一种罗汉果叶黄酮Cu配合物的表征及活性研究

Characterization and activity of Cu complex with a flavonoid from Siraitia grosvenorii(Swingle) C. Jeffrey leaves

目的分离制取罗汉果叶黄酮,并与Cu配位形成Cu配合物,分别测定两种样品的癌细胞抑制活性,验证金属配位的影响效果。方法通过高速逆流色谱分离法(HSCCC)分离罗汉果叶粗提物,从中分离得到山奈酚-3,7-O-α-L-二鼠李糖苷(黄酮苷KR)。同时以黄酮苷KR作为配体,合成Cu配合物,并对其结构进行了表征分析,探讨黄酮苷KR及其Cu配合物的抗肿瘤活性。结果在0.2 mmol/L的浓度下,黄酮苷KR对卵巢癌细胞SK-OV-3、乳腺癌细胞MCF-7、肝癌细胞株HepG-2和胃癌细胞SGC-7901的抑制率分别为13.3%、13.7%、11.0%和20.5%,而黄酮苷KR的Cu配合物的抑制率则为44.2%、27.9%、27.6%和44.2%。结论黄酮苷KR的Cu配合物的抗肿瘤活性比黄酮苷KR更好,说明黄酮苷KR与金属的结合有利于发挥其潜在的协同效应。

Objective To isolate and prepare flavonoid from Siraitia grosvenorii （Swingle） C. Jeffrey leaves, to synthesize Cu （ lI ） complex and study the effects of metal complex by determing the anti cancer activities of fla- vonoid and its complex. Methods Kaempferol-3,7-0-α-L-dirhamnopyranoside （KR） was separated from S. gros- venorii leaves by using high-speed counter-current chromatography （HSCCC）. At the same time, the Cu （ lI ） complex of KR were synthesized and characterized. Lastly, the anticancer activities of them were determined. Re- sults The inhibition rates of flavonoid KR at the concentration of 0. 2 mmol/L to ovarian cancer SK-OV-3, breast MCF-3, liver cancer HepG-2 and gastric cancer SGC-7901 cell lines were 13.3% , 13.7% , 11.0% and 20. 5% , respectively. And the Cu （ Ⅱ ） complex of KR were 44.2% , 27.9% , 27.6% and 44. 2% , respectively. Conclu- sion The Cu （ Ⅱ ） complex has higher anticancer activity. The Cu （ Ⅱ ） can exert the potential synergy effect with KR.