da Silva Filho Ademar A, Pires Bueno Paula C, Gregório Luís E, Andrade e Silva Márcio L, Albuquerque Sérgio, Bastos Jairo K
Departamento de Ciências Farmacêuticas, Faculdade de Ciências Farmacêuticas de Ribeirão Preto, Universidade de São Paulo, Avenida do café s/n, 14040-903 Ribeirão Preto, SP, Brazil.
J Pharm Pharmacol. 2004 Sep;56(9):1195-9. doi: 10.1211/0022357044067.
We have performed a trypanocidal bioactivity-guided study of Baccharis dracunculifolia (Asteraceae), the main botanical origin of Brazilian green propolis. The leaf rinse extract of B. dracunculifolia, at a concentration of 3.0 mg mL(-1), displayed 100% lysis of trypomastigote forms of the Y strain of Trypanosoma cruzi (2 x 10(6) parasites mL(-1)). The chromatographic fractionation of the leaf rinse, using several techniques, afforded the isolation of the compounds isosakuranetin (1), aromadendrin-4'-methylether (2), baccharis oxide (3), ferulic acid (4), dihydrocinnamic acid (5), 3-prenyl-4-(dihydrocinnamoyloxy)-cinnamic acid (6), and friedelanol (7). The chemical structures of all compounds were established by UV-vis, (1)H and (13)CNMR data analysis in comparison with the literature. Compounds 1 and 3 were the most active in the trypanocidal assay, showing IC50 values (inhibitory concentration required for 50% inhibition) of 247.6 and 249.8 microM, respectively. Compounds 2, 4, and 6 displayed moderate activity, whilst compounds 5 and 7 were inactive.
我们对巴西绿蜂胶的主要植物来源——菊科植物艾草（Baccharis dracunculifolia）进行了具有杀锥虫生物活性导向的研究。艾草叶冲洗提取物浓度为3.0 mg mL⁻¹时，对克氏锥虫Y株的锥鞭毛体形式（2×10⁶个寄生虫mL⁻¹）显示出100%的裂解率。采用多种技术对叶冲洗液进行色谱分离，分离出了异樱花素（1）、香豆素-4'-甲醚（2）、艾草氧化物（3）、阿魏酸（4）、二氢肉桂酸（5）、3-异戊烯基-4-（二氢肉桂酰氧基）-肉桂酸（6）和木栓醇（7）等化合物。通过紫外可见光谱、¹H和¹³C NMR数据分析，并与文献对比，确定了所有化合物的化学结构。化合物1和3在杀锥虫试验中活性最高，IC50值（50%抑制所需的抑制浓度）分别为247.6和249.8 μM。化合物2、4和6表现出中等活性，而化合物5和7无活性。
