具有酪氨酸酶抑制活性的丹参有效成分筛选研究

Screening of active components in Salvia miltiorrhiza with inhibition on tyrosinase

目的筛选丹参中对酪氨酸酶活性具有抑制作用的有效成分。方法基于受试物抑制酪氨酸酶催化底物L-多巴的反应原理,将丹参经80%乙醇提取后依次经石油醚、氯仿、醋酸乙酯、饱和正丁醇和水5种不同极性溶剂萃取,分别检测各提取部位对酪氨酸酶活性的抑制作用;并通过UPLC-MS/MS技术鉴定活性最强提取部位化学成分,结合分子对接技术预测各成分潜在活性,并通过酶学检测验证。结果丹参氯仿萃取层具有较强的酪氨酸酶抑制活性。其生物活性与丹参素、原儿茶醛等6种成分有关,酶学检测验证结果与筛选结果一致。结论丹参中丹参素和原儿茶醛等成分对酪氨酸酶活性具有显著的抑制作用。

Objective To screen the active components in Salvia miltiorrhiza with the inhibitory activity against tyrosinase. Methods The method ofL-Dopa oxidization reaction was employed to detect the tyrosinase activity. S. miltiorrhiza was first extracted by 80% ethanol and then extracted by PE, CHC13, EtOAc, n-BuOH, and H20. The inhibition of the different fractions on tyrosinase was detected. UPLC-MS/MS was used to analyze and identify the active components in the fraction with the strongest inhibition. Molecular docking was used to predict the potential activity and enzymological method was used to validate their efficacy components. Results The chloroform fraction showed a strong inhibition on tyrosinase activity. The bioactivities had the relationship with six components, such as tanshinol and protocatechualdehyde, etc. Enzymological method showed the same results with the screening. Conclusion Tanshinol, protocatechualdehyde, and so on in S. Miltiorrhiza have the significant inhibition on tyrosinase.