[Effect of Baicalin Derivative 02-036 on Burkitt Lymphoma Cell Line CA46 and Its Related Mechanisms].

题目: 黄芩苷衍生物02-036对Burkitt淋巴瘤CA46细胞株的作用及相关机制. 目的: 探讨黄芩苷（Baicalin）衍生物02-036对人Burkitt淋巴瘤CA46细胞株的增殖、凋亡的影响及其相关机制. RESULTS: Baicalin derivative 02-036 obviously inhibited the proliferation of CA46 cells, with dose- and time-dependent manner (r=0.963, r=0.992). The averaged IC50 value of CA46 cells was (6.04±0.11) μmol/L after 48-hour treatment. Low concentration of 02-036 could significantly inhibit the colony formation of CA46 cells. Flow cytometry analysis confirmed that 02-036 could effectively induce CA46 cell apoptosis. The apoptosis rate correlated with drug concentrations (r=0.959). Also, DNA ploid analysis showed that the cell cycle of CA46 was arrested in the S phase. The expression levels of BCL-2, Pro-caspase-9, Pro-caspase-3, PARP and C-MYC proteins decreased with a 02-036-dose dependent manner (r values were -0.990, -0.939, -0.971 and -0.967, respectively). In contrast, the expression level of cleaved-PARP increased with the same manner (r=0.920). 结果: 细胞生长曲线结果显示黄芩苷衍生物02-036对CA46细胞株有明显的抑制增殖作用，并且呈量效和时效关系（r=0.963，r=0.992），48 h半数抑制浓度（IC50）为（6.04±0.11） μmol/L。细胞集落形成实验显示，02-036作用 CA46细胞后，细胞集落形成能力明显降低，并在一定范围内呈量效关系（r=-0.967）。Annexin V-FITC/PI双染流式细胞术分析结果表明，02-036能有效诱导CA46细胞凋亡，并且在一定范围内，细胞凋亡率随着药物作用浓度的增高而增加（r=0.959）。DNA倍体分析检测显示02-036能将CA46的细胞周期阻滞于S期。不同浓度的02-036作用于CA46细胞后，BCL-2、Pro-caspase-9、Pro-caspase-3、PARP和C-MYC的表达逐渐下调，而Cleaved-PARP表达逐渐上调，并呈现量效关系（r值分别为-0.990、-0.939、 -0.971、-0.967、-0.936和0.920）. 结论: 黄芩苷衍生物02-036能有效抑制CA46细胞增殖，诱导其凋亡，在一定范围内呈时效和量效关系；其作用机制可能与BCL-2、Pro-caspase-9、Pro-caspase-3、PARP 及C-MYC的表达下调有关.