题名 | Effects of Polybrominated Diphenyl Ethers on Rat and Human 11 beta-Hydroxysteroid Dehydrogenase 1 and 2 Activities |
作者 | |
发表日期 | 2016-12-31 |
发表期刊 | PHARMACOLOGY 影响因子和分区 |
语种 | 英语 |
原始文献类型 | Article |
关键词 | Steroids Polybrominated diphenyl ether 11 beta-Hydroxysteroid dehydrogenase 1 11 beta-Hydroxysteroid dehydrogenase 2 Glucocorticoid metabolism |
其他关键词 | BETA-HYDROXYSTEROID DEHYDROGENASE ; APPARENT MINERALOCORTICOID EXCESS ; GLUCOCORTICOID-RECEPTOR ; LEYDIG-CELLS ; TYPE-2 ; KIDNEY ; ENZYME ; LOCALIZATION ; HYPERTENSION ; REGULATOR |
摘要 | Polybrominated diphenyl ethers (PBDEs) are a class of brominated flame retardants. PBDEs have been widely used in textiles, flexible polyurethane foams, electronic components, electrical components, and plastics. 11 beta-Hydroxysteroid dehydrogenases, isoform 1 (HSD11B1) and isoform 2 (HSD11B2), have been demonstrated to be the regulators of local glucocorticoid levels. In this study, the potencies of 4 different PBDEs (BDE-3, BDE-47, BDE-100, and BDE-153) with 1-6 bromine atoms attached in inhibition of rat and human HSD11B1 and HSD11B2 activities were compared to 4-bromobiphenyl (BBP), a structurally similar compound. All 4 PBDEs and BBP did not inhibit rat and human HSD11B1. BDE-3 and BDE-47 potently inhibited rat HSD11B2, and BDE- 47 and BDE- 153 potently inhibited human HSD11B2, with the half maximal inhibitory concentration values of 12.42, 5.95, 11.97, and 4.41 mu mol/l, respectively. All PBDEs noncompetitively inhibited HSD11B2 when a steroid substrate was used. However, PBDEs exerted uncompetitive inhibition when the cofactor NAD(+) was used. In conclusion, some PBDEs are selective inhibitors of HSD11B2, possibly causing excessive glucocorticoid action in local tissues. (C) 2016 S. Karger AG, Basel |
资助项目 | Health Bureau of Zhejiang Province [11-CX29, 2013ZDA017] |
出版者 | KARGER |
出版地 | BASEL |
ISSN | 0031-7012 |
EISSN | 1423-0313 |
卷号 | 98期号:3-4页码:115-123 |
DOI | 10.1159/000445213 |
页数 | 9 |
WOS类目 | Pharmacology & Pharmacy |
WOS研究方向 | Pharmacology & Pharmacy |
WOS记录号 | WOS:000380138800003 |
收录类别 | SCIE ; PUBMED ; SCOPUS |
URL | 查看原文 |
PubMed ID | 27198750 |
SCOPUSEID | 2-s2.0-84969903608 |
通讯作者地址 | [Ge, Ren-Shan]Wenzhou Med Univ, Affiliated Hosp 2, Ctr Sci Res, Wenzhou 325027, Peoples R China. ; [Chen, Ruijie]Wenzhou Med Univ, Affiliated Hosp 2, Dept Pharm, Wenzhou 325027, Peoples R China. |
Scopus学科分类 | Pharmacology |
引用统计 | |
文献类型 | 期刊论文 |
条目标识符 | https://kms.wmu.edu.cn/handle/3ETUA0LF/19379 |
专题 | 附属第二医院_科研中心 附属第二医院 |
通讯作者 | Chen, Ruijie; Ge, Ren-Shan |
作者单位 | 1.Wenzhou Med Univ, Affiliated Hosp 2, Ctr Sci Res, Wenzhou 325027, Peoples R China; 2.Wenzhou Med Univ, Affiliated Hosp 2, Dept Pharm, Wenzhou 325027, Peoples R China |
第一作者单位 | 附属第二医院_科研中心 |
通讯作者单位 | 附属第二医院_科研中心; 附属第二医院 |
第一作者的第一单位 | 附属第二医院_科研中心 |
推荐引用方式 GB/T 7714 | Chen, Xiaomin,Dong, Yaoyao,Cao, Shuyan,et al. Effects of Polybrominated Diphenyl Ethers on Rat and Human 11 beta-Hydroxysteroid Dehydrogenase 1 and 2 Activities[J]. PHARMACOLOGY,2016,98(3-4):115-123. |
APA | Chen, Xiaomin., Dong, Yaoyao., Cao, Shuyan., Li, Xiaoheng., Wang, Zhe., ... & Ge, Ren-Shan. (2016). Effects of Polybrominated Diphenyl Ethers on Rat and Human 11 beta-Hydroxysteroid Dehydrogenase 1 and 2 Activities. PHARMACOLOGY, 98(3-4), 115-123. |
MLA | Chen, Xiaomin,et al."Effects of Polybrominated Diphenyl Ethers on Rat and Human 11 beta-Hydroxysteroid Dehydrogenase 1 and 2 Activities".PHARMACOLOGY 98.3-4(2016):115-123. |
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