| 许爱狄,吴亚菊,周小群,苏时娟,许传鑫,杨菲菲,李芳耀.化学通报,2024,87(6):739-748. |
| 去氢枞酸异丙醇胺衍生物的合成及其细胞毒性评价 |
| Synthesis and cytotoxicity evaluation of dehydroabietic acid derivatives bearing isopropanolamine moieties |
| 投稿时间：2024-01-04 修订日期：2024-01-23 |
| DOI： |
| 中文关键词: 去氢枞酸 异丙醇胺 抗肿瘤 细胞周期 细胞凋亡 |
| 英文关键词:Dehydroabietic acid Isopropanolamine Antitumor Cell cycle Apoptosis |
| 基金项目:广西自然科学基金项目(2023GXNSFAA026277)、桂林市科学研究与技术开发计划项目(20210227-1)、广西林产化学与工程重点实验室开放课题(GXFK2202)、广西药物分子发现与成药性优化重点实验室课题(GKLPMDDO-2023-B03)、广西高等学校千名中青年骨干教师培育计划项目、桂林医学院硕士研究生科研项目(GYYK2023017)和国家级大学生创新创业训练计划项目(202210601033,202310601037)资助 |
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| 中文摘要: |
| 为了寻找高效的抗肿瘤活性化合物,设计合成了一系列去氢枞酸异丙醇胺类化合物,利用IR、NMR和MS对其结构进行表征。采用噻唑蓝(MTT)法评价了目标化合物对四种不同肿瘤细胞T24(人膀胱移行癌细胞)、HepG2(人肝癌细胞)、SK-OV-3(人卵巢癌细胞)、A549(人肺癌细胞)和LO2(人正常肝细胞)的抗增殖活性。结果表明,部分化合物对肿瘤细胞的抑制作用优于阳性对照顺铂。其中,化合物3d对四种细胞株表现出最好的抗增殖效果,IC50值分为8.10±0.28,8.65±0.10,13.21±0.35和8.24±0.42 μmol.L-1。初步机理研究表明,化合物3d使A549细胞周期阻滞在G1/G0期,并诱导A549细胞凋亡,且呈浓度依赖性。 |
| 英文摘要: |
| With the expectation to find out effective anti-tumor agents, a serious of novel dehydroabietic acid derivatives bearing isopropanolamine molecules were designed and synthesis, and the structures of target compounds were characterized by IR, NMR, and MS. In addition, the antiproliferative activity were evaluated against four different human cancer cell lines (T24, HepG2, SK-OV-3, A549) and human normal liver cell (LO2) using methyl thiazolyl tetrazolium (MTT) assay. The results demonstrated that some derivatives exhibited more potent cytotoxicity superior to cisplatin. Noticeably, compound 3d exhibited excellent anti-proliferation against the four cell lines with IC50 of 8.10±0.28 μmol.L-1(T24), 8.65±0.10 μmol.L-1(HepG2), 13.21±0.35 μmol.L-1(SK-OV-3) and 8.24±0.42 μmol.L-1(A549). The preliminary mechanism indicated that compound 3d arrest the cell cycle of A549 cancer cells in the G1/G0 phase and apoptosis of A549 cancer cells was induced in a concentration-dependent manner. |
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