Lupinalbin A as the most potent estrogen receptor α- and aryl hydrocarbon receptor agonist in Eriosema laurentii de Wild. (Leguminosae)

BMC Complementary and Alternative Medicine

Liselotte Krenn²  Alois Jungbauer³  Hanspeter Kaehlig¹  Martin Zehl²  Svjetlana Medjakovic³  Dieudonné Njamen⁴  Sylvin Benjamin Ateba² 

[1]Institut of Organic Chemistry, University of Vienna, Währingerstraße 38, A-1090 Vienna, Austria

[2]Department of Pharmacognosy, University of Vienna, Althanstrasse 14, A-1090 Vienna, Austria

[3]Christian Doppler Laboratory for Receptor Biotechnology, Muthgasse 18, A-1190 Vienna, Austria

[4]Laboratory of Animal Physiology, Department of Animal Biology and Physiology, Faculty of Science, University of Yaounde I, P.O. Box 812, Yaounde, Cameroon

关键词: Lupinalbin A;    2′-Hydroxygenistein;    Genistein;    Aryl hydrocarbon receptor;    Estrogen receptor α;    Yeast transactivation assays;    Eriosema laurentii de Wild.;   

Others  :  1087003
DOI  :  10.1186/1472-6882-14-294

 received in 2014-04-02, accepted in 2014-08-05,  发布年份 2014

【 摘 要 】

Background

Eriosema laurentii De Wild. (Leguminosae) is a plant used in Cameroon against infertility and gynecological or menopausal complaints. In our previous report, a methanol extract of its aerial parts was shown to exhibit estrogenic and aryl hydrocarbon receptor agonistic activities in vitro and to prevent menopausal symptoms in ovariectomized Wistar rats.

Methods

In order to determine the major estrogen receptor α (ERα) agonists in the extract, an activity-guided fractionation was performed using the ERα yeast screen. To check whether the ERα active fractions/compounds also accounted for the aryl hydrocarbon receptor (AhR) agonistic activity of the crude methanol extract, they were further tested on the AhR yeast screen.

Results

This study led to the identification of 2′-hydroxygenistein, lupinalbin A and genistein as major estrogenic principles of the extract. 2′-hydroxygenistein and lupinalbin A were, for the first time, also shown to possess an AhR agonistic activity, whereas genistein was not active in this assay. In addition, it was possible to deduce structure-activity relationships.

Conclusions

These results suggest that the identified compounds are the major active principles responsible for the estrogenic and AhR agonistic activities of the crude methanol extract of the aerial parts of Eriosema laurentii.

【 授权许可】

   
2014 Ateba et al.; licensee BioMed Central Ltd.

【 图 表 】

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