Solid-phase synthesis of kojic acid-tripeptides and their tyrosinase inhibitory activity, storage stability, and toxicity.
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.
Kim
Hanyoung
H
School of Chemical Engineering, Seoul National University, Seoul 151-744, South Korea.
Choi
Jaehui
J
Cho
Jin Ku
JK
Kim
Sun Yeou
SY
Lee
Yoon-Sik
YS
D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004355:Drug Stability; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology / Q000633:toxicity; D006801:Humans; D020128:Inhibitory Concentration 50; D008544:Melanocytes / Q000187:drug effects; D014442:Monophenol Monooxygenase / Q000037:antagonists & inhibitors*; D009842:Oligopeptides / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity; D019151:Peptide Library; D011753:Pyrones / Q000138:chemical synthesis / Q000494:pharmacology / Q000633:toxicity; D013329:Structure-Activity Relationship
D004791:Enzyme Inhibitors; D009842:Oligopeptides; D019151:Peptide Library; D011753:Pyrones; C011890:kojic acid; D014442:Monophenol Monooxygenase