今日药学

2011, v.21(11) 668-671+683

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姜黄素在Caco-2细胞模型中的吸收机制研究
Absorption Mechanism of Curcumin across Caco-2 Cell Model

闫文丽;黄兆胜;曾晓会;赵自明;黄雪君;房财富;
YAN Wen-li1,HUANG Zhao-sheng1,ZENG Xiao-hui2,ZHAO Zi-ming2,HUANG Xue-jun2,FANG Cai-fu1(1.Guangzhou University of Traditional Chinese Medicine,Guangzhou,Guangdong 510405,China;2.Guangdong Provincial Institute of Traditional Chinese Medicine,Guangzhou,Guangdong 510095,China)

摘要(Abstract):

目的测定姜黄素透过Caco-2单细胞层的浓度,研究其吸收特征。方法用Caco-2细胞单层模型来考察时间、浓度、不同药物酮康唑、维拉帕米、胡椒碱对姜黄素吸收的影响。采用液相色谱-质谱联用(LC-MS)法,测定姜黄素浓度并计算其表观渗透系数(Papp)。结果不同浓度姜黄素在90 min之前Papp大小顺序为:180>240>300μg/ml;与对照组比较,胡椒碱,低浓度酮康唑,维拉帕米对姜黄素的吸收均呈不同程度的促进作用(P<0.05)。结论姜黄素的吸收具有明显的高浓度饱和现象,且不呈线性变化,初步判定其吸收为主动吸收机制;促进姜黄素吸收的原因可能与酮康唑抑制Ⅰ相代谢酶CYP450 3A4和1A2酶的活性;胡椒碱抑制姜黄素Ⅱ相代谢酶—葡萄糖醛酸苷酶;维拉帕米抑制药物外排性转运蛋白—P-糖蛋白的活性有关。
Objective To determine the concentration of curcumin and study the absorption mechanism of curcumin in Caco-2 cell monolayer model.Methods Caco-2 cell monolayer model was applied to investigate the effects of conveying times,drug concentration,and other different drug,such as ketoconazole,verapamil and piperine on the absorption of curcumin.LC/MS was used to determine the concentration of curcumin and the apparent permeability coefficient(Papp) was calculated.Results The Papps of curcumin at different concentrations before the 90 min were ranked as follows: 180>240>300 μg/ml.Compared with the control group,a low concentration of ketoconazole,verapamil and piperine had different promotive actions on Papp values of curcumin(P<0.05).Conclusion Curcumin is nonlinear absorbed at higher concentration and highest saturated concentration appeared,which indicates that the absorption of curcumin in Caco-2 cell model should be an active transport.It can be promoted by Ketoconazole inhibiting CYP3A4 and 1A2,Piperine inhibiting glucuronidase enzyme,and Verapamil inhibiting P-glycoprotein.

关键词(KeyWords): 姜黄素;Caco-2细胞模型;吸收;代谢酶;P-糖蛋白
curcumin;Caco-2 cell model;absorption;metabolic enzymes;P-glycoprotein

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基金项目(Foundation): 广东省中医药局课题(编号:2009368)

作者(Author): 闫文丽;黄兆胜;曾晓会;赵自明;黄雪君;房财富;
YAN Wen-li1,HUANG Zhao-sheng1,ZENG Xiao-hui2,ZHAO Zi-ming2,HUANG Xue-jun2,FANG Cai-fu1(1.Guangzhou University of Traditional Chinese Medicine,Guangzhou,Guangdong 510405,China;2.Guangdong Provincial Institute of Traditional Chinese Medicine,Guangzhou,Guangdong 510095,China)

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