A-72363 A-1、A-2和C，来自诺尔斯链霉菌SANK 60192的新型乙酰肝素酶抑制剂，II. 生物活性。

A-72363 A-1, A-2, and C, novel heparanase inhibitors from Streptomyces nobilis SANK 60192, II. Biological activities.

作者信息

Kawase Y, Takahashi M, Takatsu T, Arai M, Nakajima M, Tanzawa K

机构信息

Biological Research Laboratories, Sankyo Co., Ltd., Tokyo 140, Japan.

出版信息

J Antibiot (Tokyo). 1996 Jan;49(1):61-4. doi: 10.7164/antibiotics.49.61.

DOI:10.7164/antibiotics.49.61

PMID:8609088

Abstract

Inhibitory activities of A-72363 A-1, A-2 and C, the diastereomers of a neuraminidase inhibitor siastatin B, against various glycosidases were tested in comparison to siastatin B. Despite these compounds differing only in their configuration, each compound showed strikingly different specificities towards the various glycosidases tested. A-72363 C inhibited bovine liver beta-glucuronidase and tumor cell heparanase with IC50 values of 1.6 microM and 12 microM, respectively.

摘要

与唾液酸酶抑制剂西他司丁B相比，对神经氨酸酶抑制剂西他司丁B的非对映异构体A-72363 A-1、A-2和C针对各种糖苷酶的抑制活性进行了测试。尽管这些化合物仅在构型上有所不同，但每种化合物对所测试的各种糖苷酶表现出显著不同的特异性。A-72363 C抑制牛肝β-葡萄糖醛酸酶和肿瘤细胞乙酰肝素酶，IC50值分别为1.6微摩尔和12微摩尔。