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塔卡隆内酯类,新型微管稳定剂,与γ 射线对细胞活力具有相加效应。

The taccalonolides, novel microtubule stabilizers, and γ-radiation have additive effects on cellular viability.

机构信息

Department of Pharmacology, University of Texas Health Science Center at San Antonio, San Antonio, TX, United States.

Department of Otolaryngology, University of Texas Health Science Center at San Antonio, San Antonio, TX, United States.

出版信息

Cancer Lett. 2011 Aug 1;307(1):104-111. doi: 10.1016/j.canlet.2011.03.022. Epub 2011 Apr 19.

Abstract

The taccalonolides are novel antimitotic microtubule stabilizers that have a unique mechanism of action independent of a direct interaction with tubulin. Cytotoxicity and clonogenic assays show that taccalonolide A and radiation act in an additive manner to cause cell death. The taxanes and epothilones have utility when combined with radiotherapy and these findings further suggest the additive effects of microtubule targeting agents with radiation on cellular proliferation are independent of direct tubulin binding and are instead a result of the downstream effects of these agents. These studies suggest that diverse antimitotic agents, including the taccalonolides, may have utility in chemoradiotherapy.

摘要

塔卡醇内酯是新型的抗有丝分裂微管稳定剂,具有与微管蛋白直接相互作用无关的独特作用机制。细胞毒性和集落形成试验表明,塔卡醇内酯 A 与辐射具有相加作用,导致细胞死亡。紫杉醇类和埃坡霉素类与放疗联合应用具有疗效,这些发现进一步表明,微管靶向药物与放疗的相加作用对细胞增殖的影响与微管蛋白直接结合无关,而是这些药物的下游作用的结果。这些研究表明,包括塔卡醇内酯在内的多种抗有丝分裂药物可能对放化疗有作用。

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