Transport mechanism of bergenin aross MDCK-MDRl cell monolayer model
- Author:
Xiu-Wen WU
1
;
Ran WEN
1
;
Na WANG
1
;
Li LI
1
;
Yuan-Yu WANG
2
Author Information
- Publication Type:Journal Article
- Keywords: bergenin; MDCK-MDRl cell monolayer model; molecular docking; P-glyco-protein; passing through blood-brain barrier; transport mechanism
- From: Chinese Pharmacological Bulletin 2022;38(11):1698-1704
- CountryChina
- Language:Chinese
- Abstract: Aim To study the transport mechanism of bergenin passing through blood-brain barrier ( BBB ) . Methods MTT assay was used to investigate the tox-icity of bergenin on MDCK-MDRl cells. Molecular docking was used to predict the binding mode and effect ability of bergenin with P-gp. In vitro MDCK-MDRl cell monolayer model was used to analyze trans¬port characteristics of bergenin and the effect of con¬centration, time and verapamil (a P-gp inhibitor) on the transport of bergenin. Results Bergenin was non-toxic to MDCK-MDRl cells within the concentration of 5 to 40 jjunol • L . There was hydrogen-bond and hy-drophobic interaction between P-gp and bergenin, and P-gp-bergenin was more stable than P-gp-verapamil. The P value of bergenin transported from AP to BL (PappAP^BL) was (1.07 ±0.27) xl0"6cm • s"1 at 20 jjumol • L for a period of 90 min; addition of vera¬pamil, PappAP^BL values of bergenin increased signifi¬cantly (P <0. 01) , while those of transport in the op¬posite direction decreased significantly ( P < 0. 05 ) ; correspondingly, the efflux ratio ( ER) for bergenin was decreased from 4. 32 to 0. 98. Conclusions Ber¬genin has moderate BBB permeability, and its transport process is driven by not only passive diffusion, but also P-gp.
