Vanhaelen M H
Laboratoire de Pharmacognosie et de Bromatologie, Université Libre de Bruxelles.
J Pharm Belg. 1992 Sep-Oct;47(5):417-24.
Phytochemical and pharmacological studies on Taxus sp extracts have resulted in the isolation and the identification of several diterpenoids, and the discovery of the potent antitumor activity of taxol. This natural compound displays a unique mechanism of action as it stabilizes microtubules and inhibits their depolymerization into free tubulin. The emergence of taxol from the screening of natural products shows the benefits and the potent interest of these constituents in the search of drugs exhibiting novel mechanisms of action. The most pressing problem in taxol or taxol derivates commercialization is the drug supply. Alternative sources of taxol are now under investigation, mainly the total synthesis of taxol, the hemisynthesis of taxol or of taxotere from 10-deacetylbaccatine III, the in vitro production of taxol by cell or tissue cultures, and the prospection of new natural sources of taxol.
对红豆杉属植物提取物的植物化学和药理学研究已导致多种二萜类化合物的分离和鉴定,并发现了紫杉醇的强大抗肿瘤活性。这种天然化合物表现出独特的作用机制,因为它能稳定微管并抑制其解聚为游离微管蛋白。从天然产物筛选中出现的紫杉醇表明了这些成分在寻找具有新作用机制的药物方面的益处和巨大吸引力。紫杉醇或紫杉醇衍生物商业化中最紧迫的问题是药物供应。目前正在研究紫杉醇的替代来源,主要包括紫杉醇的全合成、从10-去乙酰巴卡亭III半合成紫杉醇或多西他赛、通过细胞或组织培养体外生产紫杉醇,以及寻找紫杉醇的新天然来源。