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. 2017 Mar 24;61(4):e02048-16. doi: 10.1128/AAC.02048-16

TABLE 1.

Bioluminescence signal and lesion suppression rates in BALB/c mice treated with known antileishmanial compoundsa

Compound tested Dose (mg/kg) Bioluminescence signal suppression at 18 ± 1 days postinfection Lesion suppression at 60 ± 2 days postinfection
Amphotericin B formulations
    Amphotericin B 2 −88.1 −70.7
    Amphotericin B 4 −150.0 −33.0
    Amphotericin B 6 36.5 66.7
    Amphotericin B 8 67.3* 88.8*
    Amphotericin B 16 99.1* 84.5*
    ABLC 12.5 74.2* 60.9*
    ABLC 25 93.1* 77.9*
    ABLC 37.5 99.4* 96.5*
    AmBisome 12.5 99.4* 80.7*
    AmBisome 25 99.8* 99.1*
    AmBisome 37.5 100* 100.0*
    AmBisome 50 100* 100.0*
Other antileishmanial compounds
    Paromomycin 80 100* 100*
    Sodium stibogluconate 400 89.7* 65.9
    Pentamidine 50 68.9 63.1&
    Sinefungin 10b 99.9* Euthanized
    Posaconazole 100 94.9* 96.5*
    Ofloxacin 80 −52.8 −85.4
    Miltefosine 17.5 18.1 −20.1
    Fluconazole 160 −0.4 −10.6
    Glucantime 100 −13.7 −29.8
a

The lesion suppression activities of different doses of the three formulations of amphotericin B and other known antileishmanial compounds are shown. Five BALB/c mice were assigned to each treatment and vehicle-control group. Mice were infected i.d. with 1 × 107 stationary-phase luciferase-expressing L. major parasites at the base of the tail on day 0. Drug treatments were initiated on day 3 postinfection. Drugs were given for 10 consecutive days, except for paromomycin, sodium stibogluconate, sinefungin, and i.m. pentamidine, which were given for 7, 14, 8, and 3 days, respectively. The mean bioluminescence signals at the infection site (in number of photons per second per mouse) and the mean lesion size (in square millimeters) were measured on days 18 ± 1 and 60 ± 2 postinfection, respectively, and were expressed as a percentage of the bioluminescence signal compared with that for the vehicle-control group or the mean percent lesion suppression compared with that for the vehicle-control group. A single-factor ANOVA (Dunnett's test) was used to determine whether differences in group means existed across the experiment. *, a statistically significant difference (P < 0.05); &, lesion size was last measured on day 33 postinfection.

b

The bioluminescence signal was measured for the last time on day 11 postinfection, when all animals were euthanized due to drug toxicity (weight loss, ≥20%). As a result, only eight doses of sinefungin were given.