Eugenol-Rich Essential Oil from Pimenta dioica: In Vitro and In Vivo Potentialities against Leishmania amazonensis

Author:

Monzote Lianet12ORCID,Machín Laura3ORCID,González Adiel1,Scull Ramón3,Gutiérrez Yamilet I.3,Satyal Prabodh4ORCID,Gille Lars5ORCID,Setzer William N.246ORCID

Affiliation:

1. Parasitology Department, Center of Research, Diagnostic and Reference, Institute of Tropical Medicine “Pedro Kouri”, Havana 17100, Cuba

2. Research Network Natural Products against Neglected Diseases (ResNetNPND), 48149 Munster, Germany

3. Department of Pharmacy, Institute of Pharmacy and Food, Havana University, Havana 13600, Cuba

4. Aromatic Plant Research Center, 230 N 1200 E, Suite 100, Lehi, UT 84043, USA

5. Institute of Pharmacology and Toxicology, Department of Biomedical Sciences, University of Veterinary Medicine, Veterinärplatz 1, A-1210 Vienna, Austria

6. Department of Chemistry, University of Alabama in Huntsville, Huntsville, AL 35899, USA

Abstract

Pimenta dioica L. is one the most recognized species with diverse biological activities. In this study, in vitro activity and in vivo efficacy of essential oil from P. dioica (EO-Pd) was evaluated. The main compound was also included in the animal studies and its in silico prediction related to biological activities, molecular ligands, drug likeness, and ADME (absorption, distribution, metabolism, and excretion) properties are listed. The chemical composition analyzed by GC-MS retrieved 45 components, which the most abundant compound was the eugenol (80.1%). The EO-Pd was able to inhibit the growth of L. amazonensis (IC50 = 9.7 ± 0.7 and 11.3 ± 2.1 µg/mL, promastigotes and amastigotes, respectively). The cytotoxicity assay showed a CC50 of 104.5 ± 0.9 µg/mL and a selectivity index of 9. In the model of cutaneous leishmaniasis in BALB/c mice, the effect of EO-Pd and eugenol was observed after treatment at 30 mg/kg by intralesional route with 5 administrations every 4 days. In the in silico predictions, some targets that justified the antileishmanial activity of eugenol and good drug like properties for this compound, were obtained. This study showed for first time the potential of EO-Pd to inhibit L. amazonensis, which could be linked to the activity of major compound eugenol.

Funder

Austrian Science Fund

Publisher

MDPI AG

Subject

Drug Discovery,Pharmaceutical Science,Molecular Medicine

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