Isolation, characterization and biological activities of concanamycins as inhibitors of lysosomal acidification.

Isolation, characterization and biological activities of concanamycins as inhibitors of lysosomal acidification.
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作为溶酶体酸化抑制剂的刀刀霉素的分离、表征和生物活性。

DOI:
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发表时间:
1992
期刊:
Journal of antibiotics (Tokyo. 1968)
影响因子:
--
通讯作者:
A. Endo
A. Endo
中科院分区:
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文献类型:
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作者:
J. Woo;C. Shinohara;K. Sakai;K. Hasumi;A. Endo

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从链霉菌菌丝体中分离出刀那霉素家族的四种新类似物,命名为刀那霉素 D、E、F G。 A1509经溶剂萃取、硅胶柱色谱和HPLC测定。通过结合光谱分析鉴定了这些化合物的结构。所有这些化合物在结构上均与先前分离的刀刀霉素A、B和C相关,并且在10(-11)-10(-9) M浓度下抑制大鼠肝脏溶酶体的酸化。结构-活性研究表明,刀那霉素家族分子的18元大环内酯环和6元半缩酮环部分具有有效的抑制活性。
Four new analogues of concanamycin family, designated concanamycins D, E, F G, were isolated from the mycelium of Streptomyces sp. A1509 by solvent extraction, silica gel column chromatography and HPLC. Structures of these compounds were identified by the combination of spectroscopic analyses. All of these compounds were structurally related to concanamycins A, B and C, which had been isolated previously, and inhibited the acidification of rat liver lysosomes at 10(-11)-10(-9) M concentration. The structure-activity study showed that the 18-membered macrolide ring and the 6-membered hemiketal ring portions of the molecules of concanamycin family are responsible for potent inhibitory activity.
DOI: 10.1016/0076-6879(83)98152-1
发表时间: 1983
影响因子: --
作者:
J. Goldstein;S. Basu;Michael S. Brown
通讯作者: J. Goldstein;S. Basu;Michael S. Brown
DOI: 10.1073/pnas.85.21.7972
发表时间: 1988-11-01
影响因子: 11.1
作者:
BOWMAN, EJ;SIEBERS, A;ALTENDORF, K
通讯作者: ALTENDORF, K