Sferrazza Gianluca, Corti Marco, Brusotti Gloria, Pierimarchi Pasquale, Temporini Caterina, Serafino Annalucia, Calleri Enrica
Institute of Translational Pharmacology, National Research Council of Italy, Rome 03018, Italy.
Department of Drug Sciences, University of Pavia, Pavia 27100, Italy.
Acta Pharm Sin B. 2020 Oct;10(10):1814-1834. doi: 10.1016/j.apsb.2019.12.019. Epub 2020 Jan 7.
The Wnt/-catenin signaling is a conserved pathway that has a crucial role in embryonic and adult life. Dysregulation of the Wnt/-catenin pathway has been associated with diseases including cancer, and components of the signaling have been proposed as innovative therapeutic targets, mainly for cancer therapy. The attention of the worldwide researchers paid to this issue is increasing, also in view of the therapeutic potential of these agents in diseases, such as Parkinson's disease (PD), for which no cure is existing today. Much evidence indicates that abnormal Wnt/-catenin signaling is involved in tumor immunology and the targeting of Wnt/-catenin pathway has been also proposed as an attractive strategy to potentiate cancer immunotherapy. During the last decade, several products, including naturally occurring dietary agents as well as a wide variety of products from plant sources, including curcumin, quercetin, berberin, and ginsenosides, have been identified as potent modulators of the Wnt/-catenin signaling and have gained interest as promising candidates for the development of chemopreventive or therapeutic drugs for cancer. In this review we make an overview of the nature-derived compounds reported to have antitumor activity by modulating the Wnt/-catenin signaling, also focusing on extraction methods, chemical features, and bio-activity assays used for the screening of these compounds.
Wnt/β-连环蛋白信号通路是一条保守的信号通路,在胚胎期和成年期均发挥关键作用。Wnt/β-连环蛋白信号通路失调与包括癌症在内的多种疾病相关,该信号通路的组成成分已被提议作为创新的治疗靶点,主要用于癌症治疗。鉴于这些药物在帕金森病(PD)等目前尚无治愈方法的疾病中的治疗潜力,全球研究人员对这一问题的关注也在不断增加。大量证据表明,异常的Wnt/β-连环蛋白信号通路与肿瘤免疫学有关,靶向Wnt/β-连环蛋白信号通路也被认为是增强癌症免疫治疗的一种有吸引力的策略。在过去十年中,包括天然膳食剂以及多种植物来源的产品(如姜黄素、槲皮素、小檗碱和人参皂苷)在内的几种产品已被确定为Wnt/β-连环蛋白信号通路的有效调节剂,并作为癌症化学预防或治疗药物开发的有前景候选物而受到关注。在本综述中,我们概述了据报道通过调节Wnt/β-连环蛋白信号通路具有抗肿瘤活性的天然来源化合物,同时重点介绍了用于筛选这些化合物的提取方法、化学特征和生物活性测定。