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三氮唑类酪氨酸酶抑制剂的最新进展。

Recent advances in triazoles as tyrosinase inhibitors.

机构信息

Experimental Medicine Application & Research Center, Validebağ Research Park, University of Health Sciences, İstanbul, Turkiye; Department of Biotechnology, University of Health Sciences, İstanbul, Turkiye.

Department of Medical Services and Techniques, Vocational High School of Health Services, Giresun University, Giresun, Turkiye.

出版信息

Eur J Med Chem. 2023 Nov 5;259:115655. doi: 10.1016/j.ejmech.2023.115655. Epub 2023 Jul 20.

Abstract

The tyrosinase enzyme, which is widely found in microorganisms, animals and plants, has a significant position in melanogenesis, plays an important role in undesirable browning of fruits and vegetables, antibiotic resistance, skin pigment formation, sclerotization of cuticle, neurodegeneration, etc. Therefore, with the wide potential application fields of tyrosinase in food, agriculture, cosmetics and pharmaceutical industries, which has become the target enzyme for the development of therapeutic agents such as antibrowning, anticancer, antibacterial, skin whitening, insecticides, etc., a large number of synthetic tyrosinase inhibitors have been widely reported in recent years. The triazole ring, which has a broad spectrum of biological action, is of increasing interest in the synthesis of new tyrosinase inhibitors. In this review, tyrosinase inhibition effects, structure-activity relationships, enzyme inhibition kinetics and mechanisms of action of 1,2,3- or 1,2,4-triazole derivatives were investigated. The data gathered is anticipated to supply rational guidance and an influential strategy for the development of novel, potent and safe tyrosinase inhibitors for better practical application in the future.

摘要

酪氨酸酶广泛存在于微生物、动物和植物中,在黑色素生成中具有重要地位,在水果和蔬菜的非期望褐变、抗生素耐药性、皮肤色素形成、表皮角质硬化、神经退行性变等方面发挥着重要作用。因此,由于酪氨酸酶在食品、农业、化妆品和制药行业中的广泛潜在应用领域,它已成为开发抗褐变、抗癌、抗菌、皮肤美白、杀虫剂等治疗剂的目标酶,近年来已广泛报道了大量合成的酪氨酸酶抑制剂。具有广泛生物活性的三唑环在合成新型酪氨酸酶抑制剂方面引起了越来越多的关注。本综述研究了 1,2,3-或 1,2,4-三唑衍生物的酪氨酸酶抑制作用、构效关系、酶抑制动力学和作用机制。收集的数据预计将为开发新型、有效和安全的酪氨酸酶抑制剂提供合理的指导和有影响力的策略,以更好地应用于未来的实际应用。

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