Biological evaluation of tubulysin A:: a potential anticancer and antiangiogenic natural product

Biological evaluation of tubulysin A:: a potential anticancer and antiangiogenic natural product
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DOI:
10.1042/bj20051735
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发表时间:
2006-06-01
影响因子:
4.1
通讯作者:
Agarwal, Seema
Agarwal, Seema
中科院分区:
生物学3区
文献类型:
--
作者:
Kaur, Gurmeet;Hollingshead, Melinda;Agarwal, Seema

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Tubulysin A (tubA) 是从粘细菌菌株中分离出来的天然产物,已被证明可以解聚微管并诱导有丝分裂停滞。本研究探讨了 tubeA 作为抗癌和抗血管生成剂的潜力。 tubeA 在一组人类癌细胞系中显示出有效的抗增殖活性,无论其多药耐药性如何。它诱导癌细胞凋亡,但不诱导正常细胞凋亡,并在一些体外测定中显示出显着的潜在抗血管生成特性。它在使用 12 种不同人类肿瘤细胞系的中空纤维测定的初步动物研究中是有效的。这项研究表明,tubA 的体外和临床前特征可能转化为临床上有用的抗癌特性。
Tubulysin A (tubA) is a natural product isolated from a strain of myxobacteria that has been shown to depolymerize microtubules and induce mitotic arrest. The potential of tubA as an anticancer and antiangiogenic agent is explored in the present study. tubA shows potent antiproliferative activity in a panel of human cancer cell lines irrespective of their multidrug resistance properties. It induces apoptosis in cancer cells but not in normal cells and shows significant potential antiangiogenic properties in several in vitro assays. It is efficacious in initial animal studies using a hollow fibre assay with 12 different human tumour cell lines. This study suggests that both in vitro and preclinical profiles of tubA may translate into clinically useful anticancer properties.