Biological properties of ristocetin-.PSI.-aglycone.

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Abstract
Ristocetin-.PSI.-aglycone obtained by acid hydrolysis of ristocetin A, has a substantially greater antimicrobial activity against gram-positive bacteria than the parent compound. None of the substances are active against gram-negative bacteria, yeast or fungi. The .PSI.-aglycone is several times more toxic [to rats and mice] than ristocetin A when administered i.v. Both substances are well-tolerated when given s.c., i.p. and perorally. Ristocetin A and the .PSI.-aglycone have a very low absorption after oral administration. Plasma levels following i.v. administration of ristocetin A and the .PSI.-aglycone are comparable, with both showing a rapid decline during the first 60 min followed by a somewhat slower elimination. The aggregating properties of the .PSI.-aglycone could not be determined due to its low solubility at neutral pH.