Development of 5-[(3-Aminopropyl)phosphinooxy]-2-(hydroxymethyl)-4H-pyran-4-one as a Novel Whitening Agent.
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Accession number;03A0096286
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| Title;Development of 5-[(3-Aminopropyl)phosphinooxy]-2-(hydroxymethyl)-4H-pyran-4-one as a Novel Whitening Agent. |
| Author;
KIM D H
(Amore-pacific Corp., Kyounggi-do, Kor)
HWANG J-S
(Amore-pacific Corp., Kyounggi-do, Kor)
BAEK H S
(Amore-pacific Corp., Kyounggi-do, Kor)
KIM K-J
(Amore-pacific Corp., Kyounggi-do, Kor)
LEE B G
(Amore-pacific Corp., Kyounggi-do, Kor)
CHANG I
(Amore-pacific Corp., Kyounggi-do, Kor)
KANG H H
(Amore-pacific Corp., Kyounggi-do, Kor)
LEE O S
(Amore-pacific Corp., Kyounggi-do, Kor)
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Journal Title;Chem Pharm Bull
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Journal Code:G0504A
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ISSN:0009-2363
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VOL.51;NO.2;PAGE.113-116(2003)
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| Figure&Table&Reference;FIG.5, REF.15 |
| Pub. Country;Japan |
| Language;English |
| Abstract;A stable derivative of kojic acid, 5-[(3-aminopropyl)phosphinooxy]-2-(hydroxymethyl)-4H-pyran-4-one (Kojyl-APPA), was synthesized in good yield. The effects of Kojyl-APPA on tyrosinase activity and melanin synthesis were investigated. Kojyl-APPA showed tyrosinase inhibition effect (30%) in situ, but not in vitro. Kojyl-APPA inhibited tyrosinase activity significantly at 24 h after treatment in normal human melanocytes. It means that Kojyl-APPA is not a direct inhibitor of tyrosinase itself, but it is converted to a potential inhibitor kojic acid enzymatically in cells. In addition, Kojyl-APPA decreased melanin content to 75% of control in melanoma cells and decreased neomelanin synthesis to 43% of control in normal human melanocytes. Its permeation through skin increased by about 8 times as compared with kojic acid. (author abst.) |
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