双溴代马蹄金素衍生物的合成及其抗HBV活性 |
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引用本文: | 梁光平,;胡占兴,;黄正明,;刘青川,;张建新,;梁光义,;徐必学. 双溴代马蹄金素衍生物的合成及其抗HBV活性[J]. 遵义医学院学报, 2014, 0(3): 276-282 |
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作者姓名: | 梁光平, 胡占兴, 黄正明, 刘青川, 张建新, 梁光义, 徐必学 |
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作者单位: | [1]贵州省中国科学院天然产物化学重点实验室,贵州贵阳550002; [2]贵阳中医学院药学院,贵州贵阳550002; [3]中国人民解放军第302医院药学部,北京丰台100039 |
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基金项目: | 国家自然科学基金资助项目(NO:81360472);国家重大科学仪器设备开发专项项目(NO:2011YQ12003506) |
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摘 要: | 目的合成马蹄金素[N-(N-苯甲酰基-L-苯丙氨酰基)-O-乙酰基-L-苯丙氨醇,MTS]的类似物,以期寻找到高效低毒的抗乙肝病毒化合物。方法以6,8-二溴-L-酪氨酸为起始原料,通过酯化、酰化、水解、烷基化等反应,合成马蹄金素衍生物并对其进行体外抗乙肝病毒活性测试。结果合成了11个双溴取代的马蹄金素衍生物,在人肝癌细胞HepG2.2.15上对其中的9个化合物进行活性测试,其结果显示,化合物5c、5d、7b、7c在8μg·mL-1的浓度下具有较好的抑制活性,其抑制率分别为44.8%、48.8%、37.3%、38.4%。结论化合物5a在20μg·mL-1的浓度下具有较高的抑制活性,其抑制率达到89.8%,具有进一步研究开发的价值。
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关 键 词: | 马蹄金素 衍生物 合成 抗HBV活性 |
Synthesis and anti-hepatitis B virus activities of dibromo substituted Matijin-Su derivatives |
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Affiliation: | Liang Guangping,Hu Zhanxing,Huang Zhengming,Liu Qingchuan,Zhang Jianxin,Liang Guangyi,Xu Bixue(1. The Key Laboratory of Chemistry for Natural Products of Guizhou Province and Chinese Academy of Sci- ences, Guiyang Guizhou 550002, China; 2. Guiyang College of Traditional Chinese Medicine, Guiyang Guizhou 550002, China ; 3. 302 Hospital of PLA, Fengtai Beijing 100039, China) |
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Abstract: | Objective To find new anti-hepatitis B virus(HBV) compounds with high activity of anti-HBV activity and low toxicity from Matijin-Su(N-(N-benzoyl-L-phenylalanyl)-O-acetyl-L-phenylalanol,MTS).Methods A series of MTS derivatives was synthesized by esterification,acylation,hydrolysis,alkylation reactions and evaluated for their anti-HBV activity in human hepatoma HepG 2.2.15 cells.Results Eleven derivatives of MTS were synthesized and four target compounds exhibited high inhibition rate in8 μg·mL-1concentrations,5a(44.8%),5d(48.8%),7b(37.3%),7c(38.4%) respectively.Conclusion The compound 5a shows 89.8% inhibition rate of anti-HBV activity in 20 μg·mL-1concentrations,is worth of further research. |
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Keywords: | Matijin-Su derivatives synthesis anti-HBV activity |
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