp.DO1801.The cytotoxicities of compounds 1-10,12,15-17,60-61 against several human tumor cell lines were evaluated by MTT method.The results showed that only 3exhibitted moderate cytotoxities against hepatocellular carcinoma Hep G2 and Hep3B with IC₅₀ values of 31.80 and 16.54μM,respectively.The anti-inflammatory effects of compounds 1-10,12,15 and 17 on LPS-induced RAW 264.7 macrophages were evaluated by the level of nitric oxide（NO）,tumor necrosis factor-α（TNF-α）and interleukin 1-β（IL-1β）.The results showed that all the tested compounds inhibited the production of NO,TNF-α,IL-1β,indicating these compounds exhibited anti-inflammatory effects.