辣椒素衍生物 Capsicodendrin 对 MCF-7 雌激素敏感型乳腺癌细胞的活性。
Activity in MCF-7 Estrogen-sensitive Breast Cancer Cells of Capsicodendrin from .
机构信息
Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, OH, U.S.A.
出版信息
Anticancer Res. 2021 Dec;41(12):5935-5944. doi: 10.21873/anticanres.15412.
BACKGROUND/AIM: Effect of capsicodendrin on the NF-κB pathway was studied in MCF-7 cancer cells.
MATERIALS AND METHODS
The transcription factor assay was used to screen for NF-κB activity. The effect on IKKβ, ICAM-1, and caspase-7 were studied using western blot. Caspase-1 was studied using Promega Caspase-Glo assay. Reactive oxygen species (ROS) were detected using the fluorescent probe DCFH-DA. The potentiometric dye JC-1 was used to assess mitochondrial membrane potential (ΔΨm) and the cell cycle was examined using a fluorescence-activated cell sorter.
RESULTS
NF-κB p65 inhibitory effect was IC=8.6 μM and cytotoxic activity was IC=7.5 μM. The upstream IKK and the downstream ICAM-1 were down-regulated. Sub G-phase population increased to 81% after 12 h of treatment with capsicodendrin (10 μM) and there was no loss of ΔΨM.
CONCLUSION
Increased levels of intracellular ROS promoted activity of caspase-1 and induced cell death in MCF-7 cells. Capsicodendrin may be a future anticancer agent that prevents the progression of metastatic breast cancer.
背景/目的：研究辣椒素对 MCF-7 癌细胞中 NF-κB 通路的影响。
材料与方法
采用转录因子测定法筛选 NF-κB 活性。采用 Western blot 研究对 IKKβ、ICAM-1 和 caspase-7 的影响。采用 Promega Caspase-Glo 测定法研究 caspase-1。采用荧光探针 DCFH-DA 检测活性氧（ROS）。采用电势染料 JC-1 评估线粒体膜电位（ΔΨm），并采用荧光激活细胞分选术检查细胞周期。
结果
NF-κB p65 的抑制作用 IC=8.6 μM，细胞毒性作用 IC=7.5 μM。上游 IKK 和下游 ICAM-1 下调。用辣椒素（10 μM）处理 12 小时后，Sub G 期细胞群增加到 81%，而 ΔΨM 没有丢失。
结论
细胞内 ROS 水平升高可促进 caspase-1 的活性，并诱导 MCF-7 细胞死亡。辣椒素可能是一种预防转移性乳腺癌进展的新型抗癌药物。
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