Tubercidin stabilizes microtubules against vinblastine-induced depolymerization, a taxol-like effect.

Tubercidin stabilizes microtubules against vinblastine-induced depolymerization, a taxol-like effect.
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DOI:
10.1016/0304-3835(95)03940-x
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发表时间:
1995-09
期刊:
影响因子:
9.7
通讯作者:
S. Mooberry;Klemens Stratman;Richard E. Moore
S. Mooberry;Klemens Stratman;Richard E. Moore
中科院分区:
医学1区
文献类型:
--
作者:
S. Mooberry;Klemens Stratman;Richard E. Moore

文献摘要

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一种检测微管稳定剂的灵敏方法[1]被用来筛选大量的蓝藻和微藻提取物。蓝藻(Plectonema Radiosum,UH分离物IC-70-1)的亲水性提取物具有稳定微管的活性。活性化合物的生物测定定向纯化产生了一种有效的细胞毒性核苷类似物--块茎杀菌素(7-去氮腺苷)。进一步的研究表明,Tubersidin保护一组细胞微管免受长春花碱诱导的解聚,这是一种稳定微管的紫杉醇样作用。杀菌素对微管的稳定作用具有剂量依赖性,并受其细胞毒性的限制。结节杀菌素是另一种与微管相互作用的天然产物,是为数不多的使微管稳定的产品之一。
A sensitive assay for the detection of microtubule-stabilizing agents [1] was used to screen an extensive collection of cyanobacterial and microalgal extracts. The hydrophilic extract of the cyanobacterium, Plectonema radiosum (UH isolate IC-70-1), exhibited microtubule-stabilizing activity. Bioassay-directed purification of the active compound yielded tubercidin (7-deazaadenosine), a potent cytotoxic nucleoside analog. Further studies revealed that tubercidin protected a population of cellular microtubules against vinblastine-induced depolymerization, a microtubule-stabilizing, taxol-like effect. The microtubule-stabilizing effect of tubercidin is dose dependent and limited by the cytotoxicity of the agent. Tubercidin represents another natural product that interacts with microtubules and is one of the few to cause microtubule stabilization.