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中建西部建设网站,邢台市教育考试院,中国第一营销网,企业域名怎么查找Liraglutide#xff08;利拉鲁肽#xff0c;AbMole#xff0c;M45167#xff09;是一种长效的人源化GLP-1类似物#xff0c;通过激活GLP-1受体#xff08;GLP-1R#xff09;#xff0c;调节cAMP-PKA路径影响代谢#xff0c;如激活AMPK信号以改善能量代谢和抑制细胞凋亡…Liraglutide利拉鲁肽AbMoleM45167是一种长效的人源化GLP-1类似物通过激活GLP-1受体GLP-1R调节cAMP-PKA路径影响代谢如激活AMPK信号以改善能量代谢和抑制细胞凋亡。在细胞实验中LiraglutideCAS No.204656-20-2在SH-SY5Y人神经母细胞瘤细胞10-100nM中减轻β-淀粉样蛋白引起的毒性并逆转胰岛素抵抗[1]Liraglutide在MC3T3-E1小鼠成骨细胞100 nM中促进成骨分化和增加碱性磷酸酶活性[2]在HepG2人肝癌细胞以1-1000 nM的浓度进行实验抑制细胞增殖和诱导G1/S期停滞[3]。Liraglutide利拉鲁肽还能抑制βTC-6小鼠β细胞由血清剥夺诱导的细胞凋亡。Liraglutide还是研究动物代谢的重要工具。Liraglutide能用于C57BL/6J小鼠肥胖模型1mg/kg剂量并改善高脂饮食诱导的代谢紊乱以及调节肠道菌群[4]Liraglutide还在大鼠糖尿病模型Alloxan 或StreptozotocinSTZ诱导减轻了体重和改善血糖控制[5-7]。Liraglutide还能在Sprague Dawley大鼠心肌梗死模型改善心脏功能和减少心肌纤维化[8]。并且Liraglutide在Sprague Dawley大鼠肌肉萎缩模型200μg/kg/day皮下注射中成功激活cAMP信号抑制萎缩[9]。Liraglutide还具有一定的抗纤维化活性在大鼠肺纤维化模型Bleomycin 诱导中成功减少了胶原表达[10]。参考文献及鸣谢[1] Jantrapirom, S.; Nimlamool, W.; Chattipakorn, N.; et al. Liraglutide Suppresses Tau Hyperphosphorylation, Amyloid Beta Accumulation through Regulating Neuronal Insulin Signaling and BACE-1 Activity. International journal of molecular sciences2020, 21 (5).[2] Sun, Y.; Liang, Y.; Li, Z.; et al. Liraglutide Promotes Osteoblastic Differentiation in MC3T3-E1 Cells by ERK5 Pathway. International journal of endocrinology2020, 2020, 8821077.[3] Kapodistria, K.; Tsilibary, E. P.; Kotsopoulou, E.; et al. Liraglutide, a human glucagon-like peptide-1 analogue, stimulates AKT-dependent survival signalling and inhibits pancreatic beta-cell apoptosis. Journal of cellular and molecular medicine2018, 22 (6), 2970-2980.[4] Zhao, L.; Chen, Y.; Xia, F.; et al. A Glucagon-Like Peptide-1 Receptor Agonist Lowers Weight by Modulating the Structure of Gut Microbiota. Frontiers in endocrinology2018, 9, 233.[5] Mathieu, C.; Zinman, B.; Hemmingsson, J. U.; et al. Efficacy and Safety of Liraglutide Added to Insulin Treatment in Type 1 Diabetes: The ADJUNCT ONE Treat-To-Target Randomized Trial. Diabetes care2016, 39 (10), 1702-1710.[6] Cai, H.; Zhou, L.; Liu, J.; et al. Independent and combined effects of liraglutide and aerobic interval training on glycemic control and cardiac protection in diabetic cardiomyopathy rats. Biochemical and biophysical research communications2022, 629, 112-120.[7] Zhao, X. Y.; Yu, T. T.; Liu, S.; et al. Effect of liraglutide on endoplasmic reticulum stress in the renal tissue of type 2 diabetic rats. World journal of diabetes2020, 11 (12), 611-621.[8] Huang, D. D.; Huang, H. F.; Yang, Q.; et al. Liraglutide improves myocardial fibrosis after myocardial infarction through inhibition of CTGF by activating cAMP in mice. European review for medical and pharmacological sciences2018, 22 (14), 4648-4656.[9] Gurjar, A. A.; Kushwaha, S.; Chattopadhyay, S.; et al. Long acting GLP-1 analog liraglutide ameliorates skeletal muscle atrophy in rodents. Metabolism: clinical and experimental2020, 103, 154044.[10] Yang, X.; Ma, X.; Don, O.; et al. Mesenchymal stem cells combined with liraglutide relieve acute lung injury through apoptotic signaling restrained by PKA/beta-catenin. Stem cell research therapy2020, 11 (1), 182.