栀子苷与栀子柏皮汤中栀子苷在MDCK细胞跨膜转运模型上的转运研究  

Transport of geniposide and geniposide in Zhizi Bopi Decoction in MDCK cell membrane model

作　　者：韩静文[1] 李俊[1] 黄成[1] 陈昭琳[1] 胡婷婷[1] 

机构地区：[1]安徽医科大学药学院,安徽天然药物活性研究省级实验室,安徽合肥230032

出　　处：《中国药理学通报》2014年第4期468-472,共5页Chinese Pharmacological Bulletin

基　　金：安徽省自然科学基金资助项目(No 1206c0805026);安徽医科大学博士科研启动基金(No XJ201118)

摘　　要：目的考察栀子苷与栀子柏皮汤中栀子苷在MDCK细胞跨膜转运模型上的转运特性。方法利用MTT实验筛选出栀子苷和栀子柏皮汤在MDCK细胞上的安全浓度,以MDCK细胞跨膜转运模型研究药物的双向转运,考察时间、药物浓度、P-糖蛋白(P-gp)抑制剂及EDTA对栀子苷转运的影响,然后比较相同浓度的栀子苷和栀子柏皮汤中栀子苷吸收转运的差异,采用HPLC法检测栀子苷的浓度,计算其表观渗透系数(Papp)。结果栀子苷在MDCK细胞模型上的转运量具有一定的时间和浓度依赖性,P-gp抑制剂对其转运没有明显影响,EDTA能够增加其跨膜转运量,各浓度栀子柏皮汤中栀子苷的吸收Papp分别为(8.96±0.35)×10-7cm·s-1,(8.95±0.38)×10-7cm·s-1和(9.16±0.30)×10-7cm·s-1、明显高于栀子苷单体的吸收Papp(5.85±0.44)×10-7cm·s-1、(6.88±0.38)×10-7cm·s-1和(6.31±0.19)×10-7cm·s-1(P<0.05)。结论栀子苷在MDCK细胞模型上表现为被动扩散,且不受P-gp的影响,可能有细胞旁路转运,栀子柏皮汤能促进栀子苷的吸收。Aim To study the transport of geniposide and geniposide in Zhizi Bopi Decoction in MDCK cell membrane model. Methods The safety concentration of geniposide and Zhizi Bopi Decoction in MDCK cells were determined by MTT assay. Then the MDCK cell membrane model was used to investigate the transport of drugs. Firstly, the effects of time, drug concentra-tion, P-gp inhibitor and EDTA on the absorption and transport of geniposide were studied systematically. Secondly, the differences were compared between the transport of the same concentration of geniposide as single compound and that in Zhizi Bopi Decoction in MDCK cell model. The drug concentration was deter-mined by high performance liquid chromatography （ HPLC） to calculate the apparent permeability coeffi-cient （Papp）. Results Geniposide transport in MDCK cell monolayer was time and concentration dependent.＆amp;nbsp;P-gp inhibitors had no significant effect on its transport and the transport of geniposide was enhanced by ED-TA. The absorption Papp of different concentrations of geniposide in Zhizi Bopi Decoction were （ 8. 96 ＆#177; 0. 35 ） ＆#215; 10 -7 cm ＆#183; s-1 , （ 8. 95 ＆#177; 0. 38 ） ＆#215; 10 -7 cm ＆#183; s-1 and （9. 16 ＆#177; 0. 30） ＆#215; 10 -7 cm＆#183;s-1, significantly higher than the absorption Papp of geniposide as single compound（5. 85 ＆#177; 0. 44） ＆#215; 10 -7 cm＆#183;s-1, （6. 88 ＆#177; 0. 38） ＆#215; 10 -7 cm＆#183;s-1 and （6. 31 ＆#177; 0. 19） ＆#215; 10 -7 cm ＆#183;s-1 （ P＆lt;0. 05 ） . Conclusion The transport of ge-niposide in MDCK cell membrane model is passive transport and is not affected by P-gp. Geniposide may transport via the paracellular route. The Zhizi Bopi De-coction can increase the absorption of geniposide.

关 键 词：栀子苷 栀子柏皮汤 跨膜转运 被动转运 

分 类 号：R284.1[医药卫生—中药学] R329.2[医药卫生—中医学]