Lima Tamires C, Souza Rafaela J, Santos Alan D C, Moraes Milene H, Biondo Nicole E, Barison Andersson, Steindel Mário, Biavatti Maique W
a Departamento de Ciências Farmacêuticas, CCS , Universidade Federal de Santa Catarina (UFSC) , Florianópolis , SC , Brazil.
b Departamento de Química , Universidade Federal do Paraná (UFPR) , Curitiba , PR , Brazil.
Nat Prod Res. 2016;30(5):551-7. doi: 10.1080/14786419.2015.1030740. Epub 2015 Apr 16.
The phytochemical study of Calea uniflora led to the isolation of nine phenolic compounds identified as noreugenin (1), ethyl caffeate (2), a mixture of butein (3) + orobol (4), α-hydroxy-butein (5), caffeic acid (6), butein 4'-O-glucopyranosyl (7), quercetin 3-O-glucopyranosyl (8) and 3,5-di-O-caffeoylquinic acid (9). The chemical identity of the isolates was established on the basis of NMR and physical data. The chemical shifts of 5 and 7 have been reassigned and all the isolates were tested against Leishmania amazonensis and Trypanosoma cruzi amastigotes. None of the metabolites showed promising leishmanicidal activity. However, 2 and the mixture of 3 and 4 demonstrated interesting trypanocidal effect with IC50 values of 18.27 and 26.53 μM, respectively. Besides, these compounds did not present cytotoxic effect towards THP-1 cells, and compound 2 was 3.5-fold more selective than the mixture of 3+4.
对单花卡利亚草的植物化学研究导致分离出九种酚类化合物,分别鉴定为去甲丁香色原酮(1)、咖啡酸乙酯(2)、紫铆因(3)+紫铆醇(4)的混合物、α-羟基紫铆因(5)、咖啡酸(6)、紫铆因4'-O-吡喃葡萄糖苷(7)、槲皮素3-O-吡喃葡萄糖苷(8)和3,5-二-O-咖啡酰奎尼酸(9)。根据核磁共振(NMR)和物理数据确定了分离物的化学特性。重新指定了5和7的化学位移,并对所有分离物针对亚马逊利什曼原虫和克氏锥虫无鞭毛体进行了测试。没有一种代谢物显示出有前景的杀利什曼活性。然而,2以及3和4的混合物表现出有趣的杀锥虫作用,IC50值分别为18.27和26.53μM。此外,这些化合物对THP-1细胞没有细胞毒性作用,并且化合物2的选择性比3 + 4的混合物高3.5倍。