Sheptide A: an antimalarial cyclic pentapeptide from a fungal strain in the Herpotrichiellaceae
Year: 2023
Type: article
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.
Source: The Journal of Antibiotics
Language: English
Subfield: Pharmacology
Field: Medicine
Domain: Health Sciences
Open Access status: hybrid
Estimated APC paid: $4,190
Funders: National Science Foundation, U.S. Department of Health and Human Services, University of Georgia, Georgia Research Alliance, National Institutes of Health, National Cancer Institute, National Institute of Allergy and Infectious Diseases, National Institute of Environmental Health Sciences, Division of Electrical, Communications and Cyber Systems
Awards: G1593674991, Anti-Malarial Drug Leads from Fungi, NNCI: Southeastern Nanotechnology Infrastructure Corridor (SENIC), G410516402, G4528073890, G4551646662, G4590786937, G6233277208, G8666499804, G9000301046, ChicAgo Center for Health and EnvironmenT (CACHET), Discovery of Anticancer Agents of Diverse Natural Origin
OpenAlex ID: W4386892444