A newly synthesized,potent tyrosinase inhibitor: 5-(6-Hydroxy-2-naphthyl)-1,2,3-benzenetriol |
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| Authors: | Jehun Choi Sung Jin Bae Young Mi Ha Jae Kyung No Eun Kyeong Lee Jun Sik Lee Suhee Song Hyojin Lee Hongsuk Suh Byung Pal Yu Hae Young Chung |
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| Institution: | 1. Department of Pharmacy and Molecular Inflammation Research Center for Aging Intervention (MRCA), Pusan National University, Gumjung-gu, Busan 609-735, Republic of Korea;2. Department of Cosmetology, Pusan Women’s College, Busan, Republic of Korea;3. Department of Microbiology and Immunology, College of Medicine, BK21 Medical Science Education Center, Pusan National University, Busan 609-739, Republic of Korea;4. Department of Chemistry and Chemistry Institute for Functional Materials, Pusan National University, Busan 609-735, Republic of Korea;5. Department of Physiology, The University of Texas Health Science Center at San Antonio, San Antonio, TX 78229-3900, USA |
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| Abstract: | In searching for new agents with a depigmenting effect, we synthesized a derivative of resveratrol, 5-(6-hydroxy-2-naphthyl)-1,2,3-benzenetriol (5HNB) with a potent tyrosinase inhibitory activity. 5HNB inhibited mushroom tyrosinase with an IC50 value of 2.95 μM, which is more potent than the well-known anti-tyrosinase activity of kojic acid (IC50 = 38.24). The results of the enzymatic inhibition kinetics by Lineweaver–Burk analysis indicated 5HNB inhibits tyrosinase non-competitively when l-tyrosine was used as the substrate. Based on the strong inhibitory action of 5HNB, it is expected that 5HNB can suppress melanin production in which tyrosinase plays the essential role. Our expectation was confirmed by the experimentations with B16 melanoma cells in which 5HNB inhibited melanin production. We propose that 5HNB might have skin-whitening effects as well as therapeutic potential for treating skin pigmentation disorders. |
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