| 新型丹参素衍生物的合成与抗心肌缺血活性研究 |
| 投稿时间：2015-01-23 修订日期：2015-04-02 点此下载全文 |
| 引用本文：田霖,郭海霞,张洁,焦育强,吴秋业,张川.新型丹参素衍生物的合成与抗心肌缺血活性研究[J].药学实践杂志,2015,33(6):525~528,535 |
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| 中文摘要:目的 通过对丹参素进行结构改造,以改善其稳定性和药理活性。 方法 以中药提取的丹参素钠为起始化合物,经酯化反应、甲氧基保护酚羟基、硝化反应等合成新型的丹参素衍生物。建立心肌细胞缺氧模型,用MTT方法检测丹参素及其衍生物对缺氧H9c2细胞的保护作用。 结果 合成了15个全新的丹参素衍生物,并对其进行结构验证;药理活性实验显示,只有少数目标化合物在浓度为5 μmol/L时表现出强于丹参素的活性。 结论 多数化合物的最大药理活性未显现在所选浓度范围内,其活性未必低于丹参素,尚需做进一步探讨。 |
| 中文关键词:丹参素 结构修饰 合成 药理活性 |
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| Synthesis and anti-myocardial ischemia activities of novel Danshensu derivatives |
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| Abstract:Objective To design and synthesize novel Danshensu derivatives in order to improve their stability and cardio-protective effect against myocardial ischemia. Methods Novel Danshensu derivatives were synthesized chiefly via esterification,methoxy phenol hydroxyl protection,nitration and amine solution reaction. All the target compounds were evaluated their biological effects on anti-myocardial ischemia with H9c2 cells in vitro. Results 15 compounds were synthesized and further confirmed by 1H NMR and MS. Pharmacological studies showed that few synthetic derivatives at 5 μmol/L performed a higher biological effect than Danshensu. Conclusion Most derivatives didn't show the best activity at the chosen concentration gradient that a further pharmacological trial need to be done. |
| keywords:Danshensu structure modification synthesis pharmacological activity |
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