Euterpe oleracea 马尔. 马尔. 马尔. 马尔. 马尔. 马尔. 马尔. 生物活性分子:有前途的调节NLRP3炎症酶分子的药物
Carolina Bordin Davidson1,2, Dana El Soufi El Sabbagh3, Amanda Kolinski Machado2
1Graduate Program in Nanosciences, Franciscan University, Santa Maria 97010-030, RS, Brazil.
Biology
|September 28, 2024
概括
一些黄素,包括catechin,apigenin和epicatechin,通过有效调节NLRP3炎症酶通路,显示出作为抗炎药物的前景. 这些天然化合物显示出开发用于治疗慢性炎症疾病的新疗法的巨大潜力.
科学领域:
- 生物化学 生物化学
- 免疫学 免疫学 免疫学
- 药理学 药理学是指药理学的学科.
背景情况:
- 慢性炎症与NLRP3炎症酶有关,NLRP3是抗炎药物发现的关键标.
- 黄素具有已知的抗炎性质,但其精确的机制,特别是关于NLRP3,需要阐明.
研究的目的:
- 为了研究特定的黄类物质 (甲基素,亚基因素,甲基素) 调节NLRP3炎症酶的潜力.
- 使用计算和细胞模型探索孤立和组合的黄类药物效应.
主要方法:
- 在分析包括分子对接,分子动力学和MM / GBSA计算,以评估黄-NLRP3 PYD相互作用.
- 使用THP1细胞和巨细胞的体外研究,激活LPS+尼日里辛,用黄类药物治疗.
- 检测包括色度,度,显微镜和分子技术来测量NLRP3炎症酶活性和基因表达.
主要成果:
- 甲基素,阿皮基宁和基基因对NLRP3 PYD具有很高的结合亲和力,与抑制剂MCC950.0相当.
- 黄类药物在两种细胞类型中显著降低了LPS + 尼日里辛诱导的炎症反应.
- 随着黄类药物治疗,观察到促炎性细胞因子,caspase-1和NLRP3基因表达的显著下降.
结论:
- katekin,apigenin 和 epicatechin 是NLRP3炎症酶的有效调节剂.
- 这些黄类药物通过向NLRP3通路,代表了治疗慢性炎症疾病的潜在候选者.
相关概念视频
Inflammatory Response
1.9K
An inflammatory response is a localized, nonspecific immune reaction that occurs when a tissue is injured. It is characterized by redness, swelling, heat, and pain, which are commonly called the cardinal signs and symptoms of inflammation. Inflammation can sometimes result in a loss of function.
Inflammation can be triggered by various stimuli, such as impact, abrasion, chemical irritation, infections, and extreme hot or cold temperatures. These can damage cells and connective tissue fibers,...
Inflammation can be triggered by various stimuli, such as impact, abrasion, chemical irritation, infections, and extreme hot or cold temperatures. These can damage cells and connective tissue fibers,...
1.9K
Antiasthma Drugs: Mast Cell Stabilizers and Anti-IgE Drugs
241
Asthma is a chronic respiratory condition for which new therapeutic avenues, including anti-inflammatory drugs like mast cell stabilizers and anti-IgE treatments, continue to be developed.
Mast cell stabilizers, such as cromolyn (also known as sodium cromoglycate) and nedocromil (Tilade), are effective drugs in asthma management. These stabilizers hinder histamine release by skillfully obstructing the activation of mast cells and other cellular entities. Notably, they navigate this task without...
Mast cell stabilizers, such as cromolyn (also known as sodium cromoglycate) and nedocromil (Tilade), are effective drugs in asthma management. These stabilizers hinder histamine release by skillfully obstructing the activation of mast cells and other cellular entities. Notably, they navigate this task without...
241
Regulation of the Unfolded Protein Response
2.4K
Inositol-requiring kinase one or IRE1 is the most conserved eukaryotic unfolded protein response (UPR) receptor. It is a type I transmembrane protein kinase receptor with a distinctive site-specific RNase activity. As the binding mechanics of the misfolded proteins with the N-terminal domain of IRE-1 are unclear, three binding models — direct, indirect, and allosteric -- are proposed for receptor activation. Nevertheless, it is known that once a misfolded protein associates with IRE1, it...
2.4K
NF-κB-dependent Signaling Pathway
7.3K
The transcription factor NF-κB was discovered in 1986 in the lab of Nobel laureate Professor David Baltimore, for its interaction with the immunoglobulin light chain enhancer in B-cells. After more than three decades of study, it is now evident that NF-κB regulates the expression of over 100 genes. Most of these genes play an essential role in the innate and adaptive immune responses as well as the inflammatory responses of animals.
NF-κB-dependent Signaling Mechanism
The...
NF-κB-dependent Signaling Mechanism
The...
7.3K
The Unfolded Protein Response
4.5K
The ER is the hub of protein synthesis in a cell. It has robust systems to quality control protein folding and also for degradation of terminally misfolded proteins. Under normal conditions, a small proportion of misfolded proteins that cannot be salvaged need to be transported to the cytoplasm by the ER-associated degradation or ERAD pathways. However, if the ERAD cannot handle the misfolded proteins, the cell activates the unfolded protein response or UPR to adjust the protein folding...
4.5K
T Cell Types and Functions
959
When T cells with CD4 markers are activated, they give rise to two types of effector cells: helper T cells and regulatory T cells. Meanwhile, T cells with CD8 markers differentiate into effector cytotoxic T cells. The differentiation of CD4 T cells into helper T cell subsets, such as Th1, Th2, and Th17 cells, is dependent on the antigen type, antigen-presenting cell, and regulatory cytokines.
Th1 cells stimulate dendritic cells to express necessary co-stimulatory molecules on their surfaces for...
Th1 cells stimulate dendritic cells to express necessary co-stimulatory molecules on their surfaces for...
959


