Anti-inflammatory and antinociceptive effects of tilifodiolide, isolated from Salvia tiliifolia Vahl (Lamiaceae)

作者：Martin Gonzalez Chavez Marco; Josabad Alonso Castro Angel; Ramon Zapata Morales Juan; Arana Argaez Victor; Cesar Torres Romero Julio; Elisa Medina Rivera Yessica; Sanchez Mendoza Ernesto; Perez Gutierrez Salud

来源：Drug Development Research, 2018, 79(4): 165-172.

DOI：10.1002/ddr.21432

• anti-inflammatory
• antinociceptive
• Salvia tiliifolia
• tilifodiolide

Salvia tiliifolia Vahl (Lamiaceae) is used for the empirical treatment of pain and inflammation. The diterpenoid tilifodiolide (TFD) was isolated from Salvia tiliifolia. The in vitro anti-inflammatory effects of TFD (0.1-200 mu M) were assessed using murine macrophages stimulated with LPS and estimating the levels of pro-inflammatory mediators for 48 h. The in vivo anti-inflammatory activity of TFD was assessed using the carrageenan-induced paw edema test for 6 h. The antinociceptive effects of TFD were evaluated using the formalin test and the acetic acid induced-writhing test. The effects of TFD on locomotor activity were assessed using the open field test and the rotarod test. TFD inhibited the production of TNF- (IC50=5.66 mu M) and IL-6 (IC50=1.21 mu M) in macrophages. TFD (200 mg/kg) showed anti-inflammatory effects with similar activity compared to 10 mg/kg indomethacin. The administration of TFD induced antinociception in the phase 1 (ED50=48.2 mg/kg) and the phase 2 (ED50=28.9 mg/kg) of the formalin test. In the acetic acid assay, TFD showed antinociceptive effects (ED50=32.3 mg/kg) with similar potency compared to naproxen (ED50=36.2 mg/kg). In the presence of different inhibitors in the acetic acid assay, only the co-administration of TFD and naloxone reverted the antinociceptive activity shown by TFD alone. TFD did not affect locomotor activity in mice. TFD exerts in vitro and in vivo anti-inflammatory activity and in vivo antinociceptive effects.

• 出版日期2018-6