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Planta Med 2024; 90(10): 766-773
DOI: 10.1055/a-2328-2750
Biological and Pharmacological Activity
Original Papers

Estrogenic Activity of Derris scandens Stem Extract and its Major Compounds Using MCF-7 Cell Proliferation Assay and Estrogen-Related Gene Expression

Worapol Sae-Foo
1   Faculty of Pharmaceutical Sciences, Khon Kaen University, Khon Kaen, Thailand
,
Gorawit Yusakul
2   School of Pharmacy, Walailak University, Nakhon Si Thammarat, Thailand
,
Natsajee Nualkaew
1   Faculty of Pharmaceutical Sciences, Khon Kaen University, Khon Kaen, Thailand
,
Waraporn Putalun 
1   Faculty of Pharmaceutical Sciences, Khon Kaen University, Khon Kaen, Thailand
› Author AffiliationsSupported by: National Research Council of Thailand N41A650080
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Abstract

Derris scandens, which contains isoflavones and prenylated derivatives, has analgesic and anti-inflammatory properties and is an ingredient in traditional Thai medicine for perimenopause and menopause. However, the estrogenic activity of D. scandens has not yet been explored. Therefore, this study aimed to examine the estrogenic activity of the stem extract of D. scandens and its isoflavone derivatives. In this study, we conducted a proliferation assay in MCF-7 cells, and used quantitative reverse transcription polymerase chain reaction to assess gene expression. We found that the relative cell proliferation of the compounds (1 µM) was ranked in the following order as compared to 0.1 nM 17β-estradiol (100%): genistein (97.84%) > derrisisoflavone A (83.17%) > genistein-7-O-[α-rhamnopyranosyl-(1 → 6)-glucopyranoside] (69.55%) > 6,8-diprenylgenistein (51.91%) > lupalbigenin (18.72%). Furthermore, cotreatment with 1 µM lupalbigenin and 0.1 nM 17β-estradiol was performed, which decreased cell proliferation to 80.38%. In vitro results suggest that lupalbigenin has an estrogen-antagonistic effect. At a dose of 1 µM, genistein had the strongest efficacy in increasing the expression of human estrogen receptor β by 4.0-fold compared to the control. Furthermore, genistein-7-O-[α-rhamnopyranosyl-(1 → 6)]-β-glucopyranoside augmented the gene expression of human estrogen receptor α and human estrogen receptor β by 1.5- and 3.4-fold, respectively. Prenylated derivatives of genistein (derrisisoflavone A, 6,8-diprenylgenistein, and lupalbigenin) significantly suppressed the gene expression of the human androgen receptor. The administration of the crude extract at 10 µg/mL significantly suppressed human androgen receptor (0.6-fold) and transmembrane protease serine 2 (0.1-fold) expression but did not significantly affect human estrogen receptor α and human estrogen receptor β gene expression. This herbal medicine may be safe for estrogen-exposed breast cancer patients.

Keywords

estrogenic activity - Derris scandens - related estrogenic genes - isoflavone - Fabaceae


Publication History

Received: 29 February 2024

Accepted after revision: 15 May 2024

Accepted Manuscript online:
15 May 2024

Article published online:
28 June 2024

© 2024. Thieme. All rights reserved.

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