Shi Gengxuan, Lu Yaoying, Zhang Yougang, Zheng Ke, Giacomotto Jean, Tonissen Kathryn F, Feng Yunjiang
Institute for Biomedicine and Glycomics, Griffith University, Nathan, QLD 4111, Australia.
School of Environment and Science, Griffith University, Nathan, QLD 4111, Australia.
Molecules. 2025 Sep 10;30(18):3689. doi: 10.3390/molecules30183689.
Tyrosinase catalyzes the rate-limiting steps of melanin production, posing as an important target for treating skin pigmentation. This study investigates bioactive human tyrosinase inhibitors from L. using a combined strategy of cell lysate, cell-based, and zebrafish assays. In this study, the methanol extract of L. was identified as a potent inhibitor against tyrosinase in a cell lysate assay utilizing human MM418C1 melanoma cells. Subsequent phytochemical analysis resulted in the isolation of 11 natural products, including 4-hydroxybenzoic acid (4HB), three nucleotides, four caffeoylquinic acids and three alkaloids. Biological activity evaluation of isolated compounds suggested that 4HB was a potent inhibitor against tyrosinase with an IC value of 59.5 μg/mL. Further evaluations revealed that 4HB significantly reduced the melanin content by 40% at the concentration of 500 mg/mL in human MM418C1 melanoma cells. 4HB activity was finally confirmed in vivo, by the demonstration of 40% reduction in melanin production in live zebrafish at the concentration of 15.63 μg/mL.
酪氨酸酶催化黑色素生成的限速步骤，是治疗皮肤色素沉着的重要靶点。本研究采用细胞裂解物、细胞和斑马鱼试验相结合的策略，从[植物名称未给出]中研究具有生物活性的人酪氨酸酶抑制剂。在本研究中，[植物名称未给出]的甲醇提取物在利用人MM418C1黑色素瘤细胞的细胞裂解物试验中被鉴定为酪氨酸酶的有效抑制剂。随后的植物化学分析分离出11种天然产物，包括4-羟基苯甲酸（4HB）、三种核苷酸、四种咖啡酰奎宁酸和三种生物碱。对分离出的化合物进行生物活性评估表明，4HB是一种有效的酪氨酸酶抑制剂，IC值为59.5μg/mL。进一步评估显示，在人MM418C1黑色素瘤细胞中，4HB在500mg/mL浓度下可使黑色素含量显著降低40%。最终在体内证实了4HB的活性，在活斑马鱼中，15.63μg/mL浓度的4HB可使黑色素生成减少40%。
