论文部分内容阅读
目的 :合成金雀异黄素水溶性衍生物并研究它们在抗肿瘤、抗血小板作用中的影响。方法 :通过浓硫酸酯化金雀异黄素 (G) ,加入饱和NaCl溶液 ,获得二个水溶性衍生物 :金雀异黄素 4′ 硫酸酯钠 (G1 )和金雀异黄素 7,4′ 二硫酸酯二钠 (G2 )。同时研究了G与G1、G2抑制HL 60细胞生长和猪血小板聚集作用的关系。结果 :各药物抑制HL 60细胞生长 ( 2 4h)的IC50 ( μmol/L)值 :G =4 9.5;G1 >2 0 0 ;G2 >3 0 0。对猪血小板聚集的抑制作用 ,G的IC50 值为4 .8μmol/L ,而G1和G2则未表现出显著的抑制作用。 结论 :G具有较强的抑制HL 60细胞生长和猪血小板聚集的作用 ,而G1、G2由于 4′ OH的封闭导致抑制效果不显著。
OBJECTIVE : To synthesize the water-soluble derivatives of genistein and study their effects on anti-tumor and anti-platelet effects. METHODS: Two concentrated water-soluble derivatives were obtained by esterification of genistein (G) with concentrated sulfuric acid and the addition of saturated NaCl solution: genistein 4′ Sodium Sulphate (G1) and genistein 7. 4’ disulfate disodium (G2). The relationship between G and G1 and G2 inhibiting the growth of HL 60 cells and porcine platelet aggregation was also studied. RESULTS: The IC50 (μmol/L) values of each drug inhibited the growth of HL 60 cells (24 h): G = 4 9.5; G1 >200; G2 >300. Inhibition of porcine platelet aggregation, IC50 value of G was 4.8 μmol/L, while G1 and G2 did not show significant inhibitory effect. Conclusion: G has a strong inhibitory effect on the growth of HL 60 cells and porcine platelet aggregation, while G1 and G2 have no significant inhibitory effect due to the blocking of 4′ OH.