• Journal of Life Science
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• v.31 no.8
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• pp.719-728
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• 2021

Melanin pigments are abundantly distributed in mammalian skin, hair, eyes, and nervous system. Under normal physiological conditions, melanin protects the skin against various environmental stresses and acts as a physiological redox buffer to maintain homeostasis. However, abnormal melanin accumulation results in various hyperpigmentation conditions, such as chloasma, freckles, senile lentigo, and inflammatory pigmentation. Tyrosinase, a copper-containing enzyme, plays an important role in the regulation of the melanin pigment biosynthetic pathway. Although several whitening agents based on tyrosinase inhibition have been developed, their side effects, such as allergies, DNA damage, mutagenesis, and cytotoxicity of melanocytes, limit their applications. In this study, we synthesized 4-chromanone derivatives (MHY compounds) and investigated their ability to inhibit tyrosinase activity. Of these compounds, (E)-3-(4-hydroxybenzylidene)chroman-4-one (MHY1294) more potently inhibited the enzymatic activity of tyrosinase (IC₅₀ = 5.1±0.86 μM) than kojic acid (14.3±1.43 μM), a representative tyrosinase inhibitor. In addition, MHY1294 showed competitive inhibitory action at the catalytic site of tyrosinase and had greater binding affinity at this site than kojic acid. Furthermore, MHY1294 effectively inhibited α-melanocyte stimulating hormone (α-MSH)-induced melanin synthesis and intracellular tyrosinase activity in B16F10 melanoma cells. The results of the present study indicate that MHY1294 may be considered as a candidate pharmacological agent and cosmetic whitening ingredient.

• Journal of the Korean Applied Science and Technology
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• v.40 no.3
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• pp.534-546
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• 2023

In this study, we investigated the antioxidant and anti-winkle activity in human fibroblast cell (CCD-986sk) of Persimmon Leaves (PL) as a cosmetic ingredient. As a result of investigating antioxidant activity through electron-donating ability and ABTS⁺ radical scavenging assay, the PL showed concentration-dependent antioxidant activity similar to ascorbic acid, a control group, at a concentration of 1,000 ㎍/ml. As a result of investigating the anti-wrinkle effect through elastase inhibition and collagenase inhibition assay, the PL showed concentration-dependent antioxidant activity similar to epigallocatechin gallate, a control group, at a concentration of 1,000 ㎍/ml. As a result of measuring the synthesis rate of pro-collagen type I and the inhibition rate of MMP-1 in UVB-induced CCD-986sk cells, the control group EGCG showed a 90.2% pro-collagen synthesis rate at 20 ㎍/ml and PL showed an 88.5% synthesis rate at 30 ㎍/ml. In addition, the inhibition rate of MMP-1 of 33.0% and 40.8% were confirmed in EGCG 20 ㎍/ml and PL 30 ㎍/ml, respectively. As a result of measuring the protein expression of pro-collagen type I and MMP-1 in the PL through western blot, it was confirmed that the protein expression of pro-collagen type I increased, and MMP-1 decreased when the PL was treated together compared to the UVB alone group. According to the above experimental results, it is expected to be used as a natural product material for cosmetics by confirming that the PL prevent photoaging caused by UVB stimulation and have antioxidant and anti-wrinkle effects.