THE EFFICACY OF MARINE NATURAL PRODUCTS AGAINST PLASMODIUM FALCIPARUM
THE EFFICACY OF MARINE NATURAL PRODUCTS AGAINST PLASMODIUM FALCIPARUM
复制标题
DOI：
10.1645/20-93
复制
发表时间：
2021-03-01
影响因子：
1.3
通讯作者：
Kato, Kentaro
中科院分区：
文献类型：
--
作者：
Goto, Yukihiro;Kamihira, Rie;Kato, Kentaro
疟疾仍然是世界上最重要的传染病之一。仅2017年，约有2.19亿人感染疟疾，43.5万人死于疟疾。在东南亚，引起恶性疟疾的恶性疟原虫对青蒿素(ART)产生了抗药性；因此，迫切需要新的抗疟疾药物。一些优秀的抗疟疾药物，如奎宁和ART，最初是从植物中获得的。因此，我们分析了海洋天然产物的抗疟疾作用，以寻找新的抗疟疾药物。我们使用疟疾生长抑制实验来确定海洋生物衍生化合物的抗疟疾能力和半最大抑制浓度(IC50)。三个化合物(kapakahine A、kapakahine B和kulolide-1)显示出抗疟疾作用，而一个化合物(Kapakahine F)对DD2克隆显示出选择性抗疟疾作用。虽然这些化合物的IC50值大于ART，但它们对恶性疟原虫的效力足以作为可能的药物线索进行进一步研究。
Malaria remains one of the most important infectious diseases in the world. In 2017 alone, approximately 219 million people were infected with malaria, and 435,000 people died of this disease. Plasmodium falciparum, which causes falciparum malaria, is becoming resistant to artemisinin (ART) in Southeast Asia; therefore, new antimalarial drugs are urgently needed. Some excellent antimalarial drugs, such as quinine and ART, were originally obtained from plants. Hence, we analyzed the antimalarial effects of marine natural products to find new antimalarial agents. We used a malaria growth inhibition assay to determine the antimalarial ability and half-maximal inhibitory concentration (IC50) values of the marine organism-derived compounds. Three compounds (kapakahine A, kapakahine B, and kulolide-1) showed antimalarial effects, and one (kapakahine F) showed selective antimalarial effects on the Dd2 clone. Although the IC50 values obtained for these compounds were greater than that of ART, their potency against P. falciparum is sufficient to warrant further investigation of these compounds as possible drug leads.