马钱子总生物碱复合磷脂脂质体的抗肿瘤作用研究

目的: 通过比较马钱子总生物碱溶液和3种不同磷脂组成的马钱子总生物碱脂质体对H22荷瘤小鼠的抑瘤率,评价马钱子总生物碱复合磷脂脂质体的抗肿瘤作用。方法: 采用硫酸铵梯度法和隐形脂质体技术制备了3种不同磷脂组成的马钱子总生物碱脂质体。ICR小鼠接种H22肝癌瘤株造成移植性肝癌H22小鼠模型,测定马钱子总生物碱溶液、马钱子总生物碱大豆磷脂(SPC)脂质体、氢化大豆磷脂(HSPC)脂质体和复合磷脂脂质体各ip 1 mg ·kg^-1,连续10 d,观察对H22肝癌小鼠的抑瘤效果,比较给药后各组H22荷瘤小鼠的体重、免疫器官(脾和胸腺)指数和生命延长率。结果: 1 mg ·kg^-1剂量下的马钱子总生物碱溶液、SPC脂质体、HSPC脂质体和复合磷脂脂质体的抑瘤率分别为29.05%,29.29%,45.11%,37.23%;3种马钱子总生物碱脂质体未发现对免疫器官有明显的抑制作用;与对照组相比体重也无明显变化。结论: 复合磷脂脂质体是抗肿瘤中药有效部位马钱子总生物碱具有开发前景的新型载体。

Study on Antitumor Activity of Novel Liposomes Containing Total Alkaloids from Seed of Strychnos nux-vomica

Objective: Novel liposomes composed of hydrogenated soybean phosphatidylcholine (HSPC) and soybean phosphatidylcholine (SPC) was prepared to encapsulate total alkaloids from seed of Strychnos nux-vomica L. The antitumor activity of the novel liposomes was compared with corresponding HSPC or SPC liposomes. Method: Liposomes containing the total alkaloids were prepared by ammonium sulfate transmembrane gradients and stealth liposome technique. The total alkaloids liposomes with different lipid composition were administrated to H22 tumor-bearing mice. The parameters such as inhibition of tumor were calculated and compared. Result: The inhibition rate of tumor was 29.05%, 29.29%, 45.11%, 37.23% for total alkaloids solution, SPC liposomes, HSPC liposomes and novel liposomes, respectively. Results of comparison of mice weight and immune organ index revealed that no toxic effect was found as to liposomes containing total alkaloids. Conclusion: Taken together, improved antitumor activity and the reduced price of phospholipids indicate that the novel liposomes may act as promising carriers for total alkaloids extracted from seed of S.nux-vomica.