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KMID : 0043320120350091533
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Archives of Pharmacal Research
2012 Volume.35 No. 9 p.1533 ~ p.1541
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Synthesis and biological evaluation of bergenin analogues as mushroom tyrosinase inhibitors
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Kashima Yusei
Miyazawa Mitsuo
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Abstract
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In this manuscript, we synthesized a series of bergenin analogues, analyzed their structural importance for two biologic activities (anitioxidant activity (ORAC) and mushroom tyrosinase inhibitory activity). Among them, compound 5 which contains catechol moiety exhibited the most antioxidant activity (3.75 μmol of Trolox equiv. per μmol of 5). Furthermore, compound 5 was found to be the most potent (IC50 value = 17.5 ± 0.04 μM) when compared with the standard tyrosinase inhibitors of arbutin (IC50 value = 221.8 ± 1.9 μM) and kojic acid (IC50 value = 46.6 ± 3.8 μM). The bergenin moiety, the ester linkage, and benzoic acid moiety of bergenin derivatives affected two biologic activities. Tyrosinase inhibitory activity was affected by substituents of benzoic acid moiety. This manuscript provides a good foundation for the design and development of new tyrosinase inhibitors.
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KEYWORD
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Bergenin, Bergenin derivatives, Tyrosinase inhibitor, Antioxidant activity, Structureactivity relationship
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