Subhashini Brahadeeswaran, Kiran Kumar Chitluri, Leema George, Venkatraman Manickam, Isaac Arnold Emerson, Ramasamy Tamizhselvi
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引用次数: 0
摘要
我们之前的研究证实了东莨菪碱(SC)在保护小鼠免受蓝蛋白诱导的急性胰腺炎(AP)和随后的肺损伤的有效性。然而,SC保护作用的确切分子机制尚未阐明。这个研究表明,SC减少促炎细胞因子的释放和核转录因子k B (NF -κB)通过激活过氧物酶体proliferator-activatedγ受体(PPAR -γ)在老鼠遭受美联社。我们观察SC的保护作用与男性每小时瑞士小鼠腹腔注射cerulein(50µg / kg)为6个小时,其次是管理的SC(10毫克/公斤)一小时后AP感应,有或没有PPAR -γ拮抗剂GW9662(0.3毫克/公斤)。对SC抗炎作用的研究发现,浓度为25µM的SC通过激活PPAR-γ信号通路,增强对垂死胰腺腺泡细胞的吞噬清除。相反,体外评估证实GW9662的存在抵消了SC对腺泡细胞的有益影响。分子对接和模拟研究表明,SC促进PPAR-γ的显著结构变化。体内、体外和计算机分析表明,SC具有有效的抗炎特性,这可能是由蛋白诱导的实验性胰腺炎中PPAR-γ信号的激活介导的。
Scopoletin: A Validated Protector against Cerulein-induced Acute Pancreatitis & Associated Lung Injury by Regulating PPAR- γ "A Multidimensional Approach".
Our previous study established the effectiveness of scopoletin (SC) in protecting mice against acute pancreatitis (AP) induced by cerulein and subsequent pulmonary injury. However, the precise molecular mechanisms underlying SC protective effects have yet to be elucidated. This research suggests that SC reduces the release of pro-inflammatory cytokines and nuclear factor kappa B (NF-κB) by activating the peroxisome proliferator-activated receptor γ (PPAR-γ) in mice suffering from AP. We observed the protective role of SC against the male Swiss mice with hourly intraperitoneal injections of cerulein (50 µg/kg) for six hours, followed by the administration of SC (10 mg/kg) one hour after AP induction, with or without the PPAR-γ antagonist GW9662 (0.3 mg/kg). The study exploration into the anti-inflammatory effects of SC revealed that a concentration of 25 µM enhanced the phagocytic clearance of dying pancreatic acinar cells by triggering the PPAR-γ signaling activation. Conversely, an in vitro assessment confirmed the presence of GW9662 counteracted the beneficial impact of SC on acinar cells. Molecular docking and simulation studies have shown that SC prompts significant structural changes in PPAR-γ. The in vivo, in vitro, and in silico analyses suggest that SC has potent anti-inflammatory properties that may be mediated by the activation of PPAR-γ signaling in cerulein-induced experimental pancreatitis.
期刊介绍:
Molecular Biotechnology publishes original research papers on the application of molecular biology to both basic and applied research in the field of biotechnology. Particular areas of interest include the following: stability and expression of cloned gene products, cell transformation, gene cloning systems and the production of recombinant proteins, protein purification and analysis, transgenic species, developmental biology, mutation analysis, the applications of DNA fingerprinting, RNA interference, and PCR technology, microarray technology, proteomics, mass spectrometry, bioinformatics, plant molecular biology, microbial genetics, gene probes and the diagnosis of disease, pharmaceutical and health care products, therapeutic agents, vaccines, gene targeting, gene therapy, stem cell technology and tissue engineering, antisense technology, protein engineering and enzyme technology, monoclonal antibodies, glycobiology and glycomics, and agricultural biotechnology.