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Evaluation of Tyrosinase Inhibitory Activity of Carbathioamidopyrazoles and Their Potential Application in Cosmetic Products and Melanoma Treatment
Abstract
Hyperpigmentation can be prevented by regulating melanin synthesis through tyrosinase inhibition. As such, tyrosinase inhibitors like arbutin, kojic acid, and hydroquinone are commonly used for skin lightening. Recent studies suggest that certain pyrazole derivatives with tyrosinase activity may also have anticancer potential by influencing melanocyte transformation and tumor progression, positioning them as promising candidates for both cosmetic and therapeutic uses. The aim of this study was to evaluate the tyrosinase inhibitory activity of carbothioamidopyrazole derivatives. Inhibition was determined using the Dixon method, leveraging in silico molecular docking and circular dichroism (CD) spectroscopy to analyze fluorescence quenching. Carbothioamidopyrazole derivatives at the C-3 and C-5 positions in the pyrazole ring may be effective alternatives to traditional skin-lightening agents. These derivatives can induce structural changes in tyrosinase, thus altering its activity, and influence melanocyte transformation. Their dual action as tyrosinase inhibitors and potential anticancer agents makes them valuable for future research. Two compounds exhibited stronger inhibitory activity than kojic acid. Molecular docking suggests that these derivatives may block tyrosinase activity by preventing substrate access to its active site. These results underscore the potential of pyrazole derivatives for both cosmetic and therapeutic applications
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Authors (6)
-
Ewelina Namiecińska
-
Jan Jaszczak
-
Paweł Hikisz
-
Magdalena Woźniczka
-
Elzbieta Budzisz
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- Accepted or Published Version
- DOI:
- Digital Object Identifier (open in new tab) 10.3390/ijms26083882
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- Category:
- Articles
- Type:
- artykuły w czasopismach
- Published in:
-
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
no. 26,
ISSN: 1661-6596 - Language:
- English
- Publication year:
- 2025
- Bibliographic description:
- Namiecińska E., Jaszczak J., Hikisz P., Daśko M., Woźniczka M., Budzisz E.: Evaluation of Tyrosinase Inhibitory Activity of Carbathioamidopyrazoles and Their Potential Application in Cosmetic Products and Melanoma Treatment// INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES -Vol. 26, (2025), s.3882-
- DOI:
- Digital Object Identifier (open in new tab) 10.3390/ijms26083882
- Sources of funding:
-
- Financial support from the Medical University of Lodz (grant No. 503/3-066-02/503-31-001 to E. Budzisz and No. 503/3-014-02/503-31-001 to M. Świątek) is gratefully acknowledged.
- Verified by:
- Gdańsk University of Technology
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