Abstract:
Pain is the most frequent symptom of disease. In treating pain, a lower incidence of adverse effects is found for paracetamol versus other non-steroidal anti-inflammatory drugs. Nevertheless, paracetamol can trigger side effects when taken regularly. Combined therapy is a common way of lowering the dose of a drug and thus of reducing adverse reactions. Since β-caryophyllene oxide (a natural bicyclic sesquiterpene) is known to produce an analgesic effect, this study aimed to determine the anti-nociceptive and gastroprotective activity of administering the combination of paracetamol plus β-caryophyllene oxide to CD1 mice. Anti-nociception was evaluated with the formalin model and gastroprotection with the model of ethanol-induced gastric lesions. According to the isobolographic analysis, the anti-nociceptive interaction of paracetamol and β-caryophyllene oxide was synergistic. Various pain-related pathways were explored for their possible participation in the mechanism of action of the anti-nociceptive effect of β-caryophyllene oxide, finding that NO, opioid receptors, serotonin receptors, and K+ATP channels are not involved. The combined treatment showed gastroprotective activity against ethanol-induced gastric damage. Hence, the synergistic anti-nociceptive effect of combining paracetamol with β-caryophyllene oxide could be advantageous for the management of inflammatory pain, and the gastroprotective activity should help to protect against the adverse effects of chronic use.
摘要:
疼痛是疾病最常见的症状。在治疗疼痛时,对乙酰氨基酚的不良反应发生率低于其他非甾体类抗炎药.然而,定期服用扑热息痛会引发副作用。联合治疗是降低药物剂量并因此减少不良反应的常用方法。由于已知β-石竹烯氧化物(天然双环倍半萜)产生镇痛作用,这项研究旨在确定对CD1小鼠施用对乙酰氨基酚加β-石竹烯氧化物的组合的抗伤害性和胃保护活性。用福尔马林模型评估抗伤害感受,用乙醇诱导的胃病变模型评估胃保护作用。根据等值线分析,对乙酰氨基酚和β-石竹烯氧化物的抗伤害性相互作用是协同的。探索了各种与疼痛相关的途径,因为它们可能参与β-石竹烯氧化物的抗伤害性作用的作用机制,发现不,阿片受体,血清素受体,与K+ATP通道无关。联合治疗对乙醇引起的胃损伤具有胃保护活性。因此,扑热息痛与β-石竹烯氧化物联合使用的协同抗伤害性作用可能有利于治疗炎性疼痛,和胃保护活性应有助于防止长期使用的不利影响。