目的:研究白芷提取物对黄酮类成分葛根素、黄芩苷肠道转运的影响,结合白芷提取物对Caco-2细胞上Pgp功能的影响,探讨白芷提取物对葛根素、黄芩苷肠吸收的影响机制。方法:采用Cacc-2细胞模型,研究白芷提取物分别对黄酮类成分葛根素、黄芩苷吸收的影响,以P-gp底物罗丹明123(R123)为荧光探针,评价不同浓度白芷提取物和Pgp抑制剂维拉帕米对R-123细胞蓄积的影响,细胞内的R-123浓度采用荧光分光光度法检测。结果:白芷提取物对葛根中葛根素、黄芩中黄苓苷的吸收均有明显的促进作用,葛根素的表观渗透系数Papp分别提高1.6-3.6倍,黄芩苷的表观渗透系数Papp分别提高2.3-3.3倍;白芷香豆素(0.15-1.5mg·mL^-1)、白芷挥发油(0.24-6.0μL·mL^-1)、白芷香豆素+白芷挥发油均能显著增加细胞内Rh-123的摄取,对P-gp显示出明显剂量依赖性的抑制作用。结论:白芷提取物促进葛根素、黄芩苷等黄酮类成分吸收的原因可能与其抑制P-gP外排有关。
OBJECTIVE To study the effect of Radix Angelicae Dahuricae extract on intestinal transport of flavones ingredi- ents puerarin, baicalin, and combining the effect of Radix Angelicae Dahuricae extract on P glycoprotein activity, to explore the mechanism of Radix Angelicae Dahuricae extract improving the absorption of puerarin , baicalin. METHODS Caco-2 cell via- bility was measured using MTT assay in the presence of Radix Angelicae Dahuricae extract at different concentration, and using Caco-2 ceil monolayer model to study the effect of Radix Angelicae Dahuricae extract on the absorption of puerarin and baicatin respectively. Rhodamine123(R-123), a P-gp substrate, was selected as fluorescent probe. A fluorescence spectrophotometer method was used to determine the concentration of R-123 in Caco-2 cells. RESULTS Radix Angelicae Dahuricae extract could significant increase the absorption of puerarin in Puerariae and the absorption of baicalin in Radix Scutellariae, the apparent per- meability coefficients (Papp) of puerarin and baicalin was increased by 1.6 - 3.6 folds and 2. 3 - 3.3 folds respectively. Couma- rins (0. 15 - 1.5 mg·mL^-1 ) of Radix Angelicae Dahuricae extract, volatile oil (0. 24 - 6. 0 μL·mL^-1 ) of Radix Angelicae Dahuricae extract, coumarins combined with volatile oil all could significantly enhance the accumulation of R-123 in Caco-2 cell, and significantly, dose-dependently inhibited P-gp. CONCLUSION The reason of Radix Angelieae Dahuricae extract to improve the absorption of flavones ingredients is related to the inhibitory effect of Radix Angelicae Dahurieae extract on P-gp ac- tivity.