红豆杉的抗肿瘤活性成分及其衍生物研究进展

Review on Anti-tumor Components from Taxus and Their Derivatives

通过文献调研,对红豆杉中活性成分和衍生物研究成果进行总结。结果显示,从红豆杉树皮、针叶、枝叶和内生真菌中发现有潜在研究价值的二萜、木脂素、多糖成分或有效部位,可作为重要的先导化合物,具有抑制前列腺癌、宫颈癌、卵巢囊腺癌、肺癌、胃癌、肝癌、黑色素瘤、舌鳞癌、肾癌、结肠癌、肠癌、乳腺癌和白血病细胞等作用。通过对红豆杉中紫杉烷类化合物中C-1、C-2、C-7、C-8、C-10、C-13、C-14、C-2'、C-3'等结构的化学修饰,发现了一系列活性高,毒副作用小的新型抗肿瘤活性成分,如含氟多烯紫杉醇、二茂铁-紫杉烷、噁二唑-多烯紫杉醇、吡啶-紫杉醇、喹啉-多烯紫杉醇、烷基化多烯紫杉醇和丙酯化、丙烯化多烯紫杉醇衍生物及单体化合物larotaxel、carbazitaxel、5-oxo-13-TBDMS-taxchinin A、5-oxo-13,15-epoxy-13-epi-taxchinin A等,为临床应用提供了新的药源。

On the basis of the literature research, this paper summarized the studies on the active components and derivatives of Taxus. The results showed that diterpenoids, lignins, polysaccharides were found from the bark, needles, branches and leaves, endophytic fungas of Taxus, which arised the effects of inhibiting the cancer cell lines of prostate, cervical, ovarian cystadenocarcinoma, lung, gastric, liver, melanin, tongue squamous, renal, colon, intestine, breast and leukemiafrom and had some potential value as lead compounds. A series of active anti-tumor components such as fluorine-containing docetaxel, ferrocenyl-paclitaxel, oxadiazole-docetaxel, pyridine-paclitaxel, quinoline-docetaxel, alkylated docetaxel and propylene/propylene-docetaxel derivatives, and monomer compounds of larotaxe, carbazitaxe, 5-oxo-13-TBDMS-taxchinin A ,5-oxo-13,15-epoxy-13-epi-taxchinin A ,which had higher activities and lower side effects, were found by modifying the structure of taxanes in C-1, C-2, C-7, C-8, C-10, C-13, C-14, C-2＇ and C-3＇,which provided the new medicine sources for clinical application.