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The in vivo activity of 1,3,4-thiadiazolium-2-aminide compounds in the treatment of cutaneous and visceral leishmaniasis.
J Antimicrob Chemother. 2012 Jan; 67(1):182-90.JA

Abstract

OBJECTIVES

Researchers have recently investigated the biological activities of mesoionic (MI) compounds, which have shown in vitro activity against many species of Leishmania, as well as Trypanosoma cruzi. The main goal of this study was to evaluate and compare the activity of three MI compounds against Leishmania amazonensis and Leishmania infantum infection in vivo.

METHODS

The experiments were carried out using BALB/c mice infected with L. amazonensis or L. infantum as a highly sensitive murine model. The infected mice were treated with MI-HH, MI-4-OCH(3), MI-4-NO(2) or meglumine antimoniate by different routes (intralesional, topical or intraperitoneal).

RESULTS

Treatment with MI-4-OCH(3) and MI-4-NO(2) efficiently contained the progression of cutaneous and visceral leishmaniasis in comparison with the control group or mice treated with meglumine antimoniate. Interestingly, these MI compounds did not produce toxicological effects after treatment. Furthermore, treatment with these compounds led to a modulation of the immune response that was correlated with disease control. In this study, MI compounds, and MI-4-NO(2) in particular, exhibited high activity in the L. infantum murine model. In the L. amazonensis model, intralesional treatment with MI-4-OCH(3) or MI-4-NO(2) showed greater therapeutic efficacy than treatment with meglumine antimoniate, and the new topical formulations of these compounds also displayed great activity in the cutaneous leishmaniasis model.

CONCLUSIONS

Upon comparison of each MI compound, MI-4-NO(2) was clearly the compound with the greatest activity in these two in vivo infection models by each administration route tested.

Authors+Show Affiliations

Fundação Oswaldo Cruz, Instituto Oswaldo Cruz, Laboratório de Bioquímica de Tripanosomatídeos, Rio de Janeiro, Brasil. rakelbio@gmail.comNo affiliation info availableNo affiliation info availableNo affiliation info availableNo 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

21987238

Citation

Rodrigues, Raquel F., et al. "The in Vivo Activity of 1,3,4-thiadiazolium-2-aminide Compounds in the Treatment of Cutaneous and Visceral Leishmaniasis." The Journal of Antimicrobial Chemotherapy, vol. 67, no. 1, 2012, pp. 182-90.
Rodrigues RF, Charret KS, Campos MC, et al. The in vivo activity of 1,3,4-thiadiazolium-2-aminide compounds in the treatment of cutaneous and visceral leishmaniasis. J Antimicrob Chemother. 2012;67(1):182-90.
Rodrigues, R. F., Charret, K. S., Campos, M. C., Amaral, V., Echevarria, A., Dos Reis, C., Canto-Cavalheiro, M. M., & Leon, L. L. (2012). The in vivo activity of 1,3,4-thiadiazolium-2-aminide compounds in the treatment of cutaneous and visceral leishmaniasis. The Journal of Antimicrobial Chemotherapy, 67(1), 182-90. https://doi.org/10.1093/jac/dkr409
Rodrigues RF, et al. The in Vivo Activity of 1,3,4-thiadiazolium-2-aminide Compounds in the Treatment of Cutaneous and Visceral Leishmaniasis. J Antimicrob Chemother. 2012;67(1):182-90. PubMed PMID: 21987238.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - The in vivo activity of 1,3,4-thiadiazolium-2-aminide compounds in the treatment of cutaneous and visceral leishmaniasis. AU - Rodrigues,Raquel F, AU - Charret,Karen S, AU - Campos,Monica C, AU - Amaral,Veronica, AU - Echevarria,Aurea, AU - Dos Reis,Camila, AU - Canto-Cavalheiro,Marilene M, AU - Leon,Leonor L, Y1 - 2011/10/10/ PY - 2011/10/12/entrez PY - 2011/10/12/pubmed PY - 2012/3/30/medline SP - 182 EP - 90 JF - The Journal of antimicrobial chemotherapy JO - J Antimicrob Chemother VL - 67 IS - 1 N2 - OBJECTIVES: Researchers have recently investigated the biological activities of mesoionic (MI) compounds, which have shown in vitro activity against many species of Leishmania, as well as Trypanosoma cruzi. The main goal of this study was to evaluate and compare the activity of three MI compounds against Leishmania amazonensis and Leishmania infantum infection in vivo. METHODS: The experiments were carried out using BALB/c mice infected with L. amazonensis or L. infantum as a highly sensitive murine model. The infected mice were treated with MI-HH, MI-4-OCH(3), MI-4-NO(2) or meglumine antimoniate by different routes (intralesional, topical or intraperitoneal). RESULTS: Treatment with MI-4-OCH(3) and MI-4-NO(2) efficiently contained the progression of cutaneous and visceral leishmaniasis in comparison with the control group or mice treated with meglumine antimoniate. Interestingly, these MI compounds did not produce toxicological effects after treatment. Furthermore, treatment with these compounds led to a modulation of the immune response that was correlated with disease control. In this study, MI compounds, and MI-4-NO(2) in particular, exhibited high activity in the L. infantum murine model. In the L. amazonensis model, intralesional treatment with MI-4-OCH(3) or MI-4-NO(2) showed greater therapeutic efficacy than treatment with meglumine antimoniate, and the new topical formulations of these compounds also displayed great activity in the cutaneous leishmaniasis model. CONCLUSIONS: Upon comparison of each MI compound, MI-4-NO(2) was clearly the compound with the greatest activity in these two in vivo infection models by each administration route tested. SN - 1460-2091 UR - https://www.unboundmedicine.com/medline/citation/21987238/The_in_vivo_activity_of_134_thiadiazolium_2_aminide_compounds_in_the_treatment_of_cutaneous_and_visceral_leishmaniasis_ L2 - https://academic.oup.com/jac/article-lookup/doi/10.1093/jac/dkr409 DB - PRIME DP - Unbound Medicine ER -