Franciane Martins Marques1, Mariana Moreira Figueira1, Elisângela Flávia Pimentel Schmitt1, Tamara P Kondratyuk2, Denise Coutinho Endringer1, Rodrigo Scherer1, Marcio Fronza3. 1. Programa de Pós-Graduação em Ciências Farmacêuticas, Laboratório de Produtos Naturais, Department of Pharmacy, Universidade Vila Velha-UVV, Av. Comissário José Dantas de Melo,no. 21, Boa Vista, Vila Velha, Espírito Santo, 29102-920, Brazil. 2. Department of Pharmaceutical Sciences, Daniel K. Inouye College of Pharmacy, University of Hawaii at Hilo, Hilo, HI, 96720, USA. 3. Programa de Pós-Graduação em Ciências Farmacêuticas, Laboratório de Produtos Naturais, Department of Pharmacy, Universidade Vila Velha-UVV, Av. Comissário José Dantas de Melo,no. 21, Boa Vista, Vila Velha, Espírito Santo, 29102-920, Brazil. marcio.fronza@uvv.br.
Abstract
BACKGROUND AND AIMS: Terpenes are considered the main components of essential oils and an important source for the identification of novel lead molecules. This study aimed to investigate the in vitro anti-inflammatory activity of L-carveol, L-carvone, and m-cimene (monoterpenes) and of valencene and guaiene (sesquiterpenes). METHODS: The influence on intracellular nitric oxide (NO) and pro- and anti-inflammatory cytokine (TNF-α, IL-1α and IL-10) production and on nuclear factor kappa B (NF-κB) activity was determined using Griess reagent, immunoenzymatic assay kits (ELISA) and chemiluminescence measurements in cell-based assays, respectively. Antioxidant activity was assayed through the protective effect against cellular oxidative damage produced by superoxide anion production (O 2 ·- ) and hydrogen peroxide on macrophages and by the quenching activity of the NO radical. RESULTS AND DISCUSSION: Terpenes reduced the pro-inflammatory cytokines TNF-α and IL-1α and increased the production of IL-10. In addition, the terpenes, especially guaiene (53.3 ± 2.4%) and m-cymene (38.1 ± 0.6%), significantly inhibited NO production in a macrophage cell culture-based assay, whereas no effect was observed in the scavenging activity of this radical. L-carveol and m-cymene significantly inhibited O 2 ·- production with reductions of approximately 68.6 ± 2.2% and 48.2 ± 4.2%, respectively, at a concentration of 10 μM. Moreover, these terpenes were verified to suppress NF-κB activity. The results indicate that these terpenes have therapeutic potential and may be used to suppress inflammatory diseases or as a leading compounds.
BACKGROUND AND AIMS: Terpenes are considered the main components of essential oils and an important source for the identification of novel lead molecules. This study aimed to investigate the in vitro anti-inflammatory activity of L-carveol, L-carvone, and m-cimene (monoterpenes) and of valencene and guaiene (sesquiterpenes). METHODS: The influence on intracellular nitric oxide (NO) and pro- and anti-inflammatory cytokine (TNF-α, IL-1α and IL-10) production and on nuclear factor kappa B (NF-κB) activity was determined using Griess reagent, immunoenzymatic assay kits (ELISA) and chemiluminescence measurements in cell-based assays, respectively. Antioxidant activity was assayed through the protective effect against cellular oxidative damage produced by superoxide anion production (O 2 ·- ) and hydrogen peroxide on macrophages and by the quenching activity of the NO radical. RESULTS AND DISCUSSION: Terpenes reduced the pro-inflammatory cytokines TNF-α and IL-1α and increased the production of IL-10. In addition, the terpenes, especially guaiene (53.3 ± 2.4%) and m-cymene (38.1 ± 0.6%), significantly inhibited NO production in a macrophage cell culture-based assay, whereas no effect was observed in the scavenging activity of this radical. L-carveol and m-cymene significantly inhibited O 2 ·- production with reductions of approximately 68.6 ± 2.2% and 48.2 ± 4.2%, respectively, at a concentration of 10 μM. Moreover, these terpenes were verified to suppress NF-κB activity. The results indicate that these terpenes have therapeutic potential and may be used to suppress inflammatory diseases or as a leading compounds.
Entities:
Keywords:
Inflammation; Lead compounds; NF-κB; Nitric oxide; Superoxide anion; Terpenes
Authors: Rogério Marchete; Sarah Oliveira; Leonardo Bagne; Jennyffer Ione de Souza Silva; Ana Paula Valverde; Andrea Aparecida de Aro; Mariana Moreira Figueira; Marcio Fronza; Thainá Mikaela Bressam; Vivian Fernandes Furletti de Goes; Fernanda Oliveira de Gaspari de Gaspi; Gláucia Maria Tech Dos Santos; Thiago Antônio Moretti Andrade Journal: Inflammopharmacology Date: 2021-09-21 Impact factor: 4.473
Authors: Renata Evaristo Rodrigues da Silva; Andressa de Alencar Silva; Luís Pereira-de-Morais; Nayane de Sousa Almeida; Marcello Iriti; Marta Regina Kerntopf; Irwin Rose Alencar de Menezes; Henrique Douglas Melo Coutinho; Roseli Barbosa Journal: Molecules Date: 2020-06-09 Impact factor: 4.411