Study Type | Effect Studied | Experimental Model | Result | Reference |
---|---|---|---|---|
In vitro | Activity. | Susceptibility testing by the macro dilution reference method of the National Center for Clinical Laboratory Standards (NCCLS). |
In vitro inhibitory activity of SPA-S-843 against Aspergillus sp was superior than that of amphotericin B. While the activity against R oryzae, P variotti, Penicillium sp and S schenkii were similar. The MFC values were 12.53, 12.00 and 19.20 µg/ml against Aspergillus sp, Penicillium sp and S schenkii, respectively. |
374266 |
In vitro | Activity. | Broth and agar microdilution by the NCCLS. |
SPK-843 had significantly lower MIC values than amphotericin B against S cerevisae, C tropicalis, C neoformans and C glabrata. SPK-843 was most fungicidal against C krusei, C tropicalis and C albicans. |
308269 |
In vitro | Activity. | Contact test and germ tube inhibition test. |
SPK-843 killed C albicans in 3 min. The best fungicidal activity occurred in a medium with low electrical conductivity (0.001 M buffer strength) and pH 5.8. The activity of SPK-843 is associated with the induction of greater cellular damage following increasing leakage of K+. SPK-843 produced 80% leakage in 4 min, while amphotericin B produced 35% in the same time. |
358056 |
In vivo | Activity. | CD-1 mice intravenously infected with C albicans. |
The activity of SPK-843 was 2-fold higher than D-AMPH at doses of 0.2 to 0.4 mg/kg/day for 5 days. At 0.8 mg/kg/day for 5 days, SPK-843 completely eradicated C albicans in eight out of ten mice, whereas the same dose of D-AMPH had no effect. |
382489 |
In vivo | Efficacy. | CD-1 mice infected with 5 × 106 C albicans KSG-27 cells. |
SPK-843 (0.25 mg/kg) reduced viable C albicans cell count in the kidney to less than 1/100 of control on day 1. At the same dose, SPK-843 eradicated fungi by day 4 from 50 to 100% of mice, whereas amphotericin B required a dose of 1 mg/kg to reach these eradication levels. |
568943 |