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Microbial transformation of macrocyclic trichothecenes.
1Department of Chemistry, University of Maryland, College Park, Maryland 20742.
Applied and Environmental Microbiology
|August 1, 1983
Summary
Rhizopus arrhizus transforms verrucarins A and B into more potent 16-hydroxy derivatives. These modified compounds demonstrated significantly enhanced anti-leukemia activity in vivo against P388 mouse leukemia.
Area of Science:
- Microbiology
- Natural Products Chemistry
- Pharmacology
Background:
- Verrucarins A and B are mycotoxins with known biological activities.
- The fungus Rhizopus arrhizus is known for its metabolic capabilities.
Purpose of the Study:
- To investigate the biotransformation of verrucarin A and verrucarin B by Rhizopus arrhizus.
- To evaluate the anti-leukemia activity of the resulting metabolites.
Main Methods:
- Incubation of verrucarin A and verrucarin B with resting cultures of Rhizopus arrhizus (ATCC 11145).
- Identification of transformation products using analytical techniques.
- In vivo testing of compounds against P388 mouse leukemia model.
Main Results:
- Rhizopus arrhizus transformed verrucarin A into 16-hydroxyverrucarin A.
- Verrucarin B was transformed into 16-hydroxyverrucarin B and 3'-hydroxyverrucarin A.
- The 16-hydroxy derivatives exhibited markedly increased anti-leukemia activity compared to the parent compounds.
Conclusions:
- Rhizopus arrhizus effectively biotransforms verrucarins A and B into novel derivatives.
- The 16-hydroxy metabolites of verrucarins A and B possess enhanced anti-leukemia properties.
- This study highlights the potential of microbial biotransformation for generating more active pharmaceutical compounds.