期刊
PLOS ONE
卷 9, 期 4, 页码 -出版社
PUBLIC LIBRARY SCIENCE
DOI: 10.1371/journal.pone.0092905
关键词
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资金
- Hong Kong Baptist University [FRG2/12-13/021]
- Centre for Cancer and Inflammation Research, School of Chinese Medicine (CCIR-SCM, HKBU)
- Health and Medical Research Fund [HMRF/13121482]
- Research Grants Council [HKBU/201811, HKBU/204612, HKBU/201913]
- French National Research Agency/Research Grants Council Joint Research Scheme [A-HKBU201/12]
- Science and Technology Development Fund, Macao SAR [001/2012/A, 103/2012/A3]
- University of Macau [MYRG091(Y2-L2)-ICMS12-LCH, MYRG121(Y2-L2)-ICMS12-LCH, MRG023/LCH/2013/ICMS]
In this study, we applied structure- based virtual screening techniques to identify natural product or natural product- like inhibitors of iNOS. The iNOS inhibitory activity of the hit compounds was characterized using cellular assays and an in vivo zebrafish larvae model. The natural product- like compound 1 inhibited NO production in LPS- stimulated Raw264.7 macrophages, without exerting cytotoxic effects on the cells. Significantly, compound 1 was able to reverse MPTP-induced locomotion deficiency and neurotoxicity in an in vivo zebrafish larval model. Hence, compound 1 could be considered as a scaffold for the further development of iNOS inhibitors for potential anti- inflammatory or anti- neurodegenerative applications.
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