Laboratory of Immunopharmacology, Postgraduate Program in Natural and Synthetic Bioactive Products, Federal University of Paraíba, João Pessoa, PB, Brazil.
Paraíba Association of Renewed Education (ASPER), João Pessoa, PB, Brazil.
Int Immunopharmacol. 2021 Jul;96:107590. doi: 10.1016/j.intimp.2021.107590. Epub 2021 Apr 13.
The combined allergic rhinitis and asthma syndrome (CARAS) is a chronic airway inflammation of allergic individuals, with a type 2 immune response. Pharmacotherapy is based on drugs with relevant side effects. Thus, the goal of this study was to evaluate the synthetic alkaloid, MHTP in the experimental model of CARAS. Therefore, BALB/c mice were ovalbumin (OVA) -sensitized and -challenged and treated with MHTP by intranasal or oral routes. Treated animals showed a decrease (p < 0.05) of sneezing, nasal rubbings, and histamine nasal hyperactivity. Besides, MHTP presented binding energy and favorable interaction for adequate anchoring in the histamine H1 receptor. MHTP treatment inhibited the eosinophil migration into the nasal (NALF) and the bronchoalveolar (BALF) fluids. Histological analysis showed that the alkaloid decreased the inflammatory cells in the subepithelial and perivascular regions of nasal tissue and in the peribronchiolar and perivascular regions of lung tissue. The MHTP treatment also reduced the pulmonary hyperactivity by decreasing the smooth muscle layer hypertrophy and the collagen fiber deposition in the extracellular matrix. The immunomodulatory effect of the alkaloid was due to the decrease of cytokines like IL-5 and IL-17A (type 2 and 3), TSLP (epithelial), and the immunoregulatory cytokine, TGF-β. These MHTP effects on granulocytes were dependent on the p38/ERK1/2 MAP kinase signaling pathway axis. Indeed, the synthetic alkaloid reduced the frequency of activation of both kinases independent of the NF-κB (p65) pathway indicating that the molecule shut down the intracellular transduction signals underlie the cytokine gene transcription.
变应性鼻炎和哮喘综合征(CARAS)是一种过敏性个体的慢性气道炎症,具有 2 型免疫反应。药物治疗基于具有相关副作用的药物。因此,本研究的目的是评估合成生物碱 MHTP 在 CARAS 的实验模型中的作用。因此,BALB/c 小鼠用卵清蛋白(OVA)致敏和激发,并通过鼻腔或口服途径给予 MHTP 治疗。治疗动物表现出打喷嚏、鼻摩擦和组胺鼻高反应性减少(p<0.05)。此外,MHTP 表现出结合能和适当结合组胺 H1 受体的有利相互作用。MHTP 治疗抑制嗜酸性粒细胞向鼻(NALF)和支气管肺泡(BALF)液的迁移。组织学分析表明,该生物碱减少了鼻组织的上皮下和血管周围区域以及肺组织的细支气管周围和血管周围区域的炎症细胞。MHTP 治疗还通过减少平滑肌层肥大和细胞外基质中胶原纤维沉积来降低肺高反应性。该生物碱的免疫调节作用是由于细胞因子如 IL-5 和 IL-17A(2 型和 3 型)、TSLP(上皮)和免疫调节细胞因子 TGF-β的减少。该生物碱对粒细胞的这些作用依赖于 p38/ERK1/2 MAP 激酶信号通路轴。事实上,该合成生物碱减少了两种激酶的激活频率,而不依赖于 NF-κB(p65)途径,表明该分子阻断了细胞内转导信号,从而阻止了细胞因子基因的转录。