Comparison of structure-activity relationship for bisphenol analogs in the inhibition of gonadal 3S-hydroxysteroid dehydrogenases among human, rat, and mouse

doi:10.1016/j.jsbmb.2023.106424

科研成果详情

题名	Comparison of structure-activity relationship for bisphenol analogs in the inhibition of gonadal 3S-hydroxysteroid dehydrogenases among human, rat, and mouse
作者	Chen, Ya 1,2,6; Zhang, Huina1; Yu, Yang 3,4,5,6; Wang, Shaowei1; Wang, Mengyun1; Pan, Chengshuang1,2; Fei, Qianjin2; Li, Huitao1; Wang, Yiyan 1,3,4,5,6; Lv, Jieqiang1; Ge, Ren-shan1,3,4,5,6
发表日期	2024-02
发表期刊	JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY 影响因子和分区
语种	英语
原始文献类型	Article
关键词	Bisphenols Progesterone 3S-hydroxysteroid dehydrogenase Docking analysis Lipophilicity
其他关键词	EXPOSURE ; ENZYME
摘要	Bisphenol A (BPA) is a widely used plastic material and its potential endocrine disrupting effect has restricted its use and increasing use of BPA alternatives has raised health concerns. However, the effect of bisphenol alternatives on steroidogenesis remains unclear. The objective of this study was to compare inhibitory potencies of 10 BPA alternatives in the inhibition of gonadal 3S-hydroxysteroid dehydrogenase (3S-HSD) in three species (human, rat and mouse). The inhibitory potency for human 3S-HSD2, rat 3S-HSD1, and mouse 3S-HSD6 ranged from bisphenol FL (IC50, 3.32 mu M for human, 5.19 mu M for rat, and 3.26 mu M for mouse) to bisphenol E, F, and thiodiphenol (ineffective at 100 mu M). Most BPA alternatives were mixed inhibitors of gonadal 3S-HSD and they dose-dependently inhibited progesterone formation in KGN cells. Molecular docking analysis showed that all BPA analogs bind to steroid and NAD+ active sites. Lipophilicity of BPA alternatives was inversely correlated with IC50 values. In conclusion, BPA alternatives mostly can inhibit gonadal 3S-HSDs and lipophilicity determines their inhibitory strength.
资助项目	Zhejiang Provincial Health Department [11-CX29]
出版者	PERGAMON-ELSEVIER SCIENCE LTD
ISSN	0960-0760
EISSN	1879-1220
卷号	236
DOI	10.1016/j.jsbmb.2023.106424
页数	12
WOS类目	Biochemistry & Molecular Biology ; Endocrinology & Metabolism
WOS研究方向	Biochemistry & Molecular Biology ; Endocrinology & Metabolism
WOS记录号	WOS:001164167600001
收录类别	SCIE ; PUBMED ; SCOPUS
在线发表日期	2023-11
URL	查看原文
PubMed ID	37939739
SCOPUSEID	2-s2.0-85181669339
通讯作者地址	[Lv, Jieqiang]Department of Gynecology and Obstetrics,the Second Affiliated Hospital and Yuying Children's Hospital of Wenzhou Medical University,Zhejiang,Wenzhou,325027,China
Scopus学科分类	Endocrinology, Diabetes and Metabolism;Biochemistry;Molecular Medicine;Molecular Biology;Endocrinology;Clinical Biochemistry;Cell Biology
引用统计
文献类型	期刊论文
条目标识符	https://kms.wmu.edu.cn/handle/3ETUA0LF/209574
专题	第二临床医学院、附属第二医院、育英儿童医院附属第一医院附属第二医院_麻醉重点学科实验室
通讯作者	Lv, Jieqiang
作者单位	1.Department of Gynecology and Obstetrics,the Second Affiliated Hospital and Yuying Children's Hospital of Wenzhou Medical University,Zhejiang,Wenzhou,325027,China; 2.Reproductive Medicine Center,First Affiliated Hospital of Wenzhou Medical University,Wenzhou,China; 3.Department of Anesthesiology and Perioperative Medicine,the Second Affiliated Hospital and Yuying Children's Hospital,Zhejiang,Wenzhou,325027,China; 4.Key Laboratory of Pediatric Anesthesiology,Ministry of Education,Zhejiang,Wenzhou,325027,China; 5.Key Laboratory of Anesthesiology of Zhejiang Province,Wenzhou Medical University,Zhejiang,Wenzhou,325027,China; 6.Key Laboratory of Environment and Male Reproductive Medicine of Wenzhou,and Key Laboratory of Structural Malformations in Children of Zhejiang Province,Zhejiang,Wenzhou,325000,China
第一作者单位	第二临床医学院，附属第二医院、育英儿童医院; 附属第二医院; 附属第一医院
通讯作者单位	第二临床医学院，附属第二医院、育英儿童医院; 附属第二医院
第一作者的第一单位	第二临床医学院，附属第二医院、育英儿童医院
推荐引用方式 GB/T 7714	Chen, Ya,Zhang, Huina,Yu, Yang,et al. Comparison of structure-activity relationship for bisphenol analogs in the inhibition of gonadal 3S-hydroxysteroid dehydrogenases among human, rat, and mouse[J]. JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY,2024,236.
APA	Chen, Ya., Zhang, Huina., Yu, Yang., Wang, Shaowei., Wang, Mengyun., ... & Ge, Ren-shan. (2024). Comparison of structure-activity relationship for bisphenol analogs in the inhibition of gonadal 3S-hydroxysteroid dehydrogenases among human, rat, and mouse. JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY, 236.
MLA	Chen, Ya,et al."Comparison of structure-activity relationship for bisphenol analogs in the inhibition of gonadal 3S-hydroxysteroid dehydrogenases among human, rat, and mouse".JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY 236(2024).