National Research Center for Protozoan Diseases, Obihiro University of Agriculture and Veterinary Medicine, Nishi 2-13 Inada-cho, Obihiro, Hokkaido 080-8555, Japan.
Department of Chemistry and Biochemistry, Graduate School of Advanced Science and Engineering, Waseda University, 3-4-1 Okubo, Shinjuku-ku, Tokyo 169-8555, Japan.
J Parasitol. 2021 Mar 1;107(2):284-288. doi: 10.1645/20-93.
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.
疟疾仍然是世界上最重要的传染病之一。仅在 2017 年，就有约 2.19 亿人感染疟疾，43.5 万人死于这种疾病。引起恶性疟疾的疟原虫对东南亚的青蒿素（ART）产生了抗药性；因此，急需新的抗疟药物。一些优秀的抗疟药物，如奎宁和 ART，最初是从植物中提取的。因此，我们分析了海洋天然产物的抗疟作用，以寻找新的抗疟药物。我们使用疟疾生长抑制试验来确定海洋生物衍生化合物的抗疟能力和半最大抑制浓度（IC50）值。三种化合物（卡巴卡丁 A、卡巴卡丁 B 和库洛内酯-1）表现出抗疟作用，一种（卡巴卡丁 F）对 Dd2 克隆表现出选择性抗疟作用。虽然这些化合物的 IC50 值大于 ART，但它们对疟原虫的效力足以证明进一步研究这些化合物作为可能的药物先导是合理的。
