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Understanding the Antiplasmodial Action of Resistance-Refractory Xanthoquinodin A1.
Collins, Jennifer E; Jiang, Tiantian; Lee, Jin Woo; Wendt, Karen; Nardella, Flore; Jeon, Jin; Paes, Raphaella; Santos, Natalia Mojica; Rocamora, Frances; Chang, Maya; Schaefer, Samuel; Cichewicz, Robert H; Winzeler, Elizabeth A; Chakrabarti, Debopam.
Afiliação
  • Collins JE; Division of Molecular Microbiology, Burnett School of Biomedical Sciences, University of Central Florida, 12722 Research Parkway, Orlando, Florida 32826, United States.
  • Jiang T; Department of Pediatrics, School of Medicine, University of California San Diego, La Jolla, California 92093, United States.
  • Lee JW; College of Pharmacy, Duksung Women's University, Seoul 01369, Republic of Korea.
  • Wendt K; Department of Chemistry and Biochemistry, Institute for Natural Products Applications & Research Technologies, University of Oklahoma, 101 Stephenson Parkway, Norman, Oklahoma 73019, United States.
  • Nardella F; Division of Molecular Microbiology, Burnett School of Biomedical Sciences, University of Central Florida, 12722 Research Parkway, Orlando, Florida 32826, United States.
  • Jeon J; Department of Microbiology and Immunology, Columbia University Irving Medical Center, New York, New York 10032, United States.
  • Paes R; Division of Molecular Microbiology, Burnett School of Biomedical Sciences, University of Central Florida, 12722 Research Parkway, Orlando, Florida 32826, United States.
  • Santos NM; Division of Molecular Microbiology, Burnett School of Biomedical Sciences, University of Central Florida, 12722 Research Parkway, Orlando, Florida 32826, United States.
  • Rocamora F; Department of Pediatrics, School of Medicine, University of California San Diego, La Jolla, California 92093, United States.
  • Chang M; Department of Pediatrics, School of Medicine, University of California San Diego, La Jolla, California 92093, United States.
  • Schaefer S; Department of Pediatrics, School of Medicine, University of California San Diego, La Jolla, California 92093, United States.
  • Cichewicz RH; Department of Chemistry and Biochemistry, Institute for Natural Products Applications & Research Technologies, University of Oklahoma, 101 Stephenson Parkway, Norman, Oklahoma 73019, United States.
  • Winzeler EA; Department of Pediatrics, School of Medicine, University of California San Diego, La Jolla, California 92093, United States.
  • Chakrabarti D; Division of Molecular Microbiology, Burnett School of Biomedical Sciences, University of Central Florida, 12722 Research Parkway, Orlando, Florida 32826, United States.
ACS Infect Dis ; 10(6): 2276-2287, 2024 Jun 14.
Article em En | MEDLINE | ID: mdl-38810215
ABSTRACT
Our previous work identified a series of 12 xanthoquinodin analogues and 2 emodin-dianthrones with broad-spectrum activities against Trichomonas vaginalis, Mycoplasma genitalium, Cryptosporidium parvum, and Plasmodium falciparum. Analyses conducted in this study revealed that the most active analogue, xanthoquinodin A1, also inhibits Toxoplasma gondii tachyzoites and the liver stage of Plasmodium berghei, with no cross-resistance to the known antimalarial targets PfACS, PfCARL, PfPI4K, or DHODH. In Plasmodium, inhibition occurs prior to multinucleation and induces parasite death following 12 h of compound exposure. This moderately fast activity has impeded resistance line generation, with xanthoquinodin A1 demonstrating an irresistible phenotype in both T. gondii and P. falciparum.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Plasmodium berghei / Plasmodium falciparum / Toxoplasma / Resistência a Medicamentos / Antimaláricos Idioma: En Ano de publicação: 2024 Tipo de documento: Article

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Plasmodium berghei / Plasmodium falciparum / Toxoplasma / Resistência a Medicamentos / Antimaláricos Idioma: En Ano de publicação: 2024 Tipo de documento: Article