Trends in Utilization of the Pharmacological Potential of Chalcones
Trends in Utilization of the Pharmacological Potential of Chalcones
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DOI：
10.2174/157488410790410579
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发表时间：
2010-01-01
影响因子：
3.2
通讯作者：
Todorova, Iva Todorova
中科院分区：
文献类型：
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作者：
Batovska, Daniela Ilieva;Todorova, Iva Todorova
查耳酮（1，3-二芳基-2-丙烯-1-酮）是一种广泛存在于植物中的开链类黄酮。它们对花的着色很重要，因此对传粉者起引诱作用。作为黄酮类化合物，查耳酮在防御病原体和昆虫方面也起着重要作用。长期的科学研究表明，查尔酮还显示出其他有趣的生物学性质，如抗氧化剂，细胞毒性，抗癌，抗菌，抗原虫，抗溃疡，抗组胺和抗炎活性。以查尔酮为骨架的先导化合物具有多种药理活性。临床试验表明，这些化合物达到合理的血浆浓度，不会引起毒性。由于这些原因，查耳酮成为学术界和工业界持续关注的对象。如今，几种查耳酮用于治疗病毒性疾病、心血管疾病、寄生虫感染、疼痛、胃炎和胃癌，以及类似的食品添加剂和化妆品配方成分。然而，查尔酮的药理活性还没有得到充分的利用，本文综述了近年来查尔酮的药理活性筛选、作用机制和构效关系的研究进展。总之，这些活动旨在合成具有生物活性的查耳酮及其类似物。
Chalcones (1,3-diaryl-2-propen-1-ones) are open chain flavonoids that are widely biosynthesized in plants. They are important for the pigmentation of flowers and, hence, act as attractants to the pollinators. As flavonoids, chalcones also play an important role in defense against pathogens and insects. A longstanding scientific research has shown that chalcones also display other interesting biological properties such as antioxidant, cytotoxic, anticancer, antimicrobial, antiprotozoal, antiulcer, antihistaminic and anti-inflammatory activities. Some lead compounds with various pharmacological properties have been developed based on the chalcone skeleton. Clinical trials have shown that these compounds reached reasonable plasma concentrations and did not cause toxicity. For these reasons, chalcones became an object of continued interest in both academia and industry. Nowadays, several chalcones are used for treatment of viral disorders, cardiovascular diseases, parasitic infections, pain, gastritis, and stomach cancer, as well as like food additives and cosmetic formulation ingredients. However, much of the pharmacological potential of chalcones is still not utilized.The purpose of this review is to describe the recent efforts of scientists in pharmacological screening of natural and synthetic chalcones, studying the mechanisms of chalcone action and relevant structure-activity relationships. Put together, these activities aimed at synthesis of pharmacologically active chalcones and their analogs.