Physical and chemical properties of acetylated low molecular weight heparin and its antineoplastic effect in vitro
10.3969/j.issn.1001-1978.2015.01.022
- VernacularTitle: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
- Author:
Ying LIANG
;
Guixin DUAN
;
Hao LIU
;
Zhiwen JIANG
- Publication Type:Journal Article
- Keywords:
acetylated low molecular weight heparin;
chemical modification;
acetylation;
proliferation;
inva-sion of cancer cells;
anticoagulant activity
- From:
Chinese Pharmacological Bulletin
2015;(1):103-107,108
- CountryChina
- Language:Chinese
-
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.
