Abstract:
:A series of hydroxy-substituted chalcone oxime derivatives were synthesized. These compounds were then evaluated for their inhibitory activities on tyrosinase and melanogenesis in murine B16F10 melanoma cells. The structures of the synthesized compounds were confirmed by (1) H NMR, (13) C NMR, FTIR, and HRMS. Two of the compounds exhibited much higher tyrosinase inhibitory activities (IC50 values of 4.77 and 7.89 μM, respectively) than the positive control, kojic acid (IC50 : 22.25 μM). Kinetic studies revealed them to act as competitive tyrosinase inhibitors with their Ki values of 5.25 and 8.33 μM, respectively. Both the compounds inhibited melanin production and tyrosinase activity in B16 cells. Docking results confirmed that the active inhibitors strongly interacted with the mushroom tyrosinase residues.
journal_name
Arch Pharm (Weinheim)journal_title
Archiv der Pharmazieauthors
Radhakrishnan SK,Shimmon RG,Conn C,Baker ATdoi
10.1002/ardp.201500298subject
Has Abstractpub_date
2016-01-01 00:00:00pages
20-9issue
1eissn
0365-6233issn
1521-4184journal_volume
349pub_type
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