新穿心莲内酯在Caco-2细胞单层模型中的吸收机制研究  

Absorption Mechanism of Neoandrographolide in Human Caco-2 Cell Monolayer Model

作　　者：姚媛[1] 廖琼峰[2] 谢智勇[3] 曾元儿[2] 

机构地区：[1]广州中医药大学第一附属医院,广州510405 [2]广州中医药大学中药学院,广州510006 [3]中山大学药学院,广州510006

出　　处：《中国实验方剂学杂志》2014年第14期113-116,共4页Chinese Journal of Experimental Traditional Medical Formulae

基　　金：国家自然科学基金项目(30600823);国家"重大新药创制"科技重大专项(2009ZX09304-003;2009ZX09501-017)

摘　　要：目的:研究新穿心莲内酯在Caco-2细胞单层模型中的吸收机制。方法:通过研究新穿心莲内酯在模型中的双向转运,考察时间、药物浓度(50,75,100μmol·L-1)、温度(4,25,37℃)和抑制剂(碘乙酰胺、维拉帕米和MK-571)对新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:新穿心莲内酯在Caco-2细胞模型中,随时间和浓度的增加,药物吸收呈线性增加。PBA/PAB≈1.0;温度37℃时,Papp为(2.02±0.31)×10-6cm·s-1,与4℃[(5.97±0.11)×10-7cm·s-1],25℃[(9.17±0.50)×10-7cm·s-1]比较有显著性差异(P<0.05);受抑制剂碘乙酰胺影响,Papp=(4.79±0.42)×10-6cm·s-1与对照组新穿心莲内酯Papp[(1.28±0.69)×10-6cm·s-1]比较有显著性差异(P<0.05)。结论:新穿心莲内酯在Caco-2细胞中的吸收方式主要是被动转运和载体介导的主动转运。Objective： This paper was to study absorption of neoandrographolide in human Caco-2 cell monolayer model. Method： Caco-2 cell monolayer model was applied to investigate the bidirectional transport of neoandrographolide. The effect of time, drug concentration, temperature and inhibitor on the absorption of neoandrographolide was observed. Drug concentration was measured by LC-MS-MS and the apparent permeability coefficients （Papp） was calculated. Result： No time or concentration saturation were observed for the transport of neoandrographolide across Caco-2 monolayers, PBA/PAB ≈ 1. 0. For the comparison of the temperature influence, thePapp [ （2.02±0.31） × 10^-6cm·s^-1] at37 ℃ was higher than the P pp at 4 ℃ [ （5.97±0.11） × 10^-7 1 cm＇s （P 〈0. 05） With the presence of iodoacetamide, the cm.s^-1 ] and25 ℃ [ （9.17±0.50）× 10^-7 cm·s^-1] （P〈0.05）.With the presence of iodoacetamide,the Papp was （4.79± 0.42） × 10^-6, deffered significantly from the Papp [ （1.28 ± 0.69） × 10^-6] without iodoacetamide. Conclusion： The absorption of neoandrographolide in Caeo-2 cell monolayers are passive diffusion and active transportation.

关 键 词：新穿心莲内酯 CACO-2细胞模型 被动转运 主动转运 

分 类 号：R285.5[医药卫生—中药学]