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

YAO Yuan; LIAO Qiong-feng; XIE Zhi-yong; ZENG Yuan-er

doi:10.13422/j.cnki.syfjx.2014140113

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

更新时间：2024-01-04

- Absorption Mechanism of Neoandrographolide in Human Caco-2 Cell Monolayer Model
- Chinese Journal of Experimental Traditional Medical Formulae Vol. 20, Issue 14, Pages: 113-116(2014)
- 作者机构：
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- DOI：10.13422/j.cnki.syfjx.2014140113
  CLC： R285.5
- Published：2014
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YAO Yuan, LIAO Qiong-feng, XIE Zhi-yong, et al. Absorption Mechanism of Neoandrographolide in Human Caco-2 Cell Monolayer Model[J]. Chinese journal of experimental traditional medical formulae, 2014, 20(14): 113-116.
DOI：

YAO Yuan, LIAO Qiong-feng, XIE Zhi-yong, et al. Absorption Mechanism of Neoandrographolide in Human Caco-2 Cell Monolayer Model[J]. Chinese journal of experimental traditional medical formulae, 2014, 20(14): 113-116. DOI： 10.13422/j.cnki.syfjx.2014140113.

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（50，75，100 μmol·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）×10-6 cm·s-1，与4℃[（5.97±0.11）×10-7 cm·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）×10-6 cm·s-1与对照组新穿心莲内酯Papp [（1.28±0.69）×10-6 cm·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。

Abstract

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

the Papp [(2.02±0.31)×10-6 cm·s-1] at 37℃ was higher than the Papp at 4℃ [(5.97±0.11)×10-7 cm·s-1] and 25℃ [(9.17±0.50)×10-7cm·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 Caco-2 cell monolayers are passive diffusion and active transportation.

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