银杏叶聚戊烯基磷酸酯体内外抗肿瘤的生物活性研究  

Antitumor Biological Activity of Polyprenyl Phosphate from Leaves of Ginkgo biloba L.in vivo and vitro

作　　者：王成章[1,2] 沈兆邦[1,2] 郑光耀[1,2] 张思访[1,2] 曹志庆[1,2] 高彩霞[1,2] 

机构地区：[1]中国林业科学研究院林产化学工业研究所 [2]国家林业局林产化学工程重点开放性实验室,江苏南京210042

出　　处：《林产化学与工业》2006年第3期13-16,共4页Chemistry and Industry of Forest Products

基　　金：国家自然科学基金资助项目(C02060103);国家林业局948项目资助(2003436)

摘　　要：研究了聚戊烯基磷酸酯（PPH）体外对肿瘤细胞和体内抗移植性肿瘤的抑制作用。从银杏叶中分离制备聚戊烯醇混合物（C75～C110），选择POCl3为磷酰化剂和三乙胺为碱性水解剂，经过磷酰化和水解二步反应，合成聚戊烯基磷酸单酯。以氟脲嘧啶（5-Fu）为对照，体外肿瘤细胞株选择SGC-7901人胃癌、LoVo人结肠腺癌和Hela人宫颈癌；体内移植性肿瘤细胞株选择肝癌实体型（Heps）、肉瘤（S180）、艾氏癌实体（EC），用不同剂量的PPH进行抗肿瘤药效实验。结果表明，银杏叶PPH在高浓度下（0．4g／L）作用72h，对3种体外细胞株抑瘤率达到60％-80％；对Heps、S180和EC等移植性瘤株抑瘤率达到50％-65％。这说明银杏叶PPH具有明显的抑制肿瘤的生物活性。The researches of pharmacology of polyprenyl phosphate （PPH） from Ginkgo biloba L. on antitumor in vitro and in vivo were carried out. After extracting,separating and purifying the mixs of polyprenols （C75-C110 ） from leaves of G. biloba L. , polyprenyl monophosphates were synthesized from polyprenols with POCl3 and triethanylamide. In contrast to 5-Fu, the antitumor activities were studied in vitro with SGC-7901 ,LoVo and Hela, and in vivo with mice transplanted tumors of Heps,S180 and EC Heps, S180 and EC. The pharmacologic experiments were done by various doses of PPH. Results show that PPH have the inhibi- tion of 60 %-80 % against SGC-7901, LoVo and Hela in vitro at high concentration of 0.400 g/L after 72 h, and have the inhibition of 50 %-65 % against transplanted Heps, S180 and EC. This shows that PPH from leaves of G. biloba L. has distinct antitumor biological activity.

关 键 词：银杏叶 聚戊烯醇 聚戊烯基磷酸酯 抗肿瘤 

分 类 号：TQ91[化学工程]