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(玫瑰变种)丙酮提取物的抗伤害感受和抗炎活性。

Antinociceptive and Anti-Inflammatory Activities of Acetonic Extract from (var. Rose).

作者信息

Castañeda-Corral Gabriela, Cedillo-Cortezano Mayra, Aviles-Flores Magdalena, López-Castillo Misael, Acevedo-Fernández Juan José, Petricevich Vera L

机构信息

Facultad de Medicina, Universidad Autónoma del Estado de Morelos, Calle Iztaccihuatl Esq. Leñeros, Col. Volcanes, Cuernavaca 62350, Morelos, Mexico.

出版信息

Pharmaceuticals (Basel). 2024 Aug 6;17(8):1037. doi: 10.3390/ph17081037.

Abstract

is an ornamental plant with antioxidant, anti-inflammatory, and cytotoxic activities, which has been traditionally used to treat respiratory diseases. This study aimed to investigate whether the acetonic extract of var. Rose (BxbRAE-100%) has analgesic and anti-inflammatory properties and its potential action mechanisms. Analgesic and anti-inflammatory activities were evaluated using three murine pain models and two acute inflammation models. In vitro, the ability of the extract to inhibit proteolytic activity and the activities of the enzymes phospholipase A2 (PLA2) and cyclooxygenase (COX) were evaluated. In silico analysis was performed to predict the physicochemical and Absorption, distribution, metabolism, and excretion (ADME) profiles of the compounds previously identified in BxbRAE-100%. In vivo BxbRAE-100% decreased the nociceptive behaviors in the writhing model, the tail immersion, and the formalin test, suggesting that the extract has the potential to relieve pain at peripheral and central levels. Additionally, topical or oral BxbRAE-100% treatment reduced dose-dependent 12--Tetradecanoylphorbol-13-acetate (TPA)-induced ear inflammation and carrageenan-induced paw edema, respectively. In vitro, BxbRAE-100% significantly inhibited proteolytic activity and PLA2, COX-1 and COX-2 activities. In silico, the compounds previously identified in BxbRAE-100% met Lipinski's rule of five and showed adequate ADME properties. These results support the use of in Traditional Mexican Medicine and highlight its potential for the development of new treatments for pain and inflammation.

摘要

是一种具有抗氧化、抗炎和细胞毒性活性的观赏植物,传统上用于治疗呼吸道疾病。本研究旨在调查玫瑰变种(BxbRAE - 100%)的丙酮提取物是否具有镇痛和抗炎特性及其潜在作用机制。使用三种小鼠疼痛模型和两种急性炎症模型评估镇痛和抗炎活性。在体外,评估提取物抑制蛋白水解活性以及磷脂酶A2(PLA2)和环氧化酶(COX)活性的能力。进行计算机分析以预测先前在BxbRAE - 100%中鉴定的化合物的物理化学和吸收、分布、代谢及排泄(ADME)特征。在体内,BxbRAE - 100%在扭体模型、尾部浸入和福尔马林试验中降低了伤害性反应行为,表明该提取物有可能在周围和中枢水平缓解疼痛。此外,局部或口服BxbRAE - 100%治疗分别剂量依赖性地减轻了12 - 十四酰佛波醇 - 13 - 乙酸酯(TPA)诱导的耳部炎症和角叉菜胶诱导的爪部水肿。在体外,BxbRAE - 100%显著抑制蛋白水解活性以及PLA2、COX - 1和COX - 2活性。在计算机分析中,先前在BxbRAE - 100%中鉴定的化合物符合Lipinski的五规则并显示出足够的ADME特性。这些结果支持了其在墨西哥传统医学中的应用,并突出了其在开发疼痛和炎症新疗法方面的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/625e/11357402/3582800e4bd9/pharmaceuticals-17-01037-g001.jpg

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