浙江中西医结合杂志

聂根,黄旭军,张信平,徐江琳,毛园清,朱真,程时刚.毛蕊异黄酮的体外转运研究及对多药耐药基因MDR1表达的影响[J].浙江中西医结合杂志,2015,25(9):

毛蕊异黄酮的体外转运研究及对多药耐药基因MDR1表达的影响

Transport characteristics of Calycosin and its effect on multidrug resistance (MDR1) gene expression

投稿时间：2015-04-30 修订日期：2015-05-04

DOI：

英文关键词:Calycosin Caco-2 cell model Multidrug resistant gene Passive diffusion

基金项目:

作者	单位	E-mail
聂根^*	东阳市横店集团医院	sun_ming_liang@126.com
黄旭军	东阳市横店集团医院
张信平	东阳市横店集团医院
徐江琳	东阳市横店集团医院
毛园清	东阳市横店集团医院
朱真	湖北省省中医院
程时刚	湖北省妇女儿童医院

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中文摘要:

目的：研究毛蕊异黄酮在体外模型Caco-2细胞单层模型的转运特征及其对多药耐药基因MDR1表达的影响。方法：采用MTT法确定毛蕊异黄酮对Caco-2细胞模型作用的安全浓度范围；考察浓度、pH、温度及P-gp抑制剂(维拉帕米)和能量代谢抑制剂(叠氮化钠)对毛蕊异黄酮转运的影响；抑制多药耐药基因MDR1对毛蕊异黄酮转运的影响。结果：从顶侧(AP)到底侧(BL)(AP→BL),毛蕊异黄酮的P_app＞10_?6cm/s,表明其吸收性良好；毛蕊异黄酮的转运与其浓度和时间呈正相关,4℃下毛蕊异黄酮的P_app与37、25℃下的Papp有显著差异,pH=9时的P_app与pH=5、7.4时的P_app值也有明显差异(p＜0.01)。毛蕊异黄酮的转运不受MDR1基因的影响；叠毛蕊异黄酮的P_appBL→AP/P_appAP→BL＜1.5不受能量代谢异常的影响。结论：毛蕊异黄酮在Caco-2细胞模型的转运方式为被动扩散,且不受P-gp和能量代谢的影响,低温和碱性环境下不利于药物的吸收。

英文摘要:

Objective: To investigate the transport characteristics of Calycosin across Caco-2 cell monolayer and the effect on multidrug resistance (MDR1) gene expression. Methods: Safe concentration range of Calycosin against Caco-2 cell monolayer model was selected by MTT method;The effects of concentration, temperature, pH, P-gp inhibitor (Verapamil) and energy metabolism inhibitor(Sodium azide) on the absorption of Calycosin were observed by Caco-2 cell monolayer model. Results: The Papp of Calycosin transport from apical (AP) side to basolateral (BL) side was over 10_-₆ cm/s, which showed a good absorption. The transport of Calycosin was positively correlated with time and concentration.The transport of Calycosin was influenced by the change of temperature and pH. The transport of Calycosin was not influenced by the resistance (MDR1) gene expression, the number of P_appBL→AP/P_appAP→BL was less than 1.5. Conclusion: The transport of Calycosin across Caco-2 cell monolayer model is passive diffusion,and is not influenced by the change of P-gp and energy metabolism.Low temperature and alkaline environment is not conducive to the absorption of Calycosin.

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