PURPOSE: To obtain the subject new physiologically active substance inhibiting the activity of dipeptidylpeptidase III, useful as an enzyme inhibitor, analgesic, etc., by culturing in a nutritive medium fluostatin-productive bacteria belonging to Streptomyces.
CONSTITUTION: Fluostatin-productive bacteria belonging to Streptomyces [e.g. Streptomyces sp. TA-3391 strain (FERM P-13048)] is inoculated into a medium followed by shaking culture at 30°C for 3 days and the resultant culture fluid is filtered and separated into a culture filtrate and microbes, and the filtrate is put to an adsorptive resin column followed by washing with deionized water and then eluting the adsorbate with 50% acetone water. The resultant eluate is concentrated at reduced pressures to eliminate the acetone, and ethyl acetate is added to the remaining eluate to carry out extraction, and the resultant extract is concentrated and then put to a silica gel column to conduct purification, thus affording the objective fluostatin A and fluostatin B of the formula [R1-R2-R3 is formula CO-CH=C(CH3) for fluostatin A, being formula CH(OH)-CH (OH)-CH(CH3) for fluostatin B].
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