多取代合成查耳酮的体外和体内抗利什曼原虫活性。
In vitro and in vivo anti-Leishmania activity of polysubstituted synthetic chalcones.
机构信息
Department of Chemistry, University of Louisville, KY 40292, USA.
出版信息
Bioorg Med Chem Lett. 2010 Jan 1;20(1):100-3. doi: 10.1016/j.bmcl.2009.11.033. Epub 2009 Nov 14.
The in vitro screening of 43 polysubstituted chalcones against Leishmania amazonensis axenic amastigotes, led to the evaluation of 9 of them in a macrophage-infected model with the two other most infectious Leishmania species prevalent in Peru (L. braziliensis and L. peruviana). The five most active and selective chalcones were studied in vivo, resulting on the identification of two chalcones with high reduction parasite burden percentages.
体外筛选了 43 种多取代查耳酮对亚马逊利什曼原虫无细胞内变形体的抑制活性，其中 9 种在巨噬细胞感染模型中对秘鲁流行的两种最具感染性的利什曼原虫（巴西利什曼原虫和秘鲁利什曼原虫）进行了评估。对 5 种最有效和选择性的查耳酮进行了体内研究，结果发现了两种具有高寄生虫负荷百分比降低的查耳酮。
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