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目的:利用人源结肠腺癌细胞系Caco-2细胞单层模型,研究了川芎提取物中阿魏酸的吸收转运机制,以及白芷提取物对其吸收转运的影响。方法:建立人源结肠腺癌细胞系Caco-2细胞模型,利用此模型研究时间、药物浓度对川芎提取物中阿魏酸的转运影响与阿魏酸的双向转运特征;研究川芎中阿魏酸在有或无P-gp、MRP蛋白专属抑制剂存在时阿魏酸在Caco-2细胞模型的双向转运情况;并考察白芷提取物对川芎中阿魏酸吸收转运的影响。结果:阿魏酸在3h范围内转运速率保持恒定,在浓度范围(28～336mg/ml)内浓度与转运速率呈线性相关;加入P-gp和MRP蛋白抑制剂后,阿魏酸的AP侧转运增加,BL侧转运降低,PDR值下降;加入白芷有效成分(香豆素:0.45mg/ml、挥发油:0.72μl/ml、香豆素+挥发油:0.45mg/ml香豆素+0.72μl/ml挥发油)后阿魏酸的转运显著提高。结论:阿魏酸的转运过程可能为被动转运兼存在载体转运,阿魏酸的转运同时受P-gp和MRP外排影响,MRP影响较为明显,白芷有效成分对阿魏酸的转运有促进作用。
OBJECTIVE: To study the absorption and transport mechanism of ferulic acid in Chuanxiong extract and the effect of Angelica dahurica extract on its absorption and transport, using Caco-2 cell monolayer model of human colon adenocarcinoma cell line. Methods: The human colon adenocarcinoma cell line Caco-2 cell model was established. The model was used to study the effects of time and drug concentration on the transport of ferulic acid in the extract of Ligusticum chuanxiong Hort and bidirectional transport of ferulic acid. The effects of ferulic acid Ferulic acid bi-directional transport in Caco-2 cells in the presence or absence of P-gp, an MRP inhibitor, and the effect of the extract of Angelica dahurica on the absorption and transport of ferulic acid in Ligusticum chuanxiong Hort. Results: The ferulic acid transport rate remained constant within 3 h. The linearity was found between the concentration and the transport rate in the concentration range of 28 ~ 336 mg / ml. After addition of P-gp and MRP inhibitors, the ferulic acid AP The transdermal transport increased, the BL side transport decreased, and the PDR decreased; the effective components of Angelica dahurica (Coumarin: 0.45mg / ml, Volatile oil: 0.72μl / ml, Coumarin + Volatile oil: 0.45mg / ml Coumarin + 0.72μl / ml volatile oil) after ferulic acid transport was significantly increased. CONCLUSION: Ferulic acid may be transported by both passive transport and transporter. The ferulic acid transport is affected by both P-gp and MRP efflux. The effect of MRP is obvious. The effective components of Angelica dahurica promote the transport of ferulic acid .