Pluraflavins, potent antitumor antibiotics from Saccharothrix sp. DSM 12931
| Autor: | Elizabeth Cashmen, Marian Paul Segeth, Joachim Wink, Dietmar Schummer, Gerhard Seibert, Jordan Birgit Dr, Heinrich Decker, Martin Knauf, Barbone Francis P, Laszlo Vertesy, Klaus Ehrlich |
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| Rok vydání: | 2001 |
| Předmět: |
Magnetic Resonance Spectroscopy
Stereochemistry medicine.drug_class Antibiotics Epoxide Anthraquinones Biology Mass Spectrometry chemistry.chemical_compound Drug Discovery Actinomycetales medicine Side chain Tumor Cells Cultured Humans IC50 Pharmacology Antibiotics Antineoplastic Molecular Structure Biological activity Nuclear magnetic resonance spectroscopy In vitro Culture Media chemistry Biochemistry Two-dimensional nuclear magnetic resonance spectroscopy Cell Division |
| Zdroj: | The Journal of antibiotics. 54(9) |
| ISSN: | 0021-8820 |
| Popis: | The new pluramycin-type antibiotics pluraflavin A, C43H54N2O14, pluraflavin B, C43H56N2O15, and pluraflavin E, C36H41NO14 were isolated from cultures of the Saccharothrix species DSM 12931. The structures of the novel compounds were elucidated with the aid of 2D NMR and mass spectrometric investigations. The characteristic structural element of pluraflavins A and B is an additional 4-epi-vancosamine unit at position 13 of the anthraquinone-gamma-pyrone ring system. Pluraflavin E has a carboxyl group in this position. Pluraflavin A has a reactive dimethyl epoxide side chain at position 2 of the anthraquinone-gamma-pyrone aglycon, which may explain the high activity of the antibiotic. The outstanding biological characteristic of pluraflavin A is its powerful, organ-dependent cytostatic action: the IC50 in the colon carcinoma proliferation assay is in the subnanomolar range. |
| Databáze: | OpenAIRE |
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