期刊论文

Effect of 1,3-O,N spiroheterocyclic inhibitors of heparanase on the growth of HeLa cells

中文

中华妇产科杂志

Chinese Journal of Obstetrics and Gynecology

0529-567X

2015

50

7

529-536

10.3760/cma.j.issn.0529-567x.2015.07.010

国家自然科学基金(81341065);河南省教育厅科学技术研究重点项目(12A320024)

本校为其他机构

目的通过观察乙酰肝素酶(HPA)抑制剂对子宫颈癌HeLa细胞体外生长的抑制作用及HPA表达的影响,为子宫颈癌HPA分子靶向治疗提供理论依据。方法优化设计并合成了两个系列共13种1,3-O,N螺杂环类化合物,产品编号为10~22号,其中21号为HPA抑制剂——DMBO化合物,余12种为新合成的化合物。其中,1个系列含甲氧苯基,产品编号为10~14号;另1个系列不含甲氧苯基,产品编号为15~22号。(1)采用乙酰肝素降解检测试剂盒检测新合成的化合物(选择与DMBO结构类似度高的6个化合物,即14、15、16、20、21、22号化合物)对HPA活性的作用,以50%抑制浓度(IC_(50))表示作用的强弱;(2)四甲基偶氮唑蓝(MTT)比色法检测新合成的化合...

OBJECTIVE: To provide the theoretical supportting for targeted heparanase (HPA) inhibition of cervical cancer through observing the anti-proliferative effect of the HPA inhibitor on HeLa cell line of cervical cancer. METHODS: The two series of 13 kinds of novel HPA inhibitors were synthesized and optimized. Heparan degrading enzyme assay kit was used to test the effect of the inhibitors on the inhibition of HPA enzyme activity. Methyl thiazolyl tetrazolium (MTT) method and scratch test were used to observe the anti-proliferative and the migration effect of the inhibitors on HeLa cells. Flow cy...