白山毛桃根抗脑胶质瘤活性成分及其纳米胶束的制备

采用溶剂提取和萃取方法得到白山毛桃根乙酸乙酯、 正丁醇和水层萃取物. 通过噻唑蓝(MTT)比色法考察了各萃取物对脑胶质瘤细胞U87MG活性的抑制作用. 采用高效液相色谱(HPLC)指纹图谱法比对确认活性部位的主要化学成分为2α,3α,24-三羟基-12-烯-28-乌苏酸. 采用溶剂挥发法制备了2α,3α,24-三羟基-12-烯-28-乌苏酸纳米胶束, 对其包封率、 粒径及ζ电位等进行了表征, 并考察了其抗肿瘤活性. 体外细胞实验结果表明, 白山毛桃根乙酸乙酯萃取物对脑胶质瘤细胞U87MG具有抑制作用, 通过与标准品比对确认2α,3α,24-三羟基-12-烯-28-乌苏酸为乙酸乙酯部位的主要成分, 且该成分对脑胶质瘤细胞活性具有较强抑制作用. 通过溶剂挥发法制备的2α,3α,4-三羟基-12-烯-28-乌苏酸纳米胶束包封率为64.7%, 粒径为20 nm, 粒径分布宽度(PDI)为0.246, ζ电位为-5.7 mV. 细胞实验结果进一步证明, 与单体化合物相比, 2α,3α,24-三羟基-12-烯-28-乌苏酸纳米胶束对脑胶质瘤细胞活性具有更强的抑制作用, 为白山毛桃根在脑胶质瘤治疗中的应用提供了实验依据.

Anti-glioma Active Compounds and Their Nanomicelles Preparation of the Root of Actinidiaeriantha Benth†

Actinidiaeriantha Benth was extracted by ethyl acetate, n-butyl alcohol and water, and three fractions were obtained. The in vitro cell experiments showed that ethyl acetate was the anti-glioma active fraction of the root of Actinidiaeriantha Benth. The high performance liquid chromatographic fingerprint confirmed that main compound of ethyl acetate fraction was 2α,3α,24-trihydroxyurs-12-en-28-oic acid, and it could significantly inhibit the glioma cell activity. The prepared 2α,3α,24-trihydroxyurs-12-en-28-oic acid loaded nanomicelles was with high loading efficiency of 64.7%, average diameter of 20 nm with polydispersity index(PDI) of 0.246 and ζ potential of -5.7 mV. Further cell experiment demonstrated the 2α,3α,24-trihydroxyurs-12-en-28-oic acid loaded nanomicelles through solvent evaporation with better inhibitory effects on the glioma cells than free one. Taken together, the ethyl acetate fractions from the root of Actinidiaeriantha Benth were confirmed with the anti-glioma activity, and 2α,3α,24-trihydroxyurs-12-en-28-oic acid was the main active compound. The prepared 2α,3α,24-trihydroxyurs-12-en-28-oic acid loaded nanomicelles was with good water dispersity and anti-glioma activity, providing solid experimental base for the application of the root of Actinidiaeriantha Benth in glioma therapy.