2,4,6,4'-四羟基脱氧安息香的合成及其抑制酪氨酸酶活性的研究

Sythesis of 2,4,6,4'-Tetrahydroxydeoxybenzoin and Study on Its Inhibitory Activity Against Tyrosinase

合成2,4,6,4'-四羟基脱氧安息香(THDB),对其抑制酪氨酸酶活性进行评价。在无水氯化锌和氯化氢存在下,以间苯三酚和对羟基苯乙腈为原料,进行THDB的合成,并对所得化合物在0.05%、0.10%、0.20%、0.25%、0.30%、0.35%、0.40%七个浓度下与根皮素、熊果苷和曲酸进行抑制酪氨酸酶对比实验。收率由原来报导的46.5%提高到60.0%,在0.4%浓度时THDB对酪氨酸酶的抑制率达98.2%。本工艺是合成THDB的较佳工艺,THDB对酪氨酸酶的抑制作用比熊果苷和曲酸好,与根皮素相当。

To synthesize 2,4,6,4＇-tetrahydroxydeoxybenzoin and to evaluate its inhibitory activity against tyrosinase, phloroglucinol and 4-hydroxyphenylacetonitrile were used to react with anhydrous zinc chloride and hydrogen chloride to obtain THDB, and THDB was compared with phloretin arbutin and kojic acid in the inhibitory activity against tyrosinase under seven concentrations 0.05%, 0. 10%, 0. 20%, 0. 25%, 0.30%, 0.35%, 0. 40%. THDB was synthesized with a good yield of 60.0%. When concentration was 0.4%, its inhibitory activity could reach to 98.2%. This method is a better technique to synthesiz THDB, its inhibitory activity against tyrosinase is better than arbutin or kojic acid, equivalent to phloretin.