摘要
目的研究葛根素肠道吸收的机制,探讨提高其肠道吸收的方法。方法改变实验时间、温度及药物质量浓度,考察葛根素在Caco-2细胞中的转运特性,并考察不同的吸收促进剂对其跨膜转运的影响。结果葛根素的膜渗透性低,被动扩散是其跨膜转运的主要机制;十二烷基磺酸钠(SDS)破坏Caco-2单细胞层的完整性,提高葛根素转运;聚氧乙烯月桂基醚(Brij 35)、牛血清白蛋白(BSA)和分离乳清蛋白对葛根素转运有促进作用,但不影响Caco-2细胞的跨膜电阻(TEER);相对分子质量较高的壳聚糖通过可逆性地降低TEER,促进细胞间转运,提高葛根素的膜渗透性。结论葛根素的膜渗透性低是口服生物利用度低的主要原因,不同吸收促进剂可通过不同机制改善其膜渗透性。
Objective To study the mechanism of puerarin （PE） intestinal absorption and investigate the possible methods to improve its intestinal absorption. Methods The characteristics of PE transport across Caco-2 cell monolayer were determined by changing incubation time, temperature, and PE concentration. The effect of different absorption enhancers on its membrane transport permeability was studied as well. Results The intestinal permeability of PE was low and the passive diffusion was the main mechanism for its transport across Caco-2 cells. Sodium dodecyl sulfate （SDS） improved PE transport by impairing the integrity of Caco-2 cell monolayer. Brij 35, bovine serum albumin （BSA）, and whey protein isolation promoted the PE transport, without affecting the transepithelial electric resistance （TEER） of Caco-2 cells. Chitosan of relatively high molecular weight reversibly lowered TEER, thereby improving PE intercellular transport. Conclusion The low peroral bioavailability of PE is probably due to its low membrane permeability. The different absorption enhancers could improve its membrane transport permeability across Caco-2 cells via diverse mechanisms.
出处
《中草药》
CAS
CSCD
北大核心
2011年第11期2265-2269,共5页
Chinese Traditional and Herbal Drugs
基金
国家自然科学基金资助项目(30672441
30873057)
