ENZYME-INHIBITORS - NEW AND KNOWN POLYBROMINATED PHENOLS AND DIPHENYL ETHERS FROM 4 INDO-PACIFIC DYSIDEA SPONGES
ENZYME-INHIBITORS - NEW AND KNOWN POLYBROMINATED PHENOLS AND DIPHENYL ETHERS FROM 4 INDO-PACIFIC DYSIDEA SPONGES
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DOI：
10.1021/np50123a008
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发表时间：
1995-09-01
影响因子：
5.1
通讯作者：
CREWS, P
中科院分区：
文献类型：
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作者：
FU, XO;SCHMITZ, EJ;CREWS, P
从印度太平洋两个地理位置不同的地区（Chuuk Atoll和斐济）采集的四个Dysidea sp.海绵样品中分离出的提取物和纯化合物仅对五种不同的酶进行了分析，其中四种与抗癌药物发现有关，其中一种（15-脂氧合酶）可能检测到调节动脉粥样硬化斑块发展的重要化合物。对多种酶有抑制作用的纯化合物为多溴化苯酚和多溴化苯氧酚。其中14个酚类化合物得到分离，其中6个为新化合物。多种酚类物质抑制肌苷单磷酸脱氢酶（IMPDH）、鸟苷单磷酸合成酶和15-脂氧合酶。蛋白酪氨酸激酶pp60（v-src）和基质金属蛋白酶无活性。
Extracts and pure compounds isolated from four samples of Dysidea sp. sponges collected from two geographically distinct regions of the Indo-Pacific (Chuuk Atoll and Fiji) mere assayed against five different enzyme assays, four of which are relevant to anticancer drug discovery and one of which (15-lipoxygenase) may detect compounds significant in modulating the development of atherosclerotic plaque. The pure compounds that inhibited various enzymes were polybrominated phenols and polybrominated phenoxyphenols. Fourteen of these phenols were isolated, six of which were new compounds. A variety of the phenols inhibited inosine monophosphate dehydrogenase (IMPDH), guanosine monophosphate synthetase, and 15-lipoxygenase. No activity was observed with protein tyrosine kinase pp60(v-src) or matrix metalloprotease.