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Modified Hederagenin Derivatives Demonstrate Ex Vivo Anthelmintic Activity against Fasciola hepatica

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Modified Hederagenin Derivatives Demonstrate Ex Vivo Anthelmintic Activity against Fasciola hepatica. / Chakroborty, Anand; Pritchard, Deiniol; Bouillon, Marc et al.
In: Pharmaceutics, Vol. 15, No. 7, 1869, 03.07.2023.

Research output: Contribution to journal › Article › peer-review

HarvardHarvard

Chakroborty, A, Pritchard, D, Bouillon, M, Cervi, A, Kraehenbuehl, R, Wild, C, Fenn, C, Holdsworth, P, Capner, C, Padalino, G, Forde-Thomas, JE, Payne, J, Smith, BG & Hoffmann, K 2023, 'Modified Hederagenin Derivatives Demonstrate Ex Vivo Anthelmintic Activity against Fasciola hepatica', Pharmaceutics, vol. 15, no. 7, 1869. https://doi.org/10.3390/pharmaceutics15071869

APA

Chakroborty, A., Pritchard, D., Bouillon, M., Cervi, A., Kraehenbuehl, R., Wild, C., Fenn, C., Holdsworth, P., Capner, C., Padalino, G., Forde-Thomas, J. E., Payne, J., Smith, B. G., & Hoffmann, K. (2023). Modified Hederagenin Derivatives Demonstrate Ex Vivo Anthelmintic Activity against Fasciola hepatica. Pharmaceutics, 15(7), Article 1869. https://doi.org/10.3390/pharmaceutics15071869

CBE

Chakroborty A, Pritchard D, Bouillon M, Cervi A, Kraehenbuehl R, Wild C, Fenn C, Holdsworth P, Capner C, Padalino G, et al. 2023. Modified Hederagenin Derivatives Demonstrate Ex Vivo Anthelmintic Activity against Fasciola hepatica. Pharmaceutics. 15(7):Article 1869. https://doi.org/10.3390/pharmaceutics15071869

MLA

Chakroborty, Anand et al. "Modified Hederagenin Derivatives Demonstrate Ex Vivo Anthelmintic Activity against Fasciola hepatica". Pharmaceutics. 2023. 15(7). https://doi.org/10.3390/pharmaceutics15071869

VancouverVancouver

Chakroborty A, Pritchard D, Bouillon M, Cervi A, Kraehenbuehl R, Wild C et al. Modified Hederagenin Derivatives Demonstrate Ex Vivo Anthelmintic Activity against Fasciola hepatica. Pharmaceutics. 2023 Jul 3;15(7):1869. Epub 2023 Jul 3. doi: 10.3390/pharmaceutics15071869

Author

Chakroborty, Anand ; Pritchard, Deiniol ; Bouillon, Marc et al. / Modified Hederagenin Derivatives Demonstrate Ex Vivo Anthelmintic Activity against Fasciola hepatica. In: Pharmaceutics. 2023 ; Vol. 15, No. 7.

RIS

TY - JOUR

T1 - Modified Hederagenin Derivatives Demonstrate Ex Vivo Anthelmintic Activity against Fasciola hepatica

AU - Chakroborty, Anand

AU - Pritchard, Deiniol

AU - Bouillon, Marc

AU - Cervi, Anna

AU - Kraehenbuehl, Rolf

AU - Wild, Charlotte

AU - Fenn, Caroline

AU - Holdsworth, Peter

AU - Capner, Colin

AU - Padalino, Gilda

AU - Forde-Thomas, Josephine E.

AU - Payne, Joseph

AU - Smith, Brendan G.

AU - Hoffmann, Karl

PY - 2023/7/3

Y1 - 2023/7/3

N2 - Infection with Fasciola hepatica (liver fluke) causes fasciolosis (or fascioliasis) and poses a considerable economic as well as welfare burden to both the agricultural and animal health sectors. Here, we explore the ex vivo anthelmintic potential of synthetic derivatives of hederagenin, isolated in bulk from Hedera helix. Thirty-six compounds were initially screened against F. hepatica newly excysted juveniles (NEJs) of the Italian strain. Eleven of these compounds were active against NEJs and were selected for further study, using adult F. hepatica derived from a local abattoir (provenance unknown). From these eleven compounds, six demonstrated activity and were further assessed against immature liver flukes of the Italian strain. Subsequently, the most active compounds (n = 5) were further evaluated in ex vivo dose response experiments against adult Italian strain liver flukes. Overall, MC042 was identified as the most active molecule and the EC 50 obtained from immature and adult liver fluke assays (at 24 h post co-culture) are estimated as 1.07 μM and 13.02 μM, respectively. When compared to the in vitro cytotoxicity of MDBK bovine cell line, MC042 demonstrated the highest anthelmintic selectivity (44.37 for immature and 3.64 for adult flukes). These data indicate that modified hederagenins display properties suitable for further investigations as candidate flukicides.

AB - Infection with Fasciola hepatica (liver fluke) causes fasciolosis (or fascioliasis) and poses a considerable economic as well as welfare burden to both the agricultural and animal health sectors. Here, we explore the ex vivo anthelmintic potential of synthetic derivatives of hederagenin, isolated in bulk from Hedera helix. Thirty-six compounds were initially screened against F. hepatica newly excysted juveniles (NEJs) of the Italian strain. Eleven of these compounds were active against NEJs and were selected for further study, using adult F. hepatica derived from a local abattoir (provenance unknown). From these eleven compounds, six demonstrated activity and were further assessed against immature liver flukes of the Italian strain. Subsequently, the most active compounds (n = 5) were further evaluated in ex vivo dose response experiments against adult Italian strain liver flukes. Overall, MC042 was identified as the most active molecule and the EC 50 obtained from immature and adult liver fluke assays (at 24 h post co-culture) are estimated as 1.07 μM and 13.02 μM, respectively. When compared to the in vitro cytotoxicity of MDBK bovine cell line, MC042 demonstrated the highest anthelmintic selectivity (44.37 for immature and 3.64 for adult flukes). These data indicate that modified hederagenins display properties suitable for further investigations as candidate flukicides.

KW - Fasciola hepatica

KW - Hedera helix

KW - anthelmintic drug discovery

KW - saponins and hederagenin

U2 - 10.3390/pharmaceutics15071869

DO - 10.3390/pharmaceutics15071869

M3 - Article

C2 - 37514055

VL - 15

JO - Pharmaceutics

JF - Pharmaceutics

SN - 1999-4923

IS - 7

M1 - 1869

ER -