Department of Medicinal Chemistry, Pharmacy School, Jinzhou Medical University, Jinzhou, 121001, People's Republic of China.
Department of Pharmaceutical Administration, Pharmacy School, Jinzhou Medical University, Jinzhou, 121001, People's Republic of China.
Neurochem Res. 2020 Jul;45(7):1500-1509. doi: 10.1007/s11064-020-03012-3. Epub 2020 Mar 13.
The growing number of evidences suggest that neuroinflammation and synaptic damage are closely related to the onset of depression. Bexarotene (Bex), a retinoid X receptor agonist, is an U.S. Food and Drug Administration-approved drug for the treatment of cutaneous T-cell lymphoma that has recently been reported to have anti-inflammatory and neuroprotective effects in several models of neurological disease including Parkinson's disease, Alzheimer's disease, and so forth. However, the effect of Bex on depression remains unclear. In this study, we investigated effect of Bex on depression-like behaviour in mice induced by lipopolysaccharide (LPS) or corticosterone (CORT). Our results showed that treatment with Bex for 15 days significantly improved LPS-induced depression-like behaviour in social interaction test and CORT-induced depression-like behaviour in forced swimming test and tail suspension test in mice. We found that the Bex treatment depressed the increase in the number of activated microglia and astrocytes in the frontal cortex, and the increase in the levels of inflammatory cytokines TNF-α, IL-1β and IL-6 in LPS-injected mice. Furthermore, Bex treatment also rescued the decrease in the expression of BDNF, and inhibition of CREB/BDNF/ERK pathway, and improved the expression of synaptic related protein in CORT-induced mice. Based on these results, it is possible that Bex reversed depression-like behaviour in mice by reducing neuroinflammation and protecting against synaptic damage induced by LPS or CORT.
越来越多的证据表明,神经炎症和突触损伤与抑郁症的发病密切相关。倍他罗汀(Bex)是一种视黄醇 X 受体激动剂,已被美国食品和药物管理局批准用于治疗皮肤 T 细胞淋巴瘤,最近有报道称其在几种神经疾病模型中具有抗炎和神经保护作用,包括帕金森病、阿尔茨海默病等。然而,Bex 对抑郁症的影响尚不清楚。在这项研究中,我们研究了 Bex 对脂多糖(LPS)或皮质酮(CORT)诱导的小鼠抑郁样行为的影响。我们的结果表明,Bex 治疗 15 天可显著改善 LPS 诱导的社会互动测试中的抑郁样行为和 CORT 诱导的强迫游泳测试和悬尾测试中的抑郁样行为。我们发现 Bex 治疗可抑制 LPS 注射小鼠前额皮质中活化小胶质细胞和星形胶质细胞数量的增加,以及炎症细胞因子 TNF-α、IL-1β 和 IL-6 水平的升高。此外,Bex 治疗还可挽救 CORT 诱导的小鼠 BDNF 表达的下降,以及 CREB/BDNF/ERK 通路的抑制,并改善突触相关蛋白的表达。基于这些结果,Bex 可能通过减轻 LPS 或 CORT 诱导的神经炎症和保护突触损伤来逆转小鼠的抑郁样行为。