安徽医科大学学报2018，Vol.53Issue(2)：236-240,5.DOI:10.19405/j.cnki.issn1000-1492.2018.02.014
利用Caco-2细胞模型研究新型Pim-1激酶抑制剂KY-C002的表观渗透系数
Study on cell permeability coefficients of a new Pim-1 kinase inhibitor KY-C002 by using Caco-2 cell monolayer
摘要
Abstract
Objective To study the cell permeability coefficients of a new Pim-1 kinase inhibitor KY-C002 through a human colorectal cancer Caco-2 cell monolayer, providing a biological basis for the pharmacy pharmaceutical formulation design. Methods Caco-2 cell monolayer was built, and its integrity was confirmed through cell morphology observation, transepithelial electrical resistance measurement and Phenol Red Permeability experiment. The apparent permeability coefficients of Pim-1 kinase inhibitor KY-C002 from apical side (AP side) to basolateral side(BL side) or from BL side to AP side were investigated. The concentrations of KY-C002 were measured by high performance liquid chromatography. The apparent permeability coefficients (Papp) were then calculated. Results The Caco-2 cell monolayer was integrated. The Papp values of Pim-1 kinase inhibitor KY-C002 were (4. 72 ±0. 05)×10-5 cm/s, (5. 29 ±0.20) × 10-5 cm/s, (2. 10 ±0.41) × 10-5 cm/s (P <0.05) from AP side to BL side when the concentrations of KY-C002 were 5, 10, 20 μg/ml respectively. The Papp values of Pim-1 kinase inhibitor KY-C002 were (7.59 ± 0.78) × 10-6 cm/s, (1.08 ±0.04) × 10-5 cm/s, (6.23 ±0.63) × 10-6 cm/s (P < 0. 05) from BL side to AP side when the concentrations of KY-C002 were 5, 10, 20 μg/ml respectively. Conclusion The Caco-2 cell monolayer model was successfully constructed and used to investigate the properties of the permeated monolayer of Pim-1 kinase inhibitor KY-C002. The Papp of the Pim-1 kinase inhibitor KY-C002 was related to its concentration, and the Papp at the concentration of 10 μg/ml was greater than 5 μg/ml and 20 μg/ml of Papp.关键词
KY-C002/Caco-2细胞单层模型/表观渗透系数/药物转运Key words
KY-C002/Caco-2 cell monolayer model/Papp/drug transport分类
医药卫生引用本文复制引用
马雁,徐绍辉,于坤宏,郭圣荣..利用Caco-2细胞模型研究新型Pim-1激酶抑制剂KY-C002的表观渗透系数[J].安徽医科大学学报,2018,53(2):236-240,5.基金项目
国家自然科学基金(编号:81573352) （编号:81573352）
