中国药理学通报Issue(1)：103-107,108,6.DOI:10.3969/j.issn.1001-1978.2015.01.022
低分子量肝素乙酰化物的理化特性及其体外抗肿瘤活性研究
Physical and chemical properties of acetylated low molecular weight heparin and its antineoplastic effect in vitro
摘要
Abstract
Aims To synthesize acetylated low molecu-lar weight heparin( ALMWH) and to detect its physico-chemical properties and antineoplastic activity. Meth-ods LMWH was prepared by degradation of UFH with sodium periodate oxidation and sodium borohydride re-duction, then the LMWH was acetylated by acetic an-hydride where N, N′, -dicyclohexylcarbodiimide ( DCC ) and 4-dimethylaminopyridine ( DMAP ) were used as catalysts. X-ray diffraction(XRD)and Differ-ential Scanning Calorimetry ( DSC ) of ALMWH were obtained. The antiproliferative activity and anti-inva-sive activity were determined on MDA-MB-231 and MCE-7 human breast cancer cells. Results XRD a-nalysis showed that the LMWH degraded from UFH and ALMWH synthesized by acetylation of LMWH be-longed to amorphous structure, however, their DSC curves were significantly different. Compared with LM-WH, ALMWH had more powerful capacity for binding water and lowering anticoagulant activity, more signifi-cantly ALMWH exhibited stranger anti-proliferative and anti-invasive activity than LMWH, especially when it was used in low concentrations. Conclusion The syn-thesized ALMWH possesses a low anticoagulant activi-ty, certain anti-proliferative, anti-invasive and anti-metastatic activity. This study provides a basic method for screening of antineoplastic drug with low toxicity.关键词
低分子量肝素/化学修饰/乙酰化/肿瘤细胞增殖/肿瘤细胞侵袭/抗凝血活性Key words
acetylated low molecular weight heparin/chemical modification/acetylation/proliferation/inva-sion of cancer cells/anticoagulant activity分类
医药卫生引用本文复制引用
梁颖,段贵新,刘浩,蒋志文..低分子量肝素乙酰化物的理化特性及其体外抗肿瘤活性研究[J].中国药理学通报,2015,(1):103-107,108,6.基金项目
国家自然科学基金资助项目( No 30972864) （ No 30972864）
安徽省教育厅自然科学研究重点项目(No KJ2012A202) （No KJ2012A202）
安徽省教育厅自然科学研究一般项目(No KJ2013B140) （No KJ2013B140）
