来自Callicarpa bodinieri的具有抗炎活性的阿比坦二类药物
Yue Sun1, Hong-Ying Yang1, Pei-Zhi Huang1
1State Key Laboratory of Applied Organic Chemistry, College of Chemistry and Chemical Engineering, Lanzhou University, Lanzhou, 730000, People's Republic of China.
Phytochemistry
|August 17, 2023
概括
研究人员从Callicarpa bodinieri中分离出了9种新的和11种已知的阿比坦二特类物质. 化合物3和8通过抑制氧化生产和相关途径,显示出强大的抗炎活性.
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:
- 卡利卡拉巴 (Callicarpa bodinieri) 是一种生物活性化合物的植物来源.
- 亚比二烯酸是一种具有多种生物活性的自然产品.
- 炎症是一种复杂的生物反应,与各种疾病有关.
研究的目的:
- 从Callicarpa bodinieri中分离和表征新的和已知的阿比坦二特类物种.
- 评估这些分离化合物的抗炎潜力.
- 阐明活性化合物的作用机制.
主要方法:
- 使用色谱技术分离和净化化合物.
- 通过光谱数据 (NMR,MS) 和X射线晶体学阐明结构.
- 在体外抗炎试验中,使用脂多糖刺激的RAW 264.7巨细胞进行了抗炎试验.
- 西方涂抹用于研究分子标 (iNOS,p65/NF-κB通路).
主要成果:
- 成功分离了9种未被描述的和11种已知的阿比坦二特类物质.
- 化合物3和8显著抑制了氧化 (NO) 生产,IC50值约为36-37μM.
- 发现化合物3可以抑制诱导性氧化合成酶 (iNOS) 和p65的表达,这是NF-κB通路的关键组成部分.
结论:
- 卡利卡拉巴体内是一种具有抗炎性质的阿比二甲的宝贵来源.
- 化合物3和8是强大的抗炎药物.
- 化合物3的抗炎作用通过抑制NF-κB信号通路进行介导.
更多相关视频
相关概念视频
01:31Adrenergic Antagonists: ɑ and β-Receptor Blockers
511
Third-generation β-blockers, such as labetalol and carvedilol, represent a significant advancement in managing cardiovascular conditions. Unlike conventional β-blockers, which can induce peripheral vasoconstriction, third-generation drugs block α1 adrenoceptors. This promotes vasodilation through several mechanisms, such as increased nitric oxide production, inhibition of calcium ion entry, opening of potassium ion channels, and antioxidant action. Labetalol, for instance, is...
511
01:18Antihypertensive Drugs: Action of Calcium Channel Blockers
567
Calcium ions are essential to contract smooth muscle cells in blood vessels. They enter these cells through voltage-dependent calcium channels, specifically L-type calcium channels in the cell membrane. These L-type calcium channels are integral to the excitation-contraction coupling process in smooth muscle. When a stimulus is received by smooth muscle cells, their membrane depolarizes. This alteration in membrane potential instigates the opening of L-type calcium channels. As a result,...
567
01:27Adrenergic Antagonists: Pharmacological Actions of β-Receptor Blockers
890
β-receptor blockers significantly impact the cardiovascular system by counteracting catecholamine-induced sympathetic responses. These medications decrease heart rate, contractility, and cardiac output, potentially leading to cardiac depression, life-threatening bradycardia, and death. Therapeutically, β-blockers function as mild antihypertensives and are utilized in treating angina pectoris and cardiac arrhythmias. However, nonselective β-blockers inhibit β2-receptors in...
890
01:16Adrenergic Agonists: Chemistry and Structure-Activity Relationship
3.1K
Adrenergic agonists' structure-activity relationship (SAR) determines their selectivity and efficacy. These agonists comprise a phenylethylamine moiety with an aromatic ring and an ethylamine side chain.
Aromatic ring substitutions: Substituting the aromatic ring with –OH groups at positions 3 and 4 yields catecholamines (e.g., epinephrine), which have a high affinity for adrenoceptors. Hydrogen bonding between –OH groups and receptors enhances adrenergic activity.
Separation of...
Aromatic ring substitutions: Substituting the aromatic ring with –OH groups at positions 3 and 4 yields catecholamines (e.g., epinephrine), which have a high affinity for adrenoceptors. Hydrogen bonding between –OH groups and receptors enhances adrenergic activity.
Separation of...
3.1K
01:29Drugs for Treatment of Crohn's Disease in IBD Using Immunomodulatory Agents
195
Crohn's disease is an inflammatory bowel disorder marked by chronic inflammation of the GI tract. Various treatment strategies for Crohn's disease are employed, such as immunomodulatory agents, glucocorticoids, and biologics or anti-TNF therapy. Azathioprine (Imuran), a commonly used immunomodulatory drug for Crohn's disease, is converted in the body to mercaptopurine, which inhibits purine biosynthesis and cell proliferation. Both are utilized in severe cases of Inflammatory Bowel...
195
01:22Adrenergic Antagonists: Pharmacological Actions of ɑ-Receptor Blockers
887
α-Adrenergic antagonists, known as α-blockers, exert their effects by inhibiting α-adrenoceptors, leading to specific physiological actions. α1-blockers and α2-blockers have distinct pharmacological actions and therapeutic applications.
α1-blockers: These drugs inhibit α1-adrenoceptors on smooth muscle cells, resulting in vasodilation. This vasodilation lowers blood pressure, making α1-blockers valuable in treating hypertension. Additionally,...
α1-blockers: These drugs inhibit α1-adrenoceptors on smooth muscle cells, resulting in vasodilation. This vasodilation lowers blood pressure, making α1-blockers valuable in treating hypertension. Additionally,...
887