恩杂鲁胺（LY317615.HCl）对卵巢癌细胞 CA125 生物合成和脱落的影响。
The impact of enzastaurin (LY317615.HCl) on CA125 biosynthesis and shedding in ovarian cancer cells.
机构信息
Division of Gynecological Oncology, Department of Obstetrics and Gynecology, University Hospitals Leuven, Katholieke Universiteit Leuven, Belgium.
出版信息
Gynecol Oncol. 2010 Jul;118(1):64-8. doi: 10.1016/j.ygyno.2010.03.008. Epub 2010 May 1.
BACKGROUND
In this study the modulatory effect of the proteinase kinase C beta (PKC beta) selective inhibitor enzastaurin on CA125 expression and shedding in ovarian cancer cells (OVCAR-3 cells) was investigated. MATERIAL ANDMETHODS: OVCAR-3 cells were cultured in vitro and treated with increasing concentrations of carboplatin (2-1000 microM), paclitaxel (0.2-100 nM) or enzastaurin (1-100 microM) single agent. Growth inhibitory effects were evaluated by MTS and luminescence assay. CA 125 was determined in supernatans and in cell lysate using an electrochemo-iluminescence immunoassay.
RESULTS
Cell growth of OVCAR-3 cells was inhibited by single agent carboplatin, paclitaxel or enzastaurin in a dose dependent manner. Carboplatin caused a transient increase of CA125 in supernatans followed by a gradual decrease of CA125. Treatment with increasing doses of paclitaxel or enzastaurin caused an increase of CA125 shedding in culture medium but also the membrane bound fraction of CA125 was increased.
CONCLUSION
These results suggest that enzastaurin, as paclitaxel, has a direct stimulatory effect on CA 125 synthesis and shedding in vitro.
背景
在这项研究中，研究了蛋白激酶 Cβ（PKCβ）选择性抑制剂恩扎司琼对卵巢癌细胞（OVCAR-3 细胞）中 CA125 表达和脱落的调节作用。
材料和方法
将 OVCAR-3 细胞在体外培养，并分别用不同浓度的卡铂（2-1000 μM）、紫杉醇（0.2-100 nM）或恩扎司琼（1-100 μM）进行单独处理。通过 MTS 和发光测定法评估生长抑制作用。使用电化学发光免疫分析法测定上清液和细胞裂解物中的 CA125。
结果
OVCAR-3 细胞的细胞生长被单药卡铂、紫杉醇或恩扎司琼以剂量依赖的方式抑制。卡铂在培养上清液中引起 CA125 的短暂增加，随后 CA125 逐渐减少。用递增剂量的紫杉醇或恩扎司琼处理会导致 CA125 在培养基中的脱落增加，但 CA125 的膜结合部分也增加了。
结论
这些结果表明，恩扎司琼与紫杉醇一样，在体外对 CA125 的合成和脱落具有直接的刺激作用。
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