TABLE 1.

Drug disruption of cytoskeletal elements in the Apicomplexa

Drug and cytoskeletal element (drug mechanism)ConcnActionComments
Actin microfilaments
    Cytochalasin D (disrupter)a0.1-0.2 μMInhibits actin-based gliding motility (extracellular) and invasionInhibits gliding motility in extracellular parasites; use resistant host cells to avoid host cell effects.
    Latrunculin (disrupter)b10 nM-5 μMInhibits motility and invasionWill also show host cell actin effects.
    Jasplakinolide (stabilizer)c50 nM-2 μMFilament polymerization inhibits gliding and invasionActs on extracellular parasites; will also act on host cell actin in intracellular settings.
Microtubules
    Oryzalin (disrupter)dAlso other dinitroanilines such as trifluralin, ethafluralin
        Subpellicular microtubules0.5 μMParasites lack apical polarityNo effect on extracellular parasites; no effect on host cell microtubules, but intracellular parasites are affected.
        Spindle microtubules2.5 μMParasites are incapable of replicationAs for subpellicular microtubules.
    Colchicine (disrupter)e
        Subpellicular microtubules10 μM-1 mMParasites lack apical polarityNo drug effect on extracellular parasites; use resistant host cells to avoid host cell disruption (no microtubules in RBCs).
        Spindle microtubules5-10 mMParasites are incapable of replicationAs for subpellicular microtubules.
    Colcemid (disrupter)f50 μMInhibits intracellular growthNo cell biological observations accompany study.
    Vinblastine (disrupter)g15-100 nMInhibits intracellular growthNo cell biological observations accompany study.
    Vincristine (disrupter)h7 nMInhibits intracellular growthNo cell biological observations accompany study.
    Tubulozole (disrupter)i10 μMParasites are killedMay inhibit parasite protein synthesis rather than microtubules
    Taxol (stabilizer)j0.1-0.5 μMParasites are incapable of buddingNo drug effect on extracellular parasites; host cell microtubules will also be affected (no microtubules in RBCs).
    Docetaxel/taxotere (stabilizer)k10 nm-50 μMParasites are incapable of replicationNo drug effect on extracellular parasites; host cell microtubules will also be affected (no microtubules in RBCs).
    Epithalone A (stabilizer)l0.1-0.5 μMParasites are incapable of buddingNo drug effect on extracellular parasites; host cell microtubules will also be affected (no microtubules in RBCs).
Myosin
    BDM (ATPase inhibitor)m20-40 mMInhibits actin-based gliding motility (extracellular) and invasionWill also act on host cell myosins (not present in red cells).
    KT5926 (LC kinase inhibitor)n1-5 μMInhibits actin-based gliding motility (extracellular) and invasionMost probably inhibits secretion of TRAP family adhesins rather than myosin.
  • a Data from references 8, 25, 28, 35, 37, 39, 54, 56, 57, 64, 69, 85, 103, 104, 129, 131, 140, 143-145, 148, 152, 156, 163, and 170.

  • b Data from reference 145.

  • c Data from references 123, 145, and 147.

  • d Data from references 11, 17, 22, 59, 78, 96, 110, 145, and 164.

  • e Data from references 15, 23, 59, 85, 131, 156, 173, 185, 188, and 189.

  • f Data from reference 16.

  • g Data from references 16, 35, 120, 131, 156, 174, 188, and 189.

  • h Data from references 35 and 174.

  • i Data from references 16, 35, and 36.

  • j Data from references 59, 69, 85, 144, 145, 159, and 168.

  • k Data from references 137 and 159.

  • l Data from reference 168.

  • m Data from references 37, 56, 57, 64, and 119.

  • n Data from reference 37.