| L-精氨酸基姜黄素衍生物的合成及抑菌性评价 |
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| 引用本文： | 李海鹰,邱明恒,陈健,王桂静,杨文智. L-精氨酸基姜黄素衍生物的合成及抑菌性评价[J]. 河北大学学报(自然科学版), 2021, 41(2): 155-160. DOI: 10.3969/j.issn.1000-1565.2021.02.007 |
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| 作者姓名： | 李海鹰 邱明恒 陈健 王桂静 杨文智 |
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| 作者单位： | 河北大学药学院,生命科学与绿色发展研究院,河北保定 071002 |
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| 基金项目： | 河北省自然科学基金资助项目(H2018201045);河北省高等学校科学技术研究项目(ZD2018054) |
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| 摘 要： | 以4-二甲氨基吡啶(DMAP)为催化剂,1-(3-二甲氨基丙基)-3-乙基碳二亚胺(EDC)为脱水剂,琥珀酸(Sa)为连接臂,通过酯化和酰胺化反应将姜黄素接枝到L-精氨酸分子上,获得新型L-精氨酸基姜黄素(Cur-Sa-Arg)衍生物,产物经UV-Vis、FT-IR、1 H NMR和DSC表征,证明已成功合成.与姜黄素...
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| 关 键 词： | 姜黄素 L-精氨酸 化学接枝 溶解度 体外抗菌 |
| 收稿时间： | 2020-08-15 |
Synthesis and antibacterial evaluation of L-arginine curcumin derivative |
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| LI Haiying,QIU Mingheng,CHEN Jian,WANG Guijing,YANG Wenzhi. Synthesis and antibacterial evaluation of L-arginine curcumin derivative[J]. Journal of Hebei University (Natural Science Edition), 2021, 41(2): 155-160. DOI: 10.3969/j.issn.1000-1565.2021.02.007 |
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| Authors: | LI Haiying QIU Mingheng CHEN Jian WANG Guijing YANG Wenzhi |
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| Affiliation: | Institute of Life Science and Green Development, College of Pharmacy, Hebei University, Baoding 071002, China |
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| Abstract: | L-arginine based curcumin derivative with a succinic acid linker(Cur-Sa-Arg)was synthesized via esterification and amidation reaction using 4-dimethylaminopyridine(DMAP)and 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide(EDC)as catalyzer. The product was characterized by UV-Vis, FT-IR, 1H NMR and DSC, and the results indicated that Cur-Sa-Arg was successfully synthesized. The curcumin solubility in Cur-Sa-Arg was more than about 3 000 times higher than curcumin and reached up to 30.1 μg/mL. Moreover, the result of bacteriostatic experiment showed that the IC50 values against Gram-negative bacteria including Pseudomonas aeruginosa, Escherichia coli and Salmonella ratus decreased by 3—6 times, and the IC50 value against Gram-positive bacteria of Staphylococcus aureus dropped by 2 times. Compared with pure curcumin, Cur-Sa-Arg has a higher solubility and better antibacterial properties. |
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| Keywords: | curcumin L-arginine chemical grafting solubility antibacterial activity in vitro |
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