Key Specialty of Clinical Pharmacy, The First Affiliated Hospital of Guangdong Pharmaceutical University, Guangzhou, People's Republic of China.
School of Pharmacy & Clinical Pharmacy (School of Integrative Pharmacy), Guangdong Pharmaceutical University, Guangzhou, People's Republic of China.
Medicine (Baltimore). 2023 Sep 8;102(36):e34671. doi: 10.1097/MD.0000000000034671.
Research has demonstrated that obesity is an important risk factor for cancer progression. Orlistat is a lipase inhibitor with promising therapeutic effects on obesity. In addition to being regarded as a slimming drug, a growing number of studies in recent years have suggested that orlistat has anti-tumor activities, while the underlying mechanism is still not well elucidated. This paper reviewed recent pharmacological effects and mechanisms of orlistat against tumors and found that orlistat can target cancer cells through activation or suppression of multiple signaling pathways. It can induce tumor cells apoptosis or death, interfere with tumor cells' cycles controlling, suppress fatty acid synthase activity, increase ferroptosis, inhibit tumor angiogenesis, and improve tumor cells glycolytic. Thus, this review may shed new light on anti-tumor mechanism and drug repurposing of orlistat, and anti-tumor drug development.
研究表明，肥胖是癌症进展的一个重要危险因素。奥利司他是一种脂肪酶抑制剂，对肥胖症具有有前景的治疗效果。除了被视为减肥药外，近年来越来越多的研究表明，奥利司他具有抗肿瘤活性，但其潜在机制尚不清楚。本文综述了近年来奥利司他抗肿瘤的药理学作用及机制，发现奥利司他可通过激活或抑制多条信号通路靶向作用于肿瘤细胞，诱导肿瘤细胞凋亡或死亡，干扰肿瘤细胞周期调控，抑制脂肪酸合酶活性，增加铁死亡，抑制肿瘤血管生成，改善肿瘤细胞糖酵解。因此，该综述可能为奥利司他的抗肿瘤机制和药物再利用以及抗肿瘤药物的开发提供新的思路。
