Leporizines A–C: Epithiodiketopiperazines Isolated from an Aspergillus Species
| Autor: | Ricardo F. Reategui, Grant J Carr, Janet Adolphson, Ryan Newell, Joshua Rhea, Michele Luche, Ulla Mocek, John Rabenstein, Kathryn Waikins |
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| Rok vydání: | 2013 |
| Předmět: |
Stereochemistry
Cystic Fibrosis Transmembrane Conductance Regulator Pharmaceutical Science Antineoplastic Agents Diketopiperazines Respiratory Mucosa Biology Analytical Chemistry Microbiology Drug Discovery Humans Nuclear Magnetic Resonance Biomolecular Pharmacology Aspergillus species Aspergillus Molecular Structure Montana Strain (chemistry) Organic Chemistry Hep G2 Cells biology.organism_classification Complementary and alternative medicine Mutation Molecular Medicine Drug Screening Assays Antitumor Two-dimensional nuclear magnetic resonance spectroscopy |
| Zdroj: | Journal of Natural Products. 76:1523-1527 |
| ISSN: | 1520-6025 0163-3864 |
| DOI: | 10.1021/np300894y |
| Popis: | Three new compounds named leporizines A-C have been isolated from an Aspergillus sp. strain. Their structures were elucidated by analysis of 1D and 2D NMR spectra. Leporizines A and B were isolated during dereplication of hits from a high-throughput screening campaign for correctors of the cystic fibrosis transmembrane conductance regulator (CFTR), and leporizine C was isolated while preparing additional material for characterization of leporizines A and B. CFTR activity observed for leporizines A and B was highly correlated with cell toxicity and was determined to be a nonspecific effect. Leporizine C was not cytotoxic to cells and did not elicit a response in the CFTR assays. To the best of our knowledge, leporizines A-C represent the first examples of this unusual epithiodiketopiperazine skeleton. |
| Databáze: | OpenAIRE |
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