I. Taxonomy, Production, Purification and Biological Properties
نویسندگان
چکیده
WF14865Aand B, novel cathepsins B and L inhibitors, were produced and isolated separately from the culture mycelium of a fungal strain Aphanoascus fulvescens No. 14865. Spectroscopic analysis revealed that both WF14865Aand B were composed of transepoxysuccinyl moieties, 1 -//-imidazole-2-ylamine, and isoleucine or leucine. These compounds inhibited human cathepsins B and L with IC50 values in the range of 8.4-72nM in vitro. Though their in vitro properties were typical as frzms-epoxysuccinyl type inhibitors, they exerted strong bone resorption inhibitory effects in low-calcium-diet-fed mouse model at 3.2~ 10 mg/kg.
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