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Article

Rheum rhaponticum Root Extract Improves Vasomotor Menopausal Symptoms and Estrogen-Regulated Targets in Ovariectomized Rat Model

1
Plants for Human Health Institute, North Carolina Research Campus, North Carolina State University, 600 Laureate Way, Kannapolis, NC 28081, USA
2
Department of Food, Bioprocessing & Nutrition Sciences, North Carolina State University, 400 Dan Allen Drive, Raleigh, NC 27695, USA
3
Metagenics Inc., 9770 44th Ave NW, Gig Harbor, WA 98332, USA
4
Department of Biology, Catawba College, 2300 W Innes Street, Salisbury, NC 28144, USA
*
Author to whom correspondence should be addressed.
Academic Editor: Raffaele Capasso
Int. J. Mol. Sci. 2021, 22(3), 1032; https://doi.org/10.3390/ijms22031032
Received: 15 December 2020 / Revised: 14 January 2021 / Accepted: 14 January 2021 / Published: 21 January 2021
(This article belongs to the Special Issue Natural Product Pharmacology)
Ovarian insufficiency and ovariectomy are characterized by deregulated heat loss mechanisms. Unlike hormone therapy, ERr 731 (a standardized botanical extract of Siberian rhubarb Rheum rhaponticum L. high in rhaponticin) acts like a selective estrogen receptor modulator for ERβ receptors and may offer a higher degree of safety while maintaining the desired efficacy profile. In this study, we examined the relationship between oral administration of ERr 731 and the underlying components of skin vasomotion responses in an ovariectomized (OVX) rat model. ERr 731 dose-dependently reduced tail skin temperature (Tskin) values by an average of 1 °C. The rapid onset of this effect was observed in 1 and 3 mg/kg/day ERr 731 groups as early as day 2 of administration, and remained in place for the duration of the treatment (2 weeks). Substituting ERr 731 after E2 withdrawal helped maintain body temperature similarly to E2 alone, suggesting the usefulness of ERr 731 for replacing existing hormonal therapy in humans. ERr 731 also acted as a highly selective agonist for ERβ in the hypothalamus of OVX rats, as well as in ERα/β cell-based reporter assays. These data validate the OVX/Tskin rat model as a suitable screening platform to evaluate botanical and pharmaceutical treatments of menopause, while providing further evidence for the efficacy of ERr 731 towards alleviating vasomotor menopausal symptoms and improving wellbeing during the menopausal transition. View Full-Text
Keywords: postmenopausal; estrogens; hot flashes; HRT; ERr 731 postmenopausal; estrogens; hot flashes; HRT; ERr 731
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MDPI and ACS Style

Wilson, M.; Konda, V.; Heidt, K.; Rathinasabapathy, T.; Desai, A.; Komarnytsky, S. Rheum rhaponticum Root Extract Improves Vasomotor Menopausal Symptoms and Estrogen-Regulated Targets in Ovariectomized Rat Model. Int. J. Mol. Sci. 2021, 22, 1032. https://doi.org/10.3390/ijms22031032

AMA Style

Wilson M, Konda V, Heidt K, Rathinasabapathy T, Desai A, Komarnytsky S. Rheum rhaponticum Root Extract Improves Vasomotor Menopausal Symptoms and Estrogen-Regulated Targets in Ovariectomized Rat Model. International Journal of Molecular Sciences. 2021; 22(3):1032. https://doi.org/10.3390/ijms22031032

Chicago/Turabian Style

Wilson, Mickey, Veera Konda, Kathryn Heidt, Thirumurugan Rathinasabapathy, Anuradha Desai, and Slavko Komarnytsky. 2021. "Rheum rhaponticum Root Extract Improves Vasomotor Menopausal Symptoms and Estrogen-Regulated Targets in Ovariectomized Rat Model" International Journal of Molecular Sciences 22, no. 3: 1032. https://doi.org/10.3390/ijms22031032

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