Biomedicine & Pharmacotherapy (Nov 2021)

Intravitreal lupeol: A new potential therapeutic strategy for noninfectious uveitis

  • Cibele Rodrigues Toledo,
  • Mayara Rodrigues Brandão Paiva,
  • Brenda Fernanda Moreira Castro,
  • Vinicius Viana Pereira,
  • Sarah Pereira de Freitas Cenachi,
  • Daniel Vítor Vasconcelos-Santos,
  • Sílvia Ligório Fialho,
  • Armando Silva-Cunha

Journal volume & issue
Vol. 143
p. 112145

Abstract

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Lupeol is a pentacyclic triterpene with known anti-inflammatory effects. However, its role in the treatment of noninfectious uveitis has not been explored. This work investigated anti-inflammatory activity of lupeol in ocular tissues with in vitro and in vivo models. First, we evaluated the effect of lupeol (100 µM) on inflammatory response induced by lipopolysaccharide (LPS) in retinal pigment epithelium cells (ARPE-19) by measuring levels of released interleukins (IL-6 and IL-8). Then, we investigated the anti-inflammatory action of intravitreal lupeol in a rodent model of panuveitis induced by Mycobacterium bovis Calmette-Guérin Bacillus (BCG). Rats were submitted to electroretinography and clinical analyses on days 3, 7, and 15 after uveitis induction. In addition, histopathological analysis, and indirect quantification of myeloperoxidase (MPO) and N-acetylglucosaminidase (NAG) in the posterior segment were performed. Treatment with lupeol (100 µM) significantly decreased IL-6 and IL-8 levels in comparison to untreated LPS-activated ARPE-19 cells. This reduction was similar to that detected in ARPE-19 cells treated with dexamethasone. The results of the in vivo assay demonstrated that intravitreal lupeol is able to modulate inflammation in the anterior and posterior segment of the rat eyes, indicating that it should be further investigated as a novel potential candidate for management of uveitis.

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