| 引用本文: | 张莉萍,刘衍季,余卫强,杨南,李瑾,吴菁,涂丽华.橙皮素微量元素配合物的合成及其生物活性研究[J].中国现代应用药学,2021,38(16):1958-1963. |
| ZHANG Liping,LIU Yanji,YU Weiqiang,YANG Nan,LI Jin,WU Jing,TU Lihua.Study on the Synthesis and Bioactivity of the Complexes of Hesperetin with Trace Elements[J].Chin J Mod Appl Pharm(中国现代应用药学),2021,38(16):1958-1963. |
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| 摘要: |
| 目的 合成橙皮素钙、铁、硒、锌、铬配合物5种中药新药，并研究其抗菌、抗肿瘤活性和清除自由基的能力。方法 在碱性条件下通过合成得到橙皮素钙、铁、硒、锌、铬配合物，采用倍比稀释法测定橙皮素及其配合物对大肠杆菌等8种菌的抑制活性，采用MTT法测定橙皮素及其配合物对Tca-8113等6种肿瘤细胞增殖的影响，采用超氧阴离子自由基清除法测定橙皮素及其配合物对超氧阴离子自由基的清除能力。结果 合成的5种配合物配位比均为2∶1（橙皮素∶微量元素），产率均>70%，小鼠急性毒性试验显示5种配合物均无明显毒性，5种配合物最小抑菌浓度均低于橙皮素，抗菌活性至少提升至1~4倍；5种配合物对肿瘤细胞的IC50均小于橙皮素，抗肿瘤活性至少提升至1.19~2.41倍；橙皮素及其配合物对超氧阴离子自由基均有一定的清除作用，且均呈浓度依赖性，配合物对超氧阴离子自由基的清除率均高于橙皮素。结论 5种橙皮素微量元素配合物的抗菌、抗肿瘤活性和自由基清除能力均强于橙皮素。 |
| 关键词: 橙皮素 微量元素 配合物 抗菌 抗肿瘤 超氧阴离子自由基 |
| DOI：10.13748/j.cnki.issn1007-7693.2021.16.006 |
| 分类号:R914.5 |
| 基金项目:江西省中医药科研课题（2019A362） |
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| Study on the Synthesis and Bioactivity of the Complexes of Hesperetin with Trace Elements |
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ZHANG Liping1, LIU Yanji1, YU Weiqiang1, YANG Nan1, LI Jin1, WU Jing2, TU Lihua1
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1.Nanchang Health School, Nanchang 330006, China;2.Third Affiliated Hospital of Nanchang University, Nanchang 330008, China
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| Abstract: |
| OBJECTIVE To synthesize five new traditional Chinese medicines of hesperetin calcium, iron, selenium, zinc, and chromium complexes, and to study their antibacterial and anti-tumor activities and the ability to scavenge free radicals. METHODS The complexes of hesperetin with calcium, iron, selenium, zinc and chromium were synthesized under alkaline conditions. The inhibitory activity of hesperetin and its complexes on 8 kinds of bacteria was determined by multiple dilution method, and the effect of hesperetin and its complexes on the proliferation of 6 kinds of tumor cells, such as Tca-8113, was determined by MTT method, superoxide anion radical scavenging method was used to determine the scavenging ability of hesperetin and its complexes to superoxide anion radicals. RESULTS The coordination ratio of the five complexes was 2:1(hesperetin:microelements), and the yield was over 70%. The acute toxicity experiment of mice showed that the five complexes had no obvious toxicity. The minimal inhibit concentration of the five complexes was lower than that of hesperetin, and the antibacterial activity was increased to 1-4 times at least. The IC50 of the five complexes was lower than that of hesperetin, and the antitumor activity was increased to 1.19-2.41 times at least. Hesperetin and its complexes had a certain scavenging effect on superoxide anion radicals, and both of them were concentration dependent. The scavenging rate of complexes to superoxide anion radicals was higher than hesperetin. CONCLUSION The anti-bacterial and anti-tumor activities and free radical scavenging ability of five kinds of hesperetin microelement complexes were better than that of hesperetin. |
| Key words: hesperetin trace element complex antibiosis antitumor superoxide anion radical |
