Brefeldin ABFA布雷非德菌素AAbMoleM2294是一种天然大环内酯类化合物主要由真菌产生具有广泛的生物活性尤其在癌症研究和细胞生物学中应用广泛。其作用机制涉及干扰细胞内蛋白转运系统特别是高尔基体功能从而影响细胞信号通路、蛋白转运、细胞凋亡和炎症反应。在细胞中Brefeldin ACAS No.20350-15-6能通过抑制Arf-GEFs一种鸟苷酸交换因子导致Arf1蛋白失活从而破坏高尔基体结构并阻断蛋白转运。这影响了细胞因子分泌、膜蛋白表达和细胞稳态[1]。在细胞中Brefeldin A能诱导内质网应激触发未折叠蛋白反应UPR最终导致细胞凋亡。例如在小鼠皮肤黑素瘤细胞中Brefeldin A显著增加ER压力促进凋亡通路激活[2]。Brefeldin A雷非德菌素 A还参与细胞周期调控如在癌细胞中诱导有丝分裂阻滞并通过破坏不对称纺锤体定位影响减数分裂[1]。在A549人肺癌细胞、HeLa人宫颈癌细胞和HepG2人肝癌细胞中Brefeldin A的IC50值分别为101.2 nM、171.9 nM和239.1 nM显示出强效抗增殖活性[3]。Brefeldin ABFA在小鼠模型中的剂量为15 mg/kg/day采用0.5%的CMC-Na溶液溶解以抑制炎症性肠炎IBD[4]。范例详解Cell Metab. 2025 Mar 4;37(3):692-707.e9. IF30.9AbMole的Brefeldin ABFA布雷非德菌素AAbMoleM22945 μM用于抑制ARF1蛋白处理时间为1小时细胞为EMT6[5]参考文献及鸣谢[1] Cui, Z.; Yu, L.; Shi Yang, X.; et al. Brefeldin A impairs porcine oocyte meiotic maturation via interruption of organelle dynamics.Journal of cellular physiology2019,234(11), 20111-20117.[2] Taskaeva, I. S.; Gogaeva, I. S.; Bgatova, N. P. Expression of Apoptosis-Associated Proteins in Tumor Cells under Autophagy and Endoplasmic Reticulum Stress Stimulation in Mouse Skin Melanoma Model.Bulletin of experimental biology and medicine2025,179(4), 476-480.[3] Wang, C. F.; Ma, J.; Jing, Q. Q.; et al. Integrating Activity-Guided Strategy and Fingerprint Analysis to Target Potent Cytotoxic Brefeldin A from a Fungal Library of the Medicinal Mangrove Acanthus ilicifolius.Marine drugs2022,20(7).[4] Li, H.; Shen, X.; Qin, X.; et al. (R)-STU104 and Brefeldin-A Synergistically Enhance the Therapeutic Effect On IBD By Inhibiting the TAK1-MKK3-P38 Signaling Pathway.Current molecular pharmacology2024,17, e18761429377081.[5] Zhao, C.; Zhang, T.; Xue, S. T.; et al. Adipocyte-derived glutathione promotes obesity-related breast cancer by regulating the SCARB2-ARF1-mTORC1 complex.Cell metabolism2025,37(3), 692-707.e699.