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3,4′,5-trans-Trimethoxystilbene; a natural analogue of resveratrol with enhanced anticancer potency

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Summary

Resveratrol is a phytoalexin produced by many plant species as a defence mechanism. Over the last decade, this polyphenol has been reported to be active against multiple targets associated with chronic disorders. However, its poor pharmacokinetic profile, as well as multiple discrepancies related to its in vitro and in vivo profile, has resulted not only on the study of suitable delivery systems, but the use of resveratrol derivatives. In this regard, the 3,4′,5-trans-trimethoxystilbene (TMS), a natural analogue of resveratrol, has emerged as a strong candidate. TMS has an enhanced anticancer profile compared to resveratrol, exhibiting higher potency than resveratrol, as shown by multiple reports describing an improved cancer cell proliferation inhibition, induction of cell cycle arrest, decreased metastasis, reduced angiogenesis, and increased apoptosis. In this review, we provide a concise summary of results reported in the literature, related to the similarities and differences between resveratrol and TMS, and we submit to the scientific community that TMS is a promising and (still) understudied natural agent candidate, with potential applications in cancer research. Nevertheless, based on the available evidence, we also submit to the scientific community that TMS may also find a niche in any other research area in which resveratrol has been used.

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Abbreviations

AKT:

Protein kinase B

AP-1:

Activator protein 1

Bcl-2:

B-cell lymphoma 2

Bcl-XL :

B-cell lymphoma-extra large

CAT:

Catalase

CDKs:

cyclin dependent kinases

COX:

Cyclooxygenase

CYP450:

Cytochrome P450

DMBA:

7,12-dimethylbenz [a] anthracene

EGFR:

Epidermal growth factor receptor

EMT:

Epithelial mesenchymal transition

GSK:

Glycogen synthase kinase

H2O2 :

Hydrogen peroxide

HO-1:

Heme oxygenase-1

ICAM-1:

Intercellular adhesion molecule

iNOS:

Inducible nitric oxide synthase

JNK:

c-Jun N-terminal kinase

LDL:

Low density lipoproteins

LPS:

Lipopolysaccharide

MAPK:

Mitogen-activated protein kinase

MMP:

Metalloproteinase

MTA1:

Metastasis-associated protein 1

NF-κB:

Nuclear transcription factor-kappa B

PI3K:

Phosphoinositide 3-kinase

PPARγ:

Peroxisome proliferator activated receptor gamma

SOD:

Superoxide dismutase

STAT:

Signal transducer and activator of transcription

TMS:

3,4′,5-trans-trimethoxystilbene

TNF:

Tumor necrosis factor

TPA:

12-O-tetradecanoylphorbol-13-acetate

VCAM-1:

Vascular cell adhesion protein 1

VEGF:

Vascular endothelial growth factor.

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Acknowledgments

The authors gratefully acknowledge the support provided by Saudi Cultural Bureau in Canada, for a graduate scholarship to F.S.A.

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The authors report no conflict of interest.

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  1. Faculty of Pharmacy and Pharmaceutical Sciences, University of Alberta, Edmonton, AB, T6G 2E1, Canada

    Fahad S. Aldawsari & Carlos A. Velázquez-Martínez

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  1. Fahad S. Aldawsari
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  2. Carlos A. Velázquez-Martínez
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Correspondence to Fahad S. Aldawsari.

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Aldawsari, F.S., Velázquez-Martínez, C.A. 3,4′,5-trans-Trimethoxystilbene; a natural analogue of resveratrol with enhanced anticancer potency. Invest New Drugs 33, 775–786 (2015). https://doi.org/10.1007/s10637-015-0222-x

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  • DOI: https://doi.org/10.1007/s10637-015-0222-x

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