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芳醛-[5-(3,4,5-三甲氧基苯基)-1,3,4-噻二唑-2-巯基]-乙酰腙衍生物的合成及生物活性研究
  • ISSN号:0253-2786
  • 期刊名称:有机化学
  • 时间:0
  • 页码:894-898
  • 语言:中文
  • 分类:R284.1[医药卫生—中药学;医药卫生—中医学]
  • 作者机构:[1]广西中医学院,南宁市明秀东路179号530001
  • 相关基金:广西教育厅科研项目[桂科研(2003)22-3]和国家自然基金项目(20562002)
  • 相关项目:具有抑菌活性双杂环砜类衍生物合成与生物活性研究
中文摘要:

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-广精氨酸(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。10pMDMY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。

英文摘要:

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.

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期刊信息
  • 《有机化学》
  • 中国科技核心期刊
  • 主管单位:
  • 主办单位:中国化学会 中国科学院上海有机化学研究所
  • 主编:陈庆云
  • 地址:上海市枫林路354号
  • 邮编:200032
  • 邮箱:bianji@mail.sioc.ac.cn
  • 电话:021-54925244
  • 国际标准刊号:ISSN:0253-2786
  • 国内统一刊号:ISSN:31-1321/O6
  • 邮发代号:4-285
  • 获奖情况:
  • 中国期刊方阵“双效”期刊
  • 国内外数据库收录:
  • 俄罗斯文摘杂志,美国化学文摘(网络版),荷兰文摘与引文数据库,美国科学引文索引(扩展库),日本日本科学技术振兴机构数据库,中国中国科技核心期刊,中国北大核心期刊(2004版),中国北大核心期刊(2008版),中国北大核心期刊(2011版),中国北大核心期刊(2014版),中国北大核心期刊(2000版)
  • 被引量:14408