TY - JOUR
T1 - Potential anti-amoebic activity of sulfonate- and sulfamate-containing carboxamide derivatives against pathogenic Acanthamoeba castellanii belonging to the genotype T4
AU - Akbar, Noor
AU - Siddiqui, Ruqaiyyah
AU - El-Gamal, Mohammed I.
AU - Zaraei, Seyed-Omar
AU - Saeed, Balsam Qubais
AU - Alawfi, Bader Saleem
AU - Khan, Naveed Ahmed
N1 - Copyright © 2023. Published by Elsevier B.V.
PY - 2024/2
Y1 - 2024/2
N2 - Acanthamoeba are ubiquitously distributed in the environment and can cause infection of the central nervous system as well a sight-threatening eye infection. Herein, the potential anti-amoebic activity of a series of sulfonate/sulfamate derivatives against pathogenic A. castellanii was evaluated. These compounds were tested using several assays namely amoebicidal, adhesion, excystation, cytotoxic, and cytopathogenicity. Amoebicidal assays revealed that the selected compounds reduced amoebae viability significantly (P < 0.05), and exhibited IC50 values at two-digit micromolar concentrations. Sulfamate derivatives 1j & 1k inhibited 50% of amoebae at 30.65 μM and 27.21 μM, respectively. The tested compounds blocked amoebae binding to host cells as well as inhibited amoebae excystation. Notably, the selected derivatives exhibited minimal human cell cytotoxicity but reduced parasite-mediated host cell damage. Overall, our study showed that sulfamate derivatives 1j & 1k have anti-amoebic potential and offer a promising avenue in the development of potential anti-amoebic drug candidates.
AB - Acanthamoeba are ubiquitously distributed in the environment and can cause infection of the central nervous system as well a sight-threatening eye infection. Herein, the potential anti-amoebic activity of a series of sulfonate/sulfamate derivatives against pathogenic A. castellanii was evaluated. These compounds were tested using several assays namely amoebicidal, adhesion, excystation, cytotoxic, and cytopathogenicity. Amoebicidal assays revealed that the selected compounds reduced amoebae viability significantly (P < 0.05), and exhibited IC50 values at two-digit micromolar concentrations. Sulfamate derivatives 1j & 1k inhibited 50% of amoebae at 30.65 μM and 27.21 μM, respectively. The tested compounds blocked amoebae binding to host cells as well as inhibited amoebae excystation. Notably, the selected derivatives exhibited minimal human cell cytotoxicity but reduced parasite-mediated host cell damage. Overall, our study showed that sulfamate derivatives 1j & 1k have anti-amoebic potential and offer a promising avenue in the development of potential anti-amoebic drug candidates.
KW - Acanthamoeba castellanii
KW - Amoebicidal
KW - Cytopathogenicity
KW - Cytotoxicity
KW - Sulfamate
KW - Sulfonate
UR - http://www.scopus.com/inward/record.url?scp=85173763880&partnerID=8YFLogxK
U2 - 10.1016/j.parint.2023.102814
DO - 10.1016/j.parint.2023.102814
M3 - Article
C2 - 37806551
SN - 1383-5769
VL - 98
JO - Parasitology International
JF - Parasitology International
M1 - 102814
ER -