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. 2008 May 30;13(4):553–569. doi: 10.2478/s11658-008-0022-9

In Vitro evaluation of the cytotoxic and anti-proliferative properties of resveratrol and several of its analogs

Blase Billack 1,✉, Vijayalaxmi Radkar 1, Christelle Adiabouah 1
PMCID: PMC6275965  PMID: 18516504

Abstract

Resveratrol (RES), a component of red wine, possesses anti-inflammatory properties. The studies described in the present work were aimed at evaluating the potential for RES and related stilbene analogs (piceatannol, PIC; pterostilbene, TPS; trans-stilbene, TS; and trans-stilbene oxide, TSO) to exhibit toxicity towards RAW 264.7 mouse macrophages. The effect of TS, TSO, RES and TPS on RAW 264.7 macrophage viability was determined by two standard methods: (a) the MTT assay and (b) the trypan blue dye exclusion test. Whereas macrophages were more sensitive to PIC (LC50 trypan ∼ 1.3 μM) and to TPS (LC50 trypan ∼ 4.0 μM and LC50 MTT ∼ 8.3 μM) than to RES (LC50 trypan ∼ 8.9 μM and LC50 MTT ∼ 29.0 μM), they were relatively resistant to TSO (LC50 trypan ∼ 61.0 μM and LC50 MTT > 100 μM) and to TS (LC50 trypan ≥ 5.0 μM and LC50 MTT ≥ 5.0 μM). The ability of selected stilbenes (RES, TPS and PIC) to exhibit growth inhibitory effects was also examined. Although RES and TPS were observed to inhibit cell proliferation in macrophages (IC50 ≤ 25 μM), these cells were resistant to growth inhibition by PIC (IC50 ≥ 50 μM). The data obtained in the present analysis demonstrate that substituted stilbene compounds such as RES have the capacity to exhibit cytotoxic and anti-proliferative activities in macrophages.

Key words: Resveratrol, Piceatannol, Pterostilbene, Stilbenes, Cell viability, Cell proliferation, Macrophages, TLR4 (−/−), Antioxidants

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Abbreviations used

MTT

3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide

PIC

trans-piceatannol

RES

trans-resveratrol

TPS

trans-pterostilbene

TS

trans-stilbene

TSO

trans-stilbene oxide

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