Document Detail

In vitro and QSAR studies of cucurbitacins on HepG2 and HSC-T6 liver cell lines.
MedLine Citation:
PMID:  21459003     Owner:  NLM     Status:  Publisher    
The aim of this study was to evaluate cucurbitacins (Cucs) liver protective activity in vitro and conduct QSAR studies against lipophilicity and ab initio descriptors. Nine Cucs were isolated from Cucurbitaceae plants and eight prepared by C2-alkylation or C16-acylation. Ten Cucs demonstrated protective activity on human hepatocyte-derived HepG2 cells exposed to CCl(4) (EC(50)=2.4-45.3μM) with good margin to toxicity (T/A). All Cucs exhibited anti-proliferative effect on serum-activated rat stellate cells, HSC-T6 (EC(50)=0.02-4.12μM) with high T/A. While silybin is nontoxic, its protection is lower compared to Cuc D (3), iso-D (4), I (5), B (11), E (12), I-Me (6), L-Me (7), and E-Me (13) on both cell lines. Strong correlations were found for lipophilicity with both protection and toxicity on HepG2. Lipophilicity correlated only with toxicity on HSC-T6. Consequently, we suggest that Cucs are potential hepatoprotective agents against fibrosis that deserve further examination.
Judit Bartalis; Fathi T Halaweish
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2011-2-2
Journal Detail:
Title:  Bioorganic & medicinal chemistry     Volume:  -     ISSN:  1464-3391     ISO Abbreviation:  -     Publication Date:  2011 Feb 
Date Detail:
Created Date:  2011-4-4     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9413298     Medline TA:  Bioorg Med Chem     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Copyright Information:
Published by Elsevier Ltd.
Department of Chemistry & Biochemistry, SDSU, Shepard Hall 121, Box 2202 Brookings, SD 57007, USA.
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