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Table 1 Relative binding affinities of major constituents of ERr and estradiol

From: Treatment of menopausal symptoms by an extract from the roots of rhapontic rhubarb: the role of estrogen receptors

Substance

IC50 ERα

IC50 ERβ

Fold preference for ERβ

Estradiol

8 × 10-9

6.7 × 10-9

0.84

Trans-rhapontigenin

1.2 × 10-5

5.6 × 10-6

2.14

Desoxyrhapontigenin

2.6 × 10-5

2.8 × 10-5

1.1

  1. Note:
  2. Relative binding affinities of trans-rhapontigenin and desoxyrhapontigenin were assessed by a fluorescence polarization assay. IC50 values of compounds in comparison to estradiol and relative preference for the receptor subtypes are shown.
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Chinese Medicine

ISSN: 1749-8546

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