Reversal effect of a macrocyclic bisbibenzyl plagiochin E on multidrug resistance in adriamycin-resistant K562/A02 cells. Shi, Y., Qu, X., Liao, Y., Xie, C., Cheng, Y., Li, S., & Lou, H. European Journal of Pharmacology, 584(1):66-71, 2008. abstract bibtex Plagiochin E is a new macrocyclic bisbibenzyl compound isolated from Marchantia polymorpha. In the previous studies, we reported that when combined with fluconazole, plagiochin E had synergetic effects against the resistant strain of Candida albicans. Herein, we examined the reversal effect of plagiochin E on multidrug resistance in adriamycin-induced resistant K562/A02 cells and the parental K562 cells. Its cytotoxicity and reversal effects on multidrug resistance were assessed by MTT (3-4, 5-dimethylthiazol-2-yl-2, 5-diphenyl-tetrazolium bromide) assay. Apoptosis percentage of cells was obtained from Annexin V/fluorescein isothiocyanate (FITC) and propridium iodide (PI) double-staining. The effects of plagiochin E on P-glycoprotein activity were evaluated by measuring rhodamine 123 (Rh123)-associated mean fluorescence intensity and P-glycoprotein expression on the basis of the flow cytometric technology, respectively. The results showed that plagiochin E ranging from 2 to 12 mug/ml had little cytotoxicity against K562/A02 cells. When combined with adriamycin, it significantly promoted the sensitivity of K562/A02 cells toward adriamycin through increasing intracellular accumulation of adriamycin in a dose-dependent manner. Further study demonstrated that the inhibitory effect of plagiochin E on P-glycoprotein activity was the major cause of increased stagnation of adriamycin inside K562/A02 cells, indicating that plagiochin E, as a new class of mutidrug resistance inhibitor, may effectively reverse the multidrug resistance in K562/A02 cells via inhibiting expression and drug-transport function of P-glycoprotein.
@article{
title = {Reversal effect of a macrocyclic bisbibenzyl plagiochin E on multidrug resistance in adriamycin-resistant K562/A02 cells.},
type = {article},
year = {2008},
pages = {66-71},
volume = {584},
institution = {School of Pharmaceutical Sciences, Shandong University, Jinan 250012, China.},
id = {1e72847f-ca30-38ba-9af5-f3c92422d71a},
created = {2011-05-20T17:26:18.000Z},
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last_modified = {2011-05-20T17:26:18.000Z},
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abstract = {Plagiochin E is a new macrocyclic bisbibenzyl compound isolated from Marchantia polymorpha. In the previous studies, we reported that when combined with fluconazole, plagiochin E had synergetic effects against the resistant strain of Candida albicans. Herein, we examined the reversal effect of plagiochin E on multidrug resistance in adriamycin-induced resistant K562/A02 cells and the parental K562 cells. Its cytotoxicity and reversal effects on multidrug resistance were assessed by MTT (3-4, 5-dimethylthiazol-2-yl-2, 5-diphenyl-tetrazolium bromide) assay. Apoptosis percentage of cells was obtained from Annexin V/fluorescein isothiocyanate (FITC) and propridium iodide (PI) double-staining. The effects of plagiochin E on P-glycoprotein activity were evaluated by measuring rhodamine 123 (Rh123)-associated mean fluorescence intensity and P-glycoprotein expression on the basis of the flow cytometric technology, respectively. The results showed that plagiochin E ranging from 2 to 12 mug/ml had little cytotoxicity against K562/A02 cells. When combined with adriamycin, it significantly promoted the sensitivity of K562/A02 cells toward adriamycin through increasing intracellular accumulation of adriamycin in a dose-dependent manner. Further study demonstrated that the inhibitory effect of plagiochin E on P-glycoprotein activity was the major cause of increased stagnation of adriamycin inside K562/A02 cells, indicating that plagiochin E, as a new class of mutidrug resistance inhibitor, may effectively reverse the multidrug resistance in K562/A02 cells via inhibiting expression and drug-transport function of P-glycoprotein.},
bibtype = {article},
author = {Shi, Yan-Qiu and Qu, Xian-Jun and Liao, Yong-Xiang and Xie, Chun-Feng and Cheng, Yan-Na and Li, Song and Lou, Hong-Xiang},
journal = {European Journal of Pharmacology},
number = {1}
}
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Further study demonstrated that the inhibitory effect of plagiochin E on P-glycoprotein activity was the major cause of increased stagnation of adriamycin inside K562/A02 cells, indicating that plagiochin E, as a new class of mutidrug resistance inhibitor, may effectively reverse the multidrug resistance in K562/A02 cells via inhibiting expression and drug-transport function of P-glycoprotein.","bibtype":"article","author":"Shi, Yan-Qiu and Qu, Xian-Jun and Liao, Yong-Xiang and Xie, Chun-Feng and Cheng, Yan-Na and Li, Song and Lou, Hong-Xiang","journal":"European Journal of Pharmacology","number":"1","bibtex":"@article{\n title = {Reversal effect of a macrocyclic bisbibenzyl plagiochin E on multidrug resistance in adriamycin-resistant K562/A02 cells.},\n type = {article},\n year = {2008},\n pages = {66-71},\n volume = {584},\n institution = {School of Pharmaceutical Sciences, Shandong University, Jinan 250012, China.},\n id = {1e72847f-ca30-38ba-9af5-f3c92422d71a},\n created = {2011-05-20T17:26:18.000Z},\n file_attached = {false},\n profile_id = {b6c31fe8-61c6-3818-89a8-62873f3171f3},\n group_id = {7bdcaa0c-1528-351f-a09a-f8da52223946},\n last_modified = {2011-05-20T17:26:18.000Z},\n read = {false},\n starred = {false},\n authored = {false},\n confirmed = {true},\n hidden = {false},\n abstract = {Plagiochin E is a new macrocyclic bisbibenzyl compound isolated from Marchantia polymorpha. 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