目的研究来源于中药黄连中的4种生物碱成分盐酸黄连碱、盐酸药根碱、盐酸小檗碱、盐酸巴马汀经Caco-2细胞模型共同转运后的吸收特征。方法利用Caco-2细胞单层模型研究4种黄连生物碱从绒毛面到基底面的共同转运特征,并与4种生物碱单独进行的转运过程进行比较。采用超高效液相色谱法测定4种生物碱的浓度,计算表观渗透系数(Papp)及吸收率(%),并与阳性对照药普萘洛尔和阿替洛尔进行比较。结果经Caco-2细胞单层共同转运后黄连碱、药根碱、小檗碱、巴马汀的表观渗透系数(Papp)及吸收率(%)均是其单独转运时的1.63倍,1.28倍,1.55倍及1.05倍。结论 黄连4种生物碱类成分共同作用可促进其肠道吸收。
AIM To study the transport of coptisine hydrochloride,jatrorrhizine hydrochloride,berberine hydrochloride and palmatine hydrochloride coming from Coptidis Rhizoma by using Caco-2 monolayer model.METHODS Caco-2 cell was incubated and implanted to the cultured plate to form the monolayer cells available for research,and an ultra performance liquid chromatographic method was developed for the simultaneous determination of alkaloids.The concentration of four alkaloids in cell culture medium and the apparent permeability coefficients(Papp) as well as percent absorption from apical side to basolateral side were calculated,as compared with the reported values of propranolol and atenolol,as control drugs.RESULTS When the four alkaloids co-transported by the Caco-2 monolayer model,comparing with the transportation of single compound,the Papp value and percent absorption of coptisine,jatrorrhizine,berberine and palmatine increased to 163%,128%,155%,105%,respectively.CONCLUSION The results suggest that the mixture of four alkaloids in Coptidis Rhizoma should increase the intestinal absorption of the four ingredients.