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Formulation and Characterization of Bioactive Agent Containing Nanodisks
Published on: March 17, 2023
Kozupeptins, Antimalarial Agents Produced by Paracamarosporium Species: Isolation, Structural Elucidation, Total
Yumi Hayashi1, Wataru Fukasawa1, Tomoyasu Hirose1,2
1Graduate School of Infection Control Sciences , Kitasato University , 5-9-1 Shirokane , Minato-ku , Tokyo 108-8641 , Japan.
Abstract:
Kozupeptins A and B, novel antimalarial lipopeptides, were isolated from the culture broths of Paracamarosporium sp. FKI-7019. They exhibited potent antimalarial activity against chloroquine-sensitive and -resistant Plasmodium falciparum strains in vitro. The structural elucidation was accomplished by a combination of spectroscopic analyses and chemical approaches including a total synthesis of kozupeptin A. Synthetic kozupeptin A demonstrated a therapeutic effect in vivo, and an intermediate exhibited much higher antimalarial activity than kozupeptin A.
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