Effect of P-glycoprotein inhibitors erythromycin and cyclosporin A on brain pharmacokinetics of nimodipine in rats

2003 ◽  
Vol 28 (4) ◽  
pp. 309-313 ◽  
Author(s):  
X. D Liu ◽  
L. Zhang ◽  
L. Xie
Keyword(s):  
Cyclosporin A ◽  
P Glycoprotein ◽  
Glycoprotein Inhibitors

scholarly journals Inhibitory Effect of Flavonoids on the Efflux of -Acetyl 5-Aminosalicylic Acid Intracellularly Formed in Caco-2 Cells

2009 ◽  
Vol 2009 ◽  
pp. 1-8 ◽  
Author(s):  
Shin Yoshimura ◽  
Kentaro Kawano ◽  
Ryusuke Matsumura ◽  
Narumi Sugihara ◽  
Koji Furuno
Keyword(s):  
Tissue Culture ◽  
Cyclosporin A ◽  
Inhibitory Effect ◽  
Aminosalicylic Acid ◽  
Promoting Effect ◽  
Cellular Accumulation ◽  
P Glycoprotein ◽  
Apical Site ◽  
Apical Membranes ◽  
Glycoprotein Inhibitors

-acetyl 5-aminosalicylic acid (5-AcASA) that was intracellularly formed from 5-aminosalicylic acid (5-ASA) at 200 M was discharged 5.3, 7.1, and 8.1-fold higher into the apical site than into the basolateral site during 1, 2, and 4-hour incubations, respectively, in Caco-2 cells grown in Transwells. The addition of flavonols (100 M) such as fisetin and quercetin with 5-ASA remarkably decreased the apically directed efflux of 5-AcASA. When 5-ASA (200 M) was added to Caco-2 cells grown in tissue culture dishes, the formation of 5-AcASA decreased, and, in addition, the formed 5-AcASA was found to be accumulated within the cells in the presence of such flavonols. Thus, the decrease in 5-AcASA efflux by such flavonols was attributed not only to the inhibition of -acetyl-conjugation of 5-ASA but to the predominant cellular accumulation of 5-AcASA. Various flavonoids also had both of the effects with potencies that depend on their specific structures. The essential structure of flavonoids was an absence of a hydroxyl substitution at the C5 position on the A-ring of flavone structure for the inhibitory effect on the -acetyl-conjugation of 5-ASA, and a presence of hydroxyl substitutions at the C or C position on the B-ring of flavone structure for the promoting effect on the cellular accumulation of 5-AcASA. Both the decrease in 5-AcASA apical efflux and the increase in 5-AcASA cellular accumulation were also caused by MK571 and indomethacin, inhibitors of MRPs, but not by quinidine, cyclosporin A, P-glycoprotein inhibitors, and mitoxantrone, a BCRP substrate. These results suggest that certain flavonoids suppress the apical efflux of 5-AcASA possibly by inhibiting MRPs pumps located on apical membranes in Caco-2 cells.

Status of Flavonols as P-Glycoprotein Inhibitors in Cancer Chemotherapy

2009 ◽  
Vol 5 (2) ◽  
pp. 89-99 ◽  
Author(s):  
Tripta Bansal ◽  
Manu Jaggi ◽  
Roop Khar ◽  
Sushama Talegaonkar
Keyword(s):  
Cancer Chemotherapy ◽  
P Glycoprotein ◽  
Glycoprotein Inhibitors

Chemosensitization potential of P-glycoprotein inhibitors in malaria parasites

2013 ◽  
Vol 134 (2) ◽  
pp. 235-243 ◽  
Author(s):  
Laura M. Alcantara ◽  
Junwon Kim ◽  
Carolina B. Moraes ◽  
Caio H. Franco ◽  
Kathrin D. Franzoi ◽  
...  
Keyword(s):  
Malaria Parasites ◽  
P Glycoprotein ◽  
Glycoprotein Inhibitors

NEW 4-ARYL-1,4-DIHYDROPYRIDINES AND 4-ARYLPYRIDINES AS P-GLYCOPROTEIN INHIBITORS

2004 ◽  
Vol 33 (3) ◽  
pp. 321-328 ◽  
Author(s):  
Xiao-fei Zhou ◽  
Linping Zhang ◽  
Elaine Tseng ◽  
Elizabeth Scott-Ramsay ◽  
Jerome J. Schentag ◽  
...  
Keyword(s):  
P Glycoprotein ◽  
Glycoprotein Inhibitors

Contributions of intestinal P-glycoprotein and CYP3A to oral bioavailability of cyclosporin A in mice treated with or without dexamethasone

2006 ◽  
Vol 309 (1-2) ◽  
pp. 81-86 ◽  
Author(s):  
Mingji Jin ◽  
Tsutomu Shimada ◽  
Koichi Yokogawa ◽  
Masaaki Nomura ◽  
Yukio Kato ◽  
...  
Keyword(s):  
Cyclosporin A ◽  
Oral Bioavailability ◽  
P Glycoprotein

Discovery of new pyrimidopyrrolizine/indolizine-based derivatives as P-glycoprotein inhibitors: design, synthesis, cytotoxicity, and MDR reversal activities

2021 ◽  
pp. 113403
Author(s):  
Ahmed M. Shawky ◽  
Ashraf N. Abdalla ◽  
Nashwa A. Ibrahim ◽  
Mohammed A.S. Abourehab ◽  
Ahmed M. Gouda
Keyword(s):  
Design Synthesis ◽  
P Glycoprotein ◽  
Glycoprotein Inhibitors ◽  
Mdr Reversal

Discovery of New 4-Indolyl Quinazoline Derivatives as Highly Potent and Orally Bioavailable P-Glycoprotein Inhibitors

2021 ◽  
Vol 64 (19) ◽  
pp. 14895-14911
Author(s):  
Shuo Yuan ◽  
Bo Wang ◽  
Qing-Qing Dai ◽  
Xiao-Nan Zhang ◽  
Jing-Ya Zhang ◽  
...  
Keyword(s):  
P Glycoprotein ◽  
Quinazoline Derivatives ◽  
Orally Bioavailable ◽  
Glycoprotein Inhibitors

Effect of a P-glycoprotein inhibitor, cyclosporin A, on the disposition in rodent brain and blood of the 5-HT1A receptor radioligand, [11C](R)-(––)-RWAY

Synapse ◽  
2006 ◽  
Vol 61 (2) ◽  
pp. 96-105 ◽  
Author(s):  
Jeih-San Liow ◽  
Shuiyu Lu ◽  
Julie A. McCarron ◽  
Jinsoo Hong ◽  
John L. Musachio ◽  
...  
Keyword(s):  
Cyclosporin A ◽  
Rodent Brain ◽  
P Glycoprotein
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