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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10 h时顺铂累计释放率为32%,与人肝癌细胞SMMC-7721孵育72 h的IC50为(45.5±10.3),累计给药为12 mg·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。
Objective: To study the in vivo toxicity and antitumor activity of polyglutamic acid aspartate and cisplatin complex (PGA-Asp-CDDP). Methods: The sustained-release, cytotoxicity, in vivo toxicity and anti-tumor activity of PGA-Asp-CDDP were detected by dialysis method, MMT method, Kunming mouse and BALB / c nude mice SMMC- RESULTS: The cumulative release of cisplatin at 32 h after PGA-Asp-CDDP was 32%, and the IC50 of hepatocellular carcinoma cell SMMC-7721 incubated at 72 h was (45.5 ± 10.3) In vivo toxicity was significantly decreased, and the liver cancer model has significant anti-tumor effect (P <0.01). Conclusion: Polyglutamic acid aspartate cisplatin compound is expected to become a safe and effective drug for the treatment of liver cancer.