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In vitro and in vivo activities of dicationic diguanidino compounds against Echinococcus multilocularis metacestodes.
Antimicrob Agents Chemother. 2013 Aug; 57(8):3829-35.AA

Abstract

Alveolar echinococcosis (AE) is a disease predominantly affecting the liver, with metacestodes (larvae) of the tapeworm Echinococcus multilocularis proliferating and exhibiting tumor-like infiltrative growth. For many years, chemotherapeutical treatment against alveolar echinococcosis has relied on the benzimidazoles albendazole and mebendazole, which require long treatment durations and exhibit parasitostatic rather than parasiticidal efficacy. Although benzimidazoles have been and still are beneficial for the patients, there is clearly a demand for alternative and more efficient treatment options. Aromatic dications, more precisely a small panel of di-N-aryl-diguanidino compounds, were screened for efficacy against E. multilocularis metacestodes in vitro. Only those with a thiophene core group were active against metacestodes, while furans were not. The most active compound, DB1127, was further investigated in terms of in vivo efficacy in mice experimentally infected with E. multilocularis metacestodes. This diguanidino compound was effective against AE when administered intraperitoneally but not when applied orally. Thus, thiophene-diguanidino derivatives with improved bioavailability when administered orally could lead to treatment options against AE.

Authors+Show Affiliations

Institute of Parasitology, Vetsuisse Faculty, University of Berne, Berne, Switzerland.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

23716058

Citation

Küster, Tatiana, et al. "In Vitro and in Vivo Activities of Dicationic Diguanidino Compounds Against Echinococcus Multilocularis Metacestodes." Antimicrobial Agents and Chemotherapy, vol. 57, no. 8, 2013, pp. 3829-35.
Küster T, Kriegel N, Boykin DW, et al. In vitro and in vivo activities of dicationic diguanidino compounds against Echinococcus multilocularis metacestodes. Antimicrob Agents Chemother. 2013;57(8):3829-35.
Küster, T., Kriegel, N., Boykin, D. W., Stephens, C. E., & Hemphill, A. (2013). In vitro and in vivo activities of dicationic diguanidino compounds against Echinococcus multilocularis metacestodes. Antimicrobial Agents and Chemotherapy, 57(8), 3829-35. https://doi.org/10.1128/AAC.02569-12
Küster T, et al. In Vitro and in Vivo Activities of Dicationic Diguanidino Compounds Against Echinococcus Multilocularis Metacestodes. Antimicrob Agents Chemother. 2013;57(8):3829-35. PubMed PMID: 23716058.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - In vitro and in vivo activities of dicationic diguanidino compounds against Echinococcus multilocularis metacestodes. AU - Küster,Tatiana, AU - Kriegel,Nadja, AU - Boykin,David W, AU - Stephens,Chad E, AU - Hemphill,Andrew, Y1 - 2013/05/28/ PY - 2013/5/30/entrez PY - 2013/5/30/pubmed PY - 2014/1/9/medline SP - 3829 EP - 35 JF - Antimicrobial agents and chemotherapy JO - Antimicrob. Agents Chemother. VL - 57 IS - 8 N2 - Alveolar echinococcosis (AE) is a disease predominantly affecting the liver, with metacestodes (larvae) of the tapeworm Echinococcus multilocularis proliferating and exhibiting tumor-like infiltrative growth. For many years, chemotherapeutical treatment against alveolar echinococcosis has relied on the benzimidazoles albendazole and mebendazole, which require long treatment durations and exhibit parasitostatic rather than parasiticidal efficacy. Although benzimidazoles have been and still are beneficial for the patients, there is clearly a demand for alternative and more efficient treatment options. Aromatic dications, more precisely a small panel of di-N-aryl-diguanidino compounds, were screened for efficacy against E. multilocularis metacestodes in vitro. Only those with a thiophene core group were active against metacestodes, while furans were not. The most active compound, DB1127, was further investigated in terms of in vivo efficacy in mice experimentally infected with E. multilocularis metacestodes. This diguanidino compound was effective against AE when administered intraperitoneally but not when applied orally. Thus, thiophene-diguanidino derivatives with improved bioavailability when administered orally could lead to treatment options against AE. SN - 1098-6596 UR - https://www.unboundmedicine.com/medline/citation/23716058/In_vitro_and_in_vivo_activities_of_dicationic_diguanidino_compounds_against_Echinococcus_multilocularis_metacestodes_ L2 - http://aac.asm.org/cgi/pmidlookup?view=long&pmid=23716058 DB - PRIME DP - Unbound Medicine ER -