Drug Research Laboratory, Department of Pharmaceutical Sciences, Dr. Hari Singh Gour Central University, Sagar (MP)-470003, India.
Curr Med Chem. 2012;19(2):209-25. doi: 10.2174/092986712803414132.
Chalcones (1,3-diaryl-2-propen-1-ones) and their heterocyclic analogues, belong to the flavonoid family, which possess a number of interesting biological properties such as antioxidant, cytotoxic, anticancer, antimicrobial, antiprotozoal, antiulcer, antihistaminic and anti-inflammatory activities. Several pure chalcones have been approved for clinical use or tested in humans. Clinical trials have shown that these compounds reached reasonable plasma concentration and are well-tolerated. For this reason they are an object of continuously growing interest amongst the scientists. However, much of the pharmacological potential of chalcones is still not utilized. The purpose of this review is to provide an overview of the pharmacological activity of naturally occurring and synthetic chalcones. This review highlights more recent pharmacological screening of these compounds, their mechanisms of action and relevant structure-activity relationships.
查耳酮(1,3-二芳基-2-丙烯-1-酮)及其杂环类似物属于黄酮类家族,具有许多有趣的生物特性,如抗氧化、细胞毒性、抗癌、抗菌、抗寄生虫、抗溃疡、抗组胺和抗炎活性。一些纯查耳酮已被批准用于临床使用或在人体中进行测试。临床试验表明,这些化合物达到了合理的血浆浓度,并且耐受性良好。因此,它们是科学家们持续关注的对象。然而,查耳酮的许多药理学潜力尚未得到利用。本综述的目的是提供对天然和合成查耳酮的药理学活性的概述。本综述重点介绍了这些化合物最近的药理学筛选、它们的作用机制以及相关的结构-活性关系。