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Sheptide A: an antimalarial cyclic pentapeptide from a fungal strain in the Herpotrichiellaceae.
Shepherd, Robert A; Earp, Cody E; Cank, Kristof B; Raja, Huzefa A; Burdette, Joanna; Maher, Steven P; Marin, Adriana A; Ruberto, Anthony A; Mai, Sarah Lee; Darveaux, Blaise A; Kyle, Dennis E; Pearce, Cedric J; Oberlies, Nicholas H.
  • Shepherd RA; Department of Chemistry & Biochemistry, University of North Carolina at Greensboro, Greensboro, NC, USA.
  • Earp CE; Department of Chemistry & Biochemistry, University of North Carolina at Greensboro, Greensboro, NC, USA.
  • Cank KB; Department of Chemistry & Biochemistry, University of North Carolina at Greensboro, Greensboro, NC, USA.
  • Raja HA; Department of Chemistry & Biochemistry, University of North Carolina at Greensboro, Greensboro, NC, USA.
  • Burdette J; Department of Pharmaceutical Sciences, University of Illinois Chicago, Chicago, IL, USA.
  • Maher SP; Center for Tropical & Emerging Global Diseases, University of Georgia, Athens, GA, USA.
  • Marin AA; Center for Tropical & Emerging Global Diseases, University of Georgia, Athens, GA, USA.
  • Ruberto AA; Center for Tropical & Emerging Global Diseases, University of Georgia, Athens, GA, USA.
  • Mai SL; Center for Tropical & Emerging Global Diseases, University of Georgia, Athens, GA, USA.
  • Darveaux BA; Mycosynthetix, Inc., Hillsborough, NC, USA.
  • Kyle DE; Center for Tropical & Emerging Global Diseases, University of Georgia, Athens, GA, USA.
  • Pearce CJ; Mycosynthetix, Inc., Hillsborough, NC, USA.
  • Oberlies NH; Department of Chemistry & Biochemistry, University of North Carolina at Greensboro, Greensboro, NC, USA. n_oberli@uncg.edu.
J Antibiot (Tokyo) ; 76(11): 642-649, 2023 11.
Article en En | MEDLINE | ID: mdl-37731043
ABSTRACT
As part of ongoing efforts to isolate biologically active fungal metabolites, a cyclic pentapeptide, sheptide A (1), was discovered from strain MSX53339 (Herpotrichiellaceae). The structure and sequence of 1 were determined primarily by analysis of 2D NMR and HRMS/MS data, while the absolute configuration was assigned using a modified version of Marfey's method. In an in vitro assay for antimalarial potency, 1 displayed a pEC50 value of 5.75 ± 0.49 against malaria-causing Plasmodium falciparum. Compound 1 was also tested in a counter screen for general cytotoxicity against human hepatocellular carcinoma (HepG2), yielding a pCC50 value of 5.01 ± 0.45 and indicating a selectivity factor of ~6. This makes 1 the third known cyclic pentapeptide biosynthesized by fungi with antimalarial activity.
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Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Ascomicetos / Malaria / Antimaláricos Límite: Humans Idioma: En Año: 2023 Tipo del documento: Article
Texto completo
Imprimir
XML
PubMed Links
Search on Google

Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Ascomicetos / Malaria / Antimaláricos Límite: Humans Idioma: En Año: 2023 Tipo del documento: Article