Suh Sang Bum, Lee Nayoung, Kim Jaedeok, Kim Saeha, Jang Sooyeon, Park Jong Kook, Lee Keunwook, Choi Soo Young, Kwon Hyung-Joo, Lee Chan Hee
University of Ulsan College of Medicine, Seoul, South Korea.
Department of Biomedical Science, Hallym University, Chuncheon, South Korea.
Front Pharmacol. 2022 Oct 12;13:906717. doi: 10.3389/fphar.2022.906717. eCollection 2022.
Olanzapine (OLZ), a widely used second-generation antipsychotic drug, is known to cause metabolic side effects, including diabetes and obesity. Interestingly, OLZ-induced metabolic side effects have been demonstrated to be more profound in females in human studies and animal models. Metformin (MET) is often used as a medication for the metabolic side effects of OLZ. However, the mechanisms underlying OLZ-induced metabolic disturbances and their treatment remain unclear. Recent evidence has suggested that hypothalamic inflammation is a key component of the pathophysiology of metabolic disorders. On this background, we conducted this study with the following three objectives: 1) to investigate whether OLZ can independently induce hypothalamic microgliosis; 2) to examine whether there are sex-dependent differences in OLZ-induced hypothalamic microgliosis; and 3) to examine whether MET affects hypothalamic microgliosis. We found that administration of OLZ for 5 days induced systemic glucose intolerance and hypothalamic microgliosis and inflammation. Of note, both hypothalamic microglial activation and systemic glucose intolerance were far more evident in female mice than in male mice. The administration of MET attenuated hypothalamic microglial activation and prevented OLZ-induced systemic glucose intolerance and hypothalamic leptin resistance. Minocycline, a tetracycline derivative that prevents microgliosis, showed similar results when centrally injected. Our findings reveal that OLZ induces metabolic disorders by causing hypothalamic inflammation and that this inflammation is alleviated by MET administration.
奥氮平(OLZ)是一种广泛使用的第二代抗精神病药物,已知会引起代谢副作用,包括糖尿病和肥胖。有趣的是,在人体研究和动物模型中,OLZ诱导的代谢副作用在女性中表现得更为明显。二甲双胍(MET)常被用于治疗OLZ的代谢副作用。然而,OLZ诱导代谢紊乱的机制及其治疗方法仍不清楚。最近的证据表明,下丘脑炎症是代谢紊乱病理生理学的关键组成部分。在此背景下,我们开展了本研究,旨在实现以下三个目标:1)研究OLZ是否能独立诱导下丘脑小胶质细胞增生;2)检查OLZ诱导的下丘脑小胶质细胞增生是否存在性别差异;3)研究MET是否影响下丘脑小胶质细胞增生。我们发现,连续5天给予OLZ会导致全身葡萄糖不耐受以及下丘脑小胶质细胞增生和炎症。值得注意的是,下丘脑小胶质细胞激活和全身葡萄糖不耐受在雌性小鼠中比在雄性小鼠中更为明显。给予MET可减轻下丘脑小胶质细胞激活,并预防OLZ诱导的全身葡萄糖不耐受和下丘脑瘦素抵抗。米诺环素是一种可预防小胶质细胞增生的四环素衍生物,经中枢注射后也显示出类似结果。我们的研究结果表明,OLZ通过引起下丘脑炎症诱导代谢紊乱,而给予MET可减轻这种炎症。