The process of melanogenesis that takes place in the melanocytes of the epidermis, leads to hyperpigmentation. The biosynthetic pathway for the production of melanin involves the enzyme tyrosinase that has been an attractive target for cosmaceutical research. Numerous synthetic, semisynthetic and natural, especially plant-based, inhibitors of tyrosinase have been reported in the literature. In plants, the secondary metabolites like flavonoids, chalcones, stilbenes, tannins, hydroquinone and kojic acid, etc., have been shown to possess anti-tyrosinase activity. In the current review, we have covered the progress in this sphere that would be useful for not only further mechanistic investigations but also for the optimization of the structure of the metabolites for improved activity and selectivity. Thus, the review presents a comprehensive report on tyrosinase inhibitors of plant origin reported in the extract form or as isolated compounds. A huge gap has been found between research and industry due to inconsistent pursual of potent plant-based extracts. There is a need to completely evaluate the extracts for structure optimization using molecular docking and evaluation of the safety in order to benefit the industry with non-toxic biological friendly products through in vivo and ex vivo optimization.

发生在表皮黑色素细胞中的黑色素生成过程导致色素沉着过度。产生黑色素的生物合成途径涉及酪氨酸酶，该酶已成为药妆研究的一个有吸引力的目标。文献中已经报道了许多合成的、半合成的和天然的，尤其是基于植物的酪氨酸酶抑制剂。在植物中，次生代谢产物如黄酮类、查耳酮、芪、单宁、氢醌和曲酸等已被证明具有抗酪氨酸酶活性。在当前的综述中，我们已经介绍了该领域的进展，这些进展不仅对进一步的机理研究有用，而且对优化代谢物结构以提高活性和选择性也很有用。因此，该审查提供了一份关于以提取物形式或作为分离化合物报告的植物来源酪氨酸酶抑制剂的综合报告。由于对强效植物提取物的追求不一致，研究和工业之间存在巨大差距。需要通过分子对接对提取物进行结构优化和安全性评估进行全面评估，以便通过体内和体外优化以无毒生物友好产品造福行业。