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1
Some natural flavonoids are competitive inhibitors of Caspase-1, -3 and -7 despite their cellular toxicity.一些天然黄酮类化合物尽管具有细胞毒性,但却是半胱天冬酶-1、-3和-7的竞争性抑制剂。
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2
Flavonoids induce apoptosis in human leukemia U937 cells through caspase- and caspase-calpain-dependent pathways.类黄酮通过半胱天冬酶和半胱天冬酶-钙蛋白酶依赖性途径诱导人白血病U937细胞凋亡。
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3
Cellular, biochemical, and genetic analysis of mechanism of small molecule IAP inhibitors.小分子IAP抑制剂作用机制的细胞、生化及遗传学分析
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4
Flavonoids activated caspases for apoptosis in human glioblastoma T98G and U87MG cells but not in human normal astrocytes.类黄酮激活半胱天冬酶诱导人神经胶质瘤 T98G 和 U87MG 细胞凋亡,但不诱导人正常星形胶质细胞凋亡。
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Current opinion on 3-[2-[(2-tert-butyl-phenylaminooxalyl)-amino]-propionylamino]- 4-oxo-5-(2,3,5,6-tetrafluoro-phenoxy)-pentanoic acid, an investigational drug targeting caspases and caspase-like proteases: the clinical trials in sight and recent anti-inflammatory advances.关于3-[2-[(2-叔丁基-苯氨基草酰基)-氨基]-丙酰氨基]-4-氧代-5-(2,3,5,6-四氟-苯氧基)-戊酸(一种靶向半胱天冬酶和半胱天冬酶样蛋白酶的研究性药物)的当前观点:即将开展的临床试验及近期抗炎研究进展
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6
Engaging a Non-catalytic Cysteine Residue Drives Potent and Selective Inhibition of Caspase-6.结合非催化半胱氨酸残基可实现强效且高选择性的 caspase-6 抑制。
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A flavonoid isolated from Streptomyces sp. (ERINLG-4) induces apoptosis in human lung cancer A549 cells through p53 and cytochrome c release caspase dependant pathway.从链霉菌属(ERINLG-4)中分离得到的一种黄酮类化合物通过 p53 和细胞色素 c 释放依赖半胱天冬酶的途径诱导人肺癌 A549 细胞凋亡。
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8
Inhibitors of interleukin-1 beta-converting enzyme-family proteases (caspases) prevent apoptosis without affecting decreased cellular ability to reduce 3-(4,5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide in cerebellar granule neurons.白细胞介素-1β转化酶家族蛋白酶(半胱天冬酶)抑制剂可防止细胞凋亡,而不影响小脑颗粒神经元中3-(4,5-二甲基噻唑-2-基)-2,5-二苯基四氮唑溴盐还原能力的降低。
Brain Res. 1998 May 18;793(1-2):231-43. doi: 10.1016/s0006-8993(98)00156-5.
9
The c-IAP-1 and c-IAP-2 proteins are direct inhibitors of specific caspases.c-IAP-1和c-IAP-2蛋白是特定半胱天冬酶的直接抑制剂。
EMBO J. 1997 Dec 1;16(23):6914-25. doi: 10.1093/emboj/16.23.6914.
10
Rutinoside at C7 attenuates the apoptosis-inducing activity of flavonoids.C7位的芸香苷可减弱黄酮类化合物的诱导凋亡活性。
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本文引用的文献

