Oberlies N H, Rogers L L, Martin J M, McLaughlin J L
Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmacal Sciences, Purdue University, West Lafayette, Indiana 47907, USA.
J Nat Prod. 1998 Jun 26;61(6):781-5. doi: 10.1021/np9800304.
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.
对未成熟的鳄梨果实（牛油果，学名Persea americana）进行生物活性导向的分级分离，并通过卤虫致死试验进行监测，以分离出三种主要的生物活性成分（1 - 3）。化合物1 - 3均具有一个1,2,4 - 三醇部分和一条长脂肪链，脂肪链末端分别为烷烃、烯烃或炔烃；化合物1是新发现的，而化合物2和3此前已有报道，但未被描述为具有细胞毒性或杀虫作用的药剂。所有这些化合物在体外培养中均对六种人类肿瘤细胞系具有活性，并且对人前列腺腺癌（PC - 3）细胞具有选择性，其中化合物3的活性几乎与阿霉素相当。此外，在针对黄热病蚊子幼虫进行测试时，化合物3比鱼藤酮更有效，鱼藤酮是一种天然植物杀虫剂及阳性对照。
