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首页> 外文期刊>The Journal of Antibiotics: An International Journal >Ascotricins A and B, novel antagonists of sphingosine-1-phosphate receptor 1 from Ascotricha chartarum Berk. SANK 14186.
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Ascotricins A and B, novel antagonists of sphingosine-1-phosphate receptor 1 from Ascotricha chartarum Berk. SANK 14186.

机译：Ascotricins A和B，来自Ascotricha Crentarum Berk的鞘氨氨酸-1-磷酸盐受体1的新型拮抗剂。 沉没14186。

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摘要

Ascotricins A and B were isolated as novel sphingosine-1-phosphate receptor 1 (S1P(1)) antagonists from a cultured broth of a fungus identified as Ascotricha chartarum Berk. SANK 14186. The two compounds were purified by solvent extraction, reversed-phase (RP) column chromatography and a preparative RP-HPLC. The structures were determined by various NMR experiments and by LC/MS and GC/MS analyses. The S1P(1) antagonist activities were measured by a cyclic AMP assay using S1P(1)-expressing cells and the IC(50) values were 8.2 and 1.8 microM, respectively. In a [(33)P]sphingosine-1-phosphate/S1P(1)-binding assay, those values were 120 and 39 microM, and in a migration assay using human umbilical vein endothelial cells (HUVECs), they were 94 and 28 microM, respectively. Thus, ascotricins A and B are novel S1P(1) antagonists showing an inhibition activity toward HUVEC migration.
机译：将Ascotricins A和B分离为新的鞘氨酸-1-磷酸酯受体1（S1P（1））来自鉴定为ascoTricha crentarum berk的真菌的培养肉汤中的拮抗剂。 沉积14186.通过溶剂萃取，反相（RP）柱色谱和制备型RP-HPLC纯化两种化合物。 该结构由各种NMR实验和LC / MS和GC / MS分析测定。 通过使用S1P（1）-Expressing细胞的循环AMP测定法测量S1P（1）拮抗剂活性，并且IC（50）值分别为8.2和1.8微米。 在[（33）p]鞘氨醇-1-磷酸盐/ S1P（1） - 耦合测定中，这些值为120和39微米，并使用人脐静脉内皮细胞（HUVEC）在迁移测定中，它们为94和28 分别微米。 因此，Ascotricins A和B是新的S1P（1）拮抗剂，其显示朝鲜迁移的抑制活性。

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