Document Detail

Contribution of Cage-Shaped Structure of Physalins to Their Mode of Action in Inhibition of NF-κB Activation.
MedLine Citation:
PMID:  24900739     Owner:  NLM     Status:  PubMed-not-MEDLINE    
A library of oxygenated natural steroids, including physalins, withanolides, and perulactones, coupled with the synthetic cage-shaped right-side structure of type B physalins, was constructed. SAR studies for inhibition of NF-κB activation showed the importance of both the B-ring and the oxygenated right-side partial structure. The 5β,6β-epoxy derivatives of both physalins and withanolides showed similar profiles of inhibition of NF-κB activation and appeared to act on NF-κB signaling via inhibition of phosphorylation and degradation of IκBα. In contrast, type B physalins with C5-C6 olefin functionality inhibited nuclear translocation and DNA binding of RelA/p50 protein dimer, which lie downstream of IκBα degradation, although withanolides having the same AB-ring functionality did not. These results indicated that the right-side partial structure of these steroids influences their mode of action.
Masaaki Ozawa; Masaki Morita; Go Hirai; Satoru Tamura; Masao Kawai; Ayako Tsuchiya; Kana Oonuma; Keiji Maruoka; Mikiko Sodeoka
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Publication Detail:
Type:  Journal Article     Date:  2013-06-06
Journal Detail:
Title:  ACS medicinal chemistry letters     Volume:  4     ISSN:  1948-5875     ISO Abbreviation:  ACS Med Chem Lett     Publication Date:  2013 Aug 
Date Detail:
Created Date:  2014-06-05     Completed Date:  2014-06-05     Revised Date:  2014-08-08    
Medline Journal Info:
Nlm Unique ID:  101521073     Medline TA:  ACS Med Chem Lett     Country:  United States    
Other Details:
Languages:  eng     Pagination:  730-5     Citation Subset:  -    
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