Department of Neurology, Hubei Provincial Hospital of Integrated Chinese and Western Medicine, Wuhan, China.
Pharmacol Res Perspect. 2022 Oct;10(5):e01001. doi: 10.1002/prp2.1001.
While there is a growing interest in the use of statins, HMG-CoA reductase inhibitors, to treat neurodegenerative diseases, statins are associated with conflicting effects within the central nervous system (CNS) without clear evidence of the underlying mechanisms. This study systematically investigated effects of four statins (atorvastatin, pitavastatin, cerivastatin, and lovastatin) on neuronal cells under pathological condition using an in vitro model depicting ischemic injury, as well as tested under physiological condition. All four statins at micromolar concentrations display toxic effects on neuron cells under physiological condition. Atorvastatin and cerivastatin but not pitavastatin or lovastatin at nanomolar concentrations display protective effects on neuron cells under ischemic injury condition, via decreased ischemic injury-induced oxidative stress, oxidative damage, and inflammation. Mechanistically, atorvastatin, pitavastatin, and lovastatin induces neuron cell apoptosis via prenylation-independent manner. Other mechanisms are involved in the pro-apoptotic effect of cerivastatin. Prenylation is not involved in the protective effects of statins under ischemic injury condition. Our work provides better understanding on the multiple differential effects of statins on neuron cells under physiological condition and ischemic injury, and elucidate their underlying mechanisms, which may be of relevance to the influence of statins in CNS.
尽管人们对使用他汀类药物(HMG-CoA 还原酶抑制剂)治疗神经退行性疾病越来越感兴趣,但他汀类药物在中枢神经系统(CNS)中具有相互矛盾的作用,而其潜在机制尚不清楚。本研究使用体外模型描述缺血性损伤,系统地研究了四种他汀类药物(阿托伐他汀、匹伐他汀、西立伐他汀和洛伐他汀)在病理条件下对神经元细胞的影响,并在生理条件下进行了测试。在生理条件下,四种他汀类药物在微摩尔浓度下均对神经元细胞表现出毒性作用。阿托伐他汀和西立伐他汀,但不是匹伐他汀或洛伐他汀,在纳米摩尔浓度下对缺血性损伤条件下的神经元细胞具有保护作用,通过降低缺血性损伤诱导的氧化应激、氧化损伤和炎症。在机制上,阿托伐他汀、匹伐他汀和洛伐他汀通过非依赖于异戊烯化的方式诱导神经元细胞凋亡。西立伐他汀的促凋亡作用涉及其他机制。在缺血性损伤条件下,异戊烯化不参与他汀类药物的保护作用。我们的工作更好地理解了他汀类药物在生理条件和缺血性损伤下对神经元细胞的多种不同作用,并阐明了其潜在机制,这可能与他汀类药物对中枢神经系统的影响有关。