Both pentachlorophenol and 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) had been studied widely because of their probable anti-estrogenic activity. Sodium pentachlorophenol (PCP-Na), as a industrial product used in many fields, usually contains a trace of TCDD. The aim of this study was to assess the anti-estrogenic effect of PCP-Na in juvenile goldfish (Carassius auratus) hepatocyte cultures using vitellogenin (VTG) as the biomarker. The ID50 of PCP-Na was investigated and then a series of concentrations (0.001-0.5 microg/ml) of PCP-Na were evaluated to estimate the anti-estrogenic activity. Results showed that PCP-Na was cytotoxic for hepatocytes even at very low concentration < 1.21 microg/ml, and it could not induce VTG at any concentrations tested. Since it failed to stimulate VTG production, the possibility of its anti-estrogenic effect was tested, and a well-known anti-estrogenic compound-tamoxifen was used as positive control. PCP-Na caused a reduction in VTG synthesis in juvenile goldfish (Carassius auratus) hepatocytes at concentrations > 0.1 microg/ml when co-exposure with 1 microg/ml 17beta-estradiol (E2), making its anti-estrogenic activity approximately as potent as tamoxifen. Our results indicate that PCP-Na can act as negative modulators of estrogenic function in juvenile goldfish (Carassius auratus) hepatocytes.
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Biochem Pharmacol
November 2024
Department of Physiology, Nippon Medical School, Bunkyo-ku, Tokyo 113-8602, Japan.
This comprehensive review of estrogenic alkaloids reveals that although the number is small, they exhibit a wide range of structures, biosynthesis pathways, mechanisms of action, and applications. Estrogenic alkaloids belong to different classes, different biosynthetic pathways, different estrogenic actions (estrogenic/synergistic, anti-estrogenic/antagonistic, biphasic, and acting as a selective estrogen receptor modulator or SERM), different receptor-initiated signaling pathways, different ways of modulations of estrogen action, and different applications. The future applications of estrogenic alkaloids, such as those for diagnostics, drug development, and therapeutics, are considered with the help of new databases containing comprehensive descriptions of their relationships and more elaborate artificial intelligence-based prediction technologies.
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Department of Food Science and Technology, Graphic Era (Deemed to be University), Dehradun, Uttarakhand 248002, India. Electronic address:
Phytoestrogens, derived from plants possesses structural similarity with 17 β-estradiol found in mammals. It is abundantly present in soybean along with red clove, alfalfa as well as other legumes, nuts, vegetables and seeds. It is used as hormone replacement therapy and exhibits both anti-estrogenic and estrogenic properties that linked to therapeutic benefits as well as plays active role in sports nutrition.
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Institute for Pharmaceutical and Medicinal Chemistry, Heinrich Heine University Düsseldorf, 40225 Düsseldorf, Germany.
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Department of Biochemistry, Stellenbosch University, Van de Byl Street, Stellenbosch, 7601, South Africa.
Despite being the focal point of decades of research, female breast cancer (BC) continues to be one of the most lethal cancers in the world. Given that 80 % of all diagnosed BC cases are estrogen receptor-positive (ER+) with carcinogenesis driven by estrogen-ERα signalling, current standard of care (SOC) hormone therapies are geared towards modulating the function and expression levels of estrogen and its receptors, ERα and ERβ. Currently, aromatase inhibitors (AIs), selective ER modulators (SERMs) and selective ER degraders (SERDs) are clinically prescribed for the management and treatment of ER+ BC, with the anti-aromatase activity of AIs abrogating estrogen biosynthesis, while the anti-estrogenic SERMs and SERDs antagonise and degrade the ER, respectively.
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