Discovery and development of anticancer agents from plants.
Discovery and development of anticancer agents from plants.
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DOI：
10.1046/j.1359-4117.2002.01038.x
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发表时间：
2002-07-01
影响因子：
--
通讯作者：
McLaughlin, Steve
中科院分区：
文献类型：
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作者：
Valeriote, Fred;Grieshaber, Charles K;McLaughlin, Steve
一种用于发现抗癌剂的新型体外试验用于检测主要收集于美国西南部和西部的1847种植物的水和有机提取物。检测结果分为5类：无活性（62%）、同等活性（36%）、同等活性和有效（0.5%）、实体瘤选择性（1.4%）和人类选择性（0.8%）。后三类提取物采用体外分离法对每一步进行生物指导。骨参提取物对实体瘤具有选择性，经分离得到两种活性化合物：dalrubone和5-甲氧基dalrubone。其活性和效力相同，产生脱氧鬼臼毒素作为活性化合物。花Linanthus floribundus对人有选择性，其活性化合物为霜蝶苷。讨论了该试验从活性提取物中发现新型抗癌药物的潜力。
A novel in vitro assay for the discovery of anticancer agents was used to examine aqueous and organic extracts from 1847 plants collected mainly in the U.S. Southwest and West. The assay results were separated into 5 categories: inactive (62%), equally active (36%), equally active and potent (0.5%), solid tumor selective (1.4%), and human selective (0.8%). Extracts from the latter three categories were fractionated using the in vitro assay to biodirect each step. Psorothamnus emoryi extracts were solid tumor selective and yielded two active compounds upon fractionation: dalrubone and 5-methoxydalrubone. Calocedrus decurrens was equally active and potent and yielded deoxypodophyllotoxin as the active compound. Linanthus floribundus was human selective and yielded strophanthidin as the active compound. The potential of this assay to discover novel anticancer agents from the active extracts is discussed.