Estrogenic activity of triterpene glycosides in yeast two-hybrid assay

Estrogenic potency of six triterpene glycosides, Holothurin A, Holotoxin A 1, Frondoside A, Cucumarioside A 2-2 and Cauloside C, that are natural products and semi-synthesized Ginsenoside-Rh 2, were examined with yeast two-hybrid system, including expressed genes of human estrogen receptor, hERα, th...

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Bibliographic Details
Published in:The Journal of steroid biochemistry and molecular biology 2006-11, Vol.101 (4), p.226-231
Main Authors: Kovalchuk, S.N., Kozhemyako, V.B., Atopkina, L.N., Silchenko, A.S., Avilov, S.A., Kalinin, V.I., Rasskazov, V.A., Aminin, D.L.
Format: Article
Language:English
Subjects:
Animals
Dose-Response Relationship, Drug
Estrogenic activity
Glycosides - chemistry
Human estrogen receptor (hER)
Humans
Molecular Structure
Receptors, Estrogen - chemistry
Triterpene glycosides
Triterpenes - chemistry
Two-Hybrid System Techniques
Yeast two-hybrid screening system
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Summary:Estrogenic potency of six triterpene glycosides, Holothurin A, Holotoxin A 1, Frondoside A, Cucumarioside A 2-2 and Cauloside C, that are natural products and semi-synthesized Ginsenoside-Rh 2, were examined with yeast two-hybrid system, including expressed genes of human estrogen receptor, hERα, the co-activator TIF2 and lacZ as a reporter gene. Only Ginsenoside-Rh 2 exhibited significant moderate estrogenic activity in the concentration range of 10 −7 to 10 −6 M. Its effect was approximately 30% of the activity of 17β-estradiol applied at half-effective concentration. This indicates Ginsenosides-Rh 2 is a weak phytoestrogen. The sea cucumber triterpene glycosides, Holothurin A, Holotoxin A 1, Cucumarioside A 2-2 and Frondoside A, and plant glycoside Cauloside C had no appreciable estrogenic activity. Data obtained by yeast two-hybrid assay reflect structure–activity relationship between tested compounds and 17β-estradiol. Only Ginsenoside-Rh 2 has some similarity in chemical structure with 17β-estradiol that might explain affinity of this glycoside to the hERα receptor.
ISSN:0960-0760
1879-1220
DOI:10.1016/j.jsbmb.2006.06.022