李晓艺,邹秋萍,毛泽伟,李艳平.化学通报,2023,86(2):240-243.
去氢木香内酯衍生物的合成及其抗炎活性研究
Synthesis and anti-inflammatory Activity of dehydrocostuslactone derivatives
投稿时间:2022-06-08  修订日期:2022-07-13
DOI:
中文关键词:  去氢木香内酯  合成  抗炎活性  毒性
英文关键词:dehydrocostuslactone  synthesis  toxicity  anti-inflammatory activity
基金项目:国家自然科学基金项目(81960777)和云南省科学技术厅-云南中医药大学应用基础研究联合专项项目(2019FF002(-005),2018FF001(-029))资助
作者单位E-mail
李晓艺 云南中医药大学中药学院 2360369619@qq.com 
邹秋萍 云南中医药大学中药学院  
毛泽伟 云南中医药大学中药学院  
李艳平* 云南中医药大学中药学院 lyp8691@163.com 
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中文摘要:
      去氢木香内酯是一种含有多种生物活性的倍半萜化合物,广泛存在于药材云木香中。去氢木香内酯与伯胺化合物经Michael加成反应,合成得到5个新的去氢木香内酯衍生物(1-5),其结构均经1H NMR、13C NMR和LC-MS确证。采用小鼠巨噬细胞Raw264.7模型初步测试了衍生物的抗炎活性和毒性,结果表明,化合物1对NO的生成抑制率为88 ± 1.02,表现出较好的抗炎活性,且在MTT实验中,其对巨噬细胞的抑制率仅为3.75%,几乎无细胞毒性,可作进一步研究。
英文摘要:
      Dehydrocostuslactone, one of sesquiterpene lactone compounds with a variety of biological activities, is widely found in the natural drug mullein. Dehydrocostuslactone derivatives (1-5) were obtained by addition reactions of dehydrocostuslactone with primary amine compounds, and their structures were confirmed by IR, 1H NMR and 13C NMR. The anti-inflammatory activity of the derivatives was initially tested using the mouse macrophage Raw264.7 model, and the results showed that compound 1 exhibited good anti-inflammatory activity with an NO production inhibition rate of 88 ± 1.02 and didn’t show obvious cytotoxicity with a cytostatic rate of 3.75%.
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