Merck

In vitro and QSAR studies of cucurbitacins on HepG2 and HSC-T6 liver cell lines.

Bioorganic & medicinal chemistry (2011-04-05)
Judit Bartalis, Fathi T Halaweish
RESUMEN

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)=2.4-45.3 μM) with good margin to toxicity (T/A). All Cucs exhibited anti-proliferative effect on serum-activated rat stellate cells, HSC-T6 (EC(50)=0.02-4.12 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.

MATERIALES
Referencia del producto
Marca
Descripción del producto

Supelco
L-Ascorbic acid, analytical standard
Sigma-Aldrich
L-Ascorbic acid, FCC, FG
Sigma-Aldrich
L-Ascorbic acid, ACS reagent, ≥99%
Sigma-Aldrich
L-Ascorbic acid, puriss. p.a., ACS reagent, reag. ISO, Ph. Eur., 99.7-100.5% (oxidimetric)
Sigma-Aldrich
L-Ascorbic acid, BioUltra, ≥99.5% (RT)
Sigma-Aldrich
L-Ascorbic acid, tested according to Ph. Eur.
Sigma-Aldrich
L-Ascorbic acid, puriss. p.a., ≥99.0% (RT)
Sigma-Aldrich
L-Ascorbic acid, BioXtra, ≥99.0%, crystalline
Sigma-Aldrich
L-Ascorbic acid, reagent grade, crystalline
Sigma-Aldrich
L-Ascorbic acid, meets USP testing specifications
Sigma-Aldrich
L-Ascorbic acid, reagent grade
Sigma-Aldrich
L-Ascorbic acid, suitable for plant cell culture
Sigma-Aldrich
L-Ascorbic acid, suitable for cell culture, suitable for plant cell culture, ≥98%
Sigma-Aldrich
L-Ascorbic acid, powder, suitable for cell culture, γ-irradiated
Sigma-Aldrich
Phenylbutazone
Sigma-Aldrich
L-Ascorbic acid, 99%