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

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

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.

MeSH terms

  • Animals
  • Cattle
  • Enzyme Inhibitors / pharmacology*
  • Glucuronidase*
  • Glycoside Hydrolases / antagonists & inhibitors*
  • Piperidines / pharmacology*
  • Tumor Cells, Cultured

Substances

  • Enzyme Inhibitors
  • Piperidines
  • siastatin
  • Glycoside Hydrolases
  • heparanase
  • Glucuronidase