1. Anti-inflammatory and antinociceptive effects of tilifodiolide, isolated fromSalvia tiliifoliaVahl (Lamiaceae)
- Author
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Julio César Torres-Romero, Ernesto Sánchez-Mendoza, Victor Arana-Argáez, Yessica Elisa Medina-Rivera, Marco Martín González-Chávez, Salud Pérez-Gutiérrez, Juan Ramón Zapata-Morales, and Angel Josabad Alonso-Castro
- Subjects
Male ,0301 basic medicine ,Naproxen ,medicine.drug_class ,Indomethacin ,Anti-Inflammatory Agents ,Motor Activity ,Pharmacology ,Anti-inflammatory ,Open field ,Mice ,03 medical and health sciences ,0302 clinical medicine ,In vivo ,Drug Discovery ,medicine ,Animals ,Potency ,Salvia ,IC50 ,ED50 ,Pain Measurement ,Analgesics ,Dose-Response Relationship, Drug ,Interleukin-6 ,Naloxone ,Tumor Necrosis Factor-alpha ,Chemistry ,Macrophages ,In vitro ,030104 developmental biology ,Rotarod Performance Test ,Diterpenes ,030217 neurology & neurosurgery ,medicine.drug - Abstract
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 µM) 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-α (IC50 = 5.66 µM) and IL-6 (IC50 = 1.21 µM) 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.
- Published
- 2018