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Identification of Tyrosinase Inhibitors and Their Structure-Activity Relationships via Evolutionary Chemical Binding Similarity and Structure-Based Methods

open access: yesMolecules, 2021
Tyrosinase is an enzyme that plays a crucial role in the melanogenesis of humans and the browning of food products. Thus, tyrosinase inhibitors that are useful to the cosmetic and food industries are required.
Prasannavenkatesh Durai   +4 more
doaj   +1 more source

In Vitro and In Vivo Biological Evaluation of Indole-thiazolidine-2,4-dione Derivatives as Tyrosinase Inhibitors

open access: yesMolecules, 2023
Tyrosinase is an important rate-limiting enzyme in melanin biosynthesis. To find potential tyrosinase inhibitors with anti-melanogenic activity, a series of indole-thiazolidine-2,4-dione derivatives 5a~5z were synthesized by incorporating indole with ...
Li Lu   +5 more
doaj   +1 more source

Comparative Study of High-throughput Screening Models for Anti-hyperpigmentation Compounds

open access: yesBrazilian Archives of Biology and Technology, 2022
The mushroom tyrosinase assay, B16-F10 mouse melanoma cell model, and zebrafish model are frequently used for high-throughput screening and are widely used for developing anti-hyperpigmentation compounds, although these systems cannot be compared.
Tingwei Sun   +7 more
doaj   +1 more source

Identification of (Z)-2-benzylidene-dihydroimidazothiazolone derivatives as tyrosinase inhibitors: Anti-melanogenic effects and in silico studies

open access: yesComputational and Structural Biotechnology Journal, 2022
As part of our continuous search for novel tyrosinase inhibitors, we designed 5,6-dihydroimindazo[2,1-b]thiazol-3(2H)-one (DHIT) derivatives based on the structure of MHY773; a potent tyrosinase inhibitor with a 2-iminothiazolidin-4-one template.
Heejeong Choi   +11 more
doaj   +1 more source

In silico and in vitro insights into tyrosinase inhibitors with a 2-thioxooxazoline-4-one template

open access: yesComputational and Structural Biotechnology Journal, 2021
The β-phenyl-α,β-unsaturated carbonyl (PUSC) scaffold confers tyrosinase inhibitory activity, and in the present study, 16 (Z)-5-(substituted benzylidene)-3-phenyl-2-thioxooxazolidin-4-one analogues containing this scaffold were synthesized.
Inkyu Choi   +11 more
doaj   +1 more source

Novel Anti-Melanogenic Compounds, (Z)-5-(Substituted Benzylidene)-4-thioxothiazolidin-2-one Derivatives: In Vitro and In Silico Insights

open access: yesMolecules, 2021
To confirm that the β-phenyl-α,β-unsaturated thiocarbonyl (PUSTC) scaffold, similar to the β-phenyl-α,β-unsaturated carbonyl (PUSC) scaffold, acts as a core inhibitory structure for tyrosinase, twelve (Z)-5-(substituted benzylidene)-4-thioxothiazolidin-2-
Heejeong Choi   +15 more
doaj   +1 more source

Determination of tyrosinase-cyanidin-3-O-glucoside and (−/+)-catechin binding modes reveal mechanistic differences in tyrosinase inhibition

open access: yesScientific Reports, 2021
Tyrosinase, exquisitely catalyzes the phenolic compounds into brown or black pigment, inhibition is used as a treatment for dermatological or neurodegenerative disorders. Natural products, such as cyanidin-3-O-glucoside and (−/+)-catechin, are considered
Kyung Eun Lee   +4 more
doaj   +1 more source

Synthesis, Anti-Tyrosinase Activity, and Spectroscopic Inhibition Mechanism of Cinnamic Acid–Eugenol Esters

open access: yesMolecules, 2023
Tyrosinase plays crucial roles in mediating the production of melanin pigment; thus, its inhibitors could be useful in preventing melanin-related diseases.
Jianping Li   +5 more
doaj   +1 more source

Characterization of Tyrosinase Inhibitors in Dryopteris crassirhizoma Rhizome Using a Combination of High-Speed Counter-Current Chromatography, Affinity-Based Ultrafiltration, and Liquid Chromatography–Tandem Mass Spectrometry

open access: yesFrontiers in Nutrition, 2022
Dryopteris crassirhizoma rhizome (DCR) inhibits melanin production in B16F10 melanoma cells and tyrosinase activity. The melanin content and tyrosinase activity of DCR-treated zebrafish embryos were determined to evaluate the in vivo inhibitory effect of
Zhiqiang Wang   +4 more
doaj   +1 more source

In vitro and in silico insights into tyrosinase inhibitors with (E)-benzylidene-1-indanone derivatives

open access: yesComputational and Structural Biotechnology Journal, 2019
Tyrosinase is a key enzyme responsible for melanin biosynthesis and is effective in protecting skin damage caused by ultraviolet radiation. As part of ongoing efforts to discover potent tyrosinase inhibitors, we systematically designed and synthesized ...
Hee Jin Jung   +6 more
doaj   +1 more source

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