title: Pharmacological mechanism underlying the antinociceptive activity of vanillic acid.
abstract: Vanillic acid is found at high concentrations in many plants used in traditional medicine. It has been associated with a variety of pharmacologic activities such as carcinogenesis inhibition, apoptosis and inflammation; however, it has become most popular for its pleasant creamy odor. Since there are few reports concerning the antinociceptive activity of this phenolic compound, the aim of this work was to study this activity in in vivo animal models. Vanillic acid was administered by the intraperitoneal route producing a dose-dependent inhibition of the acetic acid-induced writhing response (ED50: 9.3mg/kg). The antinociceptive activity was inhibited by the pretreatment with ondansetron and yohimbine, indicating that the serotoninergic and adrenergic systems could participate in the mechanism underlying the analgesic activity of vanillic acid. This compound was also demonstrated to interact with ASICs (Acid-sensing Ion Channels) as well as with TPRV1, TRPA1, and TRPM8 receptors in vivo. Furthermore, vanillic acid did not interfere with the locomotor function or motor coordination. The plasmatic phenolic content, analyzed by HPLC, showed that its t1/2and AUC were 0.123h and 1.38μg·h/mL; respectively. In conclusion, vanillic acid might represent a potential therapeutic option for the treatment of pain.
authors.affiliation: Cátedra de Farmacología, Facultad de Farmacia y Bioquímica - Universidad de Buenos Aires, Junín 956, C1113AAD Buenos Aires, Argentina.
authors.forename: María de Los Angeles
authors.initials: ML
authors.lastname: Yrbas
authors.affiliation: Cátedra de Farmacología, Facultad de Farmacia y Bioquímica - Universidad de Buenos Aires, Junín 956, C1113AAD Buenos Aires, Argentina.
authors.forename: Florencia
authors.initials: F
authors.lastname: Morucci
authors.affiliation: Cátedra de Farmacognosia - IQUIMEFA - CONICET, Facultad de Farmacia y Bioquímica - Universidad de Buenos Aires, Junín 956, C1113AAD Buenos Aires, Argentina.
authors.forename: Rosario
authors.initials: R
authors.lastname: Alonso
authors.affiliation: Cátedra de Farmacología, Facultad de Farmacia y Bioquímica - Universidad de Buenos Aires, Junín 956, C1113AAD Buenos Aires, Argentina. Electronic address: sgorza@ffyb.uba.ar.
authors.forename: Susana
authors.initials: S
authors.lastname: Gorzalczany
keywords: Antinociceptive activity; Pharmacokinetic profile; Vanillic acid; Vascular permeability