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查耳酮的药理特性:临床前研究综述,包括分子机制和临床证据

Pharmacological Properties of Chalcones: A Review of Preclinical Including Molecular Mechanisms and Clinical Evidence.

作者信息

Salehi Bahare, Quispe Cristina, Chamkhi Imane, El Omari Nasreddine, Balahbib Abdelaali, Sharifi-Rad Javad, Bouyahya Abdelhakim, Akram Muhammad, Iqbal Mehwish, Docea Anca Oana, Caruntu Constantin, Leyva-Gómez Gerardo, Dey Abhijit, Martorell Miquel, Calina Daniela, López Víctor, Les Francisco

机构信息

Medical Ethics and Law Research Center, Shahid Beheshti University of Medical Sciences, Tehran, Iran.

Facultad de Ciencias de La Salud, Universidad Arturo Prat, Iquique, Chile.

出版信息

Front Pharmacol. 2021 Jan 18;11:592654. doi: 10.3389/fphar.2020.592654. eCollection 2020.

Abstract

Chalcones are among the leading bioactive flavonoids with a therapeutic potential implicated to an array of bioactivities investigated by a series of preclinical and clinical studies. In this article, different scientific databases were searched to retrieve studies depicting the biological activities of chalcones and their derivatives. This review comprehensively describes preclinical studies on chalcones and their derivatives describing their immense significance as antidiabetic, anticancer, anti-inflammatory, antimicrobial, antioxidant, antiparasitic, psychoactive, and neuroprotective agents. Besides, clinical trials revealed their use in the treatment of chronic venous insufficiency, skin conditions, and cancer. Bioavailability studies on chalcones and derivatives indicate possible hindrance and improvement in relation to its nutraceutical and pharmaceutical applications. Multifaceted and complex underlying mechanisms of chalcone actions demonstrated their ability to modulate a number of cancer cell lines, to inhibit a number of pathological microorganisms and parasites, and to control a number of signaling molecules and cascades related to disease modification. Clinical studies on chalcones revealed general absence of adverse effects besides reducing the clinical signs and symptoms with decent bioavailability. Further studies are needed to elucidate their structure activity, toxicity concerns, cellular basis of mode of action, and interactions with other molecules.

摘要

查耳酮是主要的生物活性黄酮类化合物之一,一系列临床前和临床研究对其多种生物活性进行了调查,显示出它具有治疗潜力。在本文中,我们检索了不同的科学数据库,以获取描述查耳酮及其衍生物生物活性的研究。这篇综述全面描述了关于查耳酮及其衍生物的临床前研究,阐述了它们作为抗糖尿病、抗癌、抗炎、抗菌、抗氧化、抗寄生虫、精神活性和神经保护剂的重大意义。此外,临床试验表明它们可用于治疗慢性静脉功能不全、皮肤病和癌症。对查耳酮及其衍生物的生物利用度研究表明,在其营养保健和药物应用方面可能存在阻碍和改进之处。查耳酮作用的多方面和复杂潜在机制表明,它们有能力调节多种癌细胞系,抑制多种致病微生物和寄生虫,并控制许多与疾病改善相关的信号分子和信号级联。关于查耳酮的临床研究表明,除了能以良好的生物利用度减轻临床体征和症状外,通常没有不良反应。还需要进一步研究来阐明它们的构效关系、毒性问题、作用方式的细胞基础以及与其他分子的相互作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cc94/7849684/2eafdce07cbe/fphar-11-592654-g001.jpg

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