Department of Pharmacology, School of Medicine, Pusan National University, Yangsan 50612, Gyeongnam, Republic of Korea.
College of Pharmacy, Kyungpook National University, 80 Daehak-ro, Buk-gu, Daegu 41566, Gyeongbuk, Republic of Korea.
Int J Mol Sci. 2023 Oct 18;24(20):15288. doi: 10.3390/ijms242015288.
In individuals with Alzheimer's disease, the brain exhibits elevated levels of IL-1β and oxygenated cholesterol molecules (oxysterols). This study aimed to investigate the effects of side-chain oxysterols on IL-1β expression using HMC3 microglial cells and ApoE-deficient mice. Treatment of HMC3 cells with 25-hydroxycholesterol (25OHChol) and 27-hydroxycholesterol (27OHChol) led to increased IL-1β expression at the transcript and protein levels. Additionally, these oxysterols upregulated the surface expression of MHC II, a marker of activated microglia. Immunohistochemistry performed on the mice showed increased microglial expression of IL-1β and MHC II when fed a high-cholesterol diet. However, cholesterol and 24s-hydroxycholesterol did not increase IL-1β transcript levels or MHC II expression. The extent of IL-1β increase induced by 25OHChol and 27OHChol was comparable to that caused by oligomeric β-amyloid, and the IL-1β expression induced by the oxysterols was not impaired by polymyxin B, which inhibited lipopolysaccharide-induced IL-1β expression. Both oxysterols enhanced the phosphorylation of Akt, ERK, and Src, and inhibition of these kinase pathways with pharmacological inhibitors suppressed the expression of IL-1β and MHC II. The pharmacological agents chlorpromazine and cyclosporin A also impaired the oxysterol-induced expression of IL-1β and upregulation of MHC II. Overall, these findings suggest that dysregulated cholesterol metabolism leading to elevated levels of side-chain oxysterols, such as 25OHChol and 27OHChol, can activate microglia to secrete IL-1β through a mechanism amenable to pharmacologic intervention. The activation of microglia and subsequent neuroinflammation elicited by the immune oxysterols can contribute to the development of neurodegenerative diseases.
在阿尔茨海默病患者中,大脑表现出升高的白细胞介素 1β(IL-1β)和氧化胆固醇分子(oxysterols)水平。本研究旨在使用 HMC3 小胶质细胞和载脂蛋白 E 缺陷型小鼠来研究侧链 oxysterols 对 IL-1β 表达的影响。用 25-羟胆固醇(25OHChol)和 27-羟胆固醇(27OHChol)处理 HMC3 细胞导致 IL-1β 的转录和蛋白水平增加。此外,这些 oxysterols 上调了 MHC II 的表面表达,MHC II 是激活的小胶质细胞的标志物。对给予高胆固醇饮食的小鼠进行免疫组织化学分析显示,IL-1β 和 MHC II 的小胶质细胞表达增加。然而,胆固醇和 24s-羟胆固醇并未增加 IL-1β 转录水平或 MHC II 表达。25OHChol 和 27OHChol 诱导的 IL-1β 增加的程度与寡聚β-淀粉样蛋白引起的程度相当,并且 oxysterols 诱导的 IL-1β 表达不受多粘菌素 B 的损害,多粘菌素 B 抑制脂多糖诱导的 IL-1β 表达。两种 oxysterols 均增强 Akt、ERK 和 Src 的磷酸化,并且用药理学抑制剂抑制这些激酶途径可抑制 IL-1β 和 MHC II 的表达。药理学试剂氯丙嗪和环孢菌素 A 也损害了 oxysterol 诱导的 IL-1β 表达和 MHC II 的上调。总的来说,这些发现表明,导致侧链 oxysterols(如 25OHChol 和 27OHChol)水平升高的胆固醇代谢失调可通过易于药理学干预的机制激活小胶质细胞以分泌 IL-1β。免疫 oxysterols 激活小胶质细胞并随后引发神经炎症可能有助于神经退行性疾病的发展。