In vitro evaluation of estrogenic, antiestrogenic and antitumor effects of amentoflavone
Küçük Resim Yok
Tarih
2021
Dergi Başlığı
Dergi ISSN
Cilt Başlığı
Yayıncı
SAGE Publications Ltd
Erişim Hakkı
info:eu-repo/semantics/closedAccess
Özet
Apigenin, a flavonoid, is reported to act as an estrogen receptor (ER) agonist and inhibit aromatase enzyme. However, amentoflavone, a biflavonoid bearing two apigenin molecules, has not been evaluated for its endocrine modulatory effects. Besides, it is highly consumed by young people to build muscles, enhance mood and lose weight. In the present study, apigenin was used as a reference molecule and ER mediated as well as ER-independent estrogenic/antiestrogenic activity of amentoflavone was investigated. Antitumor activity of amentoflavone was also investigated in both ER positive (MCF-7 BUS) and triple-negative (MDA-MB-231) breast cancer cells and its cytotoxicity was evaluated in human breast epithelial cells (MCF-10A). Our data confirmed ER agonist, aromatase inhibitory and cytotoxic effects of apigenin in breast cancer cells, where no ER mediated estrogenic effect and physiologically irrelevant, slight, aromatase inhibition was found for amentoflavone. Although selective cytotoxicity of amentoflavone was found in MCF-7 BUS cells, it does not seem to be an alternative to the present cytotoxic drugs. Therefore, neither an adverse effect, mediated by an estrogenic/antiestrogenic effect of amentoflavone nor a therapeutical benefit would be expected from amentoflavone. Further studies could be performed to investigate its in vivo effects. © The Author(s) 2021.
Açıklama
Anahtar Kelimeler
amentoflavone, antiestrogenic, Apigenin, aromatase, cytotoxicity, estrogenic, amentoflavone, apigenin, aromatase, estrogen receptor, antiestrogen, antineoplastic agent, biflavonoid, adverse outcome, antineoplastic activity, Article, controlled study, drug cytotoxicity, enzyme inhibition, estrogen activity, human, human cell, in vitro study, MCF-10A cell line, MCF-7 cell line, MDA-MB-231 cell line, physiological process, breast tumor, drug effect, female, tumor cell line, Antineoplastic Agents, Biflavonoids, Breast Neoplasms, Cell Line, Tumor, Estrogen Antagonists, Female, Humans
Kaynak
Human and Experimental Toxicology
WoS Q Değeri
Scopus Q Değeri
Q2
Cilt
40
Sayı
9
