Abstract
A small library of kojic acid-tripeptides (Ko-X1X2X3) was prepared by solid-phase parallel synthesis and assayed to evaluate their tyrosinase inhibitory activity. Most of the kojic acid-tripeptides showed better activities than kojic acid. Kojic acid-FWY was the best compound, and it exhibited 100-fold tyrosinase inhibitory activity compared with kojic acid. In addition, their storage stabilities were approximately 15 times higher and their toxicity was lower than that of kojic acid.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Cell Line, Tumor
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Cell Survival / drug effects
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Drug Stability
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / pharmacology
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Enzyme Inhibitors / toxicity
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Humans
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Inhibitory Concentration 50
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Melanocytes / drug effects
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Monophenol Monooxygenase / antagonists & inhibitors*
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Oligopeptides / chemical synthesis
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Oligopeptides / pharmacology*
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Oligopeptides / toxicity
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Peptide Library
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Pyrones / chemical synthesis
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Pyrones / pharmacology
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Pyrones / toxicity
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Structure-Activity Relationship
Substances
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Enzyme Inhibitors
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Oligopeptides
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Peptide Library
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Pyrones
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kojic acid
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Monophenol Monooxygenase