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小白菊内酯,一种倍半萜内酯,具有多种抗癌和抗炎活性。

Parthenolide, a sesquiterpene lactone, expresses multiple anti-cancer and anti-inflammatory activities.

机构信息

Department of Microbiology, School of Medicine and Brain Korea 21 Program, Jeju National University, Jeju, Jeju-Do, South Korea.

出版信息

Inflammation. 2012 Apr;35(2):560-5. doi: 10.1007/s10753-011-9346-0.

DOI:10.1007/s10753-011-9346-0
PMID:21603970
Abstract

Parthenolide, a naturally occurring sesquiterpene lactone derived from feverfew (Tanacetum parthenium), exhibits exceptional anti-cancer and anti-inflammatory properties, making it a prominent candidate for further studies and drug development. In this review, we briefly investigate molecular events and cell-specific activities of this chemical in relation to cytochrome c, nuclear factor kappa-light-chain enhancer of activated B cells (NF-κB), signal transduction and activation of transcription (STAT), reactive oxygen species (ROS), TCP, HDACs, microtubules, and inflammasomes. This paper reports that parthenolide shows strong NF-κB- and STAT-inhibition-mediated transcriptional suppression of pro-apoptotic genes. This compound acts both at the transcriptional level and by direct inhibition of associated kinases (IKK-β). Similarly, this review discusses parthenolide-induced ROS-mediated apoptosis of tumor cells via the intrinsic apoptotic signaling pathway. The unique ability of this compound to not harm normal cells but at the same time induce sensitization to extrinsic as well as intrinsic apoptosis signaling in cancer cells provides an important, novel therapeutic strategy for treatment of cancer and inflammation-related disorders.

摘要

小白菊内酯是一种天然存在的倍半萜内酯,来源于小白菊(Tanacetum parthenium),具有出色的抗癌和抗炎特性,使其成为进一步研究和药物开发的重要候选物。在这篇综述中,我们简要研究了这种化学物质与细胞色素 c、核因子 kappa 轻链增强子的 B 细胞(NF-κB)、信号转导和转录激活(STAT)、活性氧物种(ROS)、TCP、HDACs、微管和炎性体相关的分子事件和细胞特异性活性。本文报道小白菊内酯通过对促凋亡基因的 NF-κB 和 STAT 抑制介导的转录抑制,表现出强烈的 NF-κB 和 STAT 抑制作用。该化合物在转录水平上发挥作用,并通过直接抑制相关激酶(IKK-β)发挥作用。同样,本文讨论了小白菊内酯通过内在凋亡信号通路诱导肿瘤细胞 ROS 介导的凋亡。该化合物具有独特的能力,不会伤害正常细胞,但同时诱导癌细胞对外部和内在凋亡信号的敏感性,为癌症和炎症相关疾病的治疗提供了一种重要的新的治疗策略。

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Parthenolide, a sesquiterpene lactone, expresses multiple anti-cancer and anti-inflammatory activities.小白菊内酯,一种倍半萜内酯,具有多种抗癌和抗炎活性。
Inflammation. 2012 Apr;35(2):560-5. doi: 10.1007/s10753-011-9346-0.
2
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J Virol. 2011 May;85(9):4167-72. doi: 10.1128/JVI.01687-10. Epub 2011 Feb 2.
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Biomedicines. 2025 May 22;13(6):1267. doi: 10.3390/biomedicines13061267.
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Parthenolide regulates microglial and astrocyte function in primary cultures from ALS mice and has neuroprotective effects on primary motor neurons.小白菊内酯可调节肌萎缩侧索硬化症(ALS)小鼠原代培养物中小胶质细胞和星形胶质细胞的功能,并对原代运动神经元具有神经保护作用。
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The NF (Nuclear factor)-κB inhibitor parthenolide interacts with histone deacetylase inhibitors to induce MKK7/JNK1-dependent apoptosis in human acute myeloid leukaemia cells.NF(核因子)-κB 抑制剂小白菊内酯与组蛋白去乙酰化酶抑制剂相互作用,诱导人急性髓系白血病细胞中 MKK7/JNK1 依赖性凋亡。
Br J Haematol. 2010 Oct;151(1):70-83. doi: 10.1111/j.1365-2141.2010.08319.x. Epub 2010 Aug 2.
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A NADPH oxidase-dependent redox signaling pathway mediates the selective radiosensitization effect of parthenolide in prostate cancer cells.NADPH 氧化酶依赖性氧化还原信号通路介导小白菊内酯在前列腺癌细胞中选择性放射增敏作用。
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The inflammasomes.炎性小体
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