皮肤抗炎潜力与减少新型葡萄皮质皮质类受体激动剂的副作用
Enrica Flori1, Sarah Mosca1, Daniela Kovacs1
1Laboratory of Cutaneous Physiopathology and Integrated Center of Metabolomics Research, San Gallicano Dermatological Institute, IRCCS, 00144 Rome, Italy.
International journal of molecular sciences
|January 11, 2024
概括
新型化合物DE.303和KL.202在皮肤细胞中表现出抗炎作用,而不会引起与葡萄糖皮质激素 (GCs) 相关的缩. 这些药物为治疗炎症性皮肤疾病提供了更安全的替代方案.
科学领域:
- 皮肤病学 皮肤病学
- 药理学 药理学是指药理学的学科.
- 分子生物学分子生物学
背景情况:
- 葡萄糖皮质类药物 (GCs) 是炎症性皮肤疾病的标准治疗方法.
- 局部GCs的一个显著的副作用是皮肤缩,与葡萄糖皮质体受体 (GR) 基因组途径有关.
- 开发可以将抗炎作用与原性分开的GC对于更安全的治疗至关重要.
研究的目的:
- 评估两种新型非转录作用的GR配体DE.303和KL.202.2的抗炎活性和安全性.
- 为了确定这些化合物是否可以减轻GC诱导的副作用,如皮肤缩.
主要方法:
- 评估了DE.303和KL.202在初级角质细胞中的抗炎性质.
- 测量了NF-κB活性和炎症性细胞因子释放的抑制.
- 评估了DE.303和KL.202对细胞外基因组件和质细胞和纤维细胞中的脂质合成的影响,并将它们与甲进行比较.
主要成果:
- 无论是DE.303还是KL.202,都通过抑制NF-κB活性和减少炎症性细胞因子释放来表现出抗炎作用.
- 与德克萨米他不同,DE.303和KL.202都没有诱导细胞外基因组件或脂质合成的改变.
- 这些新型化合物没有引起通常与GCs相关的缩效应.
结论:
- DE.303和KL.202具有与皮肤疾病相关的显著抗炎特性.
- 这些化合物表现出良好的安全性,缺乏传统GCs的原性作用.
- DE.303和KL.202代表了有希望的治疗替代方案,用于管理炎症性皮肤疾病,并减少副作用.
相关概念视频
01:21Drugs for Treatment of Crohn's Disease in IBD Using Glucocorticoids
120
Glucocorticoids, a class of anti-inflammatory drugs, are pivotal in treating moderate to severe Crohn's disease by inducing remission. They exhibit their anti-inflammatory action by inhibiting the production of inflammatory cytokines such as tumor necrosis factor (TNF)-α, interleukin (IL)-1, and chemokines like IL-8. In addition, they reduce the expression of inflammatory cell adhesion molecules and inhibit gene transcription of nitric oxide synthase, phospholipase A2, cyclooxygenase-2...
120
01:25Antiasthma Drugs: Inhaled Corticosteroids and Glucocorticoids
252
Inhaled corticosteroids (ICS) are anti-inflammatory drugs used primarily in treating persistent asthma and providing long-term maintenance. They target the bronchial mucosa, the lining of the airways, to control inflammation, a critical factor in asthma progression and exacerbation.
ICS work through a multifaceted mechanism of action. They suppress the inflammatory response caused by the proliferation of TH cells. They also reduce the transcription of the IL-2 gene, which is involved in the...
ICS work through a multifaceted mechanism of action. They suppress the inflammatory response caused by the proliferation of TH cells. They also reduce the transcription of the IL-2 gene, which is involved in the...
252
01:29Drugs for Treatment of Crohn's Disease in IBD Using Immunomodulatory Agents
166
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...
166
01:25Antiasthma Drugs: Mast Cell Stabilizers and Anti-IgE Drugs
299
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...
299
01:24Drugs for Treatment of Crohn's Disease in IBD Using Biologic Agents: Anti-TNF
139
Tumor Necrosis Factor (TNF), a proinflammatory cytokine, contributes significantly to the inflammation seen in Crohn's disease. It exists as soluble TNF and membrane-bound TNF, with actions mediated through TNF receptors (TNFR). TNFR activation leads to the release of proinflammatory cytokines, T-cell activation, collagen production, and leukocyte migration, all contributing to inflammation in Crohn's disease. Anti-TNF monoclonal antibodies, namely infliximab (Remicade), adalimumab...
139
01:19Antiasthma Drugs: Leukotriene Modifiers
302
Leukotriene modifiers, or cysteinyl leukotriene receptor antagonists, are medications used to manage chronic asthma. These agents target specific inflammatory mediators produced during arachidonic acid metabolism, an essential process in generating inflammation in the body.
Leukotriene modifiers work through two distinct mechanisms:
Leukotriene modifiers work through two distinct mechanisms:
302