水溶性双氢杨梅素复合物的制备、表征及抗肿瘤活性研究

Studies on Preparation of Water-soluble Dihydromyricetin Arginine Compound and Its Characterization and Antineoplastic Activity

目的:制备水溶性双氢杨梅素精氨酸复合物(DAC),拓宽双氢杨梅素(DMY)的给药途径,提高其抗肿瘤活性。方法:取一定量DMY和L-精氨酸(ARG)在乙醇中回流制备DAC,通过紫外吸收光谱、红外吸收光谱、质谱、核磁共振波谱等方法对DAC进行了结构表征。并采用SRB法对DMY和DAC进行体外抗肿瘤活性考察。结果:物质的量比例为1∶1的DMY和ARG形成了DAC,并且干燥的DAC在常温干燥环境下比较稳定。与DMY比较,DAC的水溶性显著增大。10μMDMY和DAC对BGC-823生长的抑制率分别为11.36%、32.67%,对BEL-7402生长的抑制率分别为2.93%、11.33%。结论:该制备方法简捷实用,极大增加了双氢杨梅素的水溶性,有助于提高DMY的生物利用度。抗肿瘤活性测试结果表明,DAC的体外抗肿瘤活性较DMY有所增强。

Objective： To prepare water - soluble dihydromyricetin arginine compound （DAC）, expand administration route of dihydromyricetin （DMY） and enhance its antineoplasfic activity. Methods： DAC was prepared by refluxing certain amount of DMY and L-arginine in ethanol. DAC was structurally characterized by ultra-violet absorption spectrum, infrared absorption spectrum, mass spectrum 、 nuclear magnetic resonance spectrum. Antineoplastic activity of DMY and DAC was observed by SRB method in vitro. Results： DAC was produced with DMY and arginine with a ratio of 1 ： 1. Dry DAC was relatively stable in a dry, common - temperature circumstance. Solubility of DAC enhanced significantly compared with that of DMY. The inhibition ratios of DMY and DAG （10μM） on BC, C-823 growth were 11.36% and 32.67%, respectively ; in terms of inhibiting growth of BEL-7402, the inhibition ratios of DMY and DAG （10μM） were 2.93% and 11.33% .Conclusions： This preparative method is sample and practical. It increases the solubility of DMY to a great extent, thus contributing to its biological availability. Antineoplastic activity test indicated that the antineoplastic activity of DAC is, to some extent, stronger than that of DMY in vitro.