发现Coixol衍生物作为强大的抗炎剂
Enjing Cui1, Shihu Qian1, Jiaming Li1,2,3
1College of Pharmacy, Anhui University of Chinese Medicine, Hefei 230012, China.
新的醇衍生物,特别是那些具有和酸结构 (9c和9j化合物) 的衍生物,显示出显著的抗炎功能. 这些化合物有效地减少了细胞和动物模型中的炎症标志物,这表明未来药物开发的前景.
科学领域:
- 自然产品化学 自然产品化学
- 药用化学 医学化学
- 药理学 药理学是指药理学的学科.
背景情况:
- 科伊克斯 (Coix) 的2-扎索林衍生物科伊克斯 (Coixol) 具有抗炎性,细胞毒性较低.
- 开发新的抗炎药物对于管理炎症性疾病至关重要.
研究的目的:
- 设计和合成与肉酸混合的新型醇衍生物.
- 评估这些新化合物的抗炎潜力.
- 识别化合物以进一步开发为抗炎药物.
主要方法:
- 合成26种醇衍生物.
- 在RAW264.7巨细胞中使用脂聚糖 (LPS) 诱导的氧化 (NO) 生产来选抗炎活性.
- 机理学研究涉及诱导性氧化合成酶 (iNOS),瘤亡因子-α (TNF-α),互白素-6 (IL-6),IL-1β和核因子-kappa B (NF-κB) 信号通路的分析.
- 在体内评估,使用烯诱导的小鼠耳朵 edem 模型.
主要成果:
- 化合物9c (furan部分) 和9j (nitrofuran部分) 与coixol和celecoxib相比表现出更高的抗炎活性.
- 化合物9c和9j显著抑制了iNOS,TNF-α,IL-6和IL-1β的表达.
- 观察到NF-κB信号通路的抑制.
- 在体内研究证实了9c和9j在小鼠模型中的抗炎作用.
结论:
- 醇衍生物,特别是9c和9j,具有显著的抗炎活性.
- 这些化合物有效调节关键的炎症中介和通路.
- 化合物9c和9j显示出开发新型抗炎疗法的潜力.
更多相关视频
08:53Investigating the Alleviating Effects of Bacillus cereus Administration on Colitis through Gut Microbiota Modulation
Published on: July 27, 2022
07:36Analysis of Raw and Processed Cyperi Rhizoma Samples Using Liquid Chromatography-Tandem Mass Spectrometry in Rats with Primary Dysmenorrhea
Published on: December 23, 2022
相关概念视频
Antiasthma Drugs: Leukotriene Modifiers
Leukotriene modifiers work through two distinct mechanisms:
Antiasthma Drugs: Methylxanthines
Theophylline is thought to inhibit phosphodiesterase enzymes, increasing intracellular levels of cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP). This rise in cAMP and cGMP concentrations stimulates cardiac function,...
Antiasthma Drugs: Mast Cell Stabilizers and Anti-IgE Drugs
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...
Drugs for Treatment of Crohn's Disease in IBD Using Immunomodulatory Agents
Local Anesthetics: Chemistry and Structure-Activity Relationship
Drugs for Peptic Ulcer Disease: Prostaglandin Analogs as Mucosal Protective Agents
Non-steroidal anti-inflammatory drugs (NSAIDs) can induce peptic ulcers by inhibiting cyclooxygenase, decreasing...
