Abstract
Curcumin bioconjugates, with folic acid, fatty acids and dipeptide, have shown much lower MIC than curcumin against clinically isolated Gram-positive, S.viridians, and Gram-negative bacterial strains, E. coli, P. mirabilis and K. pneumoniae. Polynomial regression analysis was performed to establish a correlation between lipophilicity (logP) and antibacterial activity (pMIC), which showed the efficacy of these molecules against the bacterial strains in the following order: E. coli > S viridans = K. pneumoniae > P. mirabilis. The regression coefficients (R2 = 0.62 to 0.91) derived for each strain were correlated significantly and led to a conclusion that it was the amphiphilic nature that governed the antibacterial activity. Thus, the bioconjugate 2, having folic acid attached at active methylene site of curcumin with free phenolic hydroxyls, showed the best result.
Keywords: Curcumin bioconjugates, logP, MIC, MBC, regression coefficient.
Medicinal Chemistry
Title:Curcumin Bioconjugates: Studies on Structure-Activity Relationship and Antibacterial Properties against Clinically Isolated Strains
Volume: 9 Issue: 7
Author(s): Diwakar Rai, Garima Kumari, Anuradha Singh and Ramendra K. Singh
Affiliation:
Keywords: Curcumin bioconjugates, logP, MIC, MBC, regression coefficient.
Abstract: Curcumin bioconjugates, with folic acid, fatty acids and dipeptide, have shown much lower MIC than curcumin against clinically isolated Gram-positive, S.viridians, and Gram-negative bacterial strains, E. coli, P. mirabilis and K. pneumoniae. Polynomial regression analysis was performed to establish a correlation between lipophilicity (logP) and antibacterial activity (pMIC), which showed the efficacy of these molecules against the bacterial strains in the following order: E. coli > S viridans = K. pneumoniae > P. mirabilis. The regression coefficients (R2 = 0.62 to 0.91) derived for each strain were correlated significantly and led to a conclusion that it was the amphiphilic nature that governed the antibacterial activity. Thus, the bioconjugate 2, having folic acid attached at active methylene site of curcumin with free phenolic hydroxyls, showed the best result.
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Cite this article as:
Rai Diwakar, Kumari Garima, Singh Anuradha and Singh K. Ramendra, Curcumin Bioconjugates: Studies on Structure-Activity Relationship and Antibacterial Properties against Clinically Isolated Strains, Medicinal Chemistry 2013; 9 (7) . https://dx.doi.org/10.2174/1573406411309070014
DOI https://dx.doi.org/10.2174/1573406411309070014 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
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