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Study On Structural Modification And Anti-inflammatory Activity Of Genipin

Posted on:2024-07-02Degree:MasterType:Thesis
Country:ChinaCandidate:L HeFull Text:PDF
GTID:2531307178451364Subject:Medicinal chemistry
Abstract/Summary:PDF Full Text Request
Objective(s):This study aims to modify the structure of genipin and obtain a series of genipin derivatives,so as to study the anti-inflammatory activity of genipin derivatives in order to find compounds with low toxicity and good anti-inflammatory activity.Methods:This study aims to synthesize genipin derivatives within C-10 esters,amines,and pyridinium and C-1 alkylation group through structural modification.The IC50 value and EC50 value of Genipin derivatives on RAW264.7 cells were calculated,and the therapeutic index was obtained by calculating the ratio of the IC50 value and EC50 value of the NO production value,so as to obtain the anti-inflammatory activity of genipin derivatives.Results:A total of 59 genipin derivatives were synthesized and their structures were confirmed by ESI-MS,1H-NMR and 13C-NMR.22 derivatives with good anti-inflammatory activity were obtained.Conclusion(s):Among the 22 compounds with anti-inflammatory activity,most of them were esters and amine genipin derivatives.Among the amine derivatives,alkyl amine derivatives containing allyl segments have good activity.Among the ester derivatives,the C-3-substituted benzoate is better than the C-2-substituted and C-4-substituted products.This study provides a theoretical basis for subsequent studies on the anti-inflammatory activity of genipin.
Keywords/Search Tags:Genipin, Structural transformation, Anti-inflammatory activity
PDF Full Text Request
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