Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Pivot Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Target Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Query: EC:3.6.3.44 (
P-glycoprotein
)
13,344
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
The aim of this study was to explore potential transport mechanisms of rutin deca (H-) sulfonate sodium (
RDS
) across Caco-2 cell monolayers. As an in-vitro model of human intestinal epithelial membrane, Caco-2 cells were utilized to evaluate the transepithelial transport characteristics of this hydrophilic macromolecular compound. Bi-directional transport study of
RDS
demonstrated that the apparent permeability (P(app)) in the secretory direction was 1.4 approximately 4.5-fold greater than the corresponding absorptive P(app) at concentrations in the range 50.0 approximately 2,000 microM. The transport of
RDS
was shown to be concentration, temperature and pH dependent. In the presence of ciclosporin and verapamil, potent inhibitors of
P-glycoprotein
(
P-gp
)/MRP2, the absorptive transport was enhanced and secretory efflux was diminished.
RDS
significantly reduced the efflux ratio of the
P-gp
substrate rhodamine-123 in a fashion indicative of
P-gp
activity suppression, while rhodamine-123 competitively inhibited the polarized transport of the compound. In conclusion, the results indicated that
RDS
was likely a substrate of
P-gp
. Several efflux transporters, including
P-gp
, participated in the absorption and efflux of
RDS
and they might play significant roles in limiting the oral absorption of the compound. These observations offered important information for the pharmacokinetics of
RDS
.
...
PMID:Transport characteristics of rutin deca (H-) sulfonate sodium across Caco-2 cell monolayers. 1625 58
