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小叶阿尔格里齐亚(Algrizea minor Sobral、法里亚和普罗恩萨,桃金娘科,桃金娘族)叶精油与β-环糊精络合后镇痛活性的增强。

Potentiation of analgesic activity following the complexation of Algrizea minor Sobral, Faria & Proença (Myrteae, Myrtaceae) leaf essential oil with β-cyclodextrin.

作者信息

Fernandes Paulo Henrique Eloi, de Veras Bruno Oliveira, do Nascimento Silva Paulo Henrique Andrade, de Aguiar Júlio César Ribeiro de Oliveira Farias, do Amaral Ferraz Navarro Daniela Maria, Dos Santos Correia Maria Tereza, da Silva Márcia Vanusa

机构信息

Center for Bioscience, Federal University of Pernambuco (UFPE), Recife, Pernambuco, 50670-420, Brazil.

Department of Biochemistry, Biosciences Center, Federal University of Pernambuco (UFPE), Recife, Pernambuco, 50670-420, Brazil.

出版信息

Inflammopharmacology. 2025 Sep 23. doi: 10.1007/s10787-025-01979-5.

DOI:10.1007/s10787-025-01979-5
PMID:40986264
Abstract

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.

摘要

疼痛是一种基本的生物学过程;然而,其急性表现可能导致调节失调和组织损伤。桃金娘科以其多样的药理活性而闻名,原产于巴西的小叶阿尔格里齐亚传统上被用于治疗炎症和疼痛。本研究调查了小叶阿尔格里齐亚精油(EOAm)的抗伤害感受特性,并研究了其与β-环糊精(β-CD)的络合是否能增强其药理功效。通过水蒸馏获得EOAm,产率为0.57%(w/w),其中β-蒎烯(66.99%)被确定为主要成分。使用小鼠模型评估抗伤害感受活性,包括醋酸诱导的扭体试验和福尔马林试验。游离EOAm以剂量依赖性方式显著降低伤害感受行为,在醋酸模型中产生高达89%的抑制率。值得注意的是,与β-CD络合进一步增强了镇痛效果,在测试的最高剂量(200mg/kg)下实现了对伤害感受的完全抑制。在福尔马林试验中,EOAm及其β-CD络合物在神经源性和炎症阶段均显示出显著疗效。纳洛酮部分逆转镇痛作用表明阿片系统参与了潜在机制。总体而言,这些发现表明EOAm具有强大的抗伤害感受活性,通过与β-环糊精络合可进一步增强。这种方法不仅提高了疗效,还可能增加精油的稳定性和生物利用度,突出了EOAm/β-CD络合物作为新型镇痛疗法开发的有前景的候选物。

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