首页|期刊导航|中药与临床|诱导三阴性乳腺癌细胞凋亡的Miliusol衍生物的发现及其体内外抗TNBC活性评价

诱导三阴性乳腺癌细胞凋亡的Miliusol衍生物的发现及其体内外抗TNBC活性评价OA

Identification of Miliusol derivative inducing apoptosis in triple-negative breast cancer cells and evaluation of its anti-TNBC activity in vitro and in vivo

中文摘要英文摘要

目的:合成并探究Miliusol衍生物诱导三阴性乳腺癌细胞凋亡的作用及其对肿瘤活性的影响.方法:通过对天然小分子Miliusol进行结构修饰得到了新型衍生物YH8,采用MTT法、克隆形成实验、Transwell实验及划痕实验,评估Miliusol(0.8 μΜ)及其衍生物YH8(0.4、0.8 μΜ)对4T1细胞增殖与迁移能力的影响;利用流式细胞术和Western blot法检测Miliusol及YH8对4T1细胞凋亡的诱导作用;通过建立4T1荷瘤小鼠模型,评价YH8(10 mg·kg-1)的体内抗肿瘤效应.结果:Miliusol与YH8均可在体外抑制4T1细胞的增殖与迁移,并诱导细胞凋亡;在等剂量条件下,YH8的作用效果优于Miliusol.此外,YH8在体内能够显著抑制4T1肿瘤的生长.结论:YH8在体内外均能有效抑制三阴性乳腺癌细胞的生长,其主要作用机制为诱导细胞凋亡.

Objective:To synthesize and explore the role of Miliusol derivatives in inducing apoptosis in triple-negative breast cancer cells and their effects on tumor activity.Methods:Through structural modification of the naturally occurring small molecule Miliusol,a novel derivative designated as YH8 was synthesized.The MTT assay,colony formation assay,transwell as-say,and scratch assay were used to evaluate the effects of Miliusol(0.8 μM)and its derivative YH8(0.4,0.8 μM)on the prolifera-tion and migration capacity of 4T1 cells.Flow cytometry and western blot analysis were employed to assess the apoptotic effects of Miliusol and YH8 on 4T1 cells.The in vivo antitumor effect of YH8(10 mg·kg-1)was evaluated using a 4T1 tumor-bearing mouse model.Results:Both Miliusol and YH8 inhibited the proliferation and migration of 4T1 cells in vitro and induced apopto-sis.Under equal dosage conditions,YH8 demonstrated superior efficacy compared to Miliusol.Furthermore,YH8 significantly in-hibited the growth of 4T1 tumors in vivo.Conclusion:YH8 effectively inhibits the growth of triple-negative breast cancer cells both in vitro and in vivo,with its primary mechanism of action being the induction of apoptosis.

赖玉培;赵曦;程小玲;张瑾;黄维

成都中医药大学 药学院,四川 成都 611137成都中医药大学 药学院,四川 成都 611137深圳大学 医学部药学院,广东 深圳 518055深圳大学 医学部药学院,广东 深圳 518055成都中医药大学 药学院,四川 成都 611137

医药卫生

Miliusol凋亡TNBC抗肿瘤

MiliusolapoptosisTNBCantitumor

《中药与临床》 2026 (3)

33-39,7

国家自然科学基金(W2511087)四川省科技厅重点研发计划(2024YFFK0092)深圳市基础研究面上项目(JCYJ20240813142819026)

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