南瓜中甘油糖脂分离制备及体外抗肿瘤活性研究

Preparation Separation and Antioxidant Activities of Glycoglycerolipids from Pumpkin and Anti-Tumor Activity

采用高速逆流色谱与制备型高效液相色谱相结合的方法,从南瓜中分离制备甘油糖脂,并用MTT法检测不同甘油糖脂单体对不同肿瘤细胞生长抑制作用,并阐明其构效关系。结果表明:采用高速逆流色谱-制备HPLC联合法,从南瓜中分离得到6种甘油糖脂单体,并采用电喷雾质谱(ESI-MS)以及核磁共振氢谱(1H-NMR)和碳谱(13C-NMR)对化合物结构进行了鉴定。该方法制备量大,分离效率高。6种甘油糖脂单体对人结肠癌细胞COLO205和小鼠黑色素瘤细胞B16-F103均有一定的生长抑制作用,构效关系表明,抗肿瘤能力随着脂酰基不饱和程度的增加而提高,随糖基数目的增加而降低。南瓜中糖苷类化合物作为抗肿瘤药物具有较好的开发前景。

High -speed countercurrent chromatography （HSCCC） combined with preparative liquid chromatography （PHPLC） was developed for the preparative separation of glycoglycerolipids from the pumpkin. Meanwhile, the antiproliferative activity of glyeoglycerolipids on human lung cancer cells A549, human colon cancer cells COLO205, and B16 - F10 melanoma was evaluated by MTT （ microculture tetrazolium） method. The results showed that six gly- coglycerolipid monomers were isolated by a combination of HSCCC and PHPLC. Their structures were elucidated on the basis of spectroscopic analysis including electrospray mass spectrum （ ESI - MS）, 1H nuclear magnetic resonance （^1H-NMR） and ^13C nuclear magnetic resonance （^13C -NMR）. The results indicated that the method has both high preparative capacity and high efficieney in resolution. In vitro anti - tumor activity experiment exhibited that gly- coglycerolipids possessed inhibitory effects on the growth of tumor cell lines COLO205 and B16 - F10. The prelimina- ry relationship of structure - activity revealed that the anti - tumor activity of glycoglycerolipids depended on glycerol - sugar backbone and the saturated degree of the fatty acid groups. The anti - tumor efficacy of glyeoglycerolipids decreased as increase of galactosyl group number and increased as increase of double bond number. Glycoglycerolipids is possibly a potent antiproliferative compounds.