Abstract
Ascomycin 2, a close analogue of the immunosuppressant FK506 1, was modified to incorporate a hydroxyl group at the C-33 position. This increased the aqueous solubility of ascomycin by a hundred-fold at pH 7.4 and by approximately 300-fold at pH 6.5. Ascomycin 3 also exhibited an excellent immunosuppressive activity in vitro, as tested in a human mixed lymphocyte proliferation (HuMLR) assay, and in vivo using a rat popliteal lymph node (rPLN) hyperplasia assay.
MeSH terms
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Animals
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Humans
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Hydrogen-Ion Concentration
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Hyperplasia
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Immunosuppressive Agents / chemical synthesis*
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Immunosuppressive Agents / chemistry
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Immunosuppressive Agents / pharmacology
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Indicators and Reagents
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Lymph Nodes / drug effects
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Lymph Nodes / pathology
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Lymphocyte Activation / drug effects*
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Lymphocyte Culture Test, Mixed
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Molecular Conformation
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Molecular Structure
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Rats
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Solubility
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Structure-Activity Relationship
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Tacrolimus / analogs & derivatives*
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Tacrolimus / chemical synthesis
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Tacrolimus / chemistry
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Tacrolimus / pharmacology
Substances
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Immunosuppressive Agents
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Indicators and Reagents
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immunomycin
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Tacrolimus