PURPOSE: To investigate the in vitro antiplatelet and anti-inflammatory effects of five alkyl hydroxytyrosol (HT) ether derivatives in human whole blood and compare these effects with those of HT. METHODS: Blood samples from healthy volunteers were incubated with HT and HT alkyl ether derivatives (ethyl, butyl, hexyl, octyl and dodecyl). Maximum intensity of platelet aggregation was induced with collagen, arachidonic acid or ADP. Calcium-induced thromboxane B(2) and nitric oxide production, LPS-induced prostaglandin E(2) and nitric oxide production and LPS-induced interleukin 1β production were measured. RESULTS: All compounds inhibited platelet aggregation, thromboxane B(2) and inflammatory mediators in a concentration-dependent manner. The concentrations of each compound that inhibited the corresponding variable by 50 % compared to control samples (IC(50)) were in the range of 10(-7)-10(-6) M for HT hexyl ether; for the other compounds, these values were in the range of 10(-5) M. The IC(50) for thromboxane B(2) production was in the range of 10(-4) M. The effects of HT alkyl ether derivatives were greater than those of HT. These compounds increased nitric oxide production. There was no direct relationship between the effects of these compounds and alkyl chain length. Maximum effects were observed in the C4-C6 range. CONCLUSIONS: Alkyl ether derivatives of HT exert antiplatelet and anti-inflammatory effects that are greater than those of HT.
PURPOSE: To investigate the in vitro antiplatelet and anti-inflammatory effects of five alkyl hydroxytyrosol (HT) ether derivatives in human whole blood and compare these effects with those of HT. METHODS: Blood samples from healthy volunteers were incubated with HT and HT alkyl ether derivatives (ethyl, butyl, hexyl, octyl and dodecyl). Maximum intensity of platelet aggregation was induced with collagen, arachidonic acid or ADP. Calcium-induced thromboxane B(2) and nitric oxide production, LPS-induced prostaglandin E(2) and nitric oxide production and LPS-induced interleukin 1β production were measured. RESULTS: All compounds inhibited platelet aggregation, thromboxane B(2) and inflammatory mediators in a concentration-dependent manner. The concentrations of each compound that inhibited the corresponding variable by 50 % compared to control samples (IC(50)) were in the range of 10(-7)-10(-6) M for HT hexyl ether; for the other compounds, these values were in the range of 10(-5) M. The IC(50) for thromboxane B(2) production was in the range of 10(-4) M. The effects of HT alkyl ether derivatives were greater than those of HT. These compounds increased nitric oxide production. There was no direct relationship between the effects of these compounds and alkyl chain length. Maximum effects were observed in the C4-C6 range. CONCLUSIONS:Alkyl ether derivatives of HT exert antiplatelet and anti-inflammatory effects that are greater than those of HT.
Authors: J E Freedman; C Parker; L Li; J A Perlman; B Frei; V Ivanov; L R Deak; M D Iafrati; J D Folts Journal: Circulation Date: 2001-06-12 Impact factor: 29.690
Authors: J A González-Correa; J Muñoz-Marín; M M Arrebola; A Guerrero; F Narbona; J A López-Villodres; J P De La Cruz Journal: Lipids Date: 2007-08-07 Impact factor: 1.646
Authors: André Luiz Lourenço; Max Seidy Saito; Luís Eduardo Gomes Dorneles; Gil Mendes Viana; Plínio Cunha Sathler; Lúcia Cruz de Sequeira Aguiar; Marcelo de Pádula; Thaisa Francielle Souza Domingos; Aline Guerra Manssour Fraga; Carlos Rangel Rodrigues; Valeria Pereira de Sousa; Helena Carla Castro; Lucio Mendes Cabral Journal: Molecules Date: 2015-04-20 Impact factor: 4.411