A-72363 A-1, A-2, and C, novel heparanase inhibitors from Streptomyces nobilis SANK 60192, II. Biological activities.
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.
Kawase
Y
Y
Biological Research Laboratories, Sankyo Co., Ltd., Tokyo 140, Japan.
Takahashi
M
M
Takatsu
T
T
Arai
M
M
Nakajima
M
M
Tanzawa
K
K
D000818:Animals; D002417:Cattle; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D005966:Glucuronidase; D006026:Glycoside Hydrolases / Q000037:antagonists & inhibitors*; D010880:Piperidines / Q000494:pharmacology*; D014407:Tumor Cells, Cultured; D000099175:Heparanase
D004791:Enzyme Inhibitors; D005966:Glucuronidase; D006026:Glycoside Hydrolases; D010880:Piperidines; D000099175:Heparanase; C011353:siastatin