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.

中文翻译：

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从丹参丹参中分离出来的噻菌灵的抗炎和镇痛作用。

Salvia tiliifolia Vahl（唇形科）用于疼痛和炎症的经验治疗。从丹参丹参中分离出二萜类替利福二醇（TFD）。使用LPS刺激的鼠巨噬细胞评估TFD（0.1–200 µM）的体外抗炎作用，并评估48 h的促炎介质水平。使用角叉菜胶诱导的爪水肿试验评估TFD的体内抗炎活性6小时。使用福尔马林试验和乙酸诱导扭体试验评估了TFD的抗伤害感受作用。使用开放式田间试验和旋转脚架试验评估TFD对运动能力的影响。TFD抑制TNF-α（IC ₅₀  = 5.66 µM）和IL-6（IC ₅₀ = 1.21 µM）。与10 mg / kg消炎痛相比，TFD（200 mg / kg）具有抗炎作用，且活性相似。 在福尔马林测试的第1阶段（ED ₅₀  = 48.2 mg / kg）和第2阶段（ED ₅₀ = 28.9 mg / kg）施用TFD诱导的抗伤害感受。与乙酸 萘普生（ED ₅₀  = 36.2 mg / kg）相比，在乙酸测定中，TFD表现出相似的镇痛作用（ED ₅₀ = 32.3 mg / kg）。在乙酸测定中存在不同抑制剂的情况下，只有TFD和纳洛酮的共同给药才能还原TFD单独显示的抗伤害感受活性。TFD不影响小鼠的自发活动。TFD发挥体外和体内的抗炎活性以及体内的抗伤害感受作用。