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首页> 外文期刊>The Journal of Antibiotics: An International Journal >Archazolids, New Cytotoxic Macrolactones from Archangium gephyra (Myxobacteria) Production, Isolation, Physico-chemical and Biological Properties
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Archazolids, New Cytotoxic Macrolactones from Archangium gephyra (Myxobacteria) Production, Isolation, Physico-chemical and Biological Properties

机译：恶臭唑，新的细胞毒大环内酯（粘细菌）的生产，分离，理化和生物学特性

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摘要

Novel cytotoxic compounds, archazolid A and B, were isolated from the culture broth of strains of the myxobacteria Archangium gephyra and Cystobacter sp. Archazolids consist of a macrocyclic lactone ring with a thiazole side chain and showed high activity against mammalian cells. The IC_50 values with different cell lines ranged from 0.1 to 1 ng/ml. An incubation of PtK_2 potoroo cells with archiazolid A (5 ng/ml) led to the formation of vacuoles in the ER, a phenomenon that is typical for inhibitors of V-ATPases, like concanamycin and bafilomycin. We therefore assume that archazolid is an inhibitor of the V-ATPase of higher cells.
机译：从粘细菌古生弓形虫和Cystobacter sp。的菌株的培养液中分离出新型细胞毒性化合物archazolid A和B。 Archazolids由具有噻唑侧链的大环内酯环组成，对哺乳动物细胞显示出高活性。不同细胞系的IC_50值范围为0.1到1 ng / ml。 PtK_2 potoroo细胞与ArchiazolidA（5 ng / ml）的孵育导致了ER中的液泡形成，这是V-ATPase抑制剂（例如伴刀豆霉素和巴氟霉素）的典型现象。因此，我们认为archazolid是高级细胞V-ATPase的抑制剂。

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