Evaluation of Tyrosinase Inhibitory Activity of Carbathioamidopyrazoles and Their Potential Application in Cosmetic Products and Melanoma Treatment

被引:0
作者
Namiecinska, Ewelina [1 ]
Jaszczak, Jan [2 ]
Hikisz, Pawel [3 ]
Dasko, Mateusz [4 ]
Wozniczka, Magdalena [2 ]
Budzisz, Elzbieta [1 ]
机构
[1] Med Univ Lodz, Dept Chem Cosmet Raw Mat, Muszynski 1 Str, PL-90151 Lodz, Poland
[2] Med Univ Lodz, Fac Pharm, Dept Phys & Biocoordinat Chem, Muszynskiego 1, PL-90151 Lodz, Poland
[3] Univ Lodz, Fac Biol & Environm Protect, Dept Oncobiol & Epigenet, Pomorska 141-143, PL-90236 Lodz, Poland
[4] Gdansk Univ Technol, Fac Chem, Dept Inorgan Chem, Narutowicza 11-12, PL-80233 Gdansk, Poland
关键词
tyrosinase; carbothioamidopyrazole derivatives; melanin; hyperpigmentation; molecular docking; COMPLEXES; MECHANISM; AGENTS; ACID; MELANOGENESIS; ANTIOXIDANT; PERSPECTIVE; DERIVATIVES; COPPER(II); ANTICANCER;
D O I
10.3390/ijms26083882
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
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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页数:22
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