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在小鼠癌症疼痛模型中,p-Cymene/β-Cyclodextrin包容复合物的抗毒感应效应:通过对接研究的帮助进行表征

Wagner B R Santos¹, Lícia T S Pina¹, Marlange A de Oliveira²

¹Departament of Pharmacy, Federal University of Sergipe, São Cristóvão 49100-000, SE, Brazil.

Molecules (Basel, Switzerland)

|June 10, 2023

概括

这项研究表明,将p-cymene (PC) 与β-cyclodextrin (β-CD) 复合起来可以有效地治疗癌症疼痛. 在小鼠模型中,PC/β-CD复合物显著降低了疼痛,与自由PC不同,改善了其治疗效果.

科学领域:

药理学药理学是指药理学的学科.
药用化学医学化学
疼痛管理疼痛管理

背景情况:

癌症疼痛是一种普遍且具有挑战性的症状,由于不良反应,常规药物往往无法充分控制.
单烯的p-Cymene (PC) 具有抗受性特性,但由于其脂性,它面临着物理化学和药理学的限制.
目前正在探索β-cyclodextrins (β-CD),以增强像PC这样的脂性化合物的特性.

研究的目的:

在癌症疼痛模型中创建,描述和评估p-cymene和β-cyclodextrin复合体 (PC/β-CD) 的疗效.
为了确定PC/β-CD复合是否能改善p-cymene的抗毒感受作用.
评估PC/β-CD在与肉瘤180 (S180) 瘤相关的疼痛管理中的有效性.

主要方法:

用分子对接来预测PC和β-CD复合体形成的可行性.
使用泥复合合成PC/β-CD复合体,并通过高性能液体染色学 (HPLC) 和核磁共振 (NMR) 谱学进行了特征分析.
在 Sarcoma 180 (S180) 诱导的癌症疼痛模型中评估了PC/β-CD的抗毒感应作用.

主要成果:

分子对接模拟表明PC和β-CD之间存在有利的相互作用.
PC/β-CD复合体的复合效率高达82.61%,由NMR光谱学证实,PC被封装在β-CD腔内.
在S180癌症疼痛模型中,PC/β-CD在测试剂量时显著降低了机械超痛和恶感 (p < 0.05),而不是自由PC (p > 0.05).

结论:

将p-cymene (PC) 与β-cyclodextrin (β-CD) 复合成功克服了自由PC的局限性.
与单独的p-cymene相比,PC/β-CD复合体在治疗癌症疼痛方面表现出更强的药理疗效.
这种方法提供了一个有前途的策略,通过降低所需剂量来提高p-cymene在癌症疼痛管理中的治疗潜力.

关键词:

癌症疼痛疼痛癌症疼痛包容复杂的包容复杂的包容单烯是一种单烯.自然产品是自然产品的产品.

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