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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.

Abstract

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.

摘要

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。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/be37/8750382/88ffd5d73a1f/nihms-1768376-f0001.jpg

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