Department of Breast and Thyroid Surgery, Renmin Hospital of Wuhan University, Wuhan 430060, China.
Department of Clinical Laboratory, Renmin Hospital of Wuhan University, Wuhan 430060, China.
Biomolecules. 2021 Jun 16;11(6):894. doi: 10.3390/biom11060894.
Chalcones (1,3-diaryl-2-propen-1-ones) are precursors for flavonoids and isoflavonoids, which are common simple chemical scaffolds found in many naturally occurring compounds. Many chalcone derivatives were also prepared due to their convenient synthesis. Chalcones as weandhetic analogues have attracted much interest due to their broad biological activities with clinical potentials against various diseases, particularly for antitumor activity. The chalcone family has demonstrated potential in vitro and in vivo activity against cancers via multiple mechanisms, including cell cycle disruption, autophagy regulation, apoptosis induction, and immunomodulatory and inflammatory mediators. It represents a promising strategy to develop chalcones as novel anticancer agents. In addition, the combination of chalcones and other therapies is expected to be an effective way to improve anticancer therapeutic efficacy. However, despite the encouraging results for their response to cancers observed in clinical studies, a full description of toxicity is required for their clinical use as safe drugs for the treatment of cancer. In this review, we will summarize the recent advances of the chalcone family as potential anticancer agents and the mechanisms of action. Besides, future applications and scope of the chalcone family toward the treatment and prevention of cancer are brought out.
查耳酮(1,3-二芳基-2-丙烯-1-酮)是类黄酮和异黄酮的前体,是许多天然存在的化合物中常见的简单化学支架。由于其合成方便,许多查尔酮衍生物也被制备出来。由于其广泛的生物活性和对各种疾病的临床潜力,特别是抗肿瘤活性,作为合成类似物的查尔酮引起了人们的极大兴趣。查尔酮家族通过多种机制,包括细胞周期破坏、自噬调节、细胞凋亡诱导以及免疫调节和炎症介质,在体外和体内对癌症表现出潜在的活性。将查尔酮开发为新型抗癌药物是一种很有前途的策略。此外,查尔酮与其他疗法的联合有望成为提高抗癌治疗效果的有效方法。然而,尽管在临床研究中观察到它们对癌症的反应令人鼓舞,但为了将它们作为治疗癌症的安全药物安全使用,还需要对其毒性进行全面描述。在这篇综述中,我们将总结查尔酮家族作为潜在抗癌药物的最新进展及其作用机制。此外,还提出了查尔酮家族在癌症治疗和预防方面的未来应用和前景。