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Practical Synthesis and Biological Evaluation of Bergenin Analogs

Title
Practical Synthesis and Biological Evaluation of Bergenin Analogs
Authors
Jung J.-C.Lim E.Kim S.H.Kim N.S.Jung M.Oh S.
Ewha Authors
오세관정재철
SCOPUS Author ID
오세관scopus
Issue Date
2011
Journal Title
Chemical Biology and Drug Design
ISSN
1747-0277JCR Link
Citation
vol. 78, no. 4, pp. 725 - 729
Indexed
SCI; SCIE; SCOPUS WOS scopus
Abstract
Here, we describe the practical synthesis and biological properties of bergenin and its structural analogs. Synthetic bergenin compounds were prepared by acylation of bergenin. These compounds were then evaluated for suppression of lipopolysaccharide-induced nitric oxide (NO) generation in cultured cells and anti-narcotic effects on morphine-dependent mice. We found that bergenin derivatives showed potent anti-inflammatory activity (suppression of NO generation) at concentrations ranging from 20 to 30μmin vitro, and bergenin derivatives (10-20mg/kg) exhibited significant anti-narcotic effects on morphine dependence in mice. These results suggest the potential utility of bergenin and its analogs as anti-narcotic agents and the design of more potent anti-inflammatory compounds. We have demonstrated simple and practical synthesis and evaluation of bergenin derivatives. It was found that the bergenin derivatives showed potent anti-inflammatory (suppressor of NO generation) with the concentration range 20-30μmin vitro, and bergenin derivatives (10-20mg/kg) exhibited significant anti-narcotic effect on morphine dependence in mice. © 2011 John Wiley & Sons A/S.
DOI
10.1111/j.1747-0285.2011.01194.x
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의학전문대학원 > 의학과 > Journal papers
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