Publication: Metacytofilin has potent anti-malarial activity
Issued Date
2021-04-01
Resource Type
ISSN
18730329
13835769
13835769
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2-s2.0-85097801031
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Mahidol University
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SCOPUS
Bibliographic Citation
Parasitology International. Vol.81, (2021)
Suggested Citation
Arpron Leesombun, Masatomi Iijima, Baldorj Pagmadulam, Banzragchgarav Orkhon, Hiroyasu Doi, Kunio Issiki, Ryuichi Sawa, Coh ichi Nihei, Yoshifumi Nishikawa Metacytofilin has potent anti-malarial activity. Parasitology International. Vol.81, (2021). doi:10.1016/j.parint.2020.102267 Retrieved from: https://repository.li.mahidol.ac.th/handle/20.500.14594/77307
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Title
Metacytofilin has potent anti-malarial activity
Abstract
Metacytofilin (MCF) was isolated from the fungus Metarhizium sp. TA2759. Although MCF possesses anti-Toxoplasma activity, the effects of this compound against other parasites are unknown. Here, we evaluated the in vitro anti-malarial activity of MCF against the 3D7 strain and the chloroquine-resistant K1 strain of Plasmodium falciparum. The half maximal inhibitory concentrations (IC50) of MCF against the 3D7 and K-1 strains following culture for 48 h were 666 nM and 605 nM, respectively. Artemisinin was more potent than MCF against both strains (3D7 IC50: 17.4 nM; K-1 IC50: 18.3 nM), while chloroquine was ineffective against the chloroquine-resistant strain (3D7 IC50: 39.1 nM; K-1 IC50: 1.62 μM). MCF affected the ring stage of the parasites, resulting in their death as shown by spots within red blood cells. MCF also inhibited parasite growth following culture for 72 h (3D7 IC50, 285 nM). Four optical isomers of cyclo[Leu-Phe]-diketopiperazine derivatives with modified methoxy and/or hydroxyl groups lost anti-malarial activity, suggesting that the spatial positions of the methoxy and hydroxyl groups in MCF play an important role in its anti-malarial effects. Together, these data suggest that MCF may represent a promising lead compound for treatment of drug-resistant malarial parasites.