| 程相成,海洋,王毓,等.海洋天然产物 (+)-sclerotiorin衍生物的半合成及抗菌活性研究[J].中国海洋药物,2026,45(1):59-64. |
| 海洋天然产物 (+)-sclerotiorin衍生物的半合成及抗菌活性研究 |
| Semisynthesis and Antibacterial Activity Study of Marine Natural Product (+)-sclearotiorin Derivatives |
| 投稿时间：2024-04-27 修订日期：2024-06-06 |
| DOI：10.13400/j.cnki.cjmd.2026.01.005 |
| 中文关键词: 抗菌活性 海洋天然产物 (+)-sclerotiorin衍生物 |
| English Keywords:antibacterial activity marine natural products (+)-sclearotiorin derivatives |
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| 中文摘要: |
| 目的 以海洋天然产物(+)-sclerotiorin(1)为原料,通过结构修饰制备其衍生物并进行抗菌活性研究。方法 通过取代反应、水解反应制备(+)-sclerotiorin衍生物(2–12),并使用铜绿假单胞杆菌(Pseudomonas aeruginosa)、金黄色葡萄球菌(Staphylococcus aureus)和大肠杆菌(Escherichia coli)对衍生物抗菌活性进行评价。结果 抗菌活性结果显示,衍生物5、7、8和11表现出明显铜绿假单胞杆菌生长抑制活性,MIC90(抑菌90%细菌生长的最低药物浓度)在10.5–13.7 μM之间,而衍生物对金黄色葡萄球菌和大肠杆菌的抑制活性较弱。结论 本研究以海洋天然产物(+)-sclerotiorin(1)为原料共制备11个衍生物,新衍生物8个,其中衍生物5、7、8和11对铜绿假单胞杆菌具有较好的抑制作用,为开发抗铜绿假单胞杆菌药物提供了研究基础。 |
| English Summary: |
| Objective A series of derivatives were synthesized with marine natural product (+)-sclearotiorin (1), and their antibacterial activities were evaluated. Methods (+)-sclearotiorin derivatives (2–12) were prepared through substitution and hydrolysis reactions, and evaluation of their antibacterial activity using Pseudomonas aeruginosa, Staphylococcus aureus and Escherichia coli. Results The antibacterial activity results showed that derivatives 5, 7, 8 and 11 exhibited significant growth inhibition activity against Pseudomonas aeruginosa, with MIC90 (the minimal inhibit concentration for inhibiting 90% bacterial growth) ranging from 10.5 to 13.7 μM, but derivatives had weaker inhibitory activity against Staphylococcus aureus and Escherichia coli. Conclusion This study Semisynthesized 11 derivatives (8 new derivatives) using marine natural product (+)-sclearotiorin (1). Among them, 5, 7, 8 and 11 had good inhibitory effects on Pseudomonas aeruginosa, which provided a research basis for the development of drugs against Pseudomonas aeruginosa. |
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