Archazolid A-15-O-β-D-glucopyranoside and iso-archazolid B: potent V-ATPase inhibitory polyketides from the myxobacteria Cystobacter violaceus and Archangium gephyra.
Archazolid A-15-O-β-D-glucopyranoside and iso-archazolid B: potent V-ATPase inhibitory polyketides from the myxobacteria Cystobacter violaceus and Archangium gephyra.
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Archazolid A-15-O-β-D-吡喃葡萄糖苷和异-archazolid B：来自粘细菌 Cystobacter violaceus 和 Archangium gephyra 的有效 V-ATP 酶抑制聚酮化合物。
DOI：
10.1021/np200036v
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发表时间：
2011
影响因子：
5.1
通讯作者：
D. Menche
中科院分区：
文献类型：
--
作者：
Nicole Horstmann;S. Essig;Svenja Bockelmann;H. Wieczorek;M. Huss;F. Sasse;D. Menche
从紫囊杆菌（Cystobacter violaceus）和gephyra Archangium中分离到了两个结构新颖的大环内酯类古唑烷A和B的类似物：古唑烷A-15- o- β- d -葡萄糖吡喃苷（archazolid E, 5）和异古唑烷B （archazolid F, 6）。大内酯5代表了古唑烷的第一个15- o -糖苷。异古唑烷B(6)包含一个C-3烯烃，并提出了这类天然产物的第一个组成异构体。这些聚酮的结构通过光谱分析，特别是HMBC， HMQC和ROESY核磁共振研究和化学降解来确定。异古唑啉B(6)表现出极高的抗增殖和v - atp酶抑制作用，其IC（50）值在皮摩尔范围内，而糖苷5仅具有中等活性。iso-Archazolid B是已知最强的古固形物。
Two structurally novel analogues of the macrolides archazolids A and B, archazolid A-15-O-β-D-glucopyranoside (archazolid E, 5) and iso-archazolid B (archazolid F, 6), were isolated from the myxobacterium Cystobacter violaceus and Archangium gephyra, respectively. Macrolactone 5 represents the first 15-O-glycoside of the archazolids. iso-Archazolid B (6) incorporates a C-3 alkene and presents the first constitutional isomer reported for this natural product class. The structures of these polyketides were determined by spectroscopic analysis, in particular by HMBC, HMQC, and ROESY NMR investigations and by chemical degradation. iso-Archazolid B (6) demonstrated extremely high antiproliferative and V-ATPase inhibitory effects, with IC(50) values in the picomolar range, while only moderate activity was observed for glycoside 5. iso-Archazolid B presents the most potent archazolid known.
影响因子：
5.6
作者：
Muench, Stephen P.;Huss, Markus;Harrison, Michael A.
通讯作者：
Harrison, Michael A.