藤黄酸纳米制剂的制备及其抗肿瘤活性  

Preparation and anti-tumor activity of gambogic acid nanopreparations

作　　者：李娇娇 赵梦楠 糜丹丹 王茹静[1] 李雨珂 荆倩 邹兰 谢金金 杨欢[1] 杜鑫 石三军 LI Jiaojiao;ZHAO Mengnan;MI Dandan;WANG Rujing;LI Yuke;JING Qian;ZOU Lan;XIE Jinjin;YANG Huan;DU Xin;SHI Sanjun(School of Pharmacy,Chengdu University of Traditional Chinese Medicine,Sichuan Chengdu 611137,China)

机构地区：[1]成都中医药大学药学院,四川成都611137

出　　处：《现代肿瘤医学》2023年第24期4503-4507,共5页Journal of Modern Oncology

基　　金：国家自然科学基金青年项目(编号:82003689);四川省杰出青年科技基金(编号:2022JDJQ0052)。

摘　　要：目的:优化藤黄酸脂质体(GA-LIP)及白蛋白纳米粒(GA-BSA NP)的药载比,研究GA-LIP及GA-BSA NP的体外抗肿瘤活性。方法:制备GA-LIP和GA-BSA NP,采用安东帕粒径仪分析粒径和多分散系数(PDI),高效液相色谱法(HPLC)测定包封率,透射电子显微镜表征形貌;采用MTT法检测GA-LIP及GA-BSA NP对B16F10的增殖抑制作用,细胞划痕实验检测细胞迁移能力,流式细胞术检测细胞凋亡率,通过肿瘤干细胞球增殖抑制检测对B16F10干细胞的抑制作用。结果:优化后的GA-LIP药载比为1∶5,GA-BSA NP为1∶10。GA对B16F10细胞的半抑制浓度(IC50)为0.1550μmol/L,GA-LIP为0.1078μmol/L,GA-BSA NP为0.0815μmol/L。GA-LIP和GA-BSA NP均抑制B16F10细胞迁移,促进细胞凋亡,并抑制肿瘤干细胞球生长。结论:GA-LIP和GA-BSA NP均较好抑制B16F10细胞的增殖、迁移并诱导细胞凋亡,同时可以抑制肿瘤干细胞球生长,两种制剂中BSA NP活性更强。Objective:To optimize the drug load ratio of gambogic acid liposome(GA-LIP)and albumin nanoparticles(GA-BSA NP),and to study the anti-tumor activity of GA-LIP and GA-BSA NP in vitro.Methods:GA-LIP and GA-BSA NP were prepared.The particle size and PDI were analyzed by Antonpa particle size analyzer.The encapsulation efficiency was determined by high performance liquid chromatography(HPLC).The inhibitory effect of GA,GA-LIP and GA-BSA NP on the proliferation of B16F10 was detected by MTT assay,the cell migration ability was detected by cell scab assay,the apoptosis rate was detected by flow cytometry,and the inhibitory effect of B16F10 on the proliferation of tumor stem cell spheres was detected.Results:The optimized drug load ratio of GA-LIP was 1∶5,and GA-BSA NP was 1∶10.The IC_(50)of GA on B16F10 cells was 0.1550μmol/L,GA-LIP was 0.1078μmol/L,GA-BSA NP was 0.0815μmol/L.Both GA-LIP and GA-BSA NP inhibited B16F10 cell migration,promoted cell apoptosis,and inhibited tumor stem cell spheres'growth.Conclusion:Both GA-LIP and GA-BSA NP can effectively inhibit the proliferation,migration and promote apoptosis of B16F10 cells,and inhibit the growth of tumor stem cells spheres.The NP activity of BSA in the two preparations is stronger.

关 键 词：藤黄酸 B16F10 纳米制剂 增殖 迁移 凋亡 干细胞 

分 类 号：R730.52[医药卫生—肿瘤]