酪氨酸酶
曲酸
细胞毒性
化学
香豆素
IC50型
对接(动物)
酶
立体化学
MTT法
皮肤美白
氨基脲
体外
黑色素
活动站点
组合化学
生物化学
铅化合物
DPPH
抗氧化剂
有机化学
药理学
生物
活性成分
医学
护理部
作者
Narges Hosseini Nasab,Hussain Raza,Young Seok Eom,Mubashir Hassan,Andrzej Kloczkowski,Song Ja Kim
摘要
A well-known key enzyme in melanogenesis and hyperpigmentation is tyrosinase. The present study introduces a novel series of thiophenyl-pyrazolylthiazole-coumarin hybrids (6a-6h) as tyrosinase inhibitors. The in-vitro tyrosinase inhibition results indicated that all compounds have strong tyrosinase inhibitory activity, particularly compound 6g (IC50 = 0.043 ± 0.006 μM), was identified as the most active compound compared to the positive control (kojic acid, IC50 = 18.521 ± 1.162 μM). Lineweaver-Burk plots were employed to analyze the kinetic mechanism, and compound 6g formed an enzyme-inhibitor complex by inhibiting tyrosinase non-competitively. Furthermore, all compounds demonstrated excellent antioxidant activity against DPPH. MTT assay was used to screen the cytotoxicity of all compounds on B16F10 melanoma cells, and they had no toxic effect on the cells. The binding affinity of compounds with tyrosinase was also investigated using molecular docking, and the ligands displayed good binding energy values. These molecules could be a promising lead for skin pigmentation and associated diseases as nontoxic pharmacological scaffolds.
科研通智能强力驱动
Strongly Powered by AbleSci AI