Twenty-eight tetraketones (1-28) with variable substituents at C-7 were synthesized and evaluated as tyrosinase inhibitors. Remarkably compounds 25 (IC(50)=2.06 microM), 11 (IC(50)=2.09 microM), 15 (IC(50)=2.61 microM), and 27 (IC(50)=3.19 microM) were found to be the most active compounds of the series, even better than both standards kojic acid (IC(50)=16.67 microM) and L-mimosine (IC(50)=3.68 microM). This study may lead to the discovery of therapeutically potent agents against clinically very important dermatological disorders including hyperpigmentation as well as skin melanoma.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmc.2005.08.029 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Eco-Friendly Extraction of Phlorotannins from : Identification Related to Purification Methods Towards Innovative Cosmetic Applications.
Mar Drugs
December 2024
Univ Brest, Institut de Recherche pour le Développement (IRD), CNRS, Ifremer, LEMAR, IUEM, F-29280 Plouzane, France.
This study focuses on developing innovative and eco-friendly purification methods for the isolation of bioactive compounds derived from , a brown abundant macroalga in Djibouti. Three distinct fractions, obtained via liquid-liquid extraction (LLE_FAE), solid-phase extraction (SPE_WE50), and flash chromatography (FC_EtOH20), were selected based on their high phenolic content and antioxidant activities. All fractions were also evaluated for their anti-ageing potential by assessing their ability to inhibit two vital skin-ageing enzymes, tyrosinase and elastase.
View Article and Find Full Text PDFComparative analysis of LC-HRMS profiling, ATR FT-IR spectroscopy, antioxidant, anti-diabetic, and anti-tyrosinase activities of extracts from Cotoneaster frigidus Wall. Ex Lindl. "Cornubia" fruit.
Food Res Int
February 2025
Karadeniz Technical University, Faculty of Science, Department of Chemistry, Trabzon, Türkiye. Electronic address:
The antioxidant, total phenolic, flavonoid, and anthocyanidin properties of extracts prepared from Cotoneaster frigidus Wall. ex Lindl. "Cornubia" fruit were examined.
View Article and Find Full Text PDFIL-7 secreted by keratinocytes induces melanogenesis via c-kit/MAPK signaling pathway in Melan-a melanocytes.
Arch Dermatol Res
January 2025
Department of Genetics & Biotechnology, Graduate School of Biotechnology, College of Life Sciences, Kyung Hee University, Youngin, 17104, Republic of Korea.
Abnormal melanin synthesis within melanocytes can result in pigmentary skin disorders. Although pigmentation alterations associated with inflammation are frequently observed, the precise reason for this clinical observation is still unknown. More specifically, although many cytokines are known to be critical for inflammatory skin processes, it is unclear how they affect epidermal melanocyte function.
View Article and Find Full Text PDFUnfolded protein response modulates Tyrosinase levels and melanin production during melanogenesis.
J Dermatol Sci
January 2025
Department of Biochemistry, Institute of Biomedical & Health Sciences, Hiroshima University, Hiroshima, Japan; Department of Frontier Science and Interdisciplinary Research, Faculty of Medicine, Kanazawa University, Ishikawa, Japan. Electronic address:
Background: Melanocytes protect the body from ultraviolet radiation by synthesizing melanin. Tyrosinase, a key enzyme in melanin production, accumulates in the endoplasmic reticulum (ER) during melanin synthesis, potentially causing ER stress. However, regulating ER function for melanin synthesis has been less studied than controlling Tyrosinase activity.
View Article and Find Full Text PDFStructural characterization of complex tannins from Euryale ferox fruit peels and their inhibitory mechanisms against tyrosinase activity and melanogenesis.
Int J Biol Macromol
January 2025
College of Life Science, Yangtze University, Jingzhou, China. Electronic address:
Tyrosinase is a rate-limiting enzyme for melanogenesis and abnormal melanin production can be controlled by utilizing tyrosinase inhibitory substances. To develop potent and safe inhibitors of tyrosinase, complex tannins a narrowly distributed plant polyphenols were prepared from the fruit peel of Euryale ferox (EPTs) and then structurally characterized, as well as investigated for their inhibitory effects and the involved mechanisms against tyrosinase activity and melanogenesis. The structures of EPTs were established to consist of 63.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!