Caco-2细胞单层研究淫羊藿黄酮类成分的吸收转运

目的 研究淫羊藿黄酮类成分在Caco-2细胞模型中的吸收转运.方法 采用超高压液相法测定药物浓度,计算表观渗透系数(Papp),研究淫羊藿黄酮5个主要成分淫羊藿苷、朝藿定A、朝藿定B、朝藿定C、宝藿苷I在Caco-2细胞模型中的双向转运.结果 淫羊藿苷、朝藿定A、朝藿定B、朝藿定C的吸收渗透系数(P_(AB))较小,分别为5.91×10~(-7)、3.22×10~(-7)、2.76×10~(-7)、4.23×10~(-7) cm/s,宝藿苷I相对较大,为1.46×10~(-6)cm/s;5个化合物的分泌渗透系数(P_(BA))都比其相应的吸收渗透系数要大,其中宝藿苷I的分泌渗透系数是其吸收渗透系数的9.8倍.结论 淫羊藿黄酮类成分的肠道吸收较差,可能存在肠道转运蛋白的外排机制,其中三糖苷(朝藿定A、朝藿定B、朝藿定C)的吸收要小于二糖苷(淫羊藿苷),二糖苷的吸收要小于单糖苷(宝藿苷I).

Absorption and transportation of flavonoids in Herb Epimedii across Caco-2 monolayer model

Objective To study the absorption and transportation of flavonoids in Herb Epimedii by using Caco-2 monolayer model. Methods Caco-2 cell monolayer model was used to study the bi-direction transport of icariin, epimedin A, epimedin B, epimedin C, and baohuoside I . The concentration of the five flavonoids in cell culture medium was measured by UPLC and the apparent permeability coefficients (Papp) were calculated. Results The absorptive permeability coefficients (P_(AB) of icariin, epimedin A, epimedin B, epimedin C, and baohuoside I were 5. 91×10~(-7), 3. 22×10~(-7), 2. 76×10~(-7), 4.23×10~(-7), and 1.46×10~(-6) cm/s, respectively. Except baohuoside I , the other four flavonodes had lower permeabilities, and the secretive'permeabilities (P_(BA) of all the flavonoids were larger than their absorptive permeabilities. Among them, the P_(BA) of baohuoside I was 9. 8 times as much as the P_(AB). Conclusion The results suggest that the intestinal absorption of the five flavonoids is lower, which might have efflux mechanism by transporters, and the absorption of monloglycoside (e. g. baohuoside I ) is better than that of diglycoside (e. g. icariin) and triglycoside (e. g. epimedin A, epimedin B, and epimedin C).