1
Targeting inflammatory pathways by flavonoids for prevention and treatment of cancer.黄酮类化合物通过靶向炎症通路预防和治疗癌症。
Planta Med. 2010 Aug;76(11):1044-63. doi: 10.1055/s-0030-1250111. Epub 2010 Jul 15.
2
Tangeretin sensitizes cisplatin-resistant human ovarian cancer cells through downregulation of phosphoinositide 3-kinase/Akt signaling pathway.陈皮素通过下调磷酸肌醇3-激酶/蛋白激酶B信号通路使顺铂耐药的人卵巢癌细胞致敏。
Cancer Res. 2009 Dec 1;69(23):8910-7. doi: 10.1158/0008-5472.CAN-09-1543. Epub 2009 Nov 10.
3
Flavonoids activated caspases for apoptosis in human glioblastoma T98G and U87MG cells but not in human normal astrocytes.类黄酮激活半胱天冬酶诱导人神经胶质瘤 T98G 和 U87MG 细胞凋亡,但不诱导人正常星形胶质细胞凋亡。
Cancer. 2010 Jan 1;116(1):164-76. doi: 10.1002/cncr.24699.
4
Quercetin-induced apoptosis acts through mitochondrial- and caspase-3-dependent pathways in human breast cancer MDA-MB-231 cells.槲皮素诱导人乳腺癌 MDA-MB-231 细胞凋亡通过线粒体和 caspase-3 依赖性途径发挥作用。
Hum Exp Toxicol. 2009 Aug;28(8):493-503. doi: 10.1177/0960327109107002. Epub 2009 Sep 15.
5
Clarification of the role of quercetin hydroxyl groups in superoxide generation and cell apoptosis by chemical modification.通过化学修饰阐明槲皮素羟基在超氧阴离子生成和细胞凋亡中的作用
Biosci Biotechnol Biochem. 2009 Sep;73(9):2048-53. doi: 10.1271/bbb.90253. Epub 2009 Sep 7.
6
Human caspases: activation, specificity, and regulation.人类半胱天冬酶:激活、特异性及调控
J Biol Chem. 2009 Aug 14;284(33):21777-21781. doi: 10.1074/jbc.R800084200. Epub 2009 May 26.
7
The neuroprotective potential of flavonoids: a multiplicity of effects.类黄酮的神经保护潜力:多种作用。
Genes Nutr. 2008 Dec;3(3-4):115-26. doi: 10.1007/s12263-008-0091-4.
8
Caspases as therapeutic targets.半胱天冬酶作为治疗靶点。
J Cell Mol Med. 2008 Sep-Oct;12(5A):1502-16. doi: 10.1111/j.1582-4934.2008.00292.x. Epub 2008 Feb 24.
9
Three distinct neuroprotective functions of myricetin against glutamate-induced neuronal cell death: involvement of direct inhibition of caspase-3.杨梅素对谷氨酸诱导的神经元细胞死亡的三种不同神经保护功能:直接抑制半胱天冬酶-3的作用
J Neurosci Res. 2008 Jun;86(8):1836-45. doi: 10.1002/jnr.21629.
10
Effects of dietary flavonoids on apoptotic pathways related to cancer chemoprevention.膳食类黄酮对与癌症化学预防相关的凋亡途径的影响。
J Nutr Biochem. 2007 Jul;18(7):427-42. doi: 10.1016/j.jnutbio.2006.11.004. Epub 2007 Feb 23.

一些天然黄酮类化合物尽管具有细胞毒性,但却是半胱天冬酶-1、-3和-7的竞争性抑制剂。

Some natural flavonoids are competitive inhibitors of Caspase-1, -3 and -7 despite their cellular toxicity.

作者信息

White J Brandon, Beckford Jeremy, Yadegarynia Sina, Ngo Nhi, Lialiutska Tetiana, d'Alarcao Marc

机构信息

Department of Biological Sciences, San José State University, One Washington Square, San Jose, CA 95192-0100.

出版信息

Food Chem. 2012 Apr 15;131(4):1453-1459. doi: 10.1016/j.foodchem.2011.10.026.

DOI:10.1016/j.foodchem.2011.10.026
PMID:22140296
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3226999/
Abstract

A common feature of both apoptosis and inflammation is the activation of caspases. Caspases are aspartate-directed cysteine proteases that have numerous cellular targets. It has been discovered that several flavonoids are inhibitors of caspases. Flavonoids are members of a family of polyphenolic compounds from plants that have many biological properties, one of which is the ability to induce cell death. Some flavonoids are selective inhibitors of particular caspases. Since some of the inhibitory flavonoids are nevertheless cytotoxic, these results suggest that flavonoid-induced cell death may be occurring through a non-classical apoptosis pathway that is not dependent on caspase activity.

摘要

细胞凋亡和炎症的一个共同特征是半胱天冬酶的激活。半胱天冬酶是天冬氨酸定向的半胱氨酸蛋白酶,具有众多细胞靶点。现已发现几种黄酮类化合物是半胱天冬酶的抑制剂。黄酮类化合物是植物多酚类化合物家族的成员,具有多种生物学特性,其中之一是诱导细胞死亡的能力。一些黄酮类化合物是特定半胱天冬酶的选择性抑制剂。由于某些具有抑制作用的黄酮类化合物仍具有细胞毒性,这些结果表明,黄酮类化合物诱导的细胞死亡可能通过不依赖半胱天冬酶活性的非经典凋亡途径发生。