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Inhibitory Effects of Bisphenol Z on 11β-Hydroxysteroid Dehydrogenase 1 and In Silico Molecular Docking Analysis
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Inhibitory Effects of Bisphenol Z on 11β-Hydroxysteroid Dehydrogenase 1 and In Silico Molecular Docking Analysis
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Journal Article
Inhibitory Effects of Bisphenol Z on 11β-Hydroxysteroid Dehydrogenase 1 and In Silico Molecular Docking Analysis
2025
Overview
Bisphenol A (BPA) is classified as an endocrine disruptor that mainly mimics the effects of estrogen and disrupts the synthesis of male androgens. Due to the toxicity of BPA, some new analogs, such as bisphenol BPB, BPC, BPF, PBH, and BPZ, were introduced into the market. The goal of this research was to demonstrate the applicability of kinetic analysis, in particular, Lineweaver-Burk plots, in assessing the impact of bisphenol Z on enzymatic activity. This study aimed to characterize the inhibitory effects of BPZ on 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) activity in the transformation of 11-dehydrocorticosterone (DHC) to corticosterone (CORT). During the determination of the enzymatic reaction product, chromatographic analysis conditions were optimized using gradient elution and an Acquity UPLC BEH C18 chromatographic column. The retention time of the assayed corticosterone was approximately 2 min. Also described and compared were graphical methods of analysis and data interpretation, such as Lineweaver-Burk, Eadie-Hofstee, and Hanes-Woolf plots. The experiments demonstrated that bisphenol Z is a mixed 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) inhibitor, responsible for catalyzing the conversion of 11-dehydrocorticosterone (DHC) to corticosterone (CORT). This relationship was confirmed by analyzing Lineweaver-Burk plots, which showed an increase in apparent KM with a decrease in the constant Vmax, suggesting a mixed inhibition mechanism. Molecular docking and detailed analysis of the interaction profiles revealed that BPZ consistently occupies the active site cavities of all examined enzymes (rat and human 11β-HSD1 and Arabidopsis 11β-HSD2), forming a stabilizing network of non-covalent interactions. Our research has significant biological significance considering the role of the 11β-HSD1 enzyme in the conversion of DHC to CORT and the importance of this process and its functions in adipose tissue, the liver, and the brain.
Publisher
MDPI AG,Multidisciplinary Digital Publishing Institute (MDPI)
Subject
11-beta-Hydroxysteroid Dehydrogenase Type 1 - antagonists & inhibitors
/ 11-beta-Hydroxysteroid Dehydrogenase Type 1 - chemistry
/ 11-beta-Hydroxysteroid Dehydrogenase Type 1 - metabolism
/ 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1)
/ Analysis
/ Benzhydryl Compounds - chemistry
/ Benzhydryl Compounds - pharmacology
/ Corticosterone - analogs & derivatives
/ Endocrine Disruptors - chemistry
/ Enzyme Inhibitors - chemistry
/ Enzyme Inhibitors - pharmacology
/ Enzymes
/ Estrogen
/ Hormones
/ Humans
/ Kidneys
/ Kinetics
/ Liver
/ Molecular Docking Simulation
/ Obesity
/ Steroids
/ Toxicity
