hs-1793 and kojic-acid

hs-1793 has been researched along with kojic-acid* in 2 studies

Other Studies

2 other study(ies) available for hs-1793 and kojic-acid

Article	Year
Syntheses of hydroxy substituted 2-phenyl-naphthalenes as inhibitors of tyrosinase. Bioorganic & medicinal chemistry letters, 2007, Jan-15, Volume: 17, Issue:2 Oxyresveratrol and resveratrol, with hydroxy substituted trans-stilbene structure, exert potent inhibitory effects on cyclooxygenase, rat liver mitochondrial ATPase activity, and tyrosinase. As the isosteres of oxyresveratrol, a new family of hydroxyl substituted phenyl-naphthalenes were synthesized to show excellent inhibition of mushroom tyrosinase. Compound 10, which is isostere of resveratrol, showed IC50 value of 16.52 microM in mushroom tyrosinase activity. As compared to this, the reference compound, resveratrol, showed IC50 value of 55.61 microM. Compound 4, which is isostere of oxyresveratrol, showed IC50 value of 0.49 microM. Among the other three derivatives, compound 13 showed IC50 value of 0.034 microM. Topics: Agaricales; Crystallography, X-Ray; Dealkylation; Enzyme Inhibitors; Hydroquinones; Indicators and Reagents; Magnetic Resonance Spectroscopy; Mass Spectrometry; Models, Molecular; Monophenol Monooxygenase; Morus; Naphthalenes; Pyrones; Resveratrol; Stilbenes	2007
4-(6-Hydroxy-2-naphthyl)-1,3-bezendiol: a potent, new tyrosinase inhibitor. Biological & pharmaceutical bulletin, 2007, Volume: 30, Issue:9 Tyrosinase is a key enzyme for melanin biosynthesis and known to be sensitive to ultraviolet light in the presence of oxygen. Therefore, finding effective tyrosinase inhibitors, either from synthetic or natural sources, can be beneficial in the treatment of melanin-related disorders. We synthesized 4-(6-hydroxy-2-naphthyl)-1,3-bezendiol (HNB), a new family of hydroxyl substituted phenyl naphthalenes, as the isosteres of oxyresveratrol. This study investigated inhibitory effects of HNB on tyrosinase activity. HNB inhibited mushroom tyrosinase with an IC(50) value of 0.07 microM, which is more potent than the anti-tyrosinase activity of kojic acid (IC(50)=38.24), a well-known tyrosinase inhibitor. The kinetic analysis of tyrosinase inhibition revealed that HNB is a competitive inhibitor (K(i) 4.78 x 10(-9) M at 0.125 microM and K(i) 6.21 x 10(-9) M at 0.25 microM). We further found that HNB also inhibited melanin production in B16F10 melanoma cells (B16 cells). In addition to tyrosinase inhibiting activity, melanin biosynthesis was inhibited by HNB in the B16F10 cells. These data strongly suggest that HNB can suppress the production of melanin via the modulation of tyrosinase activity. Topics: Agaricales; Animals; Cell Survival; Dose-Response Relationship, Drug; Enzyme Inhibitors; Hydroquinones; Kinetics; Melanins; Melanoma, Experimental; Mice; Monophenol Monooxygenase; Naphthalenes; Naphthols; Phenols; Pyrones; Resorcinols; Resveratrol; Stilbenes	2007

Article

Year

Syntheses of hydroxy substituted 2-phenyl-naphthalenes as inhibitors of tyrosinase.

Bioorganic & medicinal chemistry letters, 2007, Jan-15, Volume: 17, Issue:2

Oxyresveratrol and resveratrol, with hydroxy substituted trans-stilbene structure, exert potent inhibitory effects on cyclooxygenase, rat liver mitochondrial ATPase activity, and tyrosinase. As the isosteres of oxyresveratrol, a new family of hydroxyl substituted phenyl-naphthalenes were synthesized to show excellent inhibition of mushroom tyrosinase. Compound 10, which is isostere of resveratrol, showed IC50 value of 16.52 microM in mushroom tyrosinase activity. As compared to this, the reference compound, resveratrol, showed IC50 value of 55.61 microM. Compound 4, which is isostere of oxyresveratrol, showed IC50 value of 0.49 microM. Among the other three derivatives, compound 13 showed IC50 value of 0.034 microM.

Topics: Agaricales; Crystallography, X-Ray; Dealkylation; Enzyme Inhibitors; Hydroquinones; Indicators and Reagents; Magnetic Resonance Spectroscopy; Mass Spectrometry; Models, Molecular; Monophenol Monooxygenase; Morus; Naphthalenes; Pyrones; Resveratrol; Stilbenes

2007

4-(6-Hydroxy-2-naphthyl)-1,3-bezendiol: a potent, new tyrosinase inhibitor.

Biological & pharmaceutical bulletin, 2007, Volume: 30, Issue:9

Tyrosinase is a key enzyme for melanin biosynthesis and known to be sensitive to ultraviolet light in the presence of oxygen. Therefore, finding effective tyrosinase inhibitors, either from synthetic or natural sources, can be beneficial in the treatment of melanin-related disorders. We synthesized 4-(6-hydroxy-2-naphthyl)-1,3-bezendiol (HNB), a new family of hydroxyl substituted phenyl naphthalenes, as the isosteres of oxyresveratrol. This study investigated inhibitory effects of HNB on tyrosinase activity. HNB inhibited mushroom tyrosinase with an IC(50) value of 0.07 microM, which is more potent than the anti-tyrosinase activity of kojic acid (IC(50)=38.24), a well-known tyrosinase inhibitor. The kinetic analysis of tyrosinase inhibition revealed that HNB is a competitive inhibitor (K(i) 4.78 x 10(-9) M at 0.125 microM and K(i) 6.21 x 10(-9) M at 0.25 microM). We further found that HNB also inhibited melanin production in B16F10 melanoma cells (B16 cells). In addition to tyrosinase inhibiting activity, melanin biosynthesis was inhibited by HNB in the B16F10 cells. These data strongly suggest that HNB can suppress the production of melanin via the modulation of tyrosinase activity.

Topics: Agaricales; Animals; Cell Survival; Dose-Response Relationship, Drug; Enzyme Inhibitors; Hydroquinones; Kinetics; Melanins; Melanoma, Experimental; Mice; Monophenol Monooxygenase; Naphthalenes; Naphthols; Phenols; Pyrones; Resorcinols; Resveratrol; Stilbenes

2007