穿心莲内酯在Caco-2细胞单层模型中的吸收机制.PDFVIP

中草药 Chinese Traditional and Herbal Drugs 第 42 卷 第 7 期 2011 年 7 月 ·1363· 穿心莲内酯在 Caco-2 细胞单层模型中的吸收机制 廖琼峰 1*，姚 媛 1，谢智勇 2，张 蕾 1，曾元儿 1 1. 广州中医药大学中药学院，广东 广州 510006 2. 中山大学药学院，广东 广州 510006 摘 要：目的 研究穿心莲内酯在 Caco-2 细胞单层模型中的吸收机制。方法 观察穿心莲内酯在 Caco-2 细胞模型中的双向 转运，考察时间、药物浓度、温度和抑制剂对穿心莲内酯吸收的影响。用 LC/MS/MS 检测药物浓度，计算其表观渗透系数 （Papp）。结果 穿心莲内酯在 Caco-2 细胞模型中，随时间和浓度的增加，药物吸收呈饱和趋势，且受温度和碘乙酰胺影响， 但不受外???抑制剂维拉帕米和 MK-571 的影响。结论 穿心莲内酯在 Caco-2 细胞中的吸收主要是由载体介导的主动转运。 关键词：穿心莲内酯；Caco-2 细胞模型；主动转运；LC/MS/MS；载体介导 中图分类号：R285.61 文献标志码：A 文章编号：0253 - 2670(2011)07 - 1363 - 04 Absorption mechanism of andrographolide in human Caco-2 cell monolayer model LIAO Qiong-feng1, YAO Yuan1, XIE Zhi-yong2, ZHANG Lei1, ZENG Yuan-er1 1. College of Chinese Materia Medica, Guangzhou University of Chinese Medicine, Guangzhou 510006, China 2. School of Pharmaceutical Science, Sun Yat-sen University, Guangzhou 510006, China Abstract: Objective To study the absorption of andrographolide in human Caco-2 cell monolayer model. Methods Caco-2 cell monolayer model was applied to investigating the bidirectional transport of andrographolide. The effects of time, drug concentration, temperature, and inhibitor on the absorption of andrographolide were observed. Drug concentration was measured by LC/MS/MS and the apparent permeability coefficients (Papp) were calculated. Results Time and concentration saturation were observed for the absorptive transport of andrographolide across Caco-2 monolayers. The transport of andrographolide was influenced by the change of temperature and the presence of iodoacetamide, but not Verapamil or MK-571. Conclusion The absorption and transport mechanism of andrographolide in Caco-2 ce