Institute of Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine, 10 Poyang lake Road, Jinghai District, Tianjin 301617, China.
Tianjin Key Laboratory of Chinese medicine Pharmacology, 10 Poyang lake Road, Jinghai District, Tianjin 301617, China.
Molecules. 2019 Mar 26;24(6):1187. doi: 10.3390/molecules24061187.
The purpose of this research was to extract and separate the compounds from frankincense, and then evaluate their anti-inflammatory effects. The isolated compound was a representative tetracyclic triterpenes of glycine structure according to ¹H-NMR and C-NMR spectra, which is β-elemonic acid (β-EA). We determined the content of six different localities of frankincense; the average content of β-EA was 41.96 mg/g. The toxic effects of β-EA administration (400, 200, 100 mg/kg) for four weeks in Kunming (KM) mice were observed. Compared with the control group, the body weight of mice, the visceral coefficients and serum indicators in the β-EA groups showed no systematic variations. The anti-inflammatory effects of β-EA were evaluated in LPS-induced RAW264.7 cells, xylene-induced induced ear inflammation in mice, carrageenin-induced paw edema in mice, and cotton pellet induced granuloma formation in rats. β-EA inhibited overproduction of tumor necrosis factor-α(TNF-α), interleukin-6 (IL-6), monocyte chemotactic protein 1 (MCP-1), soluble TNF receptor 1 (sTNF R1), Eotaxin-2, Interleukin 10 (IL-10) and granulocyte colony-stimulating factor (GCSF) in the RAW264.7 cells. Intragastric administration with β-EA (300, 200, and 100 mg/kg in mice, and 210, 140, and 70 mg/kg in rats) all produced distinct anti-inflammatory effects in vivo in a dose-dependent manner. Following treatment with β-EA (300 mg/kg, i.g.), the NO level in mice ears and PGE2 in mice paws both decreased ( 0.01). In conclusion, our study indicates that β-EA could be a potential anti-inflammatory agent for the treatment of inflammatory diseases.
本研究旨在从乳香中提取和分离化合物,并评估其抗炎作用。根据 1H-NMR 和 C-NMR 图谱,分离得到的化合物是一种具有甘氨酸结构的四环三萜代表化合物,即 β-乳香酸(β-EA)。我们测定了 6 个不同产地乳香中 β-EA 的含量;β-EA 的平均含量为 41.96mg/g。观察了β-EA(400、200、100mg/kg)给药 4 周对昆明(KM)小鼠的毒副作用。与对照组相比,β-EA 组小鼠的体重、脏器系数和血清指标均无系统变化。在 LPS 诱导的 RAW264.7 细胞、二甲苯诱导的小鼠耳炎、角叉菜胶诱导的小鼠足肿胀和棉球诱导的大鼠肉芽肿形成中评价了β-EA 的抗炎作用。β-EA 抑制了 RAW264.7 细胞中肿瘤坏死因子-α(TNF-α)、白细胞介素-6(IL-6)、单核细胞趋化蛋白 1(MCP-1)、可溶性 TNF 受体 1(sTNF R1)、嗜酸性粒细胞趋化因子-2、白细胞介素 10(IL-10)和粒细胞集落刺激因子(GCSF)的过度产生。β-EA(小鼠灌胃 300、200 和 100mg/kg,大鼠灌胃 210、140 和 70mg/kg)在体内均表现出明显的抗炎作用,呈剂量依赖性。β-EA(300mg/kg,ig)治疗后,小鼠耳部的 NO 水平和小鼠足部的 PGE2 均降低(P<0.01)。综上所述,本研究表明β-EA 可能是治疗炎症性疾病的一种有潜力的抗炎药物。