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Fungal Metabolite Asperaculane B Inhibits Malaria Infection and Transmission
Molecules ( IF 4.6 ) Pub Date : 2020-07-01 , DOI: 10.3390/molecules25133018
Guodong Niu 1 , Yue Hao 2 , Xiaohong Wang 1 , Jin-Ming Gao 3 , Jun Li 1
Affiliation  

Mosquito-transmitted Plasmodium parasites cause millions of people worldwide to suffer malaria every year. Drug-resistant Plasmodium parasites and insecticide-resistant mosquitoes make malaria hard to control. Thus, the next generation of antimalarial drugs that inhibit malaria infection and transmission are needed. We screened our Global Fungal Extract Library (GFEL) and obtained a candidate that completely inhibited Plasmodium falciparum transmission to Anopheles gambiae. The candidate fungal strain was determined as Aspergillus aculeatus. The bioactive compound was purified and identified as asperaculane B. The concentration of 50% inhibition on P. falciparum transmission (IC50) is 7.89 µM. Notably, asperaculane B also inhibited the development of asexual P. falciparum with IC50 of 3 µM, and it is nontoxic to human cells. Therefore, asperaculane B is a new dual-functional antimalarial lead that has the potential to treat malaria and block malaria transmission.

中文翻译:

真菌代谢物 Asperaculane B 抑制疟疾感染和传播

蚊子传播的疟原虫寄生虫每年导致全世界数百万人患上疟疾。抗药性疟原虫和抗杀虫剂的蚊子使疟疾难以控制。因此,需要抑制疟疾感染和传播的下一代抗疟药物。我们筛选了我们的全球真菌提取物库 (GFEL) 并获得了一个完全抑制恶性疟原虫向冈比亚按蚊传播的候选物。候选真菌菌株被确定为棘孢曲霉。生物活性化合物被纯化并鉴定为 asperaculane B。对恶性疟原虫传播的 50% 抑制浓度 (IC50) 为 7.89 µM。值得注意的是,asperaculane B 还能抑制无性恶性疟原虫的发育,IC50 为 3 µM,对人体细胞无毒。所以,
更新日期:2020-07-01
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