Exploitation of heparanase inhibitors from microbial metabolites using an efficient visual screening system
Exploitation of heparanase inhibitors from microbial metabolites using an efficient visual screening system
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DOI：
10.7164/antibiotics.57.136
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发表时间：
2004-02-01
影响因子：
3.3
通讯作者：
Osada, H
中科院分区：
文献类型：
--
作者：
Ishida, K;Teruya, T;Osada, H
In this paper we describe the establishment of an efficient visual method for screening heparanase inhibitors, and we present the results of screening 10,000 microbial culture broths. Heparanase-overexpressing stable clones of the human. hepatocellular carcinoma HepG2 cells were established and used as an enzyme source. Digestion of heparan sulfate (HS) was detected using novel HS-containing tablets or SDS-polyacrylamide get electrophoresis. This method was able to find suramin, a known heparanase inhibitor, from a library of typical enzyme, inhibitors. By screening 10,000 culture broths of microorganisms (actinomycetes, fungi, and bacteria) an actinomycete strain, RK99-A234, was found to have heparanase inhibitory activity. RK-682 was identified in the fermentation broth as a heparanase inhibitor, IC50=17 mum.
