Cytotoxic and insecticidal constituents of the unripe fruit of Persea americana
Cytotoxic and insecticidal constituents of the unripe fruit of Persea americana
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DOI：
10.1021/np9800304
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发表时间：
1998-06-01
影响因子：
5.1
通讯作者：
McLaughlin, JL
中科院分区：
文献类型：
--
作者：
Oberlies, NH;Rogers, LL;McLaughlin, JL
对未成熟的鳄梨果实（Persea americana）进行生物活性定向分级，如通过卤虫致死性测定监测的，以分离三种主要的生物活性成分（1-3）。化合物1-3都具有1，2，4-三醇部分和长脂族链，其分别以烷烃、烯烃或炔终止; 1是新的，而2和3先前已被描述，但不是作为细胞毒性剂或杀虫剂。所有这些都对培养中的六种人肿瘤细胞系具有活性，并显示出对人前列腺腺癌（PC-3）细胞的选择性，其中3种几乎与阿霉素一样有效。此外，当对黄热病蚊子幼虫进行测试时，3比鱼藤酮（一种天然植物杀虫剂和阳性对照）更有效。
Unripe avocado fruit (Persea americana) was subjected to a bioactivity-directed fractionation, as monitored via the brine shrimp lethality assay, to isolate three major bioactive constituents (1-3). Compounds 1-3 all have a 1,2,4-triol moiety and a long aliphatic chain that terminates as either an alkane, alkene, or alkyne, respectively; 1 is new, while 2 and 3 have been described previously but not as cytotoxic or pesticidal agents. All have activity against six human tumor cell lines in culture and show selectivity for human prostate adenocarcinoma (PC-3) cells with 3 being nearly as potent as adriamycin. Also, when tested against yellow fever mosquito larva, 3 was more effective than rotenone, a natural botanical insecticide and positive control.