Characterisation of naturally occurring isothiocyanates as glutathione reductase inhibitors
文献类型：期刊论文
| 作者 | Li, Xia1,2,6; Ni, Maowei1,2,6; Xu, Xiaoling1,3,6; Chen, Wei1,2,4,5,6 |
| 刊名 | JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
 |
| 出版日期 | 2020 |
| 卷号 | 35 |
| 关键词 | Glutathione reductase isothiocyanate inhibitor thiocarbamoylation |
| ISSN号 | 1475-6366 |
| DOI | 10.1080/14756366.2020.1822828 |
| 通讯作者 | Chen, Wei(chenwei@zjcc.org.cn) |
| 英文摘要 | Glutathione reductase (GR), an essential antioxidant enzyme against oxidative stress, has become an attractive drug target for the development of anticancer and antimalarial drugs. In this regard, we evaluated the naturally occurring isothiocyanates as promising GR inhibitors and elucidated the mechanism of action. It was found that benzyl isothiocyanate (BITC) and phenethyl isothiocyanate (PEITC) inhibited yeast GR (yGR) and human GR (hGR) in a time- and concentration-dependent manner. TheK(i)andk(inact)of BITC against yGR were determined to be 259.87 mu M and 0.0266 min(-1), respectively. The GR inhibition occurred only in the presence of NADPH and persisted after extensive dialysis. The tandem mass spectrometric analysis revealed that Cys(61)rather than Cys(66)at the active site of yGR was mono-benzyl thiocarbamoylated by BITC. Inhibition of intracellular GR by BITC and PEITC in cultured cancer cells was also observed. BITC and PEITC were evaluated as competitive and irreversible inhibitors of GR. |
| WOS关键词 | PARASITE PLASMODIUM-FALCIPARUM ; PHENETHYL ISOTHIOCYANATE ; APOPTOSIS ; TARGETS ; CELLS ; ACID |
| 资助项目 | International Cooperation Fund from Science Technology Department of Zhejiang Province[LGJ19H160001] ; National Natural Science Foundation of China[81903641] ; National Natural Science Foundation of China[81802995] ; Zhejiang Provincial Natural Science Foundation of China[LQ18H160016] ; Medical Science and Technology Project of Zhejiang Province[2018268942] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000571312300001 |
| 出版者 | TAYLOR & FRANCIS LTD |
| 资助机构 | International Cooperation Fund from Science Technology Department of Zhejiang Province ; National Natural Science Foundation of China ; Zhejiang Provincial Natural Science Foundation of China ; Medical Science and Technology Project of Zhejiang Province |
| 源URL | [http://ir.hfcas.ac.cn:8080/handle/334002/104229]  |
| 专题 | 中国科学院合肥物质科学研究院 |
| 通讯作者 | Chen, Wei |
| 作者单位 | 1.Chinese Acad Sci, Inst Canc & Basic Med, Hangzhou, Peoples R China 2.Univ Chinese Acad Sci, Zhejiang Canc Res Inst, Canc Hosp, Hangzhou, Peoples R China 3.Univ Chinese Acad Sci, Dept Med Oncol, Canc Hosp, Hangzhou, Peoples R China 4.Univ Chinese Acad Sci, Zhejiang Key Lab Radiat Oncol, Canc Hosp, Hangzhou, Peoples R China 5.Zhejiang Prov Key Lab Integrated Tradit Chinese &, Hangzhou, Peoples R China 6.Univ Chinese Acad Sci, Zhejiang Canc Hosp, Canc Hosp, Hangzhou, Peoples R China |
| 推荐引用方式 GB/T 7714 | Li, Xia,Ni, Maowei,Xu, Xiaoling,et al. Characterisation of naturally occurring isothiocyanates as glutathione reductase inhibitors[J]. JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY,2020,35. |
| APA | Li, Xia,Ni, Maowei,Xu, Xiaoling,&Chen, Wei.(2020).Characterisation of naturally occurring isothiocyanates as glutathione reductase inhibitors.JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY,35. |
| MLA | Li, Xia,et al."Characterisation of naturally occurring isothiocyanates as glutathione reductase inhibitors".JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY 35(2020). |
入库方式： OAI收割
来源：合肥物质科学研究院
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