Long-term use of estrogens: benefit or risk

Pietrzak, Bogusława; Wlaźlak, Ewelina; Zwierzyńska, Ewa

doi:10.5604/17322693.1142582

Cited by 2 publications

(3 citation statements)

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“…Hormone replacement therapy (HRT) had been reported to increase salivary secretion in postmenopausal women ( Yalçin et al, 2005 ; Lago et al, 2015 ). However, HRT possesses a risk of adverse side effects, including the development of endometrial and breast cancer ( Pietrzak et al, 2015 ). Phytoestrogens are plant-derived dietary compounds with structural similarity to E2 ( Rietjens et al, 2017 ).…”

Section: Discussionmentioning

confidence: 99%

Apigenin, a Single Active Component of Herbal Extract, Alleviates Xerostomia via ERα-Mediated Upregulation of AQP5 Activation

et al. 2022

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Xerostomia is a common symptom in menopausal women, suggesting the role of sex steroids in disease development. Shreds of literature had reported the potential use of herbal extracts to relieve xerostomia. However, a cocktail of multiple components in herbal extract makes it difficult to understand the exact mechanism of action. Aquaporin5 (AQP5), the specific aquaporin expressed in salivary glands, plays an important role in salivary secretion as a downstream of estrogen signaling. In this study, we aimed to unravel a single active herbal component as a therapeutic for xerostomia and investigate its mechanism of action. The effects of apigenin (flavonoid), dauricine (alkaloids), protopine (alkaloids), and lentinan (polysaccharides) on AQP5 transcription were screened in vitro. Only apigenin robustly induced AQP5 transcription and expression, and this effect was even robust compared to the effect of estradiol (E2, a positive control). Overexpression of estrogen receptor α (ERα) in the human salivary gland cell line (HSG) upregulated the AQP5 transcription and expression and the knockdown ERα reversed this effect, suggesting the role of ERα signaling on AQP5 activation in HSG cells. Docking results showed apigenin-specific binding sites in ERα. We further analyzed the therapeutic effect of apigenin on ovariectomized mice as a xerostomia model. The saliva secretion in the xerostomia group was reduced to one-third of the sham group, whereas the apigenin or E2 treatment for 12 weeks reversed this effect. Meanwhile, the water consumption in the xerostomia group was augmented obviously compared to the sham group, whereas the water consumption in the apigenin and E2 group was declined to the level of the sham group. Immunohistochemistry of submandibular glands revealed the downregulation of AQP5 expression in xerostomia mice compared to control. Apigenin, or E2 treatment, upregulated AQP5 expression in xerostomia mice. In conclusion, apigenin, a single active component of herbal extract, upregulated AQP5 expression in HSG cells via activation of ERα signaling and restored saliva flow rates in OVX mice. These results revealed apigenin as a single active component of herbal extract with the potential to treat xerostomia.

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Section: Discussionmentioning

confidence: 99%

Apigenin, a Single Active Component of Herbal Extract, Alleviates Xerostomia via ERα-Mediated Upregulation of AQP5 Activation

et al. 2022

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“…A diagnosis made using electron microscopy revealed that the skin affected by melasma shows an excessive amount of free pigment, as well as elastosis. Moreover, an increase in the expression of estrogen receptor is also noted . Pigment cells reveal increased metabolism.…”

Section: Introductionmentioning

confidence: 93%

“…Studies using diethylstilbestrol (DES) – a synthetic estrogen in mouse melanoma cells – have shown that DES stimulates pigment cells and induces melanogenesis …”

Section: Introductionmentioning

confidence: 99%