Studies On The Chemical Constituents Of Rubus Alceaefolius Poir

The source of Cu ye xuan gouzi is roots and stems of Rosaceae plants Rubus alceaefolius poir., with the effect of activating blood circulation to dissipate, clearing heat and stopping bleeding. It is is widely distributed in Jiangsu, Fujian, Taiwan and Guangdong Province. Rubus alceaefolius Poir. has been used in traditional medicine for the treatment of hepatitis, hepatosplenomegaly, dysentery, enteritis, mumps, injuries, rheumatism bone pain and other symptoms. Modern clinical reports revealed that Cu ye xuan gouzi is certainly the effect of nasopharyngeal carcinoma. Studies in modern medicine also showed that it can be used in the treatment of lung cancer and hepatic carcinoma, but less study on material foundation and mechanism had been operated. This project takes the roots and stems of Rubus alceaefolius poir. as the research object, studies systematically on the chemical constituents of Rubus alceaefolius Poir. and the preliminary studies on some compounds’ anticancer bioactivity. All the studies provide a basic data for the further studies on the physical foundation of medicinal efficacy of Rubus alceaefolius Poir. and to lay a foundation for clarifying bioactive compounds and developing a new version of a traditional chinese medicine.To clarify physical foundation of medicinal efficacy of Rubus alceaefolius Poir., we systematically investigate the chemical constituents of this plant. The dried powdered stems and roots of Rubus alceaefolius Poir. were extracted with 95% ethanol under reflux. The residue was partitioned successively with PE(Petroleum), CHCl3, Et OAc and n-butanol. 17 compounds were isolated from PE partition and chloroform partition with many column chromatograph methods and crystal method. Their structures were elucidated on the basis of spectral analysis techniques, which resulted in the isolation of eight triterpenoids: 3-oxotirucalla-7,24-dien-21-oic acid(4), 2α, 3α-dihydroxyolean-13(18)-en-28-oic acid(5),myricadiol(6), 19-α-hydroxy-3-acetyl-ursolic acid(7), euscaphic acid(10), 2α,3α-dihydroxyolean-11,13(18)-dien-19β,28-olide(11), uvaol(12), 3β-hydroxy-20,21,22, 23,24,25,26,27-octanordammaran-17β-ol(13); five quinones: chrysophanol(1), physcion(2), emodin(14), aloe emodin(15), 2,6-dimethoxy-1,4-benzoquinone(17); two phenylalkylamines: N-benzoylphenylalaninyl-N-benzoylphenylalaninate(7), aurantiamide acetate(8); one steroid: β-sitosterol(3); one ellagitannin: 3,3’,4’-tri-O-methylellagic acid(16). Compounds 1, 4-9, 11 and 13-17 are isolated from this plant for the first time, which which of compounds 11 and 13 were new compounds and compound 5 was obtained from nature for the first time. The antitumor activities of compounds 5, 10, 11 and 13(However, compound 11 was difficult to be dissolve in DMSO) were evaluated with the CNE-1(nasopharyngeal carcinoma), Spc(gastric cancer), and HGC-27(lung cancer) by using MTT assay; Compound 10 showed moderate inhibitory activity and IC50 Value was 37.020 μg/ml. No significant cytotoxicity was observed on the Chang Liver normal cell line.