Peng Zhiyun, Wang Guangcheng, Zeng Qiao-Hui, Li Yufeng, Liu Haiquan, Wang Jing Jing, Zhao Yong
College of Food Science and Technology, Shanghai Ocean University, Shanghai, China.
Guizhou Provincial Key Laboratory of Pharmaceutics, Guizhou Medical University, Guiyang, China.
Crit Rev Food Sci Nutr. 2022;62(15):4053-4094. doi: 10.1080/10408398.2021.1871724. Epub 2021 Jan 18.
Tyrosinase is a copper-containing oxidation enzyme, which is responsible for the production of melanin. This enzyme is widely distributed in microorganisms, animals and plants, and plays an essential role in undesirable browning of fruits and vegetables, antibiotic resistance, skin pigment formation, sclerotization of cuticle, neurodegeneration, etc. Hence, it has been recognized as a therapeutic target for the development of antibrowning agents, antibacterial agents, skin-whitening agents, insecticides, and other therapeutic agents. With great potential application in food, agricultural, cosmetic and pharmaceutical industries, a large number of synthetic tyrosinase inhibitors have been widely reported in recent years. In this review, we systematically summarized the advances of synthetic tyrosinase inhibitors in the literatures, including their inhibitory activity, cytotoxicity, structure-activity relationship (SAR), inhibition kinetics, and interaction mechanisms with the enzyme. The collected information is expected to provide a rational guidance and effective strategy to develop novel, potent and safe tyrosinase inhibitors for better practical applications in the future.
酪氨酸酶是一种含铜氧化酶，负责黑色素的生成。这种酶广泛分布于微生物、动物和植物中，在水果和蔬菜的不良褐变、抗生素抗性、皮肤色素形成、角质层硬化、神经退行性变等过程中发挥着重要作用。因此，它已被公认为是开发抗褐变剂、抗菌剂、美白剂、杀虫剂及其他治疗剂的治疗靶点。由于在食品、农业、化妆品和制药行业具有巨大的潜在应用价值，近年来大量合成酪氨酸酶抑制剂被广泛报道。在本综述中，我们系统总结了文献中合成酪氨酸酶抑制剂的研究进展，包括它们的抑制活性、细胞毒性、构效关系（SAR）、抑制动力学以及与酶的相互作用机制。所收集的信息有望为开发新型、高效且安全的酪氨酸酶抑制剂提供合理指导和有效策略，以便在未来获得更好的实际应用。
