丹参中三萜酸的分离及其抗炎活性的研究

The Isolation of Triterpenoid Acids from Radix Salviae Miltiorrhizae and Their Anti-Inflammatory Activities Evaluation

目的:对丹参中三萜酸化学成分分离和鉴定及其抗炎活性进行研究。方法:采用减压硅胶柱和凝胶sephadex LH-20柱层析法和中压制备和半制备液相法进行丹参中三萜酸化学成分分离,利用1H-NMR和13C-NMR对分离化合物进行结构鉴定;运用LPS刺激RAW264.7细胞体外抗炎模型对分离化合物进行抗炎活性研究。结果:从丹参中分离得到7个三萜酸,分别鉴定为:(1)2α,3α-dihydroxyolean-12-en-28-oic acid;(2)Maslinicacid;(3) Psiguanin A;(4) 2α,3α-dihydroxyurs-12-en-28-oic acid;(5) 2α-hydroxy ursolic acid;(6) 2α,3α-dihydroxyursa-12,20 (30)-dien-28-oic acid;(7)2α,3α,23-trihydroxyurs-12,20 (30)-dien-28-oic acid 7个化合物都具有较好的抗炎活性,他们的IC50分别是35.6,36.6,40.1,37.8,34.8,32.8,32.1μM,且化合物在高剂量的情况下都能很好的抑制TNF-α和IL-6炎症因子的释放。结论:化合物1、3、6、7都属于该植物首次分离得到,且七个化合物具有一定的抗炎活性。

Objective: To isolate triterpenoid acids from Radix Salviae Miltiorrhizae and evaluate their anti-inflammatory activity. Methods: The reduced-pressure chromatography, sephadex LH-20 chromatography, MPLC, and semi-preparative HPLC were employed to isolate triterpenoids from Radix Salviae Miltiorrhizae, whose chemical structures were identified by1 H-NMR and13 C-NMR. The anti-inflammatory activities were investigated in LPS-stimulated RAW264.7 cells.Results: A total of 7 triterpenoid acids were isolated and identified from Radix Salviae Miltiorrhizae, which were listed as:1) 2α,3α-dihydroxyolean-12-en-28-oic acid, 2) Maslinic acid, 3) Psiguanin A, 4) 2α,3α-dihydroxyurs-12-en-28-oic acid, 5) 2α-hydroxy ursolic acid, 6) 2α,3α-dihydroxyursa-12, 20(30)-dien-28-oic acid, 7) and 2α,3α,23-trihydroxyurs-12,20(30)-dien-28-oic acid. They displayed significant anti-inflammatory activities, whose IC50 were calculated as 35.6, 36.6, 40.1, 37.8, 34.8, 32.8, and 32.1 μM respectively. Using ELISA, we founded that those compounds with high concentration significantly inhibited TNF-α and IL-6 release in LPS-induced RAW264.7 cells.Conclusion: A total of 4 triterpenoid acids such as 1, 3, 6, and 7 are obtained from Radix Salviae Miltiorrhizae for the first time, which exhibit anti-inflammatory activities to a certain degree.