4.7 Article

Koshidacins A and B, Antiplasmodial Cyclic Tetrapeptides from the Okinawan Fungus Pochonia boninensis FKR-0564

Journal

JOURNAL OF NATURAL PRODUCTS
Volume 85, Issue 11, Pages 2641-2649

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acs.jnatprod.2c00719

Keywords

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Funding

  1. Okinawan Create Leading Projects in Growing Fields 20172019
  2. Okinawan Create Leading Projects in Growing Fields 2020-2021, OKINAWA Prefectural Government
  3. Platform Project for Supporting Drug Discovery and Life Science Research (Basis for Supporting Innovative Drug Discovery and Life Science Research (BINDS)) from AMED [JP21am0101096, JP22ama121035]
  4. JSPS KAKENHI [JP20K07106]

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Two new antiplasmodial peptides, named koshida-cins A and B, were discovered from the culture broth of the Okinawan fungus Pochonia boninensis FKR-0564. Both compounds showed moderate in vitro antiplasmodial activity against Plasmodium falciparum strains, and compound 2 demonstrated significant suppression of malaria parasites in vivo.
Two new antiplasmodial peptides, named koshida-cins A (1) and B (2), were discovered from the culture broth of the Okinawan fungus Pochonia boninensis FKR-0564. Their structures, including absolute configurations, were elucidated by a combination of spectroscopic methods and chemical derivatiza-tion. Both compounds showed moderate in vitro antiplasmodial activity against Plasmodium falciparum strains, with IC50 values ranging from 17.1 to 0.83 mu M. In addition, compound 2 suppressed 41% of malaria parasites in vivo when administered intraperitoneally at a dose of 30 mg/kg/day for 4 days.

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