Department of Biology, Faculty of Sciences, University of Tehran, Iran.
Cardiovascular Diseases Research Center, Birjand University of Medical Sciences (BUMS), Birjand, Iran; Faculty of Pharmacy, Birjand University of Medical Sciences, Birjand, Iran.
Biomed Pharmacother. 2021 Aug;140:111782. doi: 10.1016/j.biopha.2021.111782. Epub 2021 Jun 1.
Gastrointestinal cancer is one of the most common cancers globally. Melatonin, a natural endogenous body hormone, has been of interest for years, due to its anti-cancer characteristics, such as antiproliferative, antimetastatic, and cytotoxic as well as apoptotic induction. Through regulating several proteins such as melatonin upregulated mRNAs and proteins of downregulated Bcl-2-associated X protein (Bax), and B-cell lymphoma 2 (Bcl-2), as well as cytoplasmic protein such as calcium-binding proteins calmodulin or tubulin, and nuclear receptors, including RORα/RZR, and acts by non-receptor-regulated mechanisms, melatonin can exert anti-cancer efficacy. Moreover, melatonin modulates angiogenesis by targeting mRNA and protein expression of endothelin-converting enzyme (ECE-1) protein. In the present review, we address in vivo, in vitro and clinical reports on its anti-cancer efficacies, and the molecular mechanisms of action responsible for these effects. We advance the possibility of therapeutic melatonin administration for cancer therapy.
胃肠道癌是全球最常见的癌症之一。褪黑素作为一种天然内源性的人体激素，由于其具有抗癌特性，如抗增殖、抗转移、细胞毒性和诱导细胞凋亡，多年来一直受到关注。褪黑素通过调节几种蛋白质，如褪黑素上调的 mRNA 和下调的 Bcl-2 相关 X 蛋白（Bax）和 B 细胞淋巴瘤 2（Bcl-2）的蛋白，以及细胞质蛋白，如钙结合蛋白钙调蛋白或微管蛋白，和核受体，包括 RORα/RZR，并通过非受体调节机制发挥抗癌作用。此外，褪黑素通过靶向内皮素转换酶（ECE-1）蛋白的 mRNA 和蛋白表达来调节血管生成。在本综述中，我们讨论了其抗癌功效的体内、体外和临床报告，以及负责这些效应的作用机制。我们提出了治疗性褪黑素给药治疗癌症的可能性。
