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从榼藤子中分离得到的恩他酰胺A和恩他酰胺B的合成及其对5-脂氧合酶的抑制作用。

Synthesis of entadamide A and entadamide B isolated from Entada phaseoloides and their inhibitory effects on 5-lipoxygenase.

作者信息

Ikegami F, Sekine T, Aburada M, Fujii Y, Komatsu Y, Murakoshi I

出版信息

Chem Pharm Bull (Tokyo). 1989 Jul;37(7):1932-3. doi: 10.1248/cpb.37.1932.

DOI:10.1248/cpb.37.1932
PMID:2805174
Abstract

Two new sulfur-containing amides, entadamide A (1) and entadamide B (2), isolated from the seeds of Entada phaseoloides, were synthesized by the addition reaction of methanethiol to propiolic acid (5) followed by condensation with ethanolamine by the use of dicyclohexylcarbadiimide. These compounds inhibited the 5-lipoxygenase activity of RBL-1 cells at 10(-4) g/ml. This finding suggests that entadamides A and B may be examples of a new type of antiinflammatory drug.

摘要

从榼藤子种子中分离得到的两种新型含硫酰胺,榼藤酰胺A(1)和榼藤酰胺B(2),是通过甲硫醇与丙炔酸(5)的加成反应,然后使用二环己基碳二亚胺与乙醇胺缩合而合成的。这些化合物在10⁻⁴ g/ml时抑制RBL-1细胞的5-脂氧合酶活性。这一发现表明,榼藤酰胺A和B可能是新型抗炎药物的实例。

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