摘要
目的:研究脂蟾毒配基(RBG)乳酸羟基乙酸共聚物-水溶性维生素E(PLGA-TPGS)纳米粒(RPTN)体外被人肝癌Hep G2细胞、小鼠腹水型高淋巴道转移肿瘤HCa-F细胞的摄取情况和对Hep G2细胞的毒性。方法:制备包载RBG和荧光标记物香豆素6的PLGA-TPGS纳米粒(RCPTN),荧光倒置显微镜观察Hep G2、HCa-F细胞对RCPTN的体外摄取情况。将试验分为阴性对照组、空白PLGA-TPGS纳米粒(EPTN)组、5-氟尿嘧啶溶液(FS)组、RBG溶液(RS)组、RBG/PLGA纳米粒(RPN)组、RPTN组,采用水溶性四氮唑(WST-1)法考察不同终质量浓度(1.25、2.5、5、10、20μg/m L)的FS、RS、RPN和RPTN作用24、48、72 h后Hep G2细胞在450 nm波长下的光密度,计算细胞存活率(CV)和半数抑制浓度(IC_(50))。结果:RCPTN分布在Hep G2、HCa-F细胞的细胞核周围。RPN组和RPTN组细胞的CV随RBG浓度增加而减小,随作用时间延长而减小;与FS组比较,RPTN组细胞的CV均减小(P<0.05或P<0.01)。FS、RS、RPN和RPTN作用于Hep G2细胞的IC_(50)随时间的延长而减小,且IC_(50)的大小依次为RS>FS>RPN>RPTN;RPN和RPTN作用48、72 h的IC_(50)明显小于FS与RS(P<0.05或P<0.01)。结论:RPTN可将RBG带入Hep G2、HCa-F细胞内部,其对Hep G2细胞具有抑制作用,且作用强于RPN、RS和FS。
OBJECTIVE： To study the in vitro uptake of Resibufogenin （RBG） lactic acid glycolic acid copolymer-water solu- ble vitamin E （PLGA-TPGS） in human liver cancer HepG2 cells, mouse ascites-type lymphatic metastasis of tumor HCa-F cells, and the toxicity on HepG2 cells. METHODS： RCPTN loading RBG and coumarin-6 （C6） were prepared. Fluorescent inverted mi- croscope was used to observe the in vitro uptake by RCPTN HepG2, HCa-F ceils. It was divided into negative control group, blank PLGA-TPGS nanoparticles （EPTN） group, 5-fluorouracil solution （FS） group, RBG solution （RS） group, RBG/PLGA nanoparti- cles （RPN） group and RPTN group. WST-1 was conducted to investigate the optical density at 450 nm wavelength of HepG2 cells after 24, 48, 72 h incubated by FS, RS, RPN and RPTN with different final concentrations （1.25, 2.5, 5, 10, 20 μg/mL） ; the cell viability （CV） and half inhibitory concentration （IC50） were calculated. RESULTS： RCPTN distributed around the nucleus of HepG2, HCa-F cells. CV was decreased by RBG concentration increased in RPN group and RPTN group, and decreased by time prolonged; compared with FS group, CV in RPTN group was decreased （P〈0.05 or P〈0.01）. IC50 of HepG2 cells incubated by FS, RS, RPN and RPTN was decreased by time prolonged, ordered by RS〉FS〉RPN〉RPTN; IC50 incubated by RPN and RPTN for 48, 72 h was obviously less than that of FS and RS （P〈0.05 or P〈0.01）. CONCLUSIONS： RPTN can deliver RBG in- to HepG2, HCa-F cells, showing inhibition effect on HepG2 cells which is stronger than RPN, RS and FS.
出处
《中国药房》
CAS
北大核心
2017年第16期2252-2255,共4页
China Pharmacy
基金
辽宁省科学技术计划项目(No.2015020308)
