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目的建立同时测定Caco-2细胞模型中苦参碱、氧化槐果碱和氧化苦参碱的HPLC方法,探讨苦参总生物碱在Caco-2细胞模型的吸收机制。方法利用人源结肠腺癌细胞系Caco-2细胞单层模型,研究苦参碱、氧化槐果碱和氧化苦参碱由细胞绒毛膜面供给侧(AP)→基底外侧(BL)和BL→AP侧两个方向的转运过程;HPLC-UV法测定上述3个生物碱的量;计算转运参数和表观渗透系数(Papp)。结果苦参总碱给药后,苦参碱、氧化槐果碱和氧化苦参碱由AP→BL侧的Papp分别为(1.098±0.092)×10 5、(1.434±0.098)×10 5、(3.87±0.64)×10 6cm/s,由BL→AP侧的Papp分别为(1.104±0.098)×10 5、(1.034±0.079)×10 5、(2.75±0.33)×10 6cm/s,与文献报道的单体化合物给药相比,氧化槐果碱和氧化苦参碱双向转运的Papp明显增大。苦参碱、氧化槐果碱和氧化苦参碱的表观渗透率值分别为1.01、0.72、0.71。结论苦参总生物碱中苦参碱、氧化槐果碱和氧化苦参碱仍主要以被动吸收方式进入体内,但比各单体给药吸收更好。
OBJECTIVE: To establish an HPLC method for simultaneous determination of matrine, oxycodone and oxymatrine in Caco-2 cell model and to investigate the mechanism of the absorption of matrine alkaloids in Caco-2 cell model. Methods The monolayer model of human colon adenocarcinoma cell line Caco-2 was used to study the effects of matrine, oxycodone and oxymatrine on the chorionic villi (AP) → basolateral (BL) and BL → AP two sides of the transport process; HPLC-UV method for the determination of the amount of the three alkaloids; transport parameters and the apparent permeability coefficient (Papp). Results Papp of matrine, oxycodone and oxymatrine were (1.098 ± 0.092) × 10 5, (1.434 ± 0.098) × 10 5, ( 3.87 ± 0.64) × 10 6 cm / s, Papp from BL to AP side were (1.104 ± 0.098) × 10 5, (1.034 ± 0.079) × 10 5 and (2.75 ± 0.33) × 10 6 cm / s, Compared with the reported monomeric compound administration, Papp of bidirectional transport of oxycodone and oxymatrine increased significantly. The apparent permeabilities of matrine, oxycinacin and oxymatrine were 1.01, 0.72 and 0.71, respectively. Conclusion Matrine, oxycodone and oxymatrine in the total alkaloids of Sophora flavescens still enter the body mainly by passive absorption, but they are better absorbed than the administration of each monomer.