2-Mercaptonicotinoyl glycine, a new potent melanogenesis inhibitor, exhibits a unique mode of action while preserving melanocyte integrity

IF 3.9 3区 医学 Q2 CELL BIOLOGY Pigment Cell & Melanoma Research Pub Date : 2024-04-01 DOI:10.1111/pcmr.13168
Peggy Sextius, Emilie Warrick, Amélie Prévot-Guéguiniat, Guillaume Lereaux, Florence Boirre, Ludwig Baux, Safa Ben Hassine, Jie Qiu, Xiaoming Huang, Jinzhu Xu, Sébastien Grégoire, Shosuke Ito, Kazumasa Wakamatsu, Xavier Marat
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Abstract

Research on new ingredients that can prevent excessive melanin production in the skin while considering efficacy, safety but also environmental impact is of great importance to significantly improve the profile of existing actives on the market and avoid undesirable side effects. Here, the discovery of an innovative technology for the management of hyperpigmentation is described. High-throughput screening tests on a wide chemical diversity of molecules and in silico predictive methodologies were essential to design an original thiopyridinone backbone and select 2-mercaptonicotinoyl glycine (2-MNG) as exhibiting the most favorable balance between the impact on water footprint, skin penetration potential and performance. The effectiveness of 2-MNG was confirmed by topical application on pigmented reconstructed epidermis and human skin explants. In addition, experiments have shown that unlike most melanogenesis inhibitors on the market, this molecule is not a tyrosinase inhibitor. 2-MNG binds to certain melanin precursors, preventing their integration into growing melanin and leading to inhibition of eumelanin and pheomelanin synthesis, without compromising the integrity of melanocytes.

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2-Mercaptonicotinoyl glycine 是一种新型的强效黑色素生成抑制剂,在保持黑色素细胞完整性的同时,还展现出独特的作用模式。
研究既能防止皮肤黑色素过度生成,又能兼顾功效、安全性和环境影响的新成分,对于显著改善市场上现有活性成分的特性和避免不良副作用具有重要意义。本文介绍了一种用于色素沉着治疗的创新技术。在对多种化学分子进行高通量筛选测试和采用硅学预测方法的基础上,设计出了一种独创的巯基吡啶酮骨架,并筛选出了 2-巯基烟酰甘氨酸(2-MNG),它在水足迹影响、皮肤渗透潜力和性能之间实现了最有利的平衡。在色素重建表皮和人体皮肤外植体上的局部应用证实了 2-MNG 的有效性。此外,实验还表明,与市场上大多数黑色素生成抑制剂不同,这种分子不是酪氨酸酶抑制剂。2-MNG 与某些黑色素前体结合,阻止它们整合成生长中的黑色素,从而抑制黑色素和嗜黑色素的合成,而不会损害黑色素细胞的完整性。
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来源期刊
Pigment Cell & Melanoma Research
Pigment Cell & Melanoma Research 医学-皮肤病学
CiteScore
8.90
自引率
2.30%
发文量
54
审稿时长
6-12 weeks
期刊介绍: Pigment Cell & Melanoma Researchpublishes manuscripts on all aspects of pigment cells including development, cell and molecular biology, genetics, diseases of pigment cells including melanoma. Papers that provide insights into the causes and progression of melanoma including the process of metastasis and invasion, proliferation, senescence, apoptosis or gene regulation are especially welcome, as are papers that use the melanocyte system to answer questions of general biological relevance. Papers that are purely descriptive or make only minor advances to our knowledge of pigment cells or melanoma in particular are not suitable for this journal. Keywords Pigment Cell & Melanoma Research, cell biology, melatonin, biochemistry, chemistry, comparative biology, dermatology, developmental biology, genetics, hormones, intracellular signalling, melanoma, molecular biology, ocular and extracutaneous melanin, pharmacology, photobiology, physics, pigmentary disorders
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