中文摘要：

目的：研究聚谷氨酸天冬氨酸顺铂复合物（PGA-Asp—CDDP）的体内毒性和抑瘤活性。方法：采用透析法、MMT法、昆明鼠和BALB／c裸鼠SMMC-7721肝癌模型检测PGA-Asp—CDDP的缓释作用，细胞毒性，体内毒性和抑瘤活性。结果：PGA-Asp—CDDP的10h时顺铂累计释放率为32%，与人肝癌细胞SMMC-7721孵育72h的IC50为（45．5±10．3），累计给药为12mg·kg^-1时体内毒性显著下降，并且对肝癌模型有显著抑瘤效果（P〈0．01）。结论：聚谷氨酸天冬氨顺铂复合物有望成为治疗肝癌的一种安全有效的药物。

英文摘要：

OBJECTIVE To evaluate in vivo toxicity and antitumor activity of poly （γ-glutamic acid）asp-cisplatin complex （PGA-Asp-CDDP）. METHODS The release profile of PGA-Asp-CDDP was studied with a dialysis method. The cytotoxicity of the complex was detected by MTT assay. In vivo toxicity of the complex was performed in KM mice and its anti-tumor effect was evaluated in human hepatoma cell SMMC 7721 grafted mice. RESULTS CDDP could be gradually released from PGA Asp-Pt in physiological saline at 37 ℃ and the accumulative released rate was 32% at 10 h. The IC50 value of PGA-Asp- CDDP was 45. 5±10. 3 against SMMC-7721 cell when incubation at 72 h. In vivo experiments showed that the toxicity of PGA-Asp-CDDP significantly decreased at the cumulative administration concentration of 12 mg·kg^-1 and PGA-Asp-CDDP treatment had significantly higher antitumor activity than control treatment （P〈0. 01）. CONCLUSION PGA-Asp-CDDP may become a safe and effective drug for the treatment of liver cancer.