Post-Graduation Program in Biotechnology (RENORBIO), Federal University of Piauí, Teresina, PI, Brazil.
Medicinal Plants Research Center (NPPM), Federal University of Piauí, Teresina, PI, Brazil.
Eur J Pharmacol. 2020 May 5;874:172986. doi: 10.1016/j.ejphar.2020.172986. Epub 2020 Feb 4.
Diarrhea is a condition in which the individual has about three or more daily bowel movements, followed by changes in stool consistency. It is currently considered as one of the worst public health problems due to the number of cases and deaths involved and difficulty of treatment. Thus, the use of natural products is an alternative for new treatments. Among these possibilities is Farnesol (CHO), a sesquiterpene found in different herbal species that has known biological activities. The objective of this study was to evaluate the antidiarrheal activity of Farnesol (FOH). Initially, FOH activity was evaluated in models of diarrhea and enteropooling induced by castor oil and PGE. To evaluate motility, the opioid and cholinergic pathways were studied. In addition, the effect of FOH was investigated in the secretion model in intestinal loops treated with cholera toxin. FOH was evaluated for the ability to absorb fluids in intestinal loops and interact with GM1 receptors using the ELISA method and molecular docking. The dose of 50 mg/kg of FOH showed the best results in all antidiarrheal activity tests with castor oil and PGE, being considered as the standard dose, reducing motility by anticholinergic mechanisms. There was a reduction in fluid secretion when FOH interacted directly with GM1 receptors; cholera toxin and molecular docking showed strong interaction between farnesol and these targets. In view of the results presented, the antidiarrheal activity occurs through anticholinergic, anti-inflammatory and anti-secretory action, making farnesol a potential candidate for the development of a new drug to treat diarrheal diseases.
腹泻是一种个体每天有 3 次或更多次排便，随后粪便稠度发生变化的情况。由于涉及的病例和死亡人数以及治疗难度，目前它被认为是最严重的公共卫生问题之一。因此，使用天然产品是新治疗方法的一种选择。其中一种可能性是法呢醇（CHO），它是一种倍半萜烯，存在于不同的草本物种中，具有已知的生物活性。本研究的目的是评估法呢醇（FOH）的抗腹泻活性。最初，在蓖麻油和 PGE 诱导的腹泻和肠液积聚模型中评估了 FOH 的活性。为了评估运动性，研究了阿片类和胆碱能途径。此外，还研究了 FOH 在霍乱毒素处理的肠环分泌模型中的作用。使用 ELISA 法和分子对接研究了 FOH 吸收肠环中液体的能力和与 GM1 受体的相互作用。在所有使用蓖麻油和 PGE 的抗腹泻活性测试中，50mg/kg 的 FOH 剂量显示出最佳结果，被认为是标准剂量，通过抗胆碱能机制降低运动性。当 FOH 直接与 GM1 受体相互作用时，会减少液体分泌；霍乱毒素和分子对接表明法呢醇与这些靶标之间存在强烈相互作用。鉴于所呈现的结果，抗腹泻活性是通过抗胆碱能、抗炎和抗分泌作用发生的，这使得法呢醇成为开发治疗腹泻疾病的新药的潜在候选药物。
