| 戴一,贾晓益,宋祖荣.SN38与呋咱氮氧化物偶联物的合成及抗肿瘤活性研究[J].井冈山大学自然版,2020,41(5):22-25 |
| SN38与呋咱氮氧化物偶联物的合成及抗肿瘤活性研究 |
| SYNTHESIS AND ANTI-TUMOR ACTIVITY OF CONJUGATE OF SN38 AND FUROXANS |
| 投稿时间：2020-06-06 修订日期：2020-07-29 |
| DOI：10.3969/j.issn.1674-8085.2020.05.005 |
| 中文关键词: SN38 呋咱氮氧化物 griess法 抗肿瘤 抗转移 |
| 英文关键词: SN38 furoxans griess method anti-tumor anti-metastasis |
| 基金项目:国家自然科学基金青年项目（81603362）；安徽省教育厅自然科学研究重点项目（KJ2019A0873）;安徽新华学院中药量效关系研究团队（kytd201908） |
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| 摘要点击次数: 1410 |
| 全文下载次数: 2019 |
| 中文摘要: |
| SN38为喜树碱类拓扑异构酶抑制剂。本研究以羧基呋咱氮氧化物与SN38的酚羟基成酯合成制备SN38与呋咱氮氧化物的偶联物，采用griess法、MTT法及划痕实验分别测定了该偶联物的体外NO释放、抗肿瘤活性及抗肿瘤转移活性。结果显示合成的SN38与呋咱氮氧化物偶联物24 h体外释放NO达32.4%，抗肿瘤活性比SN38及SN38与呋咱氮氧化合物的混合物更强，且具有一定的抗转移活性。可见SN38与呋咱氮氧化物的偶联物表现出显著的协同效应。 |
| 英文摘要: |
| SN38 is a topoisomerase inhibitor of camptothecin alkaloids type. The conjugate of SN38 and furoxans was synthesized through esterification of furoxan containing carboxyl with phenol hydroxyl of SN38. The NO release, antitumor activity and anti-metastasis activity of the conjugate of SN38 and furoxans in vitro were determined by Griess method, MTT method and scratch assay respectively. The results showed that the conjugate of curcumin and furoxans could be prepared. The percent of NO release from conjugate of SN38 and furoxans was 32.4% in vitro in 24 h. The anti-tumor activity of conjugate of SN38 and furoxans is more potent than those of SN38, or mixture of SN38 and furoxans. Moreover, the conjugate of SN38 and furoxans has anti-metastasis activity. These results indicated that the conjugate of SN38 and furoxans has significant synergistic effects. |
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