Takahashi M, Iwasaki S, Kobayashi H, Okuda S, Murai T, Sato Y, Haraguchi-Hiraoka T, Nagano H
J Antibiot (Tokyo). 1987 Jan;40(1):66-72. doi: 10.7164/antibiotics.40.66.
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 X 10(-5) M concentration of rhizoxin, and tubulin which had been polymerized by incubation at 37 degrees C for 30 minutes was depolymerized by addition of 1 X 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-3b, also inhibited polymerization of the purified microtuble protein at almost the same extent as rhizoxin.
对一种新型抗肿瘤大环内酯类化合物根霉素（1a）的作用方式进行了研究。根霉素抑制受精海胆卵中雄原核与雌原核的融合，并抑制去纤毛海胆胚胎中的纤毛形成。在体外，当根霉素浓度为1×10⁻⁵ M时，从猪脑中分离的微管蛋白的聚合被完全抑制，并且在37℃孵育30分钟后已聚合的微管蛋白通过添加1×10⁻⁵ M的该药物而解聚。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的活性进行了比较。根霉素的同系物1b - 3b对纯化的微管蛋白聚合的抑制程度几乎与根霉素相同。
