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| Regular issue | Vol 87, No. 3, 2013, pp.627-636
Published online, 1st February, 2013
DOI: 10.3987/COM-12-12659
Further Bisindole Alkaloids from Catharanthus roseus and Their Cytotoxicity

Wei-Ku Zhang, Jie-Kun Xu, Hai-Yan Tian, Lei Wang, Xiao-Qi Zhang, Xu-Zhi Xiao, Ping Li,* and Wen-Cai Ye*

*Department of Pharmacology, Institute of Clinical Medical Sciences, China-Japan Friendship Hospital, No.2 Ying Hua Dong Lu, ChaoYang District, Beijing, China


Two novel bisindole alkaloids, cyclovinblastine A-B (1-2), together with ten known alkaloids 4-deacetoxycyclovinblastine (3), cycloleurosine (4), leurosine (5), vinblastine (6), leurosidine (7), vinblastine N'b-oxide (8), isoleurosine (9), 4'-deoxyleurosidine (10), 4'-deoxyleurosidine N'b-oxide (11) and 4-desacetoxyvinblastine (12) were isolated from the leaves of Catharanthus roseus. The structures of 1 and 2 were established by analysis of their NMR and HR-ESI-MS spectroscopic data. All alkaloids (1-12) were evaluated for their cytotoxic activities against the human hepatocellular carcinoma (HepG2) cell line, human colorectal carcinoma (Lovo) cell line, and human breast carcinoma (MCF-7) cell line by the MTT method in vitro, respectively. The results indicated that cytotoxic activities of alkaloids 9, 10 and 12 were much more potent than those of the positive control vinblastine (6). In addition, the structure-activity relationships (SAR) were conducted on the basis of the cytotoxicity of these isolated alkaloids.