Metabolism and Transport of 7，4'-dihydroxyflavone in Caco-2 Cell Model
10.3870/j.issn.1004-0781.2017.02.003
- VernacularTitle:7,4’-二羟基黄酮在Caco-2细胞模型中的代谢及转运
- Author:
Yinglin MA
;
Yiping ZHOU
;
Yu ZHOU
;
Kunyu JIANG
;
Shengnan MENG
- Keywords:
7,4'-dihydroxyflavone;
Caco-2 cell monolayer modal;
Multidrug resistance-associated protein 2;
Breast cancer resistance protein
- From:
Herald of Medicine
2017;36(2):127-131
- CountryChina
- Language:Chinese
-
Abstract:
Objective To study the effects of different transport protein on the transport of 7,4'-dihydroxyflavone (7,4'-DHF) and its metabolite (7,4'-DHF-S) in Caco-2 cell model.Methods Ultra performance liquid chromatography was employed to determinethe content of 7,4'-DHF and 7,4'-DHF-S incubation buffer,their structures were identified by LC-MS/MS.Bidirectional transport of Caco-2 cells model was used to investigate the influence of ko143 (the inhibitor of BCRP) and MK571 (the inhibitor of MRP2) on the transport of 7,4'-DHF and 7,4'-DHF-S,respectively.Results Metabolic product of 7,4'-DHF in Caco-2 monolayer cell was identified as one monosulfate;PDR of 7,4'-DHF was (1.43 ± 0.11),PDR of ko143 and MK571 on the apparent permeability of 7,4'-DHF was (1.59 ± 0.04) and (1.48 ± 0.07) (P ＞ 0.05);PDR of 7,4'-DHF-S was (1.60 ± 0.06);ko143 could significantly reduce the apparent permeability of 7,4'-DHF-S,and the PDR was (0.23 ±0.03) (P ＜ 0.01);MK571 had no significant effect on the apparent permeability of the 7,4'-DHF-S,and the PDR was (1.51±0.04) (P ＞ 0.05).Conclusion Caco-2 cells can mediate the suffonated reaction of 7,4'-DHF;7,4'-dihydroxyflavone sulfonated combination product may be a substrate for BCRP.
