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3,4',5-反式-三甲氧基芪;一种具有增强抗癌效力的白藜芦醇天然类似物。

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

作者信息

Aldawsari Fahad S, Velázquez-Martínez Carlos A

机构信息

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

出版信息

Invest New Drugs. 2015 Jun;33(3):775-86. doi: 10.1007/s10637-015-0222-x. Epub 2015 Feb 28.

Abstract

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.

摘要

白藜芦醇是许多植物物种产生的一种植保素,作为一种防御机制。在过去十年中,据报道这种多酚对与慢性疾病相关的多个靶点具有活性。然而,其较差的药代动力学特性,以及与其体外和体内特性相关的多重差异,不仅导致了对合适给药系统的研究,还导致了白藜芦醇衍生物的使用。在这方面,白藜芦醇的天然类似物3,4',5-反式三甲氧基芪(TMS)已成为一个有力的候选者。与白藜芦醇相比,TMS具有更强的抗癌特性,表现出比白藜芦醇更高的效力,正如多篇报道所述,它能改善癌细胞增殖抑制、诱导细胞周期停滞、减少转移、降低血管生成并增加细胞凋亡。在这篇综述中,我们简要总结了文献中报道的关于白藜芦醇和TMS异同的结果,并向科学界提出,TMS是一种有前景且(仍)未被充分研究的天然候选药物,在癌症研究中具有潜在应用。然而,基于现有证据,我们也向科学界提出,TMS在任何其他使用白藜芦醇的研究领域中可能也会有一席之地。

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