School of Pharmaceutical Science, Yunnan Key Laboratory of Pharmacology for Natural Products, NHC Key Laboratory of Drug Addiction Medicine, Kunming Medical University, Kunming, 650500, PR China.
School of Pharmaceutical Science, Yunnan Key Laboratory of Pharmacology for Natural Products, NHC Key Laboratory of Drug Addiction Medicine, Kunming Medical University, Kunming, 650500, PR China; The First People's Hospital of Liangshan Yi Autonomous Prefecture, XiChang, Sichuan Province, 615000, PR China.
Neuropharmacology. 2025 Feb 1;263:110226. doi: 10.1016/j.neuropharm.2024.110226. Epub 2024 Nov 16.
This study aimed to investigate the effect of 20(R)-ginsenoside Rg3 on autophagy induced by cerebral ischemia‒reperfusion injury (CIRI) in rats and explore its regulation of the PI3K/Akt signaling pathway.
Middle cerebral artery occlusion/reperfusion (MCAO/R) in male rats was injected intraperitoneally with 20(R)-ginsenoside Rg3 (5, 10, 20 mg/kg) 12 h before modeling, 2 h after ischemia and 12 h after reperfusion. Neurobehavioral and neuronal morphological changes were detected 24 h after brain I/R. In vitro, the OGD/R-induced injury model is replicated in PC12 cells and different concentrations of 20(R)-ginsenoside Rg3 are administered to observe its effects on cell viability and autophagy and PI3K/Akt/mTOR-related protein expression.
Our findings suggest that treatment with 20 mg/kg 20(R)-ginsenoside Rg3 significantly attenuated the neuronal injury, as evidenced by a decreased number of damaged neurons, reduced dissolution of Nissl corpuscles, a fewer autophagosomes, and downregulated expression of Beclin1 and LC3-II/I compared with the MCAO/R group. Furthermore, 20(R)-ginsenoside Rg3 treatment significantly upregulated the expression of p62, p-PI3K, p-AKT, and p-mTOR. In vitro, 20(R)-ginsenoside Rg3 significantly improved the survival rate of cells following OGD/R and markedly attenuated the LY294002 and OGD/R-induced upregulation of Beclin1 and LC3 gene expression. Moreover, 20(R)-ginsenoside Rg3 could rescued the LY294002 and OGD/R-induced downregulation of p62, p-PI3K, p-AKT, and p-mTOR expression.
20(R)-ginsenoside Rg3 attenuates neuronal injury and motor dysfunction following ischemia-reperfusion by inhibiting the activation of autophagy, and its mechanism is related to the upregulation of the PI3K/Akt/mTOR signaling pathway.
本研究旨在探讨 20(R)-人参皂苷 Rg3 对大鼠脑缺血再灌注损伤(CIRI)诱导的自噬的影响,并探讨其对 PI3K/Akt 信号通路的调节作用。
雄性大鼠大脑中动脉闭塞/再灌注(MCAO/R)模型,于建模前 12 h 腹腔注射 20(R)-人参皂苷 Rg3(5、10、20 mg/kg),再灌注后 2 h 和 12 h 各注射 1 次。脑 I/R 后 24 h 检测神经行为学和神经元形态变化。体外采用 PC12 细胞建立 OGD/R 诱导损伤模型,给予不同浓度的 20(R)-人参皂苷 Rg3 观察其对细胞活力和自噬及 PI3K/Akt/mTOR 相关蛋白表达的影响。
结果表明,20(R)-人参皂苷 Rg3(20 mg/kg)治疗可显著减轻神经元损伤,与 MCAO/R 组相比,损伤神经元数量减少,尼氏小体溶解减少,自噬体减少,Beclin1 和 LC3-II/I 表达下调。此外,20(R)-人参皂苷 Rg3 治疗可显著上调 p62、p-PI3K、p-AKT 和 p-mTOR 的表达。体外,20(R)-人参皂苷 Rg3 显著提高 OGD/R 后细胞存活率,并显著降低 LY294002 和 OGD/R 诱导的 Beclin1 和 LC3 基因表达上调。此外,20(R)-人参皂苷 Rg3 可挽救 LY294002 和 OGD/R 诱导的 p62、p-PI3K、p-AKT 和 p-mTOR 表达下调。
20(R)-人参皂苷 Rg3 通过抑制自噬的激活来减轻缺血再灌注后的神经元损伤和运动功能障碍,其机制与上调 PI3K/Akt/mTOR 信号通路有关。