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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POC l3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(0.4 g/L)作用72 h,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。
Polypentenyl phosphate (PPH) was studied in vitro for inhibition of tumor cells and anti-tumor tumors in vivo. Preparation of polypentenol mixture (C75~C110) from Ginkgo biloba leaves, POC l3 as the phosphorylating agent and triethylamine as basic hydrolyzing agent, two-step reaction of phosphorylation and hydrolysis, synthesis of polypentenyl Phosphomonoesters. Using 5-Fu as control, SGC-7901 human gastric cancer, LoVo human colon adenocarcinoma and Hela human cervical cancer were selected as tumor cell lines in vitro. In vivo transplanted tumor cell lines were selected for solid hepatoma (Heps) and sarcoma ( S180), Ehrlich carcinoma entity (EC), anti-tumor efficacy experiments with different doses of PPH. The results showed that the effect of PPH in Ginkgo biloba leaves (0.4 g/L) was 72 h, and the inhibition rate of the three in vitro cell lines reached 60% to 80%; the tumor inhibition rate of Heps, S180, and EC tumors was also studied. It reaches 50%~65%. This shows that Ginkgo biloba leaf PPH has significant biological activity in inhibiting tumors.