在由瘤细胞诱导的神经病痛模型上,g-terpinene复合在β-cyclodextrin中的抗高压效应
Lícia T S Pina1, Thallita K Rabelo2, Lysandro P Borges1
1Department of Pharmacy, Federal University of Sergipe, São Cristóvão, Sergipe, Brazil.
International journal of pharmaceutics
|July 30, 2024
概括
天然化合物玛-特尔皮宁 (γ-TPN) 和它的β-环极素复合物 (γ-TPN/CD) 有效地减少了瘤诱导的神经病痛. 复杂化增强了有效性,而不会引起中枢神经系统的副作用.
科学领域:
- 药理学 药理学是指药理学的学科.
- 自然产品 化学 化学
- 疼痛管理 疼痛管理
背景情况:
- 神经病变性疼痛,通常来自癌症,治疗选择有限.
- 目前的治疗方法的疗效很低,但副作用很大.
- 植物性天然产品为治疗疼痛提供了一个有前途的替代方案.
研究的目的:
- 为了研究玛-特尔皮宁 (γ-TPN) 和其β-环氧德克斯特林复合物 (γ-TPN/CD) 的抗过敏疗效.
- 评估γ-TPN和γ-TPN/CD对由瘤细胞引起的神经病痛的疗效.
- 为了评估潜在的中枢神经系统抑郁作用.
主要方法:
- 在动物模型中,由坐骨神经瘤细胞的管理引起的神经病变性疼痛.
- 用γ-TPN和γ-TPN/β-CD (50 mg/kg, p.o.) 的治疗 每天每天六天.
- 评估机械痛,肌肉强度 (抓地力测试) 和运动协调 (Rota-rod测试).
- 分子对接研究,以预测与相关受体的结合相互作用.
主要成果:
- 无论是 γ-TPN 还是 γ-TPN/β-CD,都显著减少了机械超痛症 (p < 0.001).
- 用β-cyclopodextrin复合剂将治疗效果延长了5小时.
- 没有观察到对肌肉强度或运动协调的不良影响.
- 分子对接表明有利的与α-2上腺体,谷氨酸,阿片类和胆固醇受体的结合能量.
结论:
- γ-TPN及其β-cyclopodextrin复合体显示出治疗瘤诱导的神经病痛的显著潜力.
- 复杂化增长了作用的持续时间,并保持了治疗疗效.
- 这种方法提供了一个有希望的,可能比传统的疼痛疗法更安全的替代方案.
更多相关视频
06:54Author Spotlight: Enhanced Method for Evaluating Analgesic Effects — Dual Hind Paw Carrageenan Injection in Mice
Published on: November 15, 2024
1.4K
08:16Partial Sciatic Nerve Ligation: A Mouse Model of Chronic Neuropathic Pain to Study the Antinociceptive Effect of Novel Therapies
Published on: October 6, 2022
6.2K
相关概念视频
Analgesia and Pain Management
557
Pain is critical to various clinical pathologies, provoking an urgent need for effective management. Pain, whether acute or chronic, is a complex neurochemical process. Its alleviation depends on the type, with nonopioid analgesics effective for mild to moderate pain, such as musculoskeletal or inflammatory pain, while neuropathic pain responds best to anticonvulsants, tricyclic antidepressants, or serotonin/norepinephrine reuptake inhibitors. For severe acute or chronic pain, opioids may be...
557
Chemotherapy-Induced Nausea and Vomiting: Cannabinoids
208
Tetrahydrocannabinol (THC) is a phytocannabinoid that primarily interacts with the CB1 receptor, a type of G protein-coupled receptor (GPCR) predominantly in and around the chemoreceptor trigger zone (CTZ) and emetic center. THC also blocks the serotonin receptor activity in the dorsal vagal complex (DVC) by inhibiting serotonin release. THC exerts its anti-emetic effects through these interactions, which are beneficial for patients undergoing chemotherapy.
Two synthetic agonists of THC,...
Two synthetic agonists of THC,...
208
Chemotherapy-Induced Nausea and Vomiting: Neurokinin-1 Receptor Antagonists
157
Neurokinin 1 (NK1) receptors are distributed across the GI tract, vagal afferents, and key CNS regions including the central vomiting center and chemoreceptor trigger zone (CTZ) Chemotherapy agents stimulate enterochromaffin cells in the gastrointestinal (GI) tract to release large amounts of substance P (SP). SP is a neuropeptide released by specific sensory nerves in response to many different stressors, including those in the GI mucosa affected by chemotherapy. SP binds and activates...
157
