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首页> 外文期刊>Bioorganic and Medicinal Chemistry >Antimalarial potential of xestoquinone, a protein kinase inhibitor isolated from a Vanuatu marine sponge Xestospongia sp.
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Antimalarial potential of xestoquinone, a protein kinase inhibitor isolated from a Vanuatu marine sponge Xestospongia sp.

机译：Xestoquinone（一种从瓦努阿图海洋海绵Xestospongia sp。分离的蛋白激酶抑制剂）的抗疟疾潜力。

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摘要

As part of our search for new antimalarial drugs, we have screened for inhibitors of Pfnek-1, a protein kinase of Plas-modium falciparum, in south Pacific marine sponges. On the basis of a preliminary screening, the ethanolic crude extract of a new species of Xestospongia collected in Vanuatu was selected for its promising activity. A bioassay-guided fractionation led us to isolate xestoquinone which inhibits Pfnek-1 with an IC_(50) around 1 μM. Among a small panel of plasmodial protein kinases, xestoquinone showed modest protein kinase inhibitory activity toward PfPK5 and no activity toward PfPK7 and PfGSK-3. Xestoquinone showed in vitro antiplasmodial activity against a FCB1 P. falciparum strain with an IC_(50) of 3 μM and a weak selectivity index (SI 7). Xestoquinone exhibited a weak in vivo activity at 5 mg/kg in Plasmodium berghei NK65 infected mice and was toxic at higher doses.
机译：为了寻找新的抗疟药，我们在南太平洋海棉中筛选了恶性疟原虫蛋白激酶Pfnek-1的抑制剂。在初步筛选的基础上，选择了在瓦努阿图收集的一种新的Xestospongia的乙醇粗提物，因为它具有良好的活性。生物测定指导的分级分离导致我们分离出抑制Pfnek-1的异戊醌，其IC_（50）约为1μM。在一小部分的血浆蛋白激酶中，对甲苯醌显示对PfPK5适度的蛋白激酶抑制活性，对PfPK7和PfGSK-3无活性。异戊醌显示对FCB1恶性疟原虫菌株的体外抗疟原虫活性，IC_（50）为3μM，选择性指数（SI 7）低。异戊醌在伯氏疟原虫NK65感染的小鼠中以5 mg / kg的剂量表现出较弱的体内活性，并在较高剂量下具有毒性。

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