engleski

Umbelliferone-thiazolidinedione hybrids as potent mushroom tyrosinase inhibitors

In search for the potent mushroom tyrosinase inhibitors, six umbelliferone-thiazolidinedione hybrids, as well as their constitutive compounds, (5-substituted benzylidene)- thiazolidine-2, 4-diones were examined on their inhibitory activity both, on monophenolase and diphenolase activity. The results showed that all tested compounds exhibited tyrosinase inhibition at 100 mM concentration, but diphenolase activities were found less inhibited than monophenolase. Umbelliferone- thiazolidinedione hybrids showed the greater monophenolase and diphenolase inhibitory activity than the constitutive thiazolidinediones. The most potent inhibitors of tyrosinase were umbelliferone- thiazolidinedione hybrids bearing 4- or 3- hydroxyphenyl moiety at position five of thiazolidinedione ring, showing IC50 of 0.17 and 0.35 mM for monophenolase, and 0.25 and 1.63 mM for diphenolase activity, respectively. Obtained data indicates importance of umbelliferone moiety for increase of inhibitory activity of thiazolidinediones bearing 3- hydroxyphenyl and 4-hydroxyphenyl moiety, and vice versa.

mushroom tyrosinase ; inhibition ; umbelliferone ; thiazolidinedione

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