通过使用蛋白质学方法使用 Osthole 反应性代谢物对蛋白质进行共价修饰
Yue Zhuo1, Huiling Chen1, Chenchen Liu1
1Science and Technology Innovation Center, Guangzhou University of Chinese Medicine, Guangzhou, China.
Current drug metabolism
|July 31, 2023
概括
洞 (OST) 被代谢成修改蛋白质的活性物种,揭示了对其药理作用的新见解. 这项研究确定了16个修饰蛋白点,对OST至关重要.
科学领域:
- 药理学 药理学是指药理学的学科.
- 代谢学 代谢学 代谢学
- 蛋白质组学是指蛋白质组学.
背景情况:
- 奥斯托尔 (OST),是一种来自Cnidium monnieri的天然素,表现出多样化的生物活性.
- OST的α,β-不和乳经历了对活性代谢物 (RMs) 的代谢.
- RMs可以共同修改蛋白质氨基酸残留物,这是一个在OST中未被充分探索的机制.
研究的目的:
- 为了阐明奥斯特霍尔 (OST) 的代谢概况.
- 为了研究由OST代谢产物诱导的蛋白质修饰模式.
主要方法:
- 使用UHPLC-Q-TOF-MS.进行OST代谢物的定性鉴定.
- 用大鼠肝脏显微体 (RLM) 和模型氨基酸确认反应性代谢物 (RM) 修饰模式和氨基酸标.
- 通过纳米LC-Orbitrap-MS和蛋白质发现器识别RM修饰的蛋白质.
主要成果:
- 在RLMs中,在1小时内观察到OST的快速代谢.
- 检测了10种OST代谢物,以及包括N-乙囊 (NAC),N-乙 lysine (NAL) 和谷氨 (GSH) 在内的各种添加物.
- 确定16个RM修饰蛋白点,参与OST的抗阿尔茨海默病 (AD) 和抗瘤活动.
结论:
- 为OST的药理作用提供了一个新的分子机制.
- 识别了OST治疗应用的潜在蛋白质标.
- 强调了自然产品 (NP) 的代谢物-蛋白相互作用的重要性.
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