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Cyanoacrylamide derivatives as a novel amoebicidal agents against Acanthamoeba spp

Rubén L Rodríguez-Expósito1, Samuel Delgado-Hernández2, Ines Sifaoui1

  • 1Instituto Universitario de Enfermedades Tropicales y Salud Pública de Canarias, Universidad de La Laguna, Avda. Astrofísico Fco. Sánchez, S/N, 38203 La Laguna, Tenerife, Islas Canarias, Spain; Departamento de Obstetricia y Ginecología, Pediatría, Medicina Preventiva y Salud Pública, Toxicología, Medicina Legal y Forense y Parasitología, Universidad de La Laguna, Tenerife, Islas Canarias, Spain; CIBER de Enfermedades Infecciosas (CIBERINFEC), Instituto de Salud Carlos III, Madrid 28029, Spain.

Biomedicine & Pharmacotherapy = Biomedecine & Pharmacotherapie
|May 18, 2026
PubMed

Insights

Novel cyanoacrylamide derivatives show promise as amoebicidal agents against Acanthamoeba, a cause of severe human infections like keratitis. Compounds QOET-112 and 114 exhibit potent activity and low cytotoxicity, warranting further investigation.

Area of Science:

  • Microbiology
  • Parasitology
  • Drug Discovery

Background:

  • Acanthamoeba spp. cause severe human infections, including granulomatous amoebic encephalitis (GAE) and Acanthamoeba keratitis (AK).
  • Current treatments for Acanthamoeba infections are limited and often ineffective, necessitating the development of new therapeutic strategies.
  • The urgent need for novel amoebicidal agents is driven by the severity and prevalence of these protozoan infections.

Purpose of the Study:

  • To evaluate the in vitro amoebicidal activity of eight cyanoacrylamide derivatives (QOET) against Acanthamoeba.
  • To identify specific compounds with potent activity against both trophozoite and cyst stages of Acanthamoeba.
  • To investigate the mechanism of action and cytotoxicity of promising cyanoacrylamide derivatives.

Main Methods:

  • In vitro screening of eight cyanoacrylamide derivatives against three Acanthamoeba strains (A. castellanii, A. griffini, A. polyphaga).
  • Determination of IC50 values for trophozoite and cyst stages.
  • Cytotoxicity assessment using the murine macrophage cell line J774A.1.
  • Analysis of the mode of action, including programmed cell death (PCD), autophagy, and cytoskeletal alterations (actin and tubulin networks).

Main Results:

  • Two compounds, QOET-112 and QOET-114, exhibited the lowest IC50 values against both trophozoite and cyst stages of Acanthamoeba.
  • These effective compounds demonstrated low cytotoxicity against the J774A.1 macrophage cell line.
  • Mechanism of action studies revealed that QOET-112 and QOET-114 induce programmed cell death (PCD) and autophagy in A. griffini trophozoites.
  • Significant cytoskeletal disorganization, including actin and tubulin network disruption, was observed.

Conclusions:

  • Cyanoacrylamide derivatives, particularly QOET-112 and QOET-114, possess significant in vitro amoebicidal activity against Acanthamoeba.
  • These compounds represent potential candidates for developing new treatments against Acanthamoeba infections due to their efficacy and low cytotoxicity.
  • The observed induction of PCD, autophagy, and cytoskeletal disruption provides insights into the anti-Acanthamoeba mechanism of these novel agents.
Keywords:
5-iminopyrrol-2-onesAcanthamoebaAutophagyCyanoacrylamidesCytoskeletonProgrammed cell death

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