The flavonoid quercetin transiently inhibits the activity of taxol and nocodazole through interference with the cell cycle.
The flavonoid quercetin transiently inhibits the activity of taxol and nocodazole through interference with the cell cycle.
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类黄酮槲皮素会通过干扰细胞周期瞬时抑制紫杉醇和诺科唑的活性。
DOI：
10.1080/01635581.2010.492087
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发表时间：
2010
期刊：
影响因子：
--
通讯作者：
Yehualaeshet TE
中科院分区：
文献类型：
--
作者：
Samuel T;Fadlalla K;Turner T;Yehualaeshet TE
槲皮素是一种具有抗癌特性的类黄酮。在这项研究中，我们研究了槲皮素对癌细胞的细胞周期，生存力和增殖的影响，无论是单独或与微管靶向药物紫杉醇和诺考达唑。尽管槲皮素以剂量依赖性方式诱导细胞死亡，但12.5-50μM槲皮素抑制紫杉醇和诺考达唑诱导各种细胞系G2/M期阻滞的活性。槲皮素还部分恢复了药物诱导的经处理细胞活力丧失长达72小时。微管靶向药物的这种拮抗作用伴随着细胞周期进展的延迟和细胞周期蛋白B1在处理细胞的微管组织中心的积累的抑制。然而，槲皮素并不抑制紫杉醇或诺考达唑的微管靶向。槲皮素对HCT 116细胞具有短期的保护作用，但槲皮素或槲皮素与紫杉醇联合应用仍能抑制HCT 116细胞的集落形成和克隆形成。细胞对生长基质的粘附状态是决定HCT 116细胞对槲皮素敏感性的关键。我们的结论是，虽然长期暴露于槲皮素的癌细胞可能会阻止细胞增殖和生存，槲皮素与细胞周期进程的干扰减少了微管靶向药物的功效，以阻止细胞在G2/M。
Quercetin is a flavonoid with anticancer properties. In this study, we examined the effects of quercetin on cell cycle, viability and proliferation of cancer cells, either singly or in combination with the microtubule-targeting drugs taxol and nocodazole. Although quercetin induced cell death in a dose dependent manner, 12.5-50μM quercetin inhibited the activity of both taxol and nocodazole to induce G2/M arrest in various cell lines. Quercetin also partially restored drug-induced loss in viability of treated cells for up to 72 hours. This antagonism of microtubule-targeting drugs was accompanied by a delay in cell cycle progression and inhibition of the buildup of cyclin-B1 at the microtubule organizing center of treated cells. However, quercetin did not inhibit the microtubule targeting of taxol or nocodazole. Despite the short-term protection of cells by quercetin, colony formation and clonogenicity of HCT116 cells were still suppressed by quercetin or quercetin-taxol combination. The status of cell adherence to growth matrix was critical in determining the sensitivity of HCT116 cells to quercetin. We conclude that while long-term exposure of cancer cells to quercetin may prevent cell proliferation and survival, the interference of quercetin with cell cycle progression diminishes the efficacy of microtubule-targeting drugs to arrest cells at G2/M.
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影响因子：
11.2
作者：
Heaney ML;Gardner JR;Karasavvas N;Golde DW;Scheinberg DA;Smith EA;O'Connor OA
通讯作者：
O'Connor OA
影响因子：
9.7
作者：
Mertens-Talcott, SU;Percival, SS
通讯作者：
Percival, SS
影响因子：
3.9
作者：
Olivier, M;Eeles, R;Hainaut, P
通讯作者：
Hainaut, P
影响因子：
2.4
作者：
Lunet, Nuno;Valbuena, Carmen;Barros, Henrique
通讯作者：
Barros, Henrique
影响因子：
10.3
作者：
Bairati, I;Meyer, F;Roy, J
通讯作者：
Roy, J