槲皮素及其水溶性衍生物对HL-60细胞生长影响的比较

Comparison of effects of quercetin and its derivatives on the growth of HL-60 cells

目的 研究并比较槲皮素及其硫酸酯钠盐衍生物 (槲皮素单硫酸酯钠、槲皮素二硫酸酯钠 )对HL 6 0细胞生长的影响。方法 细胞存活力以台盼兰染色法测定 ;蛋白激酶CK 2活性以连接到CK 2底物上的 [γ 3 2 P]GTP的3 2 P放射活度来检测 ;细胞周期变化以流式细胞仪检测。结果 槲皮素、槲皮素单硫酸酯钠和槲皮素二硫酸酯钠均可抑制HL 6 0细胞的生长 ,槲皮素和槲皮素单硫酸酯钠对HL 6 0细胞生长的抑制作用差异无显著性 (P >0 0 5 ) ,槲皮素二硫酸酯钠的作用则比槲皮素弱得多 (P <0 0 1) ;槲皮素可抑制HL 6 0细胞中蛋白激酶CK 2的活性 ,而槲皮素单硫酸酯钠和槲皮1999 0 5 14收稿 ,1993 0 7 15修回 广东省自然科学基金资助课题 (No 940 5 86)和广东省高教厅重点学科资助课题 (No 93 0 4)作者简介 :翁 云 ,女 ,2 7岁 ,硕士 ;梁念慈 ,男 ,5 8岁 ,教授 ,博士生导师 ,广东医学院院长。研究方向 :生化药理学素二硫酸酯钠对HL 6 0细胞内CK 2活性无明显影响 ;槲皮素阻断HL 6 0细胞于G2 /M期 ,而槲皮素单硫酸酯钠和槲皮素二硫酸酯钠均阻断细胞于G0 /G1期。结论 槲皮素、槲皮素单硫酸酯钠和槲皮素二硫酸酯钠均为潜在的肿瘤细胞生长抑制剂 ,但它们的抑制机制却不相同 ,槲皮素 7 OH对维持槲皮素的功能有重要作用。

AIM To study and compare effects of quercetin and its derivatives, sodium quercetin monosulfate(SQMS) and sodiums quercetin disulfate(SQDS) on the growth of HL 60 cells. METHODS The number of viable cells was measured by the trypan blue dye exclusion test. The activity of CK 2 was assayed by detecting incorporation of 32 P of [γ 32 P ]GTP into the substrate. Cell cycle progression was performed by flow cytometry. RESULTS Quercetin, SQMS and SQDS all inhibited the growth of HL 60 cells. The inhibitory effect of SQMS on the growth of HL 60 cells was similar to Que(P>0 05), but the effect of SQDS on the growth of HL 60 cells was less than Que(P<0 01). Que inhibited the activity of CK 2 in HL 60 cells in vivo, but SQMS and SQDS did not affect the activity of CK 2 markedly. Que(60 μmol·L -1 ) arrested HL 60 cells in G 2/M phase, but SQMS and SQDS (60 μmol·L -1 ,respectively) arrested HL 60 cells in G 0/G 1 phase. CONCLUSIONS Que, SQMS and SQDS all are potent inhibitors of tumor cells, but the mechanisms of Que and its derivatives on inhibiting the growth of tumor cells are different, 7 OH of Que may play an important role in maintaining the biological activity of Que.