scholarly journals Distinct Approaches of Raloxifene: Its Far-Reaching Beneficial Effects Implicating the HO-System

Biomolecules ◽  
2020 ◽  
Vol 10 (3) ◽  
pp. 375
Author(s):  
Denise Börzsei ◽  
Renáta Szabó ◽  
Alexandra Hoffmann ◽  
Médea Veszelka ◽  
Imre Pávó ◽  
...  
Keyword(s):  
Estrogen Receptor ◽  
Current Knowledge ◽  
Cardiovascular Effects ◽  
The Body ◽  
General Activity ◽  
Beneficial Effects ◽  
Cell Defense ◽  
Estrogen Receptor Modulators ◽  
Pathological Conditions ◽  
Receptor Modulators

Selective estrogen receptor modulators (SERMs) were discovered in the mid-1900s in connection with estrogen-related pathological conditions. They were developed to antagonize the adverse effects of estrogen and have been shown to be effective against postmenopausal disorders manifested by estrogen deficiency. Raloxifene (RAL), one of the most widely used SERMs, expresses estrogen-like effects on bones, while it is found to be an antagonist on breast and uterus. RAL has multiple beneficial effects throughout the body, including antioxidant and anti-inflammatory properties, because of which it gains particular attention. Additionally, previous studies have revealed that RAL is an efficient modulator of heme-oxygenase (HO) expression. HO, through its general activity, participates in comprehensive cell defense processes, thus the induction of HO by RAL administration indicates a major role in its therapeutic efficacy. In this review, we compile the current knowledge about the overall metabolic, neurocognitive, and cardiovascular effects of RAL involving the cytoprotective HO-system.

scholarly journals Estrogen Receptor Modulators in Viral Infections Such as SARS−CoV−2: Therapeutic Consequences

2021 ◽  
Vol 22 (12) ◽  
pp. 6551
Author(s):  
Nikita Abramenko ◽  
Fréderic Vellieux ◽  
Petra Tesařová ◽  
Zdeněk Kejík ◽  
Robert Kaplánek ◽  
...  
Keyword(s):  
Estrogen Receptor ◽  
Viral Infections ◽  
Current Knowledge ◽  
Severe Disease ◽  
Receptor Activation ◽  
Potential Effect ◽  
Point Of View ◽  
Therapeutic Consequences ◽  
Estrogen Receptor Modulators ◽  
Receptor Modulators

COVID−19 is a pandemic respiratory disease caused by the SARS−CoV−2 coronavirus. The worldwide epidemiologic data showed higher mortality in males compared to females, suggesting a hypothesis about the protective effect of estrogens against severe disease progression with the ultimate end being patient’s death. This article summarizes the current knowledge regarding the potential effect of estrogens and other modulators of estrogen receptors on COVID−19. While estrogen receptor activation shows complex effects on the patient’s organism, such as an influence on the cardiovascular/pulmonary/immune system which includes lower production of cytokines responsible for the cytokine storm, the receptor-independent effects directly inhibits viral replication. Furthermore, it inhibits the interaction of IL−6 with its receptor complex. Interestingly, in addition to natural hormones, phytestrogens and even synthetic molecules are able to interact with the estrogen receptor and exhibit some anti-COVID−19 activity. From this point of view, estrogen receptor modulators have the potential to be included in the anti-COVID−19 therapeutic arsenal.

scholarly journals Selective Estrogen Receptor Modulators Accelerate Cutaneous Wound Healing in Ovariectomized Female Mice

Endocrinology ◽  
2007 ◽  
Vol 149 (2) ◽  
pp. 551-557 ◽  
Author(s):  
Matthew J. Hardman ◽  
Elaine Emmerson ◽  
Laura Campbell ◽  
Gillian S. Ashcroft
Keyword(s):  
Wound Healing ◽  
Estrogen Receptor ◽  
Selective Estrogen Receptor Modulators ◽  
Cutaneous Wound Healing ◽  
Cutaneous Wound ◽  
Beneficial Effects ◽  
Estrogen Receptor Modulators ◽  
Ovariectomized Mice ◽  
Receptor Modulators

A lack of systemic hormones in elderly postmenopausal women leads to delayed cutaneous wound healing. This effect can be reversed by systemic or topical estrogen replacement in both humans and rodent models. Over recent years selective estrogen receptor modulators have been developed in an attempt to achieve the beneficial effects of estrogen clinically, while minimizing the detrimental side effects. The effects of selective estrogen receptor modulators on the skin are poorly understood, and the effects on wound healing have not been assessed. In this study we treated 10-wk-old ovariectomized mice with estradiol, tamoxifen (TAM), raloxifene (RAL), or vehicle and examined the effect on healing of full-thickness incisional wounds. Both TAM and RAL substantially accelerate healing, associated with a dampened inflammatory response and altered inflammatory cytokine profile. In vitro TAM and RAL demonstrate antiinflammatory activity comparable to estrogen. These results have significant implications for the clinical modulation of wound healing.

Estrogen Receptor Modulators

2021 ◽  
pp. 1-74
Author(s):  
Carlo I. Rosales ◽  
Lauren M. Gutgesell ◽  
Kiira M. Ratia ◽  
Gregory R.J. Thatcher
Keyword(s):  
Estrogen Receptor ◽  
Estrogen Receptor Modulators ◽  
Receptor Modulators
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