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Synthesis of Stable Genipin Derivatives and Studies of Their Neuroprotective Activity in PC12 Cells
Luo J.3; Wang R.2; Huang Z.3; Yang J.3; Yao X.3; Chen H.3; Zheng W.2
2012-09-01
Source PublicationChemMedChem
ISSN18607179 18607187
Volume7Issue:9Pages:1661-1668
AbstractModifications at C1, C7, C8, and C10 of genipin were conducted, and the neurotrophic effects of all derivatives were studied. Genipin derivatives 1-4 were obtained in mild to high yield. Compounds 1 and 4 are more stable than genipin if exposed to nucleophiles. All the derivatives display higher neurotrophic activities than genipin. Compound 4 is the most active, with the least optimal dose. Both genipin and 4 up-regulated the activity of nNOS in PC12 cells. The effect of 4 is inhibited not only by 7-NI, a specific inhibitor of nNOS, but also by L-NIO, a specific inhibitor of eNOS; in the case of genipin, its effect is only inhibited by 7-NI. All the results indicate that 4 is a promising lead compound for the development of new drugs in the treatment of neurodegenerative diseases with the ability to address multiple drug targets. © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
KeywordENOS GardenamideA Genipin Neuroprotective activity NNOS
DOI10.1002/cmdc.201200258
URLView the original
Language英語
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Cited Times [WOS]:14   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionUniversity of Macau
Affiliation1.Chinese Medicines and New Drug Research
2.Zhongshan Ophthalmic Center
3.Jinan University
Recommended Citation
GB/T 7714
Luo J.,Wang R.,Huang Z.,et al. Synthesis of Stable Genipin Derivatives and Studies of Their Neuroprotective Activity in PC12 Cells[J]. ChemMedChem,2012,7(9):1661-1668.
APA Luo J..,Wang R..,Huang Z..,Yang J..,Yao X..,...&Zheng W..(2012).Synthesis of Stable Genipin Derivatives and Studies of Their Neuroprotective Activity in PC12 Cells.ChemMedChem,7(9),1661-1668.
MLA Luo J.,et al."Synthesis of Stable Genipin Derivatives and Studies of Their Neuroprotective Activity in PC12 Cells".ChemMedChem 7.9(2012):1661-1668.
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