Antiprotozoal Activity and Selectivity Index of Organic Salts of Albendazole and Mebendazole

Infections from the protozoa Entamoeba histolytica (E. histolytica), Giardia lamblia (G. lamblia), and Trichomonas vaginalis (T. vaginalis) pose a public health issue, with albendazole and mebendazole serving as the second-line medications for treating these parasitic infections. However, the low aqueous solubility of these compounds has led to the exploration of new strategies to enhance their solubility, with the formation of salts being a commonly employed strategy. The sulfonates A1, A2, and A3 of albendazole, along with M1, M2, and M3 of mebendazole, were synthesized. The antiparasitic activity in vitro was assessed against the trophozoites of E. histolytica, G. lamblia, and T. vaginalis. The salts A2, A3, M2, and M3 demonstrated a greater antiparasitic effect (IC50 37.95–125.53 µM) compared to the positive controls albendazole and mebendazole. The salts A1, A3, M2, and M3 do not exhibit cytotoxic effects at concentrations of 500 µM on the Vero cell line. Taken together, these findings indicate that the formation of these new solid saline phases enhances the antiparasitic effects in vitro, which is crucial in the current search for improved, safe, and effective antiparasitic agents.

Authors

Institutions

Publication Details

Journal
Microbiology Research
Published
2025-03-27
DOI
https://doi.org/10.3390/microbiolres16040077
Primary Topic
Pharmaceutical and Antibiotic Environmental Impacts
Type
article
Field-Weighted Citation Impact
0.00

Funders

Controls
|||
ALL TIME
JAN
FEB
MAR
APR
MAY
JUN
JUL
AUG
SEP
OCT
article

Antiprotozoal Activity and Selectivity Index of Organic Salts of Albendazole and Mebendazole

Janeth Gómez-García, Miriam Guadalupe Barón-Pichardo, Blanca Estela Duque-Montaño, Oscar Torres-Ángeles et al.
Microbiology Research
Pharmaceutical and Antibiotic Environmental Impacts
article

Antiprotozoal Activity and Selectivity Index of Organic Salts of Albendazole and Mebendazole

Janeth Gómez-García, Miriam Guadalupe Barón-Pichardo, Blanca Estela Duque-Montaño, Oscar Torres-Ángeles, Jesús Rivera-Islas, David Durán-Martínez
article en

Abstract

Infections from the protozoa Entamoeba histolytica (E. histolytica), Giardia lamblia (G. lamblia), and Trichomonas vaginalis (T. vaginalis) pose a public health issue, with albendazole and mebendazole serving as the second-line medications for treating these parasitic infections. However, the low aqueous solubility of these compounds has led to the exploration of new strategies to enhance their solubility, with the formation of salts being a commonly employed strategy. The sulfonates A1, A2, and A3 of albendazole, along with M1, M2, and M3 of mebendazole, were synthesized. The antiparasitic activity in vitro was assessed against the trophozoites of E. histolytica, G. lamblia, and T. vaginalis. The salts A2, A3, M2, and M3 demonstrated a greater antiparasitic effect (IC50 37.95–125.53 µM) compared to the positive controls albendazole and mebendazole. The salts A1, A3, M2, and M3 do not exhibit cytotoxic effects at concentrations of 500 µM on the Vero cell line. Taken together, these findings indicate that the formation of these new solid saline phases enhances the antiparasitic effects in vitro, which is crucial in the current search for improved, safe, and effective antiparasitic agents.

Microbiology ResearchVol. 16(4)
Universidad Autónoma del Estado de Morelos (MX)
Consejo Nacional de Ciencia y Tecnología
Openalex Percentile: Top 96%
Pharmaceutical and Antibiotic Environmental Impacts
AI Navigator

Ask Laika to Summarize, Analyze, and Connect papers live on the map.

Summarize Papers & Methodologies

Extract key findings, datasets, and comparative methods across publications.

Benchmark Rankings & Visual Analytics

Rank top research institutions, authors, funders, topics, and journals by Field-Weighted Citation Impact (FWCI) and paper volume with instant charts.

Connect Distant Disciplines

Bridge topological clusters on the map to find hidden collaborative intersections.

Antiprotozoal Activity and Selectivity Index of Organic Salts of Albendazole and Mebendazole — Janeth Gómez-García, Miriam Guadalupe Barón-Pichardo, et al. · Microbiology Research (2025) | TGRS Research Map | TGRS