紫杉烷类抗癌新药—紫杉特尔的研究进展（Research progress of anticancer drug taxol and taxanes.）.doc

紫杉烷类抗癌新药—紫杉特尔的研究进展（Research progress of anticancer drug taxol and taxanes.） Research progress of anticancer drug taxol and taxanes. Update Date: 2009-05-02 click: Bian Yimin, Lai Shuizhao, Jin Yanxin In 1963 the U.S. National Cancer Institute (NCI) has a unique taxane isolated from Taxus plants first (taxane) two terpene taxol - compound skeleton structure (paclitaxel), and found that it has broad-spectrum anti-tumor activity, after 30 years, in the world has formed the research upsurge of paclitaxel anticancer drugs, including paclitaxel and docetaxel (docetaxel, marketed as Taxotere) has now become the two most popular taxane anticancer drugs (Taxoid). The literature on Taxol has been reported in detail. This paper will make a comprehensive introduction to the research progress of taxol. 1 overview [1~3] Paclitaxel is a new semi synthetic taxol derivative. Early biological research shows that this product has better antitumor activity, phase I clinical trial began in 1990, and then began to phase II and III clinical trials in 1992 and 1994 respectively, phase III study is still continuing. This product has been listed in Canada, South Africa, Mexico, Norway and other countries. 2 mechanism of anticancer action [1, 4, 5] The product of the anticancer mechanism of taxol is similar, stable microtubules, promote the speed and degree of polymerization of tubulin, and by inhibiting microtubule depolymerization and tumor cell mitosis termination and make tumor cell apoptosis (apoptosis), finally lead to tumor cell death. However, this product and paclitaxel have different effects on microtubule assembly proteins (MAPS), indicating differences in activity and drug resistance between the two drugs. This product promotes tubulin polymerization and inhibits microtubule depolymerization, which is two times higher than taxol. 3 cytotoxicity [5] In vitro, docetaxel on many cells 1.3 to 12 times larger than paclitaxel for many murine and human tumor cell lines, paclitaxel and do