It has been demonstrated that the flavonoid quercetin (3,3',4',5,7-pentahydroxyflavone; Q) inhibits the growth of several cancer cell lines. There is evidence suggesting that the antiproliferative activity of this substance is mediated by the so-called type II estrogen-binding site (type II EBS). We looked for the presence of type II EBS and the effect of Q on the proliferation of an Adriamycin-resistant estrogen-receptor-negative human breast-cancer cell line (MCF-7 ADRr). By whole-cell assay using estradiol labelled with 6,7-tritium [( 3H]-E2) as a tracer, we demonstrated that MCF-7 ADRr cells contain type II EBSs. Competition analysis revealed that diethylstilbestrol (DES) and Q competed with similar potency for [3H]-Es binding to type II EBSs. The antiestrogen tamoxifen (TAM) competed for type II EBSs, albeit to a lesser extent than either DES or Q. Growth experiments demonstrated that Q and DES exerted a dose-dependent inhibition of cell proliferation in the range of concentrations between 10 nM and 10 microM, whereas TAM was less effective. Q could also inhibit colony formation in a clonogenic assay. Our results indicate that multidrug-resistant estrogen-receptor-negative MCF-7 cells express type II EBSs and are sensitive to the inhibitory effect of Q. This substance could be the parent compound of a novel class of anticancer agents.

Quercetin inhibits the growth of a multidrug-resistant estrogen-receptor-negative MCF-7 human breast-cancer cell line expressing type II estrogen-binding sites / G., Scambia; F. O., Ranelletti; BENEDETTI PANICI, Pierluigi; P. B., Panici; M., Piantelli; G., Bonanno; R. D., Vincenzo; G., Ferrandina; Pierelli, Luca; A., Capelli; S., Mancuso. - In: CANCER CHEMOTHERAPY AND PHARMACOLOGY. - ISSN 0344-5704. - 28:4(1991), pp. 255-258.

Quercetin inhibits the growth of a multidrug-resistant estrogen-receptor-negative MCF-7 human breast-cancer cell line expressing type II estrogen-binding sites.

BENEDETTI PANICI, PIERLUIGI;PIERELLI, LUCA;
1991

Abstract

It has been demonstrated that the flavonoid quercetin (3,3',4',5,7-pentahydroxyflavone; Q) inhibits the growth of several cancer cell lines. There is evidence suggesting that the antiproliferative activity of this substance is mediated by the so-called type II estrogen-binding site (type II EBS). We looked for the presence of type II EBS and the effect of Q on the proliferation of an Adriamycin-resistant estrogen-receptor-negative human breast-cancer cell line (MCF-7 ADRr). By whole-cell assay using estradiol labelled with 6,7-tritium [( 3H]-E2) as a tracer, we demonstrated that MCF-7 ADRr cells contain type II EBSs. Competition analysis revealed that diethylstilbestrol (DES) and Q competed with similar potency for [3H]-Es binding to type II EBSs. The antiestrogen tamoxifen (TAM) competed for type II EBSs, albeit to a lesser extent than either DES or Q. Growth experiments demonstrated that Q and DES exerted a dose-dependent inhibition of cell proliferation in the range of concentrations between 10 nM and 10 microM, whereas TAM was less effective. Q could also inhibit colony formation in a clonogenic assay. Our results indicate that multidrug-resistant estrogen-receptor-negative MCF-7 cells express type II EBSs and are sensitive to the inhibitory effect of Q. This substance could be the parent compound of a novel class of anticancer agents.
1991
doxorubicin; pharmacokinetics/pharmacology/therapeutic use; antitumor; diethylstilbestrol; quercetin; drug therapy/metabolism/pathology; chemical; physiology; drug; mcf-7; dose-response relationship; antagonists /&/ inhibitors; cell line; binding sites; tamoxifen; metabolism; estrogen; drug effects; receptors; humans; drug screening assays; depression; cytology/drug effects/metabolism; breast neoplasms; estrogen receptor; breast cancer; female; cell division; drug resistance; tumor cells; binding; competitive; cultured; pharmacokinetics/pharmacology; estrogens
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Quercetin inhibits the growth of a multidrug-resistant estrogen-receptor-negative MCF-7 human breast-cancer cell line expressing type II estrogen-binding sites / G., Scambia; F. O., Ranelletti; BENEDETTI PANICI, Pierluigi; P. B., Panici; M., Piantelli; G., Bonanno; R. D., Vincenzo; G., Ferrandina; Pierelli, Luca; A., Capelli; S., Mancuso. - In: CANCER CHEMOTHERAPY AND PHARMACOLOGY. - ISSN 0344-5704. - 28:4(1991), pp. 255-258.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11573/399339
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