کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1356205 981096 2011 10 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
In vitro and QSAR studies of cucurbitacins on HepG2 and HSC-T6 liver cell lines
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
In vitro and QSAR studies of cucurbitacins on HepG2 and HSC-T6 liver cell lines
چکیده انگلیسی

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 CCl4 (EC50 = 2.4–45.3 μM) with good margin to toxicity (T/A). All Cucs exhibited anti-proliferative effect on serum-activated rat stellate cells, HSC-T6 (EC50 = 0.02–4.12 μM) 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.

Cucurbitacin analogues with potential anticancer activity and hepatoprotective agents against fibrosis that deserve further examination.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 19, Issue 8, 15 April 2011, Pages 2757–2766
نویسندگان
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