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Anti-Inflammatory and Antinociceptive Properties of Kielmeyerone A, a Chromenone Isolated from the Roots of Kielmeyera reticulata
Journal of Natural Products ( IF 5.1 ) Pub Date : 2021-07-20 , DOI: 10.1021/acs.jnatprod.1c00157
Heiter V M Boness 1 , Milena S de Oliveira 1 , Carine S C Batista 1 , Leticia S Almeida 2 , Elisangela F Boffo 1 , Cristiane F Villarreal 2 , Frederico G Cruz 1
Affiliation  

Four new chromenones, kielmeyerones A–D (14), were obtained from the roots of Kielmeyera reticulata. Their structures were elucidated based on spectroscopic data (NMR and HRESIMS) interpretation. The pharmacological activity of kielmeyerone A (1), the major compound, was evaluated using in vitro and in vivo inflammation and pain models. During in vitro screening, 1, at noncytotoxic concentrations (0.097–1.56 μM), inhibited NO production by J774 macrophages stimulated with LPS and IFN-γ. In the complete Freund’s adjuvant-induced inflammation model in mice, 1 (12.5–50 mg/kg) inhibited paw edema, demonstrating an anti-inflammatory effect. Additionally, 1 (12.5–50 mg/kg) induced a dose-dependent antinociceptive effect in the late phase of the formalin test, a profile similar to those of nonsteroidal anti-inflammatory drugs. Mice treated with 1 (100 mg/kg) did not show motor performance alterations using a rota-rod test. Thus, the present study has characterized new chromenones from Kielmeyera reticulata and has provided evidence of the anti-inflammatory and antinociceptive properties of one of these, kielmeyerone A (1).

中文翻译:

Kielmeyerone A 的抗炎和镇痛特性,一种从 Kielmeyera reticulata 根中分离的 Chromenone

四个新chromenones,kielmeyerones A-d(1 - 4),从根部获得Kielmeyera网状。基于光谱数据(NMR 和 HRESIMS)解释阐明了它们的结构。使用体外和体内炎症和疼痛模型评估了主要化合物Kielmeyerone A ( 1 )的药理活性。在体外筛选过程中,1在非细胞毒性浓度 (0.097–1.56 μM) 下,抑制了 LPS 和 IFN-γ 刺激的 J774 巨噬细胞产生的 NO。在完全弗氏佐剂诱导的小鼠炎症模型中,1 (12.5–50 mg/kg) 抑制爪水肿,显示出抗炎作用。此外,1(12.5–50 mg/kg) 在福尔马林试验的后期诱导剂量依赖性镇痛作用,其特征类似于非甾体抗炎药。使用1 (100 mg/kg)处理的小鼠使用旋转杆测试未显示运动性能改变。因此,本研究表征了来自Kielmeyera reticulata 的色酮,并提供了其中之一 Kielmeyerone A ( 1 )的抗炎和镇痛特性的证据。
更新日期:2021-08-27
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