Department of Pharmacology, Kwandong University College of Medicine, Gangneung 210-701, Republic of Korea.
Biochem Biophys Res Commun. 2012 Feb 24;418(4):616-21. doi: 10.1016/j.bbrc.2012.01.049. Epub 2012 Jan 28.
In this study, we investigate an anti-mitotic potential of the novel synthetic coumarin-based compound, 7-diethylamino-3(2'-benzoxazolyl)-coumarin, in 5-fluorouracil-resistant human gastric cancer cell line SNU-620-5FU and its parental cell SNU-620. It exerts the anti-proliferative effects with similar potencies against both cancer cells, which is mediated by destabilization of microtubules and subsequent mitotic arrest. Furthermore, this compound enhances caspase-dependent apoptotic cell death via decreased expression of anti-apoptotic genes. Taken together, our data strongly support anti-mitotic potential of 7-diethylamino-3(2'-benzoxazolyl)-coumarin against drug-resistant cancer cells which will prompt us to further develop as a novel microtubule inhibitor for drug-resistant cancer chemotherapy.
在这项研究中，我们研究了新型合成香豆素基化合物 7-二乙氨基-3(2'-苯并恶唑基)-香豆素在 5-氟尿嘧啶耐药人胃癌细胞系 SNU-620-5FU 及其亲本细胞 SNU-620 中的抗有丝分裂潜力。它对两种癌细胞均表现出相似的增殖抑制作用，这是通过微管的不稳定性和随后的有丝分裂阻滞介导的。此外，该化合物通过降低抗凋亡基因的表达来增强 caspase 依赖性凋亡细胞死亡。总之，我们的数据强烈支持 7-二乙氨基-3(2'-苯并恶唑基)-香豆素对耐药癌细胞的抗有丝分裂潜力，这将促使我们进一步将其开发为用于耐药癌症化疗的新型微管抑制剂。
