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Cymbimicin A and B, two novel cyclophilin-binding structures isolated from actinomycetes
T Fehr1, V F Quesniaux, J J Sanglier
1Novartis Pharma Inc., Preclinical Research, Basel, Switzerland.
The Journal of Antibiotics
|May 21, 1998
Summary
Two new compounds, cymbimicins A and B, were discovered from Micromonospora sp. Cymbimicin A shows high affinity for cyclophilin A, offering potential for new therapeutic agents.
Area of Science:
- Microbiology
- Natural Products Chemistry
- Biochemistry
Background:
- Actinomycetes are a source of novel bioactive compounds.
- Cyclophilins are important targets in various diseases.
- Screening for cyclophilin-binding metabolites can yield new drug leads.
Purpose of the Study:
- To isolate and characterize novel cyclophilin-binding metabolites from Micromonospora sp.
- To determine the binding affinities of the novel compounds to cyclophilin A.
- To elucidate the structures of the isolated metabolites.
Main Methods:
- Fermentation of Micromonospora sp.
- Isolation and purification of metabolites using chromatographic techniques.
- Structure elucidation using spectroscopic methods (e.g., NMR, Mass Spectrometry).
- Binding assays to determine affinity for cyclophilin A.
Main Results:
- Two novel metabolites, cymbimicins A and B, were successfully isolated.
- Cymbimicin A exhibited a high binding affinity to cyclophilin A, six-fold lower than cyclosporin A.
- Cymbimicin B demonstrated a lower binding affinity, approximately 100 times lower than cyclosporin A.
- The taxonomy of the producing strain and the physical/biological properties were described.
Conclusions:
- Cymbimicins A and B are novel cyclophilin-binding metabolites from Micromonospora sp.
- Cymbimicin A represents a promising lead compound for further investigation due to its high binding affinity.
- The discovery highlights the potential of actinomycetes for identifying new therapeutic agents targeting cyclophilins.