Transportation of 8-isopropylaminomethyl hesperitin(IPHP) across human intestinal epithelial by using Caco-2 cells
10.3969/j.issn.1001-1978.2015.06.007
- VernacularTitle:8-异丙胺亚甲基橙皮素（IPHP）在Caco-2细胞模型上跨膜转运的研究
- Author:
Tingting HU
;
Cheng HUANG
;
Xiaoming MENG
;
Zhaolin CHEN
;
Chenlin SHEN
;
Jun LI
- Publication Type:Journal Article
- Keywords:
IPHP;
Caco-2 cell;
intestinal absorption;
efflux;
apparent permeability coefficients;
passive dif-fusion;
HPLC
- From:
Chinese Pharmacological Bulletin
2015;(6):769-774
- CountryChina
- Language:Chinese
-
Abstract:
Aim To study the mechanism of 8-isopro-pylaminomethyl hesperitin ( IPHP ) intestinal absorp-tion using Caco-2 cell lines. Methods Using Caco-2 cell lines as an intestinal epithelial cell model, the effects of drug concentration, temperature, pH, P-gly-coprotein ( P-gp) inhibitor verapamil and multidrug re-sistance protein 2 ( MRP2 ) inhibitors MK-571 or pro-benecid on IPHP transport across Caco-2 cell lines were all investigated. Results The transportation of IPHP was related to drug concentration. The Papp ( AP-BL) ( × 10 -5) was (2. 21 ± 0. 200) cm·s-1,(3. 56 ± 0. 306) cm·s-1,(3. 81 ± 0. 179) cm·s-1,(4. 23 ± 0. 229 ) cm · s-1 , ( 4. 17 ± 0. 262 ) cm · s-1 , re-spectively, and Papp(BL-AP) ( × 10 -5) was (3. 57 ±0. 209) cm·s-1,(4. 51 ± 0. 113) cm·s-1,(4. 97 ± 0. 229) cm·s-1,(5. 24 ± 0. 550) cm·s-1,(5. 07 ± 0. 557) cm·s-1,respectively. Efflux rate was 1. 61, 1. 26,1. 3,1. 23,1. 21,respectively. Temperature and pH both influenced the transport, While the P-gp in-hibitor verapamil had no effect on the transport of IPHP. MRP2 inhibitors MK-571 or probenecid led to an apparent decrease in the efflux of IPHP. Conclu-sion The results suggest that the transport of IPHP is mainly passive diffusion, and MRP2 but not P-gp may be involved in the transport of IPHP.
