Apigenin is a promising molecule for treatment of visceral leishmaniasis

Front Cell Infect Microbiol. 2023 Apr 5:13:1066407. doi: 10.3389/fcimb.2023.1066407. eCollection 2023.

Abstract

Current treatment for visceral leishmaniasis is based on drugs such as pentavalent antimony and amphotericin B. However, this treatment remains mostly ineffective and expensive, resulting in several side effects and generating resistance. Apigenin, a flavonoid present in fruits and vegetables, has demonstrated several biological functions. In the present study, we observed a concentration-dependent inhibition of the L. infantum promastigote in the presence of apigenin, exhibiting an IC50 value of 29.9 µM. Its effect was also evaluated in L. infantum-infected murine peritoneal macrophages, presenting an C50 value against intracellular amastigotes of 2.3 µM and a selectivity index of 34.3. In a murine model of visceral leishmaniasis, the in vivo effect of apigenin was measured using short-term and long-term treatment schemes. Treatment with apigenin demonstrated 99.7% and 94% reductions in the liver parasite load in the short-term and long-term treatment schemes, respectively. Furthermore, no alterations in serological and hematological parameters were observed. Taken together, these results suggest that apigenin is a potential candidate for visceral leishmaniasis chemotherapy by oral administration.

Keywords: flavonoid; in vitro; in vivo; leishmaniasis chemotherapy; long-term; natural products; oral treatment; short-term.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amphotericin B / pharmacology
  • Animals
  • Antiprotozoal Agents* / pharmacology
  • Antiprotozoal Agents* / therapeutic use
  • Apigenin / pharmacology
  • Apigenin / therapeutic use
  • Leishmania infantum*
  • Leishmaniasis, Visceral* / drug therapy
  • Leishmaniasis, Visceral* / parasitology
  • Mice
  • Mice, Inbred BALB C

Substances

  • Apigenin
  • Amphotericin B
  • Antiprotozoal Agents

Grants and funding

This work was supported by Fundação Carlos Chagas Filho de Amparo a Pesquisa do Estado do Rio de Janeiro (FAPERJ), Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq), Instituto Oswaldo Cruz (IOC), Coordenação de Aperfeiçoamento de Pessoal da Nivel Superior (CAPES) and Fundação Oswaldo Cruz (FIOCRUZ). YSSE received a scholarship from CAPES, and EEA-A is the recipient of a research scholarship from Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq). The funders had no role in the study design, data collection, analysis, decision to publish, or preparation of the manuscript.