Authors Ryu, IY; Choi, I; Jung, HJ; Ullah, S; Choi, H; Al-Amin, M; Chun, P; Moon, HR in ACADEMIC PRESS INC ELSEVIER SCIENCE published article about MUSHROOM TYROSINASE; INHIBITORY-ACTIVITY; MOLECULAR DOCKING; MECHANISM; MELANOMA; DESIGN; FLAVONOIDS in [Ryu, Il Young; Choi, Inkyu; Jung, Hee Jin; Choi, Heejeong; Al-Amin, Md; Moon, Hyung Ryong] Pusan Natl Univ, Coll Pharm, Busan 46241, South Korea; [Ullah, Sultan] Scripps Res Inst, Dept Mol Med, Jupiter, FL 33458 USA; [Chun, Pusoon] Inje Univ, Coll Pharm, Gimhae 50834, Gyeongnam, South Korea; [Chun, Pusoon] Inje Univ, Inje Inst Pharmaceut Sci & Res, Gimhae 50834, Gyeongnam, South Korea in 2021, Cited 63. Recommanded Product: 4-Methoxybenzaldehyde. The Name is 4-Methoxybenzaldehyde. Through research, I have a further understanding and discovery of 123-11-5
Tyrosinase is considered a key contributor to melanogenesis, and safe, potent tyrosinase inhibitors are needed for medical and cosmetic purposes to treat skin hyperpigmentation and prevent fruit and vegetable browning. According to our accumulated SAR data on tyrosinase inhibitors, the ?-phenyl-?,?-unsaturated carbonyl scaffold in either E or Z configurations, can confer potent tyrosinase inhibitory activity. In this study, twelve indanedione derivatives were synthesized as chimeric compounds with a ?-phenyl-?,?-unsaturated dicarbonyl scaffold. Two of these derivatives, that is, compounds 2 and 3 (85% and 96% inhibition, respectively), at 50 ?M inhibited mushroom tyrosinase markedly more potently than kojic acid (49% inhibition). Docking studies predicted that compounds 2 and 3 both inhibited tyrosinase competitively, and these findings were supported by LineweaverBurk plots. In addition, both compounds inhibited tyrosinase activity and reduced melanin contents in B16F10 cells more than kojic acid without perceptible cytotoxicity. These results support the notion that chimeric compounds with the ?-phenyl-?,?-unsaturated dicarbonyl scaffold represent promising starting points for the development of potent tyrosinase inhibitors.
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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles