title: Huaier aqueous extract suppresses human breast cancer cell proliferation through inhibition of estrogen receptor α signaling.
abstract: Estrogen receptor α (ERα) has been reported to play a critical role in promoting the growth of breast tumor cells. In the present study, we explored the effect of Huaier extract on estrogen receptor α signaling in breast cancer cell lines. Our data demonstrated that Huaier extract effectively inhibited the proliferation of the MCF-7, T47D and ZR-75-1 human breast cancer cell lines. For the mechanism analysis, we demonstrated that Huaier extract significantly reduced the mRNA and protein levels of ERα in all three ERα-positive cell lines. The downregulation of ERα protein levels was correlated with activation of the proteasomes. We demonstrated that Huaier extract markedly decreased the expression of both ERα and its downstream genes, inhibited the estrogen-stimulated proliferation and reversed the estrogen-induced activation of the nuclear factor κB (NFκB) pathway. Our study provides evidence that Huaier extract is a novel estrogen receptor modulator and is a promising drug for the prevention and treatment of ERα-positive human breast cancers.
authors.affiliation: Department of Breast Surgery, Qilu Hospital, Shandong University, Jinan, Shandong 250012, P.R. China.
authors.forename: Xiaolong
authors.initials: X
authors.lastname: Wang
authors.forename: Ning
authors.initials: N
authors.lastname: Zhang
authors.forename: Qiang
authors.initials: Q
authors.lastname: Huo
authors.forename: Mingjuan
authors.initials: M
authors.lastname: Sun
authors.forename: Shangge
authors.initials: S
authors.lastname: Lv
authors.forename: Qifeng
authors.initials: Q
authors.lastname: Yang
mesh_terms: D001943:Breast Neoplasms / Q000188:drug therapy* / Q000235:genetics / Q000473:pathology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects*; D015536:Down-Regulation / Q000187:drug effects; D004365:Drugs, Chinese Herbal / Q000737:chemistry / Q000494:pharmacology*; D047628:Estrogen Receptor alpha / Q000235:genetics / Q000378:metabolism*; D005260:Female; D015972:Gene Expression Regulation, Neoplastic / Q000187:drug effects; D006801:Humans; D016328:NF-kappa B / Q000378:metabolism; D015398:Signal Transduction / Q000187:drug effects; D055454:Trametes / Q000737:chemistry
chemical_list: D004365:Drugs, Chinese Herbal; C506487:ESR1 protein, human; D047628:Estrogen Receptor alpha; D016328:NF-kappa B