scholarly journals Genistein modulates the decreased drug accumulation in non-P-glycoprotein mediated multidrug resistant tumour cells

1993 ◽  
Vol 68 (5) ◽  
pp. 939-946 ◽  
Author(s):  
CHM Versantvoort ◽  
GJ Schuurhuis ◽  
HM Pinedo ◽  
CA Eekman ◽  
CM Kuiper ◽  
...  
1996 ◽  
Vol 48 (5) ◽  
pp. 522-525 ◽  
Author(s):  
KEN-ICHI MIYAMOTO ◽  
KEIKO KOGA-TAKEDA ◽  
KENJIRO KOGA ◽  
TAEYUKI OHSHIMA ◽  
MASAAKI NOMURA

1996 ◽  
Vol 32 (5) ◽  
pp. 857-861 ◽  
Author(s):  
R. Boer ◽  
V. Gekeler ◽  
W.-R. Ulrich ◽  
P. Zimmermann ◽  
W. Ise ◽  
...  

2012 ◽  
Vol 32 (6) ◽  
pp. 559-566 ◽  
Author(s):  
Yan Xu ◽  
Feng Zhi ◽  
Guangming Xu ◽  
Xiaolei Tang ◽  
Sheng Lu ◽  
...  

MDR (multidrug-resistance) represents a major obstacle to successful cancer chemotherapy and is usually accomplished by overexpression of P-gp (P-glycoprotein). Much effort has been devoted to developing P-gp inhibitors to modulate MDR. However, none of the inhibitors on the market have been successful. 1416 [1-(2,6-dimethylphenoxy)-2-(3,4-dimethoxyphenylethylamino)propane hydrochloride (phenoprolamine hydrochloride)] is a new VER (verapamil) analogue with a higher IC50 for blocking calcium channel currents than VER. In the present paper, we examined the inhibition effect of 1416 on P-gp both in vitro and in vivo. 1416 significantly enhanced cytotoxicity of VBL (vinblastine) in P-gp-overexpressed human multidrug-resistant K562/ADM (adriamycin) and KBV cells, but had no such effect on the parent K562 and KB cells. The MDR-modulating function of 1416 was further confirmed by increasing intracellular Rh123 (rhodanmine123) content in MDR cells. Human K562/ADM xenograft-nude mice model verified that 1416 potentiates the antitumour activity of VBL in vivo. RT-PCR (reverse transcriptase-PCR) and FACS analysis demonstrated that the expression of MDR1/P-gp was not affected by 1416 treatment. All these observations suggest that 1416 could be a promising agent for overcoming MDR in cancer chemotherapy.


2009 ◽  
Vol 28 (4) ◽  
pp. 391-403 ◽  
Author(s):  
L. Gibalová ◽  
J. Sedlák ◽  
M. Labudová ◽  
M. Barančík ◽  
A. Reháková ◽  
...  

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