Department of Gastroenterology, the First Affiliated Hospital of Shandong First Medical University & Shandong Provincial Qianfoshan Hospital, Jinan, Shandong, China.
Center for Health and the Environment, University of California, Davis, California, United States of America.
PLoS One. 2022 Apr 20;17(4):e0266608. doi: 10.1371/journal.pone.0266608. eCollection 2022.
Asthma currently affects more than 339 million people worldwide. In the present preliminary study, we examined the efficacy of a new, inhalable soluble epoxide hydrolase inhibitor (sEHI), 1-trifluoromethoxyphenyl-3-(1-propionylpiperidin-4-yl) urea (TPPU), to attenuate airway inflammation, mucin secretion, and hyper-responsiveness (AHR) in an ovalbumin (OVA)-sensitized murine model. Male BALB/c mice were divided into phosphate-buffered saline (PBS), OVA, and OVA+TPPU (2- or 6-h) exposure groups. On days 0 and 14, the mice were administered PBS or sensitized to OVA in PBS. From days 26-38, seven challenge exposures were performed with 30 min inhalation of filtered air or OVA alone. In the OVA+TPPU groups, a 2- or 6-h TPPU inhalation preceded each 30-min OVA exposure. On day 39, pulmonary function tests (PFTs) were performed, and biological samples were collected. Lung tissues were used to semi-quantitatively evaluate the severity of inflammation and airway constriction and the volume of stored intracellular mucosubstances. Bronchoalveolar lavage (BAL) and blood samples were used to analyze regulatory lipid mediator profiles. Significantly (p < 0.05) attenuated alveolar, bronchiolar, and pleural inflammation; airway resistance and constriction; mucosubstance volume; and inflammatory lipid mediator levels were observed with OVA+TPPU relative to OVA alone. Cumulative findings indicated TPPU inhalation effectively inhibited inflammation, suppressed AHR, and prevented mucosubstance accumulation in the murine asthmatic model. Future studies should determine the pharmacokinetics (i.e., absorption, distribution, metabolism, and excretion) and pharmacodynamics (i.e., concentration/dose responses) of inhaled TPPU to explore its potential as an asthma-preventative or -rescue treatment.
哮喘目前影响着全球超过 3.39 亿人。在本初步研究中,我们研究了一种新型可吸入可溶性环氧化物水解酶抑制剂(sEHI),1-三氟甲氧基苯基-3-(1-丙酰基哌啶-4-基)脲(TPPU),在卵清蛋白(OVA)致敏的小鼠模型中减轻气道炎症、粘蛋白分泌和高反应性(AHR)的疗效。雄性 BALB/c 小鼠分为磷酸盐缓冲盐水(PBS)、OVA 和 OVA+TPPU(2 或 6 小时)暴露组。在第 0 天和第 14 天,给小鼠注射 PBS 或用 PBS 致敏 OVA。从第 26 天到第 38 天,用 30 分钟过滤空气或单独 OVA 吸入进行 7 次挑战暴露。在 OVA+TPPU 组中,在每次 30 分钟 OVA 暴露前进行 2 或 6 小时 TPPU 吸入。在第 39 天进行肺功能测试(PFT)并收集生物样本。使用肺组织对半定量评估炎症和气道收缩的严重程度以及储存的细胞内粘蛋白物质的体积。支气管肺泡灌洗(BAL)和血液样本用于分析调节脂质介质谱。与 OVA 单独相比,OVA+TPPU 显著(p<0.05)减轻肺泡、细支气管和胸膜炎症;气道阻力和收缩;粘蛋白物质体积;和炎症性脂质介质水平。累积研究结果表明,TPPU 吸入可有效抑制炎症,抑制 AHR,并防止在小鼠哮喘模型中粘蛋白物质的积累。未来的研究应确定吸入 TPPU 的药代动力学(即吸收、分布、代谢和排泄)和药效学(即浓度/剂量反应),以探索其作为预防或挽救哮喘治疗的潜力。