雷公藤红素同时诱导活性氧，抑制 NF-κB 活性，并增强氟尿嘧啶在结直肠癌细胞系中的敏感性。
Triptolide simultaneously induces reactive oxygen species, inhibits NF-kappaB activity and sensitizes 5-fluorouracil in colorectal cancer cell lines.
机构信息
Research Institute in Healthcare Science, School of Applied Sciences, University of Wolverhampton, Wolverhampton WV1 1SB, UK.
出版信息
Cancer Lett. 2010 May 28;291(2):200-8. doi: 10.1016/j.canlet.2009.10.013. Epub 2009 Nov 10.
The in vitro chemosensitizing effect of triptolide (PG490) on the cytotoxicity of 5-fluorouracil (5-FU) was determined in three colorectal cancer (CRC) cell lines. PG490 alone was toxic to CRC cell lines (IC(50)s: 1.39-5.51nM). The cytotoxicity of 5-FU to CRC cell lines was 4-15-fold sensitized by combining use of low concentration of PG490. CI-isobologram indicated that the effect of PG490 plus 5-FU was synergistic. PG490 and 5-FU treatment induced activated caspase 3 and Bax expression and inhibited Bcl-2 expression. PG490 simultaneously induced generation of reactive oxygen species (ROS) and inhibited NF-kappaB transcriptional activity.
雷公藤内酯醇（PG490）对三种结直肠癌细胞系中氟尿嘧啶（5-FU）细胞毒性的体外增敏作用。PG490 单独对结直肠癌细胞系有毒性（IC50：1.39-5.51nM）。低浓度 PG490 联合使用可使 5-FU 对结直肠癌细胞系的细胞毒性提高 4-15 倍。CI 等效应图表明 PG490 加 5-FU 的作用是协同的。PG490 和 5-FU 处理诱导激活的 caspase 3 和 Bax 表达，并抑制 Bcl-2 表达。PG490 同时诱导活性氧（ROS）的产生并抑制 NF-kappaB 转录活性。
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