| 芒果苷衍生物的合成及其PTP1B酶抑制活性研究 |
| 投稿时间：2011-01-06 修订日期：2011-03-10 点此下载全文 |
| 引用本文：周宇,胡丽娜,罗剑飞,俞世冲,吴秋业.芒果苷衍生物的合成及其PTP1B酶抑制活性研究[J].药学实践杂志,2011,29(3):193~196 |
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| 基金项目:上海市科委基础重点项目 ( 08JC1405500). |
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| 中文摘要:目的 设计合成一系列芒果苷衍生物并进行体外蛋白酪氨酸磷酸酶1B(PTP1B)抑制活性实验。 方法 利用亲核取代反应在芒果苷上引入疏水苄基,设计合成8个新化合物4~11,采用比色法对化合物进行PTP1B抑制活性研究。 结果 设计合成的8个化合物对PTP1B酶都有一定的抑制作用。 结论 芒果苷衍生物的活性明显好于芒果苷本身的活性,苄基的对位取代活性要优于邻位和间位取代,且苄基上氯原子取代的衍生物要高于其它原子取代的化合物活性。 |
| 中文关键词:芒果苷 蛋白酪氨酸磷酸酶1B 化学合成 抑制活性 |
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| Synthesis and PTP1B activity of enzyme inhibition of mangiferin derivates |
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| Abstract:Objective To synthetize and conduct PTP1B inhibitory activity experiment of series of novel mangiferin derivates. Methods Different benzyl groups were introduced to mangiferin framework by nucleophilic substitution reaction. All the compounds were screened against protein tyrosine phosphatase 1B(PTP1B)with the colorimetrie assay. Results Eight compounds were synthesized and all the compounds exhibited PTP1B inhibitory activity to some extent. Conclusions Derivates of mangiferin remarkably enhanced the activity compared with mangiferin itself. In addition, the benzylated derivates with chloro atom had better inhibitory activity than other substitution groups. Furthermore,the para position of the benzyl was a better place for introducing substituent than meta and ortho position. |
| keywords:mangiferin protein tyrosine phosphatase 1B chemical synthesis inhibition |
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