Ortiz Mario I, Fernández-Martínez Eduardo, Soria-Jasso Luis Enrique, Lucas-Gómez Isaac, Villagómez-Ibarra Roberto, González-García Martha P, Castañeda-Hernández Gilberto, Salinas-Caballero Mireya
Área Académica de Medicina del Instituto de Ciencias de la Salud, Universidad Autónoma del Estado de Hidalgo, Pachuca, Hidalgo, Mexico; Coordinación de Posgrado de la Universidad del Fútbol y Ciencias del Deporte, San Agustín Tlaxiaca, Hidalgo, Mexico.
Área Académica de Medicina del Instituto de Ciencias de la Salud, Universidad Autónoma del Estado de Hidalgo, Pachuca, Hidalgo, Mexico.
Biomed Pharmacother. 2016 Mar;78:248-256. doi: 10.1016/j.biopha.2016.01.029. Epub 2016 Feb 2.
Chamomile (Matricaria chamomilla L., Asteraceae) is a medicinal plant widely used as remedy for pain and gastric disorders. The association of non-steroidal anti-inflammatory drugs (NSAIDs) with medicinal plant extracts may increase its antinociceptive activity, permit the use of lower doses and limit side effects. The aim was to isolate and identify the main chemical constituents of Matricaria chamomilla ethanolic extract (MCE) as well as to explore their activity as cyclooxygenase (COX) inhibitors in silico; besides, to examine the interaction between MCE and diclofenac on nociception in the formalin test by isobolographic analysis, and to determine the level of gastric injury in rats. Three terpenoids, α-bisabolol, bisabolol oxide A, and guaiazulene, were isolated and identified by (1)H NMR. Docking simulation predicted COX inhibitory activity for those terpenoids. Diclofenac, MCE, or their combinations produced an antinociceptive effect. The sole administration of diclofenac and the highest combined dose diclofenac-MCE produced significant a gastric damage, but that effect was not seen with MCE alone. An isobologram was constructed and the derived theoretical ED35 for the antinociceptive effect was significantly different from the experimental ED35; hence, the interaction between diclofenac and MCE that mediates the antinociceptive effect is synergist. The MCE contains three major terpenoids with plausible COX inhibitory activity in silico, but α-bisabolol showed the highest affinity. Data suggest that the diclofenac-MCE combination can interact at the systemic level in a synergic manner and may have therapeutic advantages for the clinical treatment of inflammatory pain.
洋甘菊（母菊，菊科）是一种药用植物，广泛用于治疗疼痛和胃部疾病。非甾体抗炎药（NSAIDs）与药用植物提取物联合使用可能会增强其镇痛活性，允许使用更低剂量并限制副作用。本研究旨在分离和鉴定母菊乙醇提取物（MCE）的主要化学成分，并通过计算机模拟探索它们作为环氧化酶（COX）抑制剂的活性；此外，通过等效应线图分析研究MCE与双氯芬酸在福尔马林试验中对伤害感受的相互作用，并确定大鼠胃损伤的程度。通过¹H NMR分离并鉴定了三种萜类化合物，α-红没药醇、红没药醇氧化物A和愈创蓝油烃。对接模拟预测了这些萜类化合物的COX抑制活性。双氯芬酸、MCE或它们的组合产生了镇痛作用。单独给予双氯芬酸和最高剂量的双氯芬酸-MCE组合会产生明显的胃损伤，但单独使用MCE时未观察到这种效应。构建了等效应线图，得出的镇痛作用理论ED35与实验ED35有显著差异；因此，双氯芬酸和MCE之间介导镇痛作用的相互作用是协同的。MCE含有三种主要萜类化合物，在计算机模拟中具有合理的COX抑制活性，但α-红没药醇显示出最高的亲和力。数据表明，双氯芬酸-MCE组合可以在全身水平上以协同方式相互作用，可能对炎症性疼痛的临床治疗具有治疗优势。
