广东紫珠中的萜类化合物及其抗炎活性

对岭南药材广东紫珠(Callicarpa kwangtungensis)地上部分进行化学成分研究,得到11个萜类化合物,分别鉴定为sambucunlin A(1)、2α-羟基羽扇豆醇(2)、swinhoeic acid(3)、3β-羟基-乌苏烷-11-烯-13β,28-内酯(4)、蔷薇酸(5)、2α,3β,6β,18β,23-pentahydroxy-olean-12-en-28-oic acid(6)、rel-5-(3 S,8 S-dihydroxy-1 R,5 S-dimethyl-7-oxa-6-oxobicyclo-oct-8-yl)-3-methyl-2 Z,4 E-pentadienoic acid(7)、salvionoside B(8)、齐墩果酸(9)、白桦脂酸(10)和α-香树脂醇(11)。其中,化合物1~4和6~8为首次从该属植物中分离得到。在化学成分分离基础上,进一步选择脂多糖(LPS)诱导的RAW 264.7小鼠巨噬细胞炎症模型进行萜类化合物抗炎活性测试。结果表明:化合物3和9具有显著的抗炎活性,对比结构发现,三萜类化合物(3~6、9和11)抗炎活性优于倍半萜类化合物(7和8)。研究结果广东紫珠萜类成分在抗炎方面的临床应用提供了实验依据。

Terpenoids from Callicarpa kwangtungensis and their anti-inflammatory activity

Eleven terpenoids were isolated and purified from the ethanol extract of Callicarpa kwangtungensis of Lingnan Herbs.Based on spectral analysis and the comparition of literatures,these compounds were identified as sambucunlin A(1),2α-hydroxy-lupeol(2),swinhoeic acid(3),3β-hydroxy-urs-11-en-13β,28-olide(4),euscaphic acid(5),2α,3β,6β,18β,23-pentahydroxy-olean-12-en-28-oic acid(6),rel-5-(3 S,8 S-dihydroxy-1 R,5 S-dimethyl-7-oxa-6-oxobicyclo-oct-8-yl)-3-methyl-2 Z,4 E-pentadienoic acid(7)and salvionoside B(8),oleanolic acid(9),betulinic acid(10),α-amyrin(11),respectively.Compounds 1-4,6-8 was firstly isolated from the genus of Callicarpa.Further the lipopolysaccharide(LPS)-induced RAW 264.7 mouse macrophages was explored as inflammatory model to measure the anti-inflammatory activity of the terpenoids.The experimental results revealed that compounds 3 and 9 had obvious anti-inflammatory activity.It was found that the anti-inflammatory activity of triterpenoids(3-6,9 and 11)was better than that of sesquiterpenoids(7 and 8).This study provided the experimental basis for the clinical application of C.kwangtungensis in anti-inflammatory fields.