title: Quercetin synergizes with 2-methoxyestradiol inhibiting cell growth and inducing apoptosis in human prostate cancer cells.
abstract: Lack of effective treatment options for castration-resistant prostate cancer reinforces the great need to develop novel drug therapies. Quercetin is a plant-derived ﬂavonoid that can induce apoptosis in prostate cancer cells. 2-Methoxyestradiol (2-ME) is an endogenous estrogenic metabolite that also has antineoplastic activity. However, these two agents have limited bioavailability. Herein, we explored the antiproliferative and proapoptotic activities of quercetin combined with 2-ME in both androgen-dependent LNCaP and androgen-independent PC-3 human prostate cancer cell lines. Compared to quercetin and 2-ME alone, combining quercetin with 2-ME at appropriate concentrations i) showed synergistic antiproliferative and proapoptotic activities; ii) increased G2/M phase population of cells; iii) decreased the ratio of Bcl-2/Bax significantly. The combination of quercetin and 2-ME is a new clinically relevant treatment regimen which has the potential of enhancing the antitumor effect on prostate cancer and lessening the side effect of either quercetin or 2-ME alone.
authors.affiliation: Department of Urology, Beijing Chaoyang Hospital, Capital Medical University, Beijing 100020, P.R. China.
authors.forename: Guodong
authors.initials: G
authors.lastname: Wang
authors.forename: Liming
authors.initials: L
authors.lastname: Song
authors.forename: Huiping
authors.initials: H
authors.lastname: Wang
authors.forename: Nianzeng
authors.initials: N
authors.lastname: Xing
mesh_terms: D000077584:2-Methoxyestradiol; D000975:Antioxidants / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D002453:Cell Cycle / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004357:Drug Synergism; D004958:Estradiol / Q000031:analogs & derivatives* / Q000494:pharmacology; D006801:Humans; D008297:Male; D011471:Prostatic Neoplasms / Q000188:drug therapy*; D011794:Quercetin / Q000494:pharmacology*; D050257:Tubulin Modulators / Q000494:pharmacology*; D051028:bcl-2-Associated X Protein / Q000378:metabolism
chemical_list: D000975:Antioxidants; D050257:Tubulin Modulators; D051028:bcl-2-Associated X Protein; D004958:Estradiol; D000077584:2-Methoxyestradiol; D011794:Quercetin