Pires Claudia Terencio Agostinho, Brenzan Mislaine Adriana, Scodro Regiane Bertin de Lima, Cortez Diógenes Aparício Garcia, Lopes Luciana Dias Ghiraldi, Siqueira Vera Lucia Dias, Cardoso Rosilene Fressatti
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Mem Inst Oswaldo Cruz. 2014 Jun;109(3):324-9. doi: 10.1590/0074-0276130323. Epub 2014 Mar 4.
We evaluated the in vitro anti-Mycobacterium tuberculosis activity and the cytotoxicity of dichloromethane extract and pure compounds from the leaves of Calophyllum brasiliense. Purification of the dichloromethane extract yielded the pure compounds (-) mammea A/BB (1), (-) mammea B/BB (2) and amentoflavone (3). The compound structures were elucidated on the basis of spectroscopic and spectrometric data. The contents of bioactive compounds in the extracts were quantified using high performance liquid chromatography coupled to an ultraviolet detector. The anti-M. tuberculosis activity of the extracts and the pure compounds was evaluated using a resazurin microtitre assay plate. The cytotoxicity assay was performed in J774G.8 macrophages using the 3-(4,5-dimethyl thiazol-2-yl)-2,5-diphenyl tetrazolium bromide colourimetric method. The quantification of the dichloromethane extract showed (1) and (2) at concentrations of 31.86 ± 2.6 and 8.24 ± 1.1 µg/mg of extract, respectively. The dichloromethane and aqueous extracts showed anti-M. tuberculosis H37Rv activity of 62.5 and 125 µg/mL, respectively. Coumarins (1) and (2) showed minimal inhibitory concentration ranges of 31.2 and 62.5 µg/mL against M. tuberculosis H37Rv and clinical isolates. Compound (3) showed no activity against M. tuberculosis H37Rv. The selectivity index ranged from 0.59-1.06. We report the activity of the extracts and coumarins from the leaves of C. brasiliense against M. tuberculosis.
我们评估了巴西红厚壳树叶的二氯甲烷提取物及纯化合物的体外抗结核分枝杆菌活性和细胞毒性。二氯甲烷提取物经纯化得到纯化合物（-）山竹子素A/BB（1）、（-）山竹子素B/BB（2）和穗花杉双黄酮（3）。根据光谱和光谱数据阐明了化合物结构。使用配备紫外检测器的高效液相色谱法对提取物中的生物活性化合物含量进行定量。采用刃天青微量滴定板法评估提取物和纯化合物的抗结核分枝杆菌活性。使用3-（4,5-二甲基噻唑-2-基）-2,5-二苯基四氮唑溴盐比色法在J774G.8巨噬细胞中进行细胞毒性测定。二氯甲烷提取物的定量分析显示，（1）和（2）的浓度分别为31.86±2.6和8.24±1.1μg/mg提取物。二氯甲烷提取物和水提取物对结核分枝杆菌H37Rv的活性分别为62.5和125μg/mL。香豆素（1）和（2）对结核分枝杆菌H37Rv和临床分离株的最低抑菌浓度范围分别为31.2和62.5μg/mL。化合物（3）对结核分枝杆菌H37Rv无活性。选择性指数范围为0.59 - 1.06。我们报道了巴西红厚壳树叶提取物和香豆素对结核分枝杆菌的活性。
