Table 3
Other compounds evaluated on Echinococcus multilocularis larvae. Effective concentration at 50% (EC50) is given for in vitro tests when specified in the original publication. Otherwise, the concentration used or the minimum concentration leading to a significant effect is given. For in vivo studies, comparison with albendazole is provided, when available.
Compound | In vitro method | Animal model | Conclusion | Reference |
---|---|---|---|---|
Anti-infective compounds | ||||
DB1127 (dicationic derivative of pentamidine) | PGI | Peritoneal secondary | Active in vitro (EC50 = 6.1 μM) and in vivo through IP (=ABZ) but not oral route | [52, 108] |
Buparvaquone | PGI and resazurin assay | Peritoneal secondary | Active in vitro (EC50 = 2.9 μM) but not in vivo | [97] |
Atovaquone | PSC viability | Primary liver | Active in vitro (50 μM) and in vivo (<ABZ) | [26, 27] |
MMV665807 | PGI and resazurin assay, PCGC viability | Peritoneal secondary | Active in vitro (EC50 = 1.2 μM) but not in vivo | [109] |
Clarithromycin | Metacestode viability | Not applicable | Active in vitro (13 μM) | [77] |
Artesunate and dihydroartemisinin | EmAP | Peritoneal secondary | Active in vitro (40 μM) and in vivo (synergy with ABZ) | [106] |
Itraconazole | Metacestode viability | Not applicable | Active in vitro (1 mM) | [91] |
Artemether, caspofungin, miltefosine, rifampicin, cotrimoxazole | Not active in vitro | |||
HIV protease inhibitors | Metacestode and PSC viability | Peritoneal secondary | Nelfinavir active in vitro (EC50 = 29 μM) and in vivo (=ABZ) | [69] |
Antineoplastic compounds | ||||
Nilotinib, everolimus | PGI | Subcutaneous secondary | Active in vitro (nilotinib EC50 = 77 μM, everolimus EC50 = 33 μM) but not in vivo | [42] |
Imatinib | Metacestode morphology, PSC and PCGC viability | Not applicable | Active in vitro (25 μM) | [34] |
Afatinib, U0126 | Metacestode morphology, PSC viability | Peritoneal secondary | Active in vitro (10 μM Afatinib, 200 μM U0126) and in vivo (=ABZ) | [19] |
BI 2536 | PCGC viability | Not applicable | Active in vitro (10 nM) | [102] |
Vincristine, navelbine, methotrexate | Metacestode viability (inoculation) | Not applicable | Vincristine and navelbine active in vitro (0.1–60 nM), methotrexate increases parasite growth | [39] |
Docetaxel, paclitaxel, doxorubicin, vorinostat, navelbine | Metacestode viability (inoculation) | Not applicable | Docetaxel (2–10 μM) and paclitaxel (2–10 μM) active in vitro | [38] |
Bortezomib | PGI | Peritoneal secondary | Active in vitro (EC50 = 0.6 μM) but not in vivo | [107] |
PIM kinases inhibitors: SGI-1776, CX-6258 | Metacestode morphology, PCGC viability | Not applicable | Active in vitro (10 μM) | [48] |
2-methoxyestradiol | Em14-3-3 RT-qPCR | Peritoneal secondary | Active in vitro (5 μM) but not in vivo | [105] |
2-deoxy-D-glucose | EmAP | Peritoneal secondary | Active in vitro (80 μM) and in vivo (=ABZ) | [128] |
3-bromopyruvate | EmAP | Peritoneal secondary | Active in vitro (40 μM) and in vivo (=ABZ) | [130] |
Lonidamine | EmAP | Not applicable | Active in vitro (40 μM) | [131] |
Plant-extracted compounds | ||||
Osthole | Not applicable | Peritoneal secondary | Active in vivo (=ABZ) | [135] |
Ampelopsin | EmAP | Not applicable | Active in vitro (40 μM) | [129] |
Thymol | PSC viability | Peritoneal secondary | Active in vitro (67 μM) and in vivo (=ABZ) | [2, 3] |
Carvacrol | Metacestode viability | Peritoneal secondary | Potentialization of ABZ in vitro and in vivo | [71] |
Crocin | PGI, PSC and PCGC viability | Peritoneal secondary | Active in vitro (EC50 = 11.4 μM) and in vivo (=ABZ) | [65] |
Others | ||||
Metformin | PSC and PCGC viability | Peritoneal secondary | Active in vitro (10 mM) and in vivo | [70] |
Endochin-like quinolones | PGI and resazurin assay, PCGC viability | Not applicable | Active in vitro (EC50 = 0.2–1.7 μM) | [18] |
Verapamil | Not applicable | Liver secondary | Active in vivo (=ABZ) | [29] |
Thiacloprid | PGI and PSC viability | Peritoneal secondary | Active in vitro (5 μM) et in vivo (=ABZ) | [66] |
Isoprinosine, inosine, L-Phe-Phe-Ome | PSC viability | Not applicable | Active in vitro (inosine and L-Phe-Phe-Ome EC50 ≈ 50 μM, isoprinosine EC50 ≈ 250 μM) | [59] |
R-propylamine | PSC viability | Peritoneal secondary | Active in vitro (20 μM) and in vivo (=ABZ) | [20] |
Ruthenium complexes | PGI | Not applicable | Active in vitro (EC50 = 1.4–4.7 μM) | [53] |
Note: ABZ, albendazole; PCGC, primary culture of germinative cells; EmAP, E. multilocularis alkaline phosphatase assay; IP, intraperitoneal; PGI, phosphoglucose isomerase assay; PSC, protoscolex; =ABZ, equivalent to albendazole; >ABZ, superior to albendazole; <ABZ, inferior to albendazole.
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