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KMID : 0604520010270010119
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Journal of the Society of Cosmetic Scientists of Korea
2001 Volume.27 No. 1 p.119 ~ p.132
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New Whitening agent: Kojyl-APPA
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황재성/Hwang JS
김덕희/안수미/백흥수/최현중/이진영/이병곤/장이섭/강학희/Kim DH/Anh SM/Baek HS/Choi HJ/Lee JY/Lee BG/Chang IS/Kang HH
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Abstract
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Exposure of the human skin to UV-light can cause sun-tanning, photoaging and even photo-carcinogenesis. Melanin is important in protecting the skin against UV damage, but excessive or uneven melanin production can lead to the formation of freckles and aged spot. Control of hyperpigmentation is becoming even more important as aged population continues to grow. These needs led us to develop effective and safe depigmenting-agent, kojyl 3-aminopropyl phosphate (kojyl-APPA), called Whitegen.
The development of whitegen was based on the fact that phosphate group of 3-aminopropyl phosphate can make kojic acid more compatible to the skin membrane and more stable. Instability of kojic acid has been a problem in cosmetic use. The insertion of phosphoester group has been recognized as a powerful tool to improve such physical properties as solubility and stability, because the phosphodiester residue is well characterized as a non-toxic moiety, having a high affinity for cell membranes.
Kojyl-APPA showed no tyrosinase inhibition effect compared to kojic acid in vitro, but showed tyrosinase inhibition effect in situ. It means that kojyl-APPA is converted to kojic acid enzymatically in cells. Kojyl-APPA showed the inhibitory activity on melanin synthesis in mouse melanoma and normal humal melnaocytes and also showed long-lasting stability in comparison with its original form (kojic acid). Kojyl-APPA showed depigmenting effects when applied to UVB-induced hyperpigmentated region of guinea pig skin.
Based on these results, kojyl 3-aminopropyl phosphate can be used as a safe and effective ingredient for the brightness and cleanness of skin.
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