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新补骨脂异黄酮为中药补骨脂中的黄酮类成分,具有抗菌、抗炎、抗癌、抗骨质疏松等多种药理作用。该文研究了新补骨脂异黄酮在Caco-2细胞模型中的吸收机制。采用Thermo Syncronis C18柱,流动相为甲醇-0.1%甲酸水溶液(90∶10),流速0.2 m L·min~(-1),电喷雾电离正离子模式(ESI+),以柳胺酚为内标物质建立新补骨脂异黄酮在Caco-2细胞孵育液中浓度的检测方法,考察时间、浓度、P-gp蛋白抑制剂维拉帕米、MRP-2蛋白抑制剂MK-571和BCRP蛋白抑制剂Ko143对新补骨脂异黄酮吸收的影响。研究结果表明,新补骨脂异黄酮在10~2 000μg·L~(-1)具有良好的线性,且专属性、基质效应、提取回收率、精密度、准确度和稳定性均符合测定要求。新补骨脂异黄酮在Caco-2细胞模型中的转运与时间和浓度呈正相关。15,30,50μmol·~(L-1)的新补骨脂异黄酮ER分别为1.64,1.94,0.99。与对照组相比,盐酸维拉帕米,MK-571,Ko143均可促进新补骨脂异黄酮的转运,其中盐酸维拉帕米和Ko143的作用较为显著。新补骨脂异黄酮在Caco-2细胞模型中的吸收以主动转运为主,同时存在被动转运,可能存在肠道转运蛋白的外排机制。
The new psoralen is a flavonoid component in the traditional Chinese medicine psoralen, and has various pharmacological effects such as antibacterial, anti-inflammatory, anti-cancer and anti-osteoporosis. This paper studies the absorption mechanism of neoforhinol isoflavones in Caco-2 cell model. The mobile phase consisted of methanol-0.1% formic acid aqueous solution (90:10), flow rate 0.2 m L · min -1 and electrospray ionization positive ion mode (ESI +) on the Thermo Syncronis C18 column. Substance to establish a new method for the determination of the concentration of psoralen in Caco-2 cell culture medium. The effects of P-gp inhibitor verapamil, MRP-2 protein inhibitor MK-571 and BCRP protein inhibition Effect of the agent Ko143 on the absorption of. The results showed that the new isoflavone had a good linearity in the range of 10 ~ 2 000 μg · L -1, and the specificity, matrix effect, extraction recovery, precision, accuracy and stability were all in accordance with the determination requirements . The transport of new psoralen in Caco-2 cell model was positively correlated with time and concentration. The norepinephrine ER of 15, 30, 50μmol · L-1 were 1.64, 1.94, 0.99 respectively. Compared with the control group, verapamil hydrochloride, MK-571, and Ko143 all promoted the transport of neoforhinis isoflavones, and the effect of verapamil hydrochloride and Ko143 was significant. The absorption of new psoralen in Caco-2 cell model is mainly active transport, and there is passive transport, there may be efflux mechanism of intestinal transport protein.