Morimoto Masanori, Cantrell Charles L, Khan Shabana, Tekwani Babu L, Duke Stephen O
USDA-ARS, Natural Products Utilization Research Unit, Thad Cochran Center, University, MS, 38677, USA.
Department of Applied Chemistry, Graduated School of Agriculture, Kindai University, 3327-204 Nakamachi, Nara City, Nara, 631-8505, Japan.
Chem Biodivers. 2017 Dec;14(12). doi: 10.1002/cbdv.201700324. Epub 2017 Dec 5.
Thirty-seven phytophenolics and their synthetic analogues were evaluated for activity against two protozoal pathogens, Leishmania donovani and Plasmodium falciparum (D6 and W2 clones), respectively. 4,6-Dimethoxyaurone demonstrated the highest activity with IC values of 13.2 and 16.9 μm against L. donovani and P. falciparum (W2 clone), respectively, without undesired cytotoxicity against VERO cells. The moiety having two benzene rings was critical to maintain the antiprotozoal activities based on the observation that both coumaranones and chromones were inactive while other test compounds, including coumarans and aurones, remained active. There was no correlation between antiprotozoal activities and previously evaluated insect antifeedant activity against common cutworms (Spodoptera litura). Flavonoids, including aurones, pterocarpans, and lignan like dihydrobenzofurans, structural analogues of coumarans, are abundant in fruits and vegetables, so these phytophenolics may act as natural antiprotozoal agents in humans.
对37种植物酚类化合物及其合成类似物分别针对两种原生动物病原体——杜氏利什曼原虫和恶性疟原虫（D6和W2克隆株）的活性进行了评估。4,6-二甲氧基奥酮表现出最高活性，对杜氏利什曼原虫和恶性疟原虫（W2克隆株）的IC值分别为13.2和16.9μm，且对VERO细胞没有不良细胞毒性。基于香豆满酮和色酮均无活性而其他测试化合物（包括香豆素和奥酮）仍有活性这一观察结果，具有两个苯环的部分对于维持抗原生动物活性至关重要。抗原生动物活性与先前评估的对普通夜蛾（斜纹夜蛾）的昆虫拒食活性之间没有相关性。黄酮类化合物，包括奥酮、紫檀烷和类似香豆素结构类似物的木脂素类二氢苯并呋喃，在水果和蔬菜中含量丰富，因此这些植物酚类化合物可能在人体内充当天然抗原生动物剂。
