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评估香茅醇单萜异构体产生的镇痛效果。

Evaluation of the antinociceptive effect generated by citronellal monoterpene isomers.

机构信息

Universidade Federal da Paraíba - UFPB, Centro de Ciências da Saúde, Programa de Pós-graduação em Produtos Naturais e Sintéticos Bioativos, João Pessoa, PB, Brasil.

Universidade Federal da Paraíba - UFPB, Centro de Ciências da Saúde, Instituto de Pesquisa em Fámacos e Medicamentos, Laboratório de Psicofarmacologia, João Pessoa, PB, Brasil.

出版信息

Braz J Biol. 2023 May 29;83:e271781. doi: 10.1590/1519-6984.271781. eCollection 2023.

Abstract

Due to the complex nature of pain and the participation of physical, cognitive, psychological and behavioral aspects, pain management has several approaches. The use of medicinal plants in developing countries is quite expressive. Seeking new options for the treatment of emerging or debilitating diseases. Therefore, the present study seeks to elucidate the effects of the monoterpene, citronellal, differentiating its activity by isomers (R)-(+) and (S)-(-) citronellal. The study used several methods to evaluate the effects of citronellal isomers on motor coordination, nociceptive response, and the involvement of opioid, glutamatergic, and transient receptor pathways. The methods included rota-rod, hot-plate, and formalin tests, as well as the use of specific inhibitors and agonists. Data were analyzed using inferential statistics with a 95% confidence level. Both isomers did not significantly affect the motor coordination of the studied animals. The isomer (S)-(-) citronellal showed better results in relation to its structural counterpart, managing to have an antinociceptive effect in the formalin and hot plate tests with a lower concentration (100 mg/kg) and presenting fewer side effects, however, the this study was not able to elucidate the mechanism of action of this isomer despite having activity in studies with substances that act on specific targets such as glutamate and capsaicin, its activity was not reversed with the use of antagonists for pathways related to nociception. While the (R)-(+) citronellal isomer, despite showing total activity only at a concentration of 150 mg/kg, was able to determine its mechanism of action related to the opioid pathway by reversing its activity by the antagonist naloxone, being this is a pathway already correlated with nociception control treatments, however, it is also related to some unwanted side effects. In this way, new studies are sought to elucidate the mechanism related to the isomer (S)-(-) citronellal and a possibility of use in other areas related to the treatment of pain or inflammation.

摘要

由于疼痛的复杂性以及涉及身体、认知、心理和行为等方面,疼痛管理有几种方法。在发展中国家,药用植物的使用相当广泛。为了寻找新兴或衰弱疾病的治疗新选择。因此,本研究旨在阐明单萜柠檬醛及其异构体(R)-(+)和(S)-(-)柠檬醛的作用。该研究使用了几种方法来评估柠檬醛异构体对运动协调、伤害性反应以及阿片类、谷氨酸能和瞬时受体途径的影响。方法包括转棒、热板和福马林测试,以及使用特定的抑制剂和激动剂。数据采用 95%置信水平的推断统计学进行分析。两种异构体都没有显著影响研究动物的运动协调。(S)-(-)柠檬醛异构体表现出更好的结果,与其结构对应物相比,在福马林和热板测试中以较低浓度(100mg/kg)具有抗伤害作用,且副作用较少,但本研究未能阐明这种异构体的作用机制,尽管它在作用于特定靶点的物质(如谷氨酸和辣椒素)的研究中具有活性,但它的活性不能通过使用与伤害性有关的途径的拮抗剂来逆转。虽然(R)-(+)柠檬醛异构体仅在 150mg/kg 的浓度下表现出完全活性,但通过拮抗剂纳洛酮逆转其对阿片途径的活性,能够确定其与阿片途径相关的作用机制,而阿片途径已经与疼痛控制治疗相关联,但它也与一些不良副作用有关。因此,需要进行新的研究来阐明与(S)-(-)柠檬醛异构体相关的机制,并探讨其在疼痛或炎症治疗等其他相关领域的应用可能性。

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