Department of Clinical Pharmacy, Faculty of Pharmacy, Al-Azhar University, Assiut Branch, Assiut 71524, Egypt.
Department of Pharmacology, Faculty of Medicine, Assiut University, Assiut, Egypt.
Int Immunopharmacol. 2024 Oct 25;140:112904. doi: 10.1016/j.intimp.2024.112904. Epub 2024 Aug 7.
One of the best antipsychotics for treating schizophrenia and bipolar disorders is olanzapine (OLA). However, its use is restricted owing to unfavorable adverse effects as liver damage, dyslipidemia, and weight gain. The primary objective of the present investigation was to examine the signaling mechanisms that underlie the metabolic disruption generated by OLA. Besides, the potential protective effect of sulforaphane (SFN) and β-sitosterol (βSS) against obesity and metabolic toxicity induced by OLA were inspected as well. A total of five groups of male Wistar rats were established, including the control, OLA, SFN+OLA, βSS+OLA, and the combination + OLA groups. Hepatic histopathology, biochemical analyses, ultimate body weights, liver function, oxidative stress, and pro-inflammatory cytokines were evaluated. In addition to the relative expression of FOXO, the signaling pathways for PI3K/AKT, JAK/STAT3, and MAPK were assessed as well. All biochemical and hepatic histopathological abnormalities caused by OLA were alleviated by SFN and/or βSS. A substantial decrease in systolic blood pressure (SBP), proinflammatory cytokines, serum lipid profile parameters, hepatic MDA, TBIL, AST, and ALT were reduced through SFN or/and βSS. To sum up, the detrimental effects of OLA are mediated by alterations in the Akt/FOXO3a/ATG12, Ras/SOS2/Raf-1/MEK/ERK1/2, and Smad3,4/TGF-β signaling pathways. The administration of SFN and/or βSS has the potential to mitigate the metabolic deficit, biochemical imbalances, hepatic histological abnormalities, and the overall unfavorable consequences induced by OLA by modulating the abovementioned signaling pathways.
奥氮平(OLA)是治疗精神分裂症和双相情感障碍的最佳抗精神病药之一。然而,由于其会导致肝损伤、血脂异常和体重增加等不良副作用,其应用受到限制。本研究的主要目的是研究导致 OLA 代谢紊乱的信号转导机制。此外,还研究了萝卜硫素(SFN)和β-谷甾醇(βSS)对 OLA 引起的肥胖和代谢毒性的潜在保护作用。共建立了五组雄性 Wistar 大鼠,包括对照组、OLA 组、SFN+OLA 组、βSS+OLA 组和联合+OLA 组。评估了肝组织病理学、生化分析、最终体重、肝功能、氧化应激和促炎细胞因子。除了 FOXO 的相对表达外,还评估了 PI3K/AKT、JAK/STAT3 和 MAPK 信号通路。SFN 和/或 βSS 减轻了 OLA 引起的所有生化和肝组织病理学异常。SFN 或/和 βSS 降低了收缩压(SBP)、促炎细胞因子、血清脂质谱参数、肝 MDA、TBIL、AST 和 ALT。总之,OLA 的有害作用是通过改变 Akt/FOXO3a/ATG12、Ras/SOS2/Raf-1/MEK/ERK1/2 和 Smad3,4/TGF-β信号通路来介导的。SFN 和/或 βSS 的给药通过调节上述信号通路,有可能减轻 OLA 引起的代谢缺陷、生化失衡、肝组织学异常和整体不良后果。