Flavonoids from Herba epimedii selectively activate estrogen receptor alpha (ERα) and stimulate ER-dependent osteoblastic functions in UMR-106 cells.

Xiao, HH ; Fung, CY ; et al.

In: The Journal of steroid biochemistry and molecular biology, Jg. 143 (2014-09-01), S. 141

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Total flavonoids in Herba epimedii (HEP) have been demonstrated to protect against bone loss and bone deterioration associated with estrogen deficiency without exerting any uterotrophic effects. However, it is unclear how flavonoids in HEP exert their protective effects on bone and if different flavonoids exert estrogenic actions in bone cells via similar mechanism of actions. The present study aims to investigate the bone anabolic effects of four major flavonoids isolated from HEP, namely icariin, baohuoside-I, epimedin B and sagittatoside A as well as the mechanism involved in mediating their estrogenic actions in rat osteoblastic-like UMR-106 cells. All tested compounds significantly stimulated the cell proliferation rate, alkaline phosphate (ALP) activity and osteoprotegerin (OPG)/receptor activator of nuclear factor κ-B ligand (RANKL) mRNA expression in UMR-106 cells and their effects could be abolished by co-incubation with 10(-6)M ICI 182,780. None of the flavonoids exhibited binding affinities toward ERα and ERβ. However, sagittatoside A selectively activated estrogen response element (ERE)-luciferase activity via ERα. In addition, icariin and sagittatoside A induced ERα phosphorylation at serine 118 residue. Taken together, our results indicated that all four flavonoids from HEP stimulated ER-dependent osteoblastic functions in UMR-106 cells, but only two of them appeared to exert their actions by ligand-independent activation of ERα. Our study provides evidence to support the hypothesis that the estrogen-like protective effects on bone by flavonoids are mediated via mechanisms that are distinct from the classical actions of estrogen.

Titel:	Flavonoids from Herba epimedii selectively activate estrogen receptor alpha (ERα) and stimulate ER-dependent osteoblastic functions in UMR-106 cells.
Autor/in / Beteiligte Person:	Xiao, HH ; Fung, CY ; Mok, SK ; Wong, KC ; Ho, MX ; Wang, XL ; Yao, XS ; Wong, MS
Link:	Zum Volltext
Zeitschrift:	The Journal of steroid biochemistry and molecular biology, Jg. 143 (2014-09-01), S. 141
Veröffentlichung:	Oxford ; New York : Pergamon, c1990-, 2014
Medientyp:	academicJournal
ISSN:	1879-1220 (electronic)
DOI:	10.1016/j.jsbmb.2014.02.019
Schlagwort:	Animals Blotting, Western Cell Differentiation drug effects Cells, Cultured Immunoenzyme Techniques Osteoblasts cytology Osteoblasts metabolism RNA, Messenger genetics Rats Real-Time Polymerase Chain Reaction Response Elements genetics Reverse Transcriptase Polymerase Chain Reaction Diterpenes pharmacology Drugs, Chinese Herbal pharmacology Estrogen Receptor alpha metabolism Estrogens pharmacology Flavonoids pharmacology Glucosides pharmacology Osteoblasts drug effects
Sonstiges:	Nachgewiesen in: MEDLINE Sprachen: English Publication Type: Journal Article; Research Support, Non-U.S. Gov't Language: English [J Steroid Biochem Mol Biol] 2014 Sep; Vol. 143, pp. 141-51. <i>Date of Electronic Publication: </i>2014 Mar 06. MeSH Terms: Diterpenes / pharmacology ; Drugs, Chinese Herbal / pharmacology ; Estrogen Receptor alpha / metabolism ; Estrogens / pharmacology ; Flavonoids / pharmacology ; Glucosides / pharmacology ; Osteoblasts / *drug effects ; Animals ; Blotting, Western ; Cell Differentiation / drug effects ; Cells, Cultured ; Immunoenzyme Techniques ; Osteoblasts / cytology ; Osteoblasts / metabolism ; RNA, Messenger / genetics ; Rats ; Real-Time Polymerase Chain Reaction ; Response Elements / genetics ; Reverse Transcriptase Polymerase Chain Reaction Contributed Indexing: Keywords: Estrogen receptor; Flavonoids; Herba epimedii; Osteoblastic cells; Phytoestrogens Substance Nomenclature: 0 (Diterpenes) ; 0 (Drugs, Chinese Herbal) ; 0 (ESR1 protein, human) ; 0 (Estrogen Receptor alpha) ; 0 (Estrogens) ; 0 (Flavonoids) ; 0 (Glucosides) ; 0 (RNA, Messenger) ; 0 (sagittarioside a) ; 110623-73-9 (epimedin B) ; 113558-15-9 (baohuoside I) ; VNM47R2QSQ (icariin) Entry Date(s): Date Created: 20140311 Date Completed: 20141229 Latest Revision: 20220330 Update Code: 20231215

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