HepG2细胞对丹酚酸B的摄取实验研究

Experimental study on the uptake of salvianolic acid B in HepG2 cells

目的研究丹酚酸B(SAB)在肝癌细胞中的摄取动力学特性。方法首先考察系列浓度SAB对HepG2细胞的毒性反应,确定SAB的安全浓度范围,然后建立UPLC-MS法检测SAB浓度,最后考察时间对HepG2细胞摄取SAB的影响,同时研究系列浓度的SAB作用于HepG2细胞后其摄取量,推算摄取动力学参数。结果1~128μmol·L^-1浓度的SAB作用24 h对HepG2细胞活力无明显影响;作用20 min后HepG2细胞对SAB的摄取开始趋于饱和;系列浓度的SAB作用HepG2细胞10 min后,细胞摄取SAB的量亦随着SAB浓度增加而增加,摄取动力学参数Vmax和Km分别为(9.59±1.75)ng/(mL·min)和(24.91±8.59)mmol·L^-1。结论HepG2细胞对SAB的摄取与时间及药物浓度相关,但尚不明确是主动摄取还是被动摄取过程。

Objective To determine the uptake kinetics of salvianolic acid B(SAB)in hepatocytes.Methods Firstly,the toxic reaction of SAB to HepG2 cells was investigated at different concentrations,and the safe concentration range of the drug was confirmed.UPLC-MS was established to detect the concentration of SAB.and the effect of time on the uptake of SAB in HepG2 cells was determined.The intake amount was calculated and the kinetic parameters were calculated after series concentrations of SAB acted on HepG2 cells.Results SAB at 1-128μmol·L^-1 had no obvious toxicity effect on HepG2 cells.After 20 min treatment,HepG2 cells began to saturate.After 10 min treatment,the amount of SAB intake was increased with the increase of SAB concentration.The uptake kinetics parameters Vmax and Km were(9.59±1.75)ng/(mL·min)and(24.91±8.59)mmol·L^-1.Conclusion The uptake of SAB in HepG2 cells is related to the time and concentration of drugs.It is not clear whether the uptake of SAB is active or passive.