The hypopigmentary action of KI-063 (a new tyrosinase inhibitor) combined with terrein

Dong Seok Kim, Sangku Lee, Hyun Kyung Lee, Seo Hyoung Park, In Ja Ryoo, Ick Dong Yoo, Sun Bang Kwon, Jin Baek Kwang, Jung Im Na, Kyungchan Park

Research output: Contribution to journalArticle

8 Citations (Scopus)

Abstract

Resorcinol derivatives are known to inhibit melanin synthesis. In this study, resorcinol derivatives were synthesized and screened for their activity on melanogenesis. KI-063 (a tyrosinase inhibitor) was examined for its effects on melanogenesis using a spontaneously immortalized mouse melanocyte cell line (Mel-Ab). In a cell-free system, KI-063 directly inhibited tyrosinase, the rate-limiting melanogenic enzyme. Moreover, in a cell system, it inhibited melanin synthesis in a concentration-dependent manner. In addition, KI-063 inhibited the activity of cellular tyrosinase. Thus, this study examined the effects of a combination of KI-063 with terrein, an agent that down-regulates microphthalmia-associated transcription factor. The data suggest that KI-063 has an additive effect in combination with terrein. Thus, the suppression of tyrosinase activity by KI-063 and the inhibition of tyrosinase production by terrein appear to be an optimal combination for skin whitening.

Original languageEnglish
Pages (from-to)343-348
Number of pages6
JournalJournal of Pharmacy and Pharmacology
Volume60
Issue number3
DOIs
StatePublished - 1 Mar 2008

Fingerprint

Monophenol Monooxygenase
Melanins
Microphthalmia-Associated Transcription Factor
Cell-Free System
Melanocytes
terrein
2-butyl-5-hydroxyphenyl dihydrocaffeate
Down-Regulation
Cell Line
Skin
Enzymes

Cite this

Kim, Dong Seok ; Lee, Sangku ; Lee, Hyun Kyung ; Park, Seo Hyoung ; Ryoo, In Ja ; Yoo, Ick Dong ; Kwon, Sun Bang ; Kwang, Jin Baek ; Na, Jung Im ; Park, Kyungchan. / The hypopigmentary action of KI-063 (a new tyrosinase inhibitor) combined with terrein. In: Journal of Pharmacy and Pharmacology. 2008 ; Vol. 60, No. 3. pp. 343-348.
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abstract = "Resorcinol derivatives are known to inhibit melanin synthesis. In this study, resorcinol derivatives were synthesized and screened for their activity on melanogenesis. KI-063 (a tyrosinase inhibitor) was examined for its effects on melanogenesis using a spontaneously immortalized mouse melanocyte cell line (Mel-Ab). In a cell-free system, KI-063 directly inhibited tyrosinase, the rate-limiting melanogenic enzyme. Moreover, in a cell system, it inhibited melanin synthesis in a concentration-dependent manner. In addition, KI-063 inhibited the activity of cellular tyrosinase. Thus, this study examined the effects of a combination of KI-063 with terrein, an agent that down-regulates microphthalmia-associated transcription factor. The data suggest that KI-063 has an additive effect in combination with terrein. Thus, the suppression of tyrosinase activity by KI-063 and the inhibition of tyrosinase production by terrein appear to be an optimal combination for skin whitening.",
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The hypopigmentary action of KI-063 (a new tyrosinase inhibitor) combined with terrein. / Kim, Dong Seok; Lee, Sangku; Lee, Hyun Kyung; Park, Seo Hyoung; Ryoo, In Ja; Yoo, Ick Dong; Kwon, Sun Bang; Kwang, Jin Baek; Na, Jung Im; Park, Kyungchan.

In: Journal of Pharmacy and Pharmacology, Vol. 60, No. 3, 01.03.2008, p. 343-348.

Research output: Contribution to journalArticle

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AU - Kim, Dong Seok

AU - Lee, Sangku

AU - Lee, Hyun Kyung

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AU - Ryoo, In Ja

AU - Yoo, Ick Dong

AU - Kwon, Sun Bang

AU - Kwang, Jin Baek

AU - Na, Jung Im

AU - Park, Kyungchan

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N2 - Resorcinol derivatives are known to inhibit melanin synthesis. In this study, resorcinol derivatives were synthesized and screened for their activity on melanogenesis. KI-063 (a tyrosinase inhibitor) was examined for its effects on melanogenesis using a spontaneously immortalized mouse melanocyte cell line (Mel-Ab). In a cell-free system, KI-063 directly inhibited tyrosinase, the rate-limiting melanogenic enzyme. Moreover, in a cell system, it inhibited melanin synthesis in a concentration-dependent manner. In addition, KI-063 inhibited the activity of cellular tyrosinase. Thus, this study examined the effects of a combination of KI-063 with terrein, an agent that down-regulates microphthalmia-associated transcription factor. The data suggest that KI-063 has an additive effect in combination with terrein. Thus, the suppression of tyrosinase activity by KI-063 and the inhibition of tyrosinase production by terrein appear to be an optimal combination for skin whitening.

AB - Resorcinol derivatives are known to inhibit melanin synthesis. In this study, resorcinol derivatives were synthesized and screened for their activity on melanogenesis. KI-063 (a tyrosinase inhibitor) was examined for its effects on melanogenesis using a spontaneously immortalized mouse melanocyte cell line (Mel-Ab). In a cell-free system, KI-063 directly inhibited tyrosinase, the rate-limiting melanogenic enzyme. Moreover, in a cell system, it inhibited melanin synthesis in a concentration-dependent manner. In addition, KI-063 inhibited the activity of cellular tyrosinase. Thus, this study examined the effects of a combination of KI-063 with terrein, an agent that down-regulates microphthalmia-associated transcription factor. The data suggest that KI-063 has an additive effect in combination with terrein. Thus, the suppression of tyrosinase activity by KI-063 and the inhibition of tyrosinase production by terrein appear to be an optimal combination for skin whitening.

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