The selective estrogen receptor modulator DT56a (Femarelle) does not affect platelet reactivity in normal or thrombophilic postmenopausal women

Nachtigall, Margaret J.; Jessel, Rebecca H.; Flaumenhaft, Robert; Nachtigall, Richard; Yoles, Israel; Naftolin, Frederick; Nachtigall, Lila E.

doi:10.1097/gme.0b013e3181f2f01a

Cited by 11 publications

(10 citation statements)

References 22 publications

(18 reference statements)

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“…In addition, femarelle does not effect cell proliferation in the human MCF-7 breast cancer cell line (Yoles and Lilling, 2007). Femarelle shows efficacy in preserving bone mineral density (BMD) in both female rats and clinically in postmenopausal women without risk of thrombogenicity (Yoles et al, , 2004Somjen et al, 2005Somjen et al, , 2006Nachtigall et al, 2011). Femarelle and other ER agonists have been shown to abolish fat cell content in rat bone marrow.…”

Section: Nuclear Receptors and Their Selective Modulatorsmentioning

confidence: 99%

Nuclear Receptors and Their Selective Pharmacologic Modulators

et al. 2013

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Section: Nuclear Receptors and Their Selective Modulatorsmentioning

confidence: 99%

Nuclear Receptors and Their Selective Pharmacologic Modulators

et al. 2013

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“…A positive impact on the acute climacteric syndrome was recorded in all women. The coagulable risk increased in none (21).…”

Section: Clinical Studiesmentioning

confidence: 97%

DT56a in treatment of climacteric syndrome in the Central European population sample

Fait¹,

Borovský²

2021

BLL

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The aim of this study was to assess the possibility of using the DT56a for the therapy of acute climacteric syndrome in women in Slovakia and the Czech Republic. DESIGN: Prospective interventional unblinded study. RESULTS: A sample of 453 women with symptoms of acute climacteric syndrome took 644 mg of soybeans´ phyotestrogenes DT56a in the period of 4 weeks. In course of the therapy, the total number of hot fl ushes decreased by 48 %, and the intensity decreased by 35 % (p < 0.01). In 85 % of women, the quantity or intensity of hot fl ushes decreased. Sleep quality increased in 65 % of women, headaches improved or signifi cantly improved in 51 % of women, muscle aches and joint pains decreased by 40 %. Life quality improved in 72 % of women. CONCLUSIONS: DT56a is a possible alternative for the treatment of acute climacteric syndrome. In the Central European population, the effi cacy of a daily dose of 644 mg corresponds with the effects observed in the Mediterranean population (Tab. 2, Fig. 3, Ref.

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“… 10 , 53 , 54 Recall, 17β-estradiol is the most potent steroid hormone produced by the ovaries until menopause ( Figure 3 ). 10 , 53 , 54 All estrogens and their estrogenic analogs, such as tamoxifen, 56 phenytoin, 57 DT56a 58 and even some androgens 59 act through binding to ERα and ERβ. 53 Since the majority of cells express ERs, estrogen actions influence almost all tissues and are responsible for: a) homeostatic regulation, b) cell proliferation and apoptosis, c) liver protein expression, d) lipid metabolism, e) energy balance, f) glucose metabolism, g) immune and cardiovascular alterations, h) gonadotrophin feedback and gametogenesis, i) brain-neuronal development/memory processing and repair/neurodegeneration, j) bone growth, etc., 7 , 15 , 53 , 60 including estrogen’s positive (agonist) or negative (antagonist) actions on skin, especially in women.…”

Section: Estrogensmentioning

confidence: 99%

“… 47 , 53 The presence (expression) of estrogen receptors in the majority of tissues and the presence of EREs in the majority of genes make it possible for estrogen action to occur in almost all cells in the body including the skin. 50 , 51 , 57 , 58 …”

Section: Estrogen Receptors (Nuclear Membrane-bound and Mitochondria)...mentioning

confidence: 99%

“… 10 , 86 Concurrent with the loss of 17β-estradiol production from the ovaries at menopause estrogen production in the body occurs at peripheral adipose tissue sites. 7 , 15 , 58 , 62 , 72 , 82 While skin cells can produce estrogens locally, the aromatase enzyme activity is 30-times lower compared to premenopausal ovarian tissue. 15 , 53 , 86 Moreover, the negative androgenic impact on skin cells via the 5α-reductase type I enzyme can counteract the positive estrogenic influence, especially after menopause.…”

Section: Skin Collagen and Elastin Profiles With Changes In 17beta-es...mentioning

confidence: 99%

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Factors Influencing Skin Aging and the Important Role of Estrogens and Selective Estrogen Receptor Modulators (SERMs)

Lephart¹,

Naftolin²

2022

CCID

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The narrative for this overview focuses on updating the factors that influence skin aging and the important role estrogens and selective estrogen receptor modulators (SERMs) play in this process (mainly utilizing journal reports and reviews from the last four years). Estrogens have been known and studied for over a century. For many years, it has been recognized that estrogens are important in the maintenance of human skin. Women seek cosmetic and medical treatments to improve dermal health and physical characteristics to enhance their self-perception and inhibit skin aging, particularly in highly visible body areas. The goal: to retain estrogen’s positive benefits while aging and especially at/after menopause where estrogen-deficient skin contributes to the dramatic decline in skin health. In this overview, both background information and recent novel findings are included that cover aging (general mechanisms), skin aging, and factors that influence skin aging (intrinsic, extrinsic, skin microbiome and gut microbiome.) Plus, estrogen’s general role in maintaining skin health is presented through the classical estrogen receptors alpha (α) and beta (β) and non-classical (or non-genomic) estrogen receptor (G protein-coupled seven transmembrane receptor). More importantly, the various benefits of 17β-estradiol in skin health are examined (ie, skin collagen and elastin profiles that follow 17β-estradiol levels during aging and at/after menopause). Finally, a revision of information for estrogenic skin topical applications involving isoflavonoid compounds that act as SERMs, but are classified as endocrine disruptors, and a topical estrogen analog are explored to update the known and unknown characteristics of these treatments. Further study is warranted to understand the biological and molecular mechanisms by which estrogens support and enhance dermal health and wellbeing.

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The selective estrogen receptor modulator DT56a (Femarelle) does not affect platelet reactivity in normal or thrombophilic postmenopausal women

Cited by 11 publications

References 22 publications

Nuclear Receptors and Their Selective Pharmacologic Modulators

Nuclear Receptors and Their Selective Pharmacologic Modulators

DT56a in treatment of climacteric syndrome in the Central European population sample

Factors Influencing Skin Aging and the Important Role of Estrogens and Selective Estrogen Receptor Modulators (SERMs)

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