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标题：Cytotoxic Constituents of Propolis from Myanmar and Their Structure–Activity Relationship
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作者：Feng Li ; Suresh Awale ; Yasuhiro Tezuka 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：2009
卷号：32
期号：12
页码：2075-2078
DOI：10.1248/bpb.32.2075
出版社：The Pharmaceutical Society of Japan
摘要：Thirteen cycloartane-type tritepenes (1—13) and four prenylated flavanones (14—17) isolated from propolis collected in Myanmar, were evaluated for their cytotoxic activity against a panel of six different cancer cell lines; three murine cancer cell lines (colon 26-L5 carcinoma, B16-BL6 melanoma, and Lewis lung carcinoma) and three human cancer cell lines (lung A549 adenocarcinoma, cervix HeLa adenocarcinoma and HT-1080 fibrosarcoma). Among them, a cycloartane-type triterpene, 3α,27-dihydroxycycloart-24 E -en-26-oic acid (3), showed the most potent cytotoxicity against B16-BL6 cells with an IC₅₀ value of 5.91 μ M , comparable to those of positive controls, doxorubicin (IC₅₀, 5.66 μ M ) and 5-fluorouracil (IC₅₀, 4.88 μ M ). In addition, (2 S )-5,7-dihydroxy-4′-methoxy-8,3′-diprenylflavanone (14) exhibited strong cytotoxicity against all the tested cancer cell lines with the IC₅₀ values ranging from 14.0 to 26.4 μ M . Based on the observed results, the structure–activity relationships are discussed.
关键词：propolis;cytotoxicity;cycloartane-type triterpene;flavanone;structure–activity relationship