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杀稻瘟菌素、黑杀菌素A和黑杀菌素B的5'-核苷酸酶抑制活性。构效关系。

5'-Nucleotidase inhibitory activity of nucleoticidin, melanocidin A and melanocidin B. Structure-activity relationships.

作者信息

Uchino K, Ogawara H, Akiyama T, Fukuchi A

出版信息

J Antibiot (Tokyo). 1985 Nov;38(11):1564-7. doi: 10.7164/antibiotics.38.1564.

DOI:10.7164/antibiotics.38.1564
PMID:3001014
Abstract

Nucleoticidin and melanocidins A and B exhibited potent inhibitory activity against 5'-nucleotidases from rat liver membrane and snake venom. These inhibitors are polysaccharides with highly branched side chains having at least disaccharide units. This conclusion was supported by the results with polysaccharides of known chemical structures. The inhibitors showed non-competitive inhibition with respect to AMP, and urea-treatment caused a marked decrease or a disappearance of the 5'-nucleotidase inhibitory activity. Therefore, it is concluded that steric factors also play an important role in their inhibitory activity.

摘要

核苷杀菌素以及黑素杀菌素A和B对大鼠肝膜和蛇毒中的5'-核苷酸酶表现出强大的抑制活性。这些抑制剂是具有高度分支侧链且至少含有二糖单元的多糖。已知化学结构的多糖的实验结果支持了这一结论。这些抑制剂对AMP表现出非竞争性抑制,并且尿素处理导致5'-核苷酸酶抑制活性显著降低或消失。因此,可以得出结论,空间因素在它们的抑制活性中也起着重要作用。

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