Activity of Diosgenyl 2-amino-2-deoxy-β-D-glucopyranoside, its Hydrochloride, and N,N-dialkyl Derivatives Against Non-albicans Candida Isolates

摘要

Background: Candida albicans belongs to the most common fungal pathogens in humans,but recently an increased proliferation of strains called non-albicans Candida has been reported.Species belonging to this group are often characterised by a reduced susceptibility to antifungalagents.Objective: In view of the emergence of non-albicans Candida and their resistance to available antifungals,an attempt has been made to develop novel effective agents. Biological activities of theN,N-dialkyl diosgenyl glycosides, which were previously synthesized, were determined.Method: Minimum inhibitory concentration (MIC) was determined for group of clinical nonalbicansCandida isolates by serial dilution method in Sabouraud liquid medium. In order to assessthe toxicity towards human cells the minimum haemolytic concentration (MHC) was determinedon human erythrocytes by serial dilution method in phosphoric buffer.Results: The saponins exhibited a strong activity towards clinical isolates of C. glabrata and C.parapsilosis comparable or even stronger than that of conventional antimicrobials. A high rate ofresistance to fluconazole was shown among C. glabrata isolates. Among clinical strains of C.krusei and C. tropicalis, isolates with a decreased susceptibility to saponins were identified. All thetested C. krusei isolates showed resistance to fluconazole, while among C. tropicalis numerousstrains were resistant to all tested azoles. The saponins did not show haemolytic activities at theirmicrobiologically active concentrations.Conclusion: Results of the present work encourage to continue the study on steroidal saponins andtheir potential application for the treatment of candidemia.