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Updated: May 17, 2026

Quantification of Hypopigmentation Activity In Vitro
Published on: March 6, 2019
Discovery of small molecules that inhibit melanogenesis via regulation of tyrosinase expression
Jiho Song1, Hyun-e Lee, Young Jin Kim
1College of Pharmacy, Chung-Ang University, Seoul 156-756, Republic of Korea.
Abstract:
5,6,7,8-Tetrahydro-4H-cyclohepta[d]isoxazole derivatives were synthesized and evaluated as a novel class of inhibitors for α-melanocyte-stimulating hormone (α-MSH) induced melanogenesis in a mouse melanoma B16F10 cell line. Compound 8e (IC(50)=0.67 μM), 8h (IC(50)=1.01 μM) and 9b (IC(50)=0.99 μM) exhibited a potent inhibitory activity approximately 85- to 126-fold greater than kojic acid, a well-known potent inhibitor. A biochemical study indicates that the activity of this series should be displayed via down-regulation of the expression of tyrosinase.
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Melanin occurs in two primary forms: eumelanin that provides black and brown pigment and pheomelanin that provides red color. Dark-skinned individuals produce more melanin than those with pale...
