β-环糊精与金娘科金娘叶精油络合后镇痛活性的增强。

IF 5.3 2区 医学 Q2 IMMUNOLOGY
Paulo Henrique Eloi Fernandes, Bruno Oliveira de Veras, Paulo Henrique Andrade do Nascimento Silva, Júlio César Ribeiro de Oliveira Farias de Aguiar, Daniela Maria do Amaral Ferraz Navarro, Maria Tereza Dos Santos Correia, Márcia Vanusa da Silva
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引用次数: 0

摘要

疼痛是一个基本的生物过程;然而,其急性表现可能导致失调和组织损伤。桃金娘科以其多样的药理活性而闻名,而小桃金娘是一种原产于巴西的物种,传统上被用于治疗炎症和疼痛。本研究研究了小黄花精油(EOAm)的抗伤性,并考察了其与β-环糊精(β-CD)络合是否能增强其药理作用。通过加氢蒸馏得到EOAm,收率为0.57% (w/w),主要成分为β-蒎烯(66.99%)。使用小鼠模型,包括醋酸诱导的扭体和福尔马林试验来评估抗伤性活性。游离EOAm以剂量依赖的方式显著降低伤害性行为,在乙酸模型中产生高达89%的抑制作用。值得注意的是,β-CD络合进一步增强了镇痛效果,在最高剂量(200 mg/kg)下实现了对伤害感觉的完全抑制。在福尔马林实验中,EOAm及其β-CD复合物在神经原性和炎症期均表现出显著的疗效。纳洛酮部分逆转镇痛作用提示阿片系统参与其潜在机制。综上所述,这些发现表明EOAm具有较强的抗伤感受活性,并通过β-环糊精络合进一步增强。这种方法不仅提高了疗效,而且可能增加精油的稳定性和生物利用度,突出了EOAm/β-CD复合物作为开发新型镇痛疗法的有希望的候选者。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Potentiation of analgesic activity following the complexation of Algrizea minor Sobral, Faria & Proença (Myrteae, Myrtaceae) leaf essential oil with β-cyclodextrin.

Pain is a fundamental biological process; however, its acute manifestation may result in dysregulation and tissue injury. The Myrtaceae family is well known for its diverse pharmacological activities, and Algrizea minor, a species native to Brazil, has traditionally been used for the management of inflammation and pain. The present study investigated the antinociceptive properties of essential oil Algrizea minor (EOAm) and examined whether its complexation with β-cyclodextrin (β-CD) could enhance its pharmacological efficacy. EOAm was obtained by hydrodistillation, yielding 0.57% (w/w), with β-pinene (66.99%) identified as the major constituent. Antinociceptive activity was evaluated using murine models, including the acetic acid-induced writhing and formalin tests. Free EOAm significantly reduced nociceptive behavior in a dose-dependent manner, producing up to 89% inhibition in the acetic acid model. Remarkably, complexation with β-CD further potentiated the analgesic effect, achieving complete inhibition of nociception at the highest dose tested (200 mg/kg). In the formalin assay, both EOAm and its β-CD complex displayed significant efficacy during the neurogenic and inflammatory phases. Partial reversal of the analgesic effect by naloxone indicates the involvement of the opioid system in the underlying mechanism. Overall, these findings demonstrate that EOAm possesses strong antinociceptive activity, which is further enhanced through β-cyclodextrin complexation. This approach not only improves efficacy but also may increase the stability and bioavailability of the essential oil, highlighting the EOAm/β-CD complex as a promising candidate for the development of novel analgesic therapies.

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来源期刊
Inflammopharmacology
Inflammopharmacology IMMUNOLOGYTOXICOLOGY-TOXICOLOGY
CiteScore
8.00
自引率
3.40%
发文量
200
期刊介绍: Inflammopharmacology is the official publication of the Gastrointestinal Section of the International Union of Basic and Clinical Pharmacology (IUPHAR) and the Hungarian Experimental and Clinical Pharmacology Society (HECPS). Inflammopharmacology publishes papers on all aspects of inflammation and its pharmacological control emphasizing comparisons of (a) different inflammatory states, and (b) the actions, therapeutic efficacy and safety of drugs employed in the treatment of inflammatory conditions. The comparative aspects of the types of inflammatory conditions include gastrointestinal disease (e.g. ulcerative colitis, Crohn''s disease), parasitic diseases, toxicological manifestations of the effects of drugs and environmental agents, arthritic conditions, and inflammatory effects of injury or aging on skeletal muscle. The journal has seven main interest areas: -Drug-Disease Interactions - Conditional Pharmacology - i.e. where the condition (disease or stress state) influences the therapeutic response and side (adverse) effects from anti-inflammatory drugs. Mechanisms of drug-disease and drug disease interactions and the role of different stress states -Rheumatology - particular emphasis on methods of measurement of clinical response effects of new agents, adverse effects from anti-rheumatic drugs -Gastroenterology - with particular emphasis on animal and human models, mechanisms of mucosal inflammation and ulceration and effects of novel and established anti-ulcer, anti-inflammatory agents, or antiparasitic agents -Neuro-Inflammation and Pain - model systems, pharmacology of new analgesic agents and mechanisms of neuro-inflammation and pain -Novel drugs, natural products and nutraceuticals - and their effects on inflammatory processes, especially where there are indications of novel modes action compared with conventional drugs e.g. NSAIDs -Muscle-immune interactions during inflammation [...]
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