尤德斯曼 (Eudesmane) 六烯酸具有抑制作用,可以抑制Artemisia princeps中NO的产生
Hong-Xia Li1, Ning Diao2, Ya-Jie Hu2
1Guangxi Key Laboratory of Drug Discovery and Optimization, Guangxi Engineering Research Center for Pharmaceutical Molecular Screening and Druggability Evaluation, Key Laboratory of Medical Biotechnology and Translational Medicine, School of Pharmacy, Guilin Medical University, Guilin 541199, Guangxi, People's Republic of China.
Phytochemistry
|January 28, 2024
概括
研究人员从Artemisia princeps.中分离出了新的eudesmane化合物. 许多人对微质细胞中氧化 (NO) 生产产生显著的抑制作用,表明治疗潜力.
科学领域:
- 自然产品化学 自然产品化学
- 药理学 药理学是指药理学的学科.
- 药用化学 医学化学
背景情况:
- 阿尔特米西亚王子是一种具有传统药用历史的植物.
- 炎症,特别是微质细胞的炎症,与各种神经系统疾病有关.
- 尤德斯曼 (Eudesmane sesquiterpenoids) 是一类具有多种生物活动的自然产品.
研究的目的:
- 从Artemisia princeps.中分离和描述新的化学成分.
- 评估这些化合物对BV-2微质细胞中脂聚糖 (LPS) 诱导的氧化 (NO) 生产的抑制作用.
- 为了探索抗炎性质的潜在结构-活性关系 (SAR).
主要方法:
- 使用色谱技术分离化合物.
- 使用核磁共振 (NMR) 谱学和高分辨率电喷射电离化质谱学 (HRESIMS) 阐明结构.
- 通过单晶X射线衍射和电子循环二元化 (ECD) 计算来确定绝对配置.
- 在LPS刺激的BV-2微质细胞中进行NO抑制的体外生物试验.
主要成果:
- 确定了5种新的eudesmane甲基 (1-5) 和3种新的eudesmane-12,6-olides (6-8),以及21种已知的类似物.
- 化合物1-9,12-29对LPS诱导的NO生产表现出显著的抑制活性.
- IC50值在0.73至18.66μM之间,表明大多数隔离物具有强烈的抗炎作用.
结论:
- 阿尔特梅西亚王子是一种丰富的结构多样化的eudesmane sesquiterpenoids的来源.
- 一些孤立的化合物,特别是新型化合物,通过抑制微质细胞中NO的产生,表现出显著的抗炎活性.
- 这些发现突出了Artemisia princeps衍生化合物的潜力,作为治疗炎症病的治疗剂.
相关概念视频
01:28Nitric Oxide Signaling Pathway
5.0K
Nitric oxide (NO), an inorganic gas, acts as a potent second messenger in most animal and plant tissues. NO diffuses out of the cells that produce it and enters the neighboring cells to generate a downstream response. NO synthase (NOS) catalyzes NO production by the deamination of the amino acid arginine. There are three isoforms of NOS. Endothelial cells have endothelial NOS (eNOS), nerve and muscle cells have neuronal NOS (nNOS), and macrophages produce inducible NOS (iNOS) upon exposure...
5.0K
01:23Antihypertensive Drugs: Vasodilators
525
Vasodilators, primarily affecting the smooth muscles within arterial and venous walls, are commonly used for hypertension treatment. Medications such as minoxidil and hydralazine primarily target arteries and arterioles, while sodium nitroprusside acts on arterioles and venules. Minoxidil, functioning as a prodrug, is metabolized by hepatic sulfotransferase into its active form, minoxidil sulfate, after oral administration. This metabolite binds to the sulfonylurea receptor (SUR) component of...
525
01:16Antianginal Drugs: Nitrates and β-Blockers
592
In cardiovascular health, antianginal drugs combat angina pectoris — a condition marked by chest pain owing to diminished blood flow to the heart.
Organic nitrates, such as nitroglycerin, play a pivotal role. Once metabolized, they liberate nitric oxide, a molecular marvel. Nitric oxide triggers guanylyl cyclase and augments cGMP production. This biochemical cascade orchestrates the relaxation of vascular smooth muscles, ushering in vasodilation and enhancing coronary blood flow....
Organic nitrates, such as nitroglycerin, play a pivotal role. Once metabolized, they liberate nitric oxide, a molecular marvel. Nitric oxide triggers guanylyl cyclase and augments cGMP production. This biochemical cascade orchestrates the relaxation of vascular smooth muscles, ushering in vasodilation and enhancing coronary blood flow....
592
01:28Treatment for Pulmonary Arterial Hypertension: Phosphodiesterase Inhibitors
158
Phosphodiesterase 5 (PDE5) inhibitors are potent enzymes that function to hydrolyze cyclic nucleotides to their corresponding 5' monophosphates. Their unique biochemical properties have been applied in treating Pulmonary Arterial Hypertension (PAH).
Among the PDE5 inhibitors, sildenafil (Revatio) stands out as a competitive and selective inhibitor. It operates by elevating cellular levels of cGMP and augmenting signaling through the cGMP-PKG pathway, promoting vasodilation. Upon oral...
Among the PDE5 inhibitors, sildenafil (Revatio) stands out as a competitive and selective inhibitor. It operates by elevating cellular levels of cGMP and augmenting signaling through the cGMP-PKG pathway, promoting vasodilation. Upon oral...
158
01:18Treatment for Pulmonary Arterial Hypertension: Endothelin Receptor Antagonists
165
Endothelins (ETs) are potent vasoactive peptides critical in the human body's various physiological and pathological processes. One of the most promising therapeutic strategies for treating pulmonary arterial hypertension (PAH) involves counteracting the effects of these endothelins using a class of drugs known as endothelin receptor antagonists.
ETs are synthesized through a complex sequence of enzymatic steps, primarily involving an enzyme referred to as endothelin-converting enzyme...
ETs are synthesized through a complex sequence of enzymatic steps, primarily involving an enzyme referred to as endothelin-converting enzyme...
165
01:28Adrenergic Agonists: Mixed-Action Agents
716
Mixed-action adrenergic agonists, like ephedrine and pseudoephedrine, directly and indirectly affect adrenergic receptors. These agents stimulate adrenoceptors and indirectly release stored neurotransmitters, amplifying the adrenergic response.
Ephedrine and pseudoephedrine lack a catecholamine group, making them less susceptible to degradation by metabolic enzymes. They have increased oral bioavailability and lipophilicity, resulting in a longer duration of action. Their response is reduced by...
Ephedrine and pseudoephedrine lack a catecholamine group, making them less susceptible to degradation by metabolic enzymes. They have increased oral bioavailability and lipophilicity, resulting in a longer duration of action. Their response is reduced by...
716