STUDIES ON MACROCYCLIC LACTONE ANTIBIOTICS .11. ANTI-MITOTIC AND ANTITUBULIN ACTIVITY OF NEW ANTITUMOR ANTIBIOTICS, RHIZOXIN AND ITS HOMOLOGS
STUDIES ON MACROCYCLIC LACTONE ANTIBIOTICS .11. ANTI-MITOTIC AND ANTITUBULIN ACTIVITY OF NEW ANTITUMOR ANTIBIOTICS, RHIZOXIN AND ITS HOMOLOGS
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DOI：
10.7164/antibiotics.40.66
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发表时间：
1987-01-01
影响因子：
3.3
通讯作者：
NAGANO, H
中科院分区：
文献类型：
--
作者：
TAKAHASHI, M;IWASAKI, S;NAGANO, H
本文研究了一种新的抗肿瘤大环内酯类化合物根霉素（1a）的作用机制。根霉毒素抑制受精卵中雄性和雌性原核的融合，并抑制去纤毛海胆胚胎中纤毛的形成。在体外，从猪脑中分离的微管蛋白的聚合在1X-100 μ mol/L时被完全抑制。10-5 M浓度的根霉素，并通过在37 ℃温育30分钟使已聚合的微管蛋白解聚。 10-5药物的M。将根霉素对微管蛋白聚合的活性与其他抗微管蛋白药物如秋水仙碱、长春碱和安丝菌素P-3的活性进行比较。根霉素的同系物1b apprx 3b也以几乎与根霉素相同的程度抑制纯化的微管蛋白的聚合。
The mode of action of rhizoxin (1a), a new antitumor macrolide, was investigated. Rhizoxin inhibited fusion of the male and the female pronuclei in fertilized sea urchin eggs and inhibited cilia formation in the deciliated sea urchin embryos. In vitro, polymerization of tubulin isolated from porcine brains was completely inhibited at a 1 .times. 10-5 M concentration of rhizoxin, and tubulin which had been polymerized by incubation at 37.degree.C for 30 minutes was depolymerized by addition of 1 .times. 10-5 M of the drug. Activity of rhizoxin against tubulin polymerization was compared with those of other anti-tubulin drugs such as colchicine, vinblastine and ansamitocin P-3. The homologues of rhizoxin, 1b.apprx.3b, also inhibited polymerization of the purified microtuble protein at almost the same extent as rhizoxin.