IN-VITRO BIOLOGICAL-ACTIVITIES OF ALKALOIDS FROM CRYPTOLEPIS-SANGUINOLENTA

In our biological screening of higher plants, an aqueous and an 80 % E tOH extract from the root bark of Cryptolepis sanguinolenta showed pot ent antibacterial, anticomplementary, and moderate antiviral activitie s, but no antifungal effect could be detected. Bioassay-guided fractio nation of the 80 % EtOH extract led to the isolation of three alkaloid s: quindoline (1), hydroxycryptolepine (2), cryptolepine HCl (3), and the corresponding base cryptolepine (4). All compounds strongly inhibi ted the growth of Gram-positive bacteria (MIC less than or equal to 10 0 mu g/ml) and showed a moderate (MIC = 125 or 250 mu g/ml), a weak (M IC = 500 mu g/ml), or no activity (MIC > 500 mu g/ml) against selected Gram-negative bacteria. They also possessed a bactericidal effect dep ending on the bacterial strain. Compounds 1, 2, and 3 displayed a dose -dependent inhibitory effect on the classical pathway of the complemen t system while compounds 2 and 3 activated the alternative pathway, ex cept for compound 1. Compound 3 was found to possess an antiherpetic a ctivity. Compounds 1 and 4 showed no antiviral effect, but were quite cytotoxic in the antiviral test system down to a concentration of 1 mu g/ml.