Estrogen Sulfotransferase (SULT1E1): Its Molecular Regulation, Polymorphisms, and Clinical Perspectives

Estrogen sulfotransferase (SULT1E1) is a phase II enzyme that sulfates estrogens to inactivate them and regulate their homeostasis. This enzyme is also involved in the sulfation of thyroid hormones and several marketed medicines. Though the profound action of SULT1E1 in molecular/pathological biology has been extensively studied, its genetic variants and functional studies have been comparatively rarely studied. Genetic variants of this gene are associated with some diseases, especially sex-hormone-related cancers. Comprehending the role and polymorphisms of SULT1E1 is crucial to developing and integrating its clinical relevance; therefore, this study gathered and reviewed various literature studies to outline several aspects of the function, molecular regulation, and polymorphisms of SULT1E1.

Protective Effects of Aqueous Extract of Mentha suaveolens against Oxidative Stress-Induced Damages in Human Keratinocyte HaCaT Cells

Mentha suaveolens is an aromatic herb that has a wide range of biological activities, including antimicrobial, antifungal, anti-inflammatory, and hepatoprotective properties. Although there are a few reports on the antioxidant property of M. suaveolens, its cytoprotective activity against oxidative stress has not been reported yet. The objective of this study was to determine the protective activity of M. suaveolens aqueous extract (MSAE) against hydrogen peroxide- (H2O2-) induced oxidative stress and apoptosis in human keratinocyte HaCaT cells. MSAE pretreatment decreased H2O2-induced cytotoxicity and suppressed H2O2-induced intracellular ROS generation. Furthermore, MSAE suppressed expression levels of H2O2-induced apoptotic genes such as cleaved caspase-3, caspase-9, and cleaved poly (ADP-ribose) polymerase (PARP). Pretreatment with MSAE induced expression of phase II enzyme such as HO-1 through translocation of NF-E2-related factor (Nrf2) upon H2O2 exposure. These results revealed that the cytoprotective effect of MSAE against oxidative stress-induced cell death was associated with activation of Nrf2-mediated phase II enzyme expression.

miR-503 Is Involved in the Protective Effect of Phase II Enzyme Inducer (CPDT) in Diabetic Cardiomyopathy via Nrf2/ARE Signaling Pathway

Diabetic cardiomyopathy (DCM) is a common heart disease. The Phase II enzyme inducer (CPDT) is a complex enzyme that promotes the expression of antioxidant enzymes through activating nuclear factor erythroid 2-related factor 2 (Nrf2); these compounds have been shown to protect against oxidative stress. However, whether these compounds have similar protective effects in DCM still remains unclear. The purpose of this study is to investigate the protective effects and potential mechanism of CPDT in diabetic cardiomyopathy. In the results, firstly, compared with control rats, myocardial cell size, left ventricular mass index, and myocardial apoptosis index were increased, miR-503 was increased, and Nrf2, malondialdehyde (MDA), and heme oxygenase 1 (HO-1) were decreased in diabetic cardiomyopathy rats. Furthermore, compared with diabetic cardiomyopathy rats, these above parameters show the opposite change in CPDT treatment rats. In addition, the bioinformatics and luciferase reporter assay demonstrated that Nrf2 is a direct target of miR-503. Finally, the miR-503 could also regulate Nrf2 in the myocardial cells. Therefore, miR-503 is involved in the protective effect of CPDT in diabetic cardiomyopathy via Nrf2/ARE signaling pathway; miR-503 and Nrf2 may be a promising therapeutic target for the management of diabetic cardiomyopathy.

New hybrid bromopyridine-chalcones as in vivo phase II enzyme inducers: potential chemopreventive agents

We report the synthesis of eighteen new potential cancer chemopreventive agents, structurally designed to combine (naphtho)chalcone and (bromo)pyridine skeletons.