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介绍了制备一种γ-聚谷氨酸-D-半乳糖酯化衍生物-顺铂复合物[poly(γ-glutamic acid)-D-galactose esterifiable derivative-cisplatin complex compound,γ-D+-DDP],并考察其抗肿瘤活性。主要通过生物发酵获得大分子γ-聚谷氨酸[poly(γ-glutamic acid),γ-PGA],利用酸降解得到可以作为药物载体的小分子γ-聚谷氨酸;利用凝胶色谱柱检验小分子γ-聚谷氨酸的分子量;利用MTT法检测该复合物的体外抗肿瘤作用。结果表明:成功获得γ-聚谷氨酸-D-半乳糖酯化衍生物-顺铂复合物,该复合物载药率达9.4%~10.2%;该复合物对人肝癌细胞BEL-7402具有显著的杀伤作用,能引起细胞凋亡(HE染色观察得到)。因此,γ-聚谷氨酸-D-半乳糖酯化衍生物-顺铂复合物是一种有效的抗肿瘤药物,具有潜在的临床应用价值;生物发酵的γ-聚谷氨酸可用于药物载体,赋予药物新的特点。
The preparation of a poly (γ-glutamic acid) -D-galactose esterifiable derivative-cisplatin complex compound (γ-D + -DDP) , And investigated its anti-tumor activity. Mainly through biofermentation to obtain γ-polyglutamic acid (γ-polyglutamic acid), γ-PGA], which is degraded by acid to obtain small molecule γ-polyglutamic acid which can be used as drug carrier; The molecular weight of the small molecule γ-polyglutamic acid was tested. The antitumor activity of the complex in vitro was tested by MTT assay. The results showed that the drug-loaded rate of the compound was 9.4% -10.2%, and the compound was successfully obtained on human hepatocellular carcinoma cell BEL-7402 Significant killing effect, can cause apoptosis (observed by HE staining). Therefore, γ-polyglutamic acid-D-galactose esterified derivatives - cisplatin complex is a potent anti-tumor drug with potential clinical value; bio-fermented γ-polyglutamic acid can be used for drugs Vector that gives the drug new features.