在体内,equisetin通过与STAT3结合并抑制其活性来防止动脉样硬化
Yuting Yang1, Jingzhu Wang1, Yang Tian1
1State Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources, Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources (Ministry of Education of China), Collaborative Innovation Center for Guangxi Ethnic Medicine, School of Chemistry and Pharmaceutical Sciences, Guangxi Normal University, Guilin 541004, China.
Pharmacological research
|July 3, 2024
概括
乙素 (EQST) 通过减少炎症和脂质积累来对抗动脉样硬化. 这种来自海洋的化合物向STAT3,为这种血管疾病提供了潜在的新疗法.
科学领域:
- 药理学 药理学是指药理学的学科.
- 心血管研究研究心血管研究
- 分子生物学分子生物学
背景情况:
- 动脉样硬化是一种慢性炎症性血管疾病,由脂质代谢功能障碍和积累驱动.
- 素 (EQST),一种来自海洋海绵的半烯,表现出已知的抗菌,抗炎,降脂和减肥特性.
- 之前没有研究过EQST的抗动脉样硬化潜力.
研究的目的:
- 为了研究Equisetin (EQST) 的抗动脉样硬化活性.
- 阐明EQST对动脉样硬化的影响背后的分子机制.
- 评估EQST作为动脉样硬化的潜在治疗剂.
主要方法:
- 在体外测试评估巨细胞的炎症反应,脂质吸收和泡细胞的形成.
- 在体内研究中,使用脂蛋白E缺陷 (AopE-/-) 的小鼠食高脂肪饮食 (HFD) 来诱导动脉样硬化.
- 分子对接和生物化学测试以确定EQST与信号转换器和转录激活器3 (STAT3) 的相互作用.
主要成果:
- 在试验室中,EQST通过抑制巨细胞炎症,脂质吸收和泡细胞形成,显示出显著的抗动脉样硬化作用.
- 在体内,EQST改善了AopE-/-小鼠的高脂肪饮食引起的动脉样硬化.
- 通过疏水和键,EQST直接与STAT3结合,与蛋白质发生物理相互作用,并抑制其转录活性.
结论:
- 乙素 (EQST) 具有强大的抗动脉样硬化性质.
- EQST通过调节巨细胞反应,减少脂质积累和抑制STAT3信号来发挥其作用.
- 这些发现支持EQST作为开发新型抗动脉样硬化疗法的有希望的候选人.
相关概念视频
Lipid-Lowering Drugs: Statins and Miscellaneous Agents
628
Hyperlipidemia, a medical condition often referred to as high cholesterol, is characterized by abnormally elevated levels of lipids in the bloodstream. When present in excess, these lipids, specifically cholesterol and triglycerides, can lead to serious health complications, often involving cardiovascular diseases. Illnesses like atherosclerosis, heart attacks, and pancreatitis have all been linked to untreated hyperlipidemia. This means controlling and regulating cholesterol and triglyceride...
628
The JAK-STAT Signaling Pathway
8.8K
Several cytokine receptors have tightly bound Janus kinase or JAK proteins attached at their cytosolic tail. Small signaling molecules such as cytokines, growth hormones, or prolactins bind to the cytokine receptors and initiate their dimerization. The dimerization brings the cytosolic JAKs together that trans-phosphorylate and activates each other. The activated JAKs now phosphorylate cytosolic tails of the cytokine receptors, which serve as binding sites for adaptor proteins such as SH2...
8.8K
Intracellular Signaling Affects Focal Adhesions
2.7K
Integrins act both as extracellular input receivers and as intracellular processing activators. As their name suggests, integrins are entirely integrated into the membrane structure. Their hydrophobic membrane-spanning regions interact with the phospholipid bilayer's hydrophobic region. These membrane receptors provide extracellular attachment sites for effectors like hormones and growth factors. They activate intracellular response cascades when their effectors are bound and active.
Some...
Some...
2.7K
Cholesterol: Significance and Regulation
533
Although not a source of energy, cholesterol plays a significant role as a foundational structure for bile salts, steroid hormones, and vitamin D, as well as being a crucial component of plasma membranes. Approximately 15% of blood cholesterol is derived from our diet, with the remainder synthesized from acetyl CoA by the liver and intestines. Cholesterol is eliminated from the body through its conversion into bile salts, which are eventually discarded in the feces.
Considering cholesterol and...
Considering cholesterol and...
533


