Placental passage of olomoucine II, but not purvalanol A, is affected by p-glycoprotein (ABCB1), breast cancer resistance protein (ABCG2) and multidrug resistance-associated proteins (ABCCs)

Xenobiotica ◽  
2015 ◽  
Vol 46 (5) ◽  
pp. 416-423 ◽  
Author(s):  
Jakub Hofman ◽  
Radim Kučera ◽  
Zuzana Neumanova ◽  
Jiri Klimes ◽  
Martina Ceckova ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Multidrug Resistance ◽  
Breast Cancer Resistance Protein ◽  
Cancer Resistance ◽  
P Glycoprotein ◽  
Associated Proteins ◽  
Resistance Protein ◽  
Placental Passage

scholarly journals Folium Sennae Increased the Bioavailability of Methotrexate through Modulation on MRP 2 and BCRP

2021 ◽  
Vol 14 (10) ◽  
pp. 1036
Author(s):  
Chung-Ping Yu ◽  
Yu-Hsuan Peng ◽  
Ching-Ya Huang ◽  
Yow-Wen Hsieh ◽  
Yu-Chi Hou ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Multidrug Resistance ◽  
Breast Cancer Resistance Protein ◽  
Systemic Exposure ◽  
Cancer Resistance ◽  
Parallel Design ◽  
Dosage Regimens ◽  
Combined Use ◽  
Associated Proteins ◽  
Resistance Protein

Folium Sennae (FS), a popular laxative (Senna), contains polyphenolic anthranoids, whose conjugation metabolites are probable modulators of multidrug resistance-associated proteins (MRPs) and breast cancer resistance protein (BCRP). We suspected that the combined use of FS might alter the pharmacokinetics of various medicines transported by MRPs or BCRP. This study investigated the effect of FS on the pharmacokinetics of methotrexate (MTX), an anticancer drug and a probe substrate of MRPs/BCRP. Rats were orally administered MTX alone and with two dosage regimens of FS in a parallel design. The results show that 5.0 g/kg of FS significantly increased the AUC0–2880, AUC720–2880 and MRT of MTX by 45%, 102% and 42%, and the seventh dose of 2.5 g/kg of FS significantly enhanced the AUC720–2880 and MRT by 78% and 42%, respectively. Mechanism studies indicated that the metabolites of FS (FSM) inhibited MRP 2 and BCRP. In conclusion, the combined use of FS increased the systemic exposure and MRT of MTX through inhibition on MRP 2 and BCRP.

Enniatin B1 is a substrate of intestinal P-glycoprotein, multidrug resistance-associated protein 2 and breast cancer resistance protein

2010 ◽  
Vol 3 (3) ◽  
pp. 271-281 ◽  
Author(s):  
L. Ivanova ◽  
S. Uhlig ◽  
G. Eriksen ◽  
L. Johannessen
Keyword(s):  
Breast Cancer ◽  
Multidrug Resistance ◽  
Breast Cancer Resistance Protein ◽  
Cancer Resistance ◽  
P Glycoprotein ◽  
Apical Direction ◽  
Resistance Protein ◽  
First Time ◽  
Fumitremorgin C ◽  
Absorption Characteristics

Enniatins are cyclic hexadepsipeptides produced by various fungi, known to have ionophoric, antibiotic and insecticidal activity. The aim of the present study was to evaluate the intestinal absorption characteristics of enniatin B1 (ENN-B1). Using the human intestinal Caco-2 cell line, we found that the permeability of ENN-B1 in the basolateral to apical direction was 6.7× higher as compared to the permeability in the opposite direction, indicating involvement of apically located transporters. Transport of ENN-B1 in the apical to basolateral direction was increased significantly upon treatment of Caco-2 cells with the P-glycoprotein (Pgp) inhibitor verapamil and the multidrug resistance-associated protein 2 (MRP2) inhibitor MK571, but only weakly and not significantly after treatment with the breast cancer resistance protein (BCRP) inhibitor fumitremorgin C. Additionally, MDCK II cells over-expressing Pgp, MRP2 or BCRP, showed reduced sensitivity towards ENN-B1. These data demonstrate for the first time that ENN-B1 is a substrate of MRP2 and suggests that Pgp, MRP2 and possibly BCRP are involved in transport of ENN-B1 across the intestine.

scholarly journals Effect of GenX on P-Glycoprotein, Breast Cancer Resistance Protein, and Multidrug Resistance–Associated Protein 2 at the Blood–Brain Barrier

2020 ◽  
Vol 128 (3) ◽  
pp. 037002 ◽  
Author(s):  
Ronald E. Cannon ◽  
Alicia C. Richards ◽  
Andrew W. Trexler ◽  
Christopher T. Juberg ◽  
Birandra Sinha ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Multidrug Resistance ◽  
Blood Brain Barrier ◽  
Breast Cancer Resistance Protein ◽  
Brain Barrier ◽  
Cancer Resistance ◽  
P Glycoprotein ◽  
Blood Brain ◽  
Resistance Protein
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