红花中酪氨酸酶抑制成分的快速筛选和分析

Quick screening and analysis on components from Carthami Flos with tyrosinase inhibitory activity

目的通过红花中酪氨酸酶抑制剂的筛选,明确红花中酪氨酸酶抑制剂成分,为美白祛斑剂的研发提供实验依据。方法采用索氏提取法依次提取红花石油醚、氯仿、醋酸乙酯、正丁醇和水5种提取物,分别检测其对酪氨酸酶的抑制作用;针对活性组分通过UPLC-Q/TOF鉴定活性成分,并结合分子对接和酶学检测验证药效成分。结果初步筛选结果显示红花水层提取物具有较强的抑制作用,并进一步通过液相色谱分离,质谱检测,以及分子对接预测技术,推测其中9种成分可能具有酪氨酸酶抑制作用,选取代表性单体羟基红花黄色素A进行验证,确认其具有较强的抑制作用。结论谱效结合构效的筛选模式为天然产物中美白祛斑成分的筛选提供了便捷方法;红花中羟基红花黄色素A对酪氨酸酶具有明显的抑制作用。

Objective To confirm the effective inhibitory components through screening the tyrosinase inhibitor from Carthami Flos,and to provide a basis for the development of whitening agent.Methods Soxhlet extraction system was used by petroleum ether,chloroform,ethyl acetate,butanol,and water solvent in proper sequence to extract the effective fraction of Carthami Flos and to detect the inhibition of tyrosinase activity.UPLC-Q/TOF was used to analyze and identify the active ingredients,and the molecular docking and enzymological method were used to validate their efficacy composition.Results The water layer showed a strong inhibition on the activity of tyrosinase.Through UPLC-Q/TOF system and molecular docking prediction technology,nine kinds of compounds were confirmed.Hydroxyl safflower yellow pigment A was validated to have an observable inhibition on tyrosinase activity by comparison with the standard product.Conclusion The high throughput screening system established for the white spot component screening provides a convenient method in the natural product.Especially the hydroxyl safflower yellow pigment A extracted from Carthami Flos has a significant tyrosinase inhibitory effect.