2. Academic Validation
  3. Neuroprotective effects of prenylated flavanones isolated from Dalea species, in vitro and in silico studies

Neuroprotective effects of prenylated flavanones isolated from Dalea species, in vitro and in silico studies

  • Eur J Med Chem. 2020 Nov 15;206:112718. doi: 10.1016/j.ejmech.2020.112718.
María D Santi 1,  Florencia Arredondo 2,  Diego Carvalho 3,  Carolina Echeverry 3,  Giselle Prunell 3,  Mariana A Peralta 4,  José L Cabrera 5,  María G Ortega 4,  Eduardo Savio 6,  Juan A Abin-Carriquiry 7
Affiliations

Affiliations

  • 1 Instituto Multidisciplinario de Biología Vegetal (IMBIV-CONICET), Ciudad Universitaria, Córdoba, Argentina; I&D Biomédico y Químico Farmacéutico, Centro Uruguayo de Imagenología Molecular (CUDIM), Montevideo, Uruguay.
  • 2 Departamento de Neuroquímica, Instituto de Investigaciones Biológicas Clemente Estable (IIBCE), Montevideo, Uruguay; I&D Biomédico y Químico Farmacéutico, Centro Uruguayo de Imagenología Molecular (CUDIM), Montevideo, Uruguay. Electronic address: florencia.arredondo@cudim.org.
  • 3 Departamento de Neuroquímica, Instituto de Investigaciones Biológicas Clemente Estable (IIBCE), Montevideo, Uruguay.
  • 4 Farmacognosia, Departamento de Ciencias Farmacéuticas, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba, Ciudad Universitaria, Haya de La Torre y Medina Allende, Edificio Ciencias II, Córdoba, Argentina; Instituto Multidisciplinario de Biología Vegetal (IMBIV-CONICET), Ciudad Universitaria, Córdoba, Argentina.
  • 5 Instituto Multidisciplinario de Biología Vegetal (IMBIV-CONICET), Ciudad Universitaria, Córdoba, Argentina.
  • 6 I&D Biomédico y Químico Farmacéutico, Centro Uruguayo de Imagenología Molecular (CUDIM), Montevideo, Uruguay.
  • 7 Departamento de Neuroquímica, Instituto de Investigaciones Biológicas Clemente Estable (IIBCE), Montevideo, Uruguay; Laboratorio de Biofármacos, Instituto Pasteur de Montevideo, Montevideo, Uruguay. Electronic address: jaabin@iibce.edu.uy.
PMID: 32861919 DOI: 10.1016/j.ejmech.2020.112718
Abstract

Neurodegenerative diseases (NDs) represent a global problem on public health, with a growing incidence as human longevity increases. Currently, although there are palliative strategies available for most of these diseases, there is a lack of effective therapies for their cure. Flavonoids are extensively studied for their multi-target behavior. Among numerous biological activities, it has been reported that they act at the CNS level, presenting neuroprotective activity through different mechanisms of action. Dalea L. (Fabaceae) is an American genus, with about 172 species. Dalea elegans Gillies ex. Hook. & Arn and Dalea pazensis Rusby, both South American species, are the important source of natural compounds of the prenylated flavanones type. In the present study, five prenylated flavanones isolated from Dalea species were assayed for their neuroprotective activity in two in vitro models of neurodegeneration. Flavanones 1 and 2 exhibited neuroprotective effects against oxidative stress-induced death in both models, granular cerebellar neurons and (NGF)-differentiated PC12 cells. Structure-activity relationships were also reported. Our results indicated that an 8-prenyl group at the A-ring accompanied by an unsubstituted B-ring, or a 2',4'-dihydroxy-5'-dimethylallyl substitution, lead to the most potent flavanones. Furthermore, in silico studies were performed, and several putative targets in NDs were identified for compounds 1 and 2. Between them, the Enzyme acetylcholinesterase was selected for its validation in vitro. The present in vitro and in silico results imply that prenylated flavanones 1 and 2 may be useful in the development and design of future strategies for the treatment of NDs diseases.

Keywords

Dalea elegans; Dalea pazensis; Neuroprotection; Prenylated flavanones.

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