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异黄酮的治疗潜力专利研究综述(2012-2016 年)

A patent review of the therapeutic potential of isoflavones (2012-2016).

机构信息

a UoN Chair of Oman's Medicinal Plants and Marine Natural Products , University of Nizwa , Nizwa , Sultanate of Oman.

b Center for Marine Biotechnology and Biomedicine, Scripps Institution of Oceanography , University of California , San Diego , CA , USA.

出版信息

Expert Opin Ther Pat. 2017 Oct;27(10):1135-1146. doi: 10.1080/13543776.2017.1339791. Epub 2017 Jun 13.

Abstract

Isoflavones are well-studied natural products isolated from natural sources with interesting chemodiversity and possess a wide variety of biological effects. Moreover, chemical modifications based on the isoflavone scaffold, has generated synthetic chemodiversity to enhance the bioactivities of isoflavones. Areas covered: The current review summarizes the discovery of new chemotherapeutic agents possessing the isoflavone skeleton. This review incorporates patents filed between 2012 and 2016 mostly related to anticancer, antidiabetic, antimicrobial, anti-HIV, anti-gastric ulcer, anti-gastritis, antiparasitic and some other biological effects demonstrated by isoflavone analogs. Expert opinion: The number of interesting patents published during the five year period (2012-2016) on the therapeutic potential of isoflavones indicated the importance of this molecule. Natural isoflavones possess potent anticancer, anti-HIV and antidiabetic activities and chemical analogs of natural isoflavones increase the abovementioned biological effects. Additionally isoflavones have only been tested for a limited number of biological activities and thus future research should focus on additional biological activities viz., anti-inflammatory, antimalarial, and anti-leishmanial effects. However, the absence of SAR studies and in vivo data restricted the rational design of more potent isoflavone analogs and we believe that in order to get lead compounds, there needs to be a greater focus on SAR and in vivo studies.

摘要

异黄酮是从天然来源中分离出来的研究充分的天然产物,具有有趣的化学多样性,并具有广泛的生物活性。此外,基于异黄酮支架的化学修饰,产生了合成的化学多样性,以增强异黄酮的生物活性。

涵盖领域

本综述总结了具有异黄酮骨架的新化疗药物的发现。本综述纳入了 2012 年至 2016 年间申请的专利,主要涉及抗癌、抗糖尿病、抗菌、抗 HIV、抗胃溃疡、胃炎、抗寄生虫和一些其他由异黄酮类似物表现出的生物活性。

专家意见

在 2012-2016 年五年期间发表的关于异黄酮治疗潜力的有趣专利数量表明了该分子的重要性。天然异黄酮具有很强的抗癌、抗 HIV 和抗糖尿病活性,天然异黄酮的化学类似物增加了上述生物活性。此外,异黄酮仅经过有限数量的生物活性测试,因此未来的研究应集中在其他生物活性上,如抗炎、抗疟和抗利什曼原虫作用。然而,缺乏 SAR 研究和体内数据限制了更有效的异黄酮类似物的合理设计,我们认为,为了获得先导化合物,需要更加关注 SAR 和体内研究。

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