高良姜素；_L精氨酸；_水溶性衍生物；

水溶性高良姜素精氨酸酯的制备研究

http://www.100md.com 《时珍国医国药》 2006年第6期

高良姜素；,L精氨酸；,水溶性衍生物；,K562细胞,,高良姜素；,L精氨酸；,水溶性衍生物；,K562细胞,摘要,关键词,1仪器与材料,2方法与结果,3讨

     摘要：目的制备水溶性高良姜素衍生物，提高高良姜素的生物利用度。方法采用过量的L精氨酸与高良姜素在乙醇中回流反应，反应混合物经柱层析分离纯化，得3个水溶性化合物B，C，D。结果经TLC，UV，IR谱初步分析，确定B，C，D分别为：高良姜素一精氨酸酯、高良姜素二精氨酸酯、高良姜素三精氨酸酯。高良姜素，B，C，D 抑制红白血病K562细胞生长的IC50(μg/ml)值分别为：26.2，40.4，47.9，60.5。结论此高良姜素水溶性衍生物的制备反应为一酯化过程；但高良姜素结构中羟基封闭不利于其生物活性的保持。

    关键词：高良姜素； L精氨酸；水溶性衍生物； K562细胞

    Study on Preparation of the Water Soluble Galangin-arginine Ester

    FU Weiyu, ZHANG Jianhe, LUO Hui, SHE Ji*, LIANG Nianci

    (Department of Chemistry, Guangdong Medical College, Zhanjiang, 524023, China)

    Abstract：ObjectiveTo prepare the water solubte galanginarginine derivative and improve the bioavailability of galangin (Ga). MethodsOverdosly Larginine and Ga were refluxed in alcohol. Reaction compounds were isolated on silica gel column chromatography and their structures were identified by spectral and chemical analysis. ResultsThree water solube compounds were isolated and identified as galanginmonoargininate(B), galangindiargininate (C) and galangin-triargininate (D). Ga, B, C and D inhibited the growth of erythroleukoemia K562 cells, and the inhibited IC50(μg/ml) values were 26.2, 40.4, 47.9 and 60.5. ConclusionThe above preparation of the water soluble Galanginarginine derivative were esterification process,but the blocking of Hydroxyl in Ga structure was disadvantageous to keep its bioavailability. ......

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