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白藜芦醇衍生物:最新专利综述(2012 - 2015年)

Resveratrol derivatives: an updated patent review (2012-2015).

作者信息

Li Chang, Xu Xiaofei, Tao Zhihao, Sun Cuirong, Pan Yuanjiang

机构信息

a Department of Chemistry , Zhejiang University , Hangzhou , P. R. China.

b College of Pharmaceutical Sciences , Zhejiang University , Hangzhou , P. R. China.

出版信息

Expert Opin Ther Pat. 2016 Oct;26(10):1189-1200. doi: 10.1080/13543776.2016.1215435. Epub 2016 Aug 4.

Abstract

Resveratrol is a well-studied natural small molecule that possesses diverse bioactivities. Chemical derivation based on the resveratrol scaffold is of great importance to overcome the drawbacks of resveratrol and to improve its therapeutic potential. Continuous efforts have been established to develop resveratrol derivatives that target different therapeutic applications. Areas covered: This review covers patents published from 2012 to 2015. All resveratrol derivatives discussed are classified based on its derivation strategy as simple derivatives, conjugated derivatives and miscellaneous derivatives. Their therapeutic related activities are reviewed and discussed. Expert opinion: Chemical derivation is an effective strategy to enhance the benefits of resveratrol and ameliorate its disadvantages. Recent studies on resveratrol derivatives have made great progress in the treatment of cancer and neurodegenerative diseases to name a few, demonstrating improved activity compared with resveratrol. Notably, its bioavailability was also improved in some cases. However, the 'next generation' of resveratrol derivatives still requires the development of new strategies and techniques.

摘要

白藜芦醇是一种经过充分研究的天然小分子,具有多种生物活性。基于白藜芦醇骨架的化学衍生对于克服白藜芦醇的缺点并提高其治疗潜力具有重要意义。人们一直在不断努力开发针对不同治疗应用的白藜芦醇衍生物。涵盖领域:本综述涵盖了2012年至2015年发表的专利。所讨论的所有白藜芦醇衍生物均根据其衍生策略分为简单衍生物、共轭衍生物和杂类衍生物。对它们与治疗相关的活性进行了综述和讨论。专家观点:化学衍生是增强白藜芦醇益处并改善其缺点的有效策略。最近关于白藜芦醇衍生物的研究在癌症和神经退行性疾病等治疗方面取得了很大进展,与白藜芦醇相比,活性有所提高。值得注意的是,在某些情况下其生物利用度也有所提高。然而,白藜芦醇衍生物的“下一代”仍需要开发新的策略和技术。

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