| 黄士杰,唐娅,马钦博,等.Plinabulin衍生物的设计、合成及抗肿瘤活性研究[J].中国海洋药物,2025,(6):-. |
| Plinabulin衍生物的设计、合成及抗肿瘤活性研究 |
| Design, synthesis and anti-tumor evaluation of plinabulin derivatives |
| 投稿时间：2024-07-24 修订日期：2024-09-06 |
| DOI： |
| 中文关键词: Plinabulin衍生物 抗肿瘤 β-微管蛋白 细胞周期阻滞 细胞凋亡 |
| English Keywords:Plinabulin derivatives, Antitumor β-tubulin, Cell cycle arrest, Apoptosis |
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| 中文摘要: |
| 目的 对Plinabulin B环4位的NH进行修饰，共设计合成了7个新衍生物，并对其抗肿瘤活性进行评价。方法 利用MTT法，评价了所有衍生物的抗肿瘤活性，利用流式细胞术评价了细胞周期阻滞和促凋亡作用，利用免疫荧光实验，评价了破坏微管蛋白形态的作用。通过免疫荧光实验评价了微管破坏作用。结果 其中，P6对被试细胞系具有较好的抑制活性。免疫荧光试验显示，作用浓度在180 nmol/L时的P6可以显著扰乱微管结构。流式细胞术分析表明，P6以剂量依赖性方式诱导细胞的G2/M细胞周期停滞和细胞凋亡，可以作为抗微管剂用于癌症治疗的候选药物。 |
| English Summary: |
| Objective To modify the 4-position of the B ring of Plinabulin, a total of 7 novel compounds were synthesized, and their antitumor activity were evaluated.Methods The cytotoxic activities of all derivatives against cancer cell lines were evaluated using MTT assay, and the cell cycle arrest and apoptosis promotion effects were evaluated using flow cytometry. Tubulin destructive effect were evaluated using Immunofluorescence experiments.Results Among these derivatives, P6 exerted comparable inhibitory effect against tested cell lines. Immunofluorescence assay showed that P6 at a concentration of 180 nmol/L significantly disturbed tubulin structure. Flow cytometry analysis demonstrated that P6 induced obvious G2/M cell cycle arrest and apoptosis in dose dependent manner. This study developed a potential candidate for cancer treatment as antimicrotubule agent. |
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