Integrated Biosciences Graduate Program, University of Minnesota, Duluth, MN, 55812, USA.
Department of Cell Biology and Biochemistry, Texas Tech University Health Sciences Center, Lubbock, TX, 79430, USA.
Biochem Biophys Res Commun. 2021 Jul 12;562:127-132. doi: 10.1016/j.bbrc.2021.05.062. Epub 2021 May 26.
A novel nitrogen mustard CBISC has been synthesized and evaluated as an anticancer agent. CBISC has been shown to exhibit enhanced cell proliferation inhibition properties against mutant p53 cell lines colorectal cancer WiDr, pancreatic cancer (MIAPaCa-2 and PANC-1), and triple negative breast cancer (MDA-MB-231 and MDA-MB-468). In vitro mechanism of action studies revealed perturbations in the p53 pathway and increased cell death as evidenced by western blotting, immunofluorescent microscopy and MTT assay. Further, in vivo studies revealed that CBISC is well tolerated in healthy mice and exhibited significant in vivo tumor growth inhibition properties in WiDr and MIAPaCa-2 xenograft models. These studies illustrate the potential utility of CBISC as an anticancer agent.
一种新型氮芥 CBISC 已被合成并评估为抗癌剂。研究表明，CBISC 对突变型 p53 细胞系结直肠癌 WiDr、胰腺癌 (MIAPaCa-2 和 PANC-1) 和三阴性乳腺癌 (MDA-MB-231 和 MDA-MB-468) 的细胞增殖抑制作用增强。体外作用机制研究表明，CBISC 通过 Western blot、免疫荧光显微镜和 MTT 检测导致 p53 通路紊乱和细胞死亡增加。此外，体内研究表明，CBISC 在健康小鼠中耐受性良好，并在 WiDr 和 MIAPaCa-2 异种移植模型中表现出显著的体内肿瘤生长抑制作用。这些研究说明了 CBISC 作为抗癌剂的潜在用途。
