Antimelanogenic activity of a novel adamantyl benzylbenzamide derivative, <scp>AP</scp>736: a randomized, double‐blind, vehicle‐controlled comparative clinical trial performed in patients with hyperpigmentation during the summer

Jeong, Yeon Su; Kim, Jeong‐Hwan; Choi, Joonho; Baek, Hye Jin; Joo, Yung Hyup; Lee, Chang Seok; Shin, Hong-Ju; Kim, Beom Joon; Shin, Song Seok

doi:10.1111/ijd.13150

Int J Dermatology

2015

DOI: 10.1111/ijd.13150

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Antimelanogenic activity of a novel adamantyl benzylbenzamide derivative, AP736: a randomized, double‐blind, vehicle‐controlled comparative clinical trial performed in patients with hyperpigmentation during the summer

Yeon Su Jeong

Jeong‐Hwan Kim

Joonho Choi

et al.

Abstract: A formulation containing a novel skin whitening ingredient, AP736, effectively reduced pigmentation and was well tolerated by study subjects in summer season.

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Tyrosinase Inhibition and Antimelanogenic Effects of Resorcinol‐Containing Compounds

Beaumet,

Lazinski,

Maresca

et al. 2024

ChemMedChem

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Tyrosinases (TYRs) are copper‐containing metalloenzymes present in a large diversity of species. In human, hTYR is responsible for pivotal steps in melanogenesis, catalysing the oxidation of l‐tyrosine to l‐DOPA and further to dopaquinone. While numerous TYR inhibitors have been reported, polyphenolic compounds tend to dominate the literature. However, many of these compounds, particularly monophenols and catechols, have been identified as alternative substrates rather than true inhibitors, given their structural similarity to natural substrates. Resorcinol‐containing compounds have emerged as promising candidates to address this challenge, as the meta‐dihydroxy moiety in resorcinol demonstrates resistance to TYR‐mediated oxidation, while retaining the favourable interactions with copper ions provided by the hydroxy groups. Although their precise mechanism of action remains debated, resorcinol derivatives have yielded some of the most active compounds against isolated mushroom and human TYRs, as well as clinically used dermocosmetic agents like rucinol and thiamidol, which exhibited very promising effects in patients with facial melasma. This review outlines the development of resorcinol‐containing TYR inhibitors, categorized by scaffold type, ranging from simple alkyl analogues to intricate synthetic derivatives. Mechanistic insights about the resorcinol–TYR interaction are also presented and debated.

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Tyrosinase Inhibition and Antimelanogenic Effects of Resorcinol‐Containing Compounds

Beaumet,

Lazinski,

Maresca

et al. 2024

ChemMedChem

View full text Add to dashboard Cite

show abstract

Development and evaluation of topical formulations for a novel skin whitening agent (AP736) using Hansen solubility parameters and PEG-PCL polymers

Shin

Beak

Kim

et al. 2018

International Journal of Pharmaceutics

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Antimelanogenic activity of a novel adamantyl benzylbenzamide derivative, AP736: a randomized, double‐blind, vehicle‐controlled comparative clinical trial performed in patients with hyperpigmentation during the summer

Abstract: A formulation containing a novel skin whitening ingredient, AP736, effectively reduced pigmentation and was well tolerated by study subjects in summer season.

Cited by 2 publications

References 18 publications

Tyrosinase Inhibition and Antimelanogenic Effects of Resorcinol‐Containing Compounds

Tyrosinase Inhibition and Antimelanogenic Effects of Resorcinol‐Containing Compounds

Development and evaluation of topical formulations for a novel skin whitening agent (AP736) using Hansen solubility parameters and PEG-PCL polymers

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