Department of Medicinal Chemistry and Pharmaceutical Sciences Research Center, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran.
Chem Biol Drug Des. 2022 Aug;100(2):290-303. doi: 10.1111/cbdd.14065. Epub 2022 May 24.
Kojic acid (KA) is a hydroxypyranone natural metabolite mainly known as tyrosinase inhibitor. Currently, this compound is used as a whitening agent in cosmetics and as an anti-browning agent in food industry. Given the easy-manipulation in different positions of the KA molecule, many investigations have been carried out to find new tyrosinase inhibitors derived from KA. Beside anti-tyrosinase activity, many KA-based compounds have been designed for targeting other enzymes including human neutrophil elastase, catechol-O-methyltransferase, matrix metalloproteinases, monoamine oxidase, human lactate dehydrogenase, endonucleases, D-amino acid oxidase, and receptors such as histamine H and apelin (APJ) receptors. This review could help biochemists and medicinal chemists in designing diverse KA-derived enzyme inhibitors.
曲酸(KA)是一种羟基吡喃酮天然代谢物,主要作为酪氨酸酶抑制剂而被人们熟知。目前,这种化合物被应用于化妆品中的增白剂和食品工业中的防褐变剂。鉴于 KA 分子在不同位置易于操作,人们进行了许多研究以寻找新的源于 KA 的酪氨酸酶抑制剂。除了抑制酪氨酸酶的活性,许多基于 KA 的化合物还被设计用于靶向其他酶,包括人中性粒细胞弹性蛋白酶、儿茶酚-O-甲基转移酶、基质金属蛋白酶、单胺氧化酶、人乳酸脱氢酶、核酸内切酶、D-氨基酸氧化酶以及组胺 H 和阿片肽(APJ)受体等。这篇综述可以帮助生化学家及药物化学家设计各种源于 KA 的酶抑制剂。