| 摘要 |
NEW MATERIAL:The substance of formula I (R is H or OH) (named as estatin), its salt or its hydrate. EXAMPLE:Estatin A (R=H). USE:Pharmaceuticals or reagents for investigation. A thiol protease inhibitor. It exhibits strong enzyme-inhibiting activity against thiol protease such as papain and expected to be effective as a remedy for inflammation, muscular dystrophy, etc. Also expected to have anti-allergy activity. PREPARATION:A microbial strain separated from soil, belonging to Myceliophthora genus and capable of producing the substance of formula I is cultured in a medium, and the substance of formula I is separated from the culture product. As an alternative method, the substance of formula I can be produced by reacting the compound of formula III (R' is H, etc.) with the compound of formula IV (B1 is ester residue, etc., eliminable by saponification), and saponifying the resultant compound of formula II with KOH, etc., in methanol. |
