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Susceptibility

Antileishmanial Activities of Aphidicolin and Its Semisynthetic Derivatives

O. Kayser, A. F. Kiderlen, S. Bertels, K. Siems
O. Kayser
Institute of Pharmacy and Department of Pharmaceutical Biotechnology, Freie Universität, D-12169 Berlin,
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A. F. Kiderlen
Department of Infectious Diseases, Robert Koch-Institut, D-13353 Berlin,and
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S. Bertels
AnalytiCon AG, Hermannswerder, 14473 Potsdam, Germany
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K. Siems
AnalytiCon AG, Hermannswerder, 14473 Potsdam, Germany
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DOI: 10.1128/AAC.45.1.288-292.2001
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    Fig. 1.

    Chemical structures of aphidicolans used in this study.

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  • Table 1.

    Antileishmanial activities of aphidicolin and derivatives

    CompoundaEC50 (μg/ml) against parasite:EC50 (μg/ml) for cytotoxicity to cells:SIb
    L. major (extracellular)L. donovani (extracellular)L. infantum (extracellular)L. enriettii (extracellular)L. donovani (intracellular)BMMφKBSK-Mel
    10.190.540.140.310.12>25.0>25.0>25.0208
    21.772.501.701.880.95>25.0>25.0>25.026
    31.830.620.991.320.1124.9>25.0>25.0226
    40.400.600.420.420.21>22.4>25.0>25.0106
    50.090.080.100.100.0518.2>25.0>25.0364
    60.050.040.060.040.20>25.0>25.0>25.0125
    70.510.310.500.510.36>25.0>25.0>25.069
    81.090.631.701.141.11>25.0>25.0>25.023
    90.380.310.950.330.20>25.0>25.0>25.0125
    100.410.320.950.650.25>25.0>25.0>25.0100
    110.370.270.890.610.24>25.0>25.0>25.0104
    120.541.250.673.300.56>25.0>25.0>25.044
    13>5.0>5.0>5.0>5.0>5.0>25.0>25.0>25.05
    140.120.080.120.120.09>25.0>25.0>25.0277
    150.450.660.440.570.20>25.0>25.0>25.016
    161.25>5.0>5.03.30>5.0>25.0>25.0>25.05
    171.251.841.880.851.51>25.0>25.0>25.016
    180.120.200.210.110.0211.3>25.0>25.0565
    AMB0.030.030.040.020.025>25.0>25.0>25.01,000
    MF0.020.050.060.020.002>25.0>25.0>25.0<12,500
    • ↵a AMB, amphotericin B; MF, miltefosin.

    • ↵b SI, ratio of EC50 for cytotoxicity to BMMφ to EC50 for intracellular L. donovani.

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Antileishmanial Activities of Aphidicolin and Its Semisynthetic Derivatives
O. Kayser, A. F. Kiderlen, S. Bertels, K. Siems
Antimicrobial Agents and Chemotherapy Jan 2001, 45 (1) 288-292; DOI: 10.1128/AAC.45.1.288-292.2001

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Antileishmanial Activities of Aphidicolin and Its Semisynthetic Derivatives
O. Kayser, A. F. Kiderlen, S. Bertels, K. Siems
Antimicrobial Agents and Chemotherapy Jan 2001, 45 (1) 288-292; DOI: 10.1128/AAC.45.1.288-292.2001
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KEYWORDS

Antiprotozoal Agents
Aphidicolin
Leishmania

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