Gu Jia, Zhu Neng, Li Hong-Fang, Zhang Chan-Juan, Gong Yong-Zhen, Liao Duan-Fang, Qin Li
Laboratory of Stem Cell Regulation With Chinese Medicine and its Application, HunanUniversity of Chinese Medicine, Changsha, China.
Department of Urology, The First Hospital of Hunan University of Chinese Medicine, Changsha, China.
Front Pharmacol. 2022 Jul 18;13:831657. doi: 10.3389/fphar.2022.831657. eCollection 2022.
The high level of serum cholesterol caused by the excessive absorption of cholesterol can lead to hypercholesteremia, thus promoting the occurrence and development of cancer. Ezetimibe is a drug that reduces cholesterol absorption and has been widely used for the treatment of patients with high circulating cholesterol levels for many years. Mechanistically, ezetimibe works by binding to NPC1L1, which is a key mediator of cholesterol absorption. Accumulating data from preclinical models have shown that ezetimibe alone could inhibit the development and progression of cancer through a variety of mechanisms, including anti-angiogenesis, stem cell suppression, anti-inflammation, immune enhancement and anti-proliferation. In the past decade, there has been heated discussion on whether ezetimibe combined with statins will increase the risk of cancer. At present, more and more evidence shows that ezetimibe does not increase the risk of cancers, which supports the role of ezetimibe in anti-cancer. In this review, we discussed the latest progress in the anti-cancer properties of ezetimibe and elucidated its underlying molecular mechanisms. Finally, we highlighted the potential of ezetimibe as a therapeutic agent in future cancer treatment and prevention.
胆固醇吸收过多导致的高血清胆固醇水平可引发高胆固醇血症，进而促进癌症的发生和发展。依折麦布是一种降低胆固醇吸收的药物，多年来已广泛用于治疗循环胆固醇水平高的患者。从机制上讲，依折麦布通过与NPC1L1结合发挥作用，NPC1L1是胆固醇吸收的关键介质。临床前模型积累的数据表明，依折麦布单独使用可通过多种机制抑制癌症的发展和进展，包括抗血管生成、抑制干细胞、抗炎、增强免疫和抗增殖。在过去十年中，关于依折麦布与他汀类药物联合使用是否会增加癌症风险一直存在激烈讨论。目前，越来越多的证据表明依折麦布不会增加癌症风险，这支持了依折麦布在抗癌方面的作用。在这篇综述中，我们讨论了依折麦布抗癌特性的最新进展，并阐明了其潜在的分子机制。最后，我们强调了依折麦布作为未来癌症治疗和预防治疗药物的潜力。
