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目的研究柯拉斯那沉香Aquilaria crassna的倍半萜类化学成分。方法采用多种柱色谱和高效液相色谱相结合的方法对化合物进行分离纯化;通过波谱数据结合理化性质分析对所得单体化合物的结构进行鉴定;分别采用Ellman比色法和p NPG法对化合物的乙酰胆碱酯酶抑制活性及α-葡萄糖苷酶抑制活性进行测试。结果从柯拉斯那沉香的乙醇提取物的醋酸乙酯萃取部分共分离得到7个倍半萜类化合物,分别鉴定为2-[(2β,8β,8aα)-8,8a-dimethyl-1,2,3,4,6,7,8,8a-octahydronaphthalen-2-yl]-3-hydroxy-2-methoxpropanoic acid(1)、2-[(2β,8α,8aα)-8,8a-dimethyl-1,2,3,4,6,7,8,8a-octahydronaphthalen-2-yl]propane-1,2-diol(2)、(1β,3α,4aβ,5β,8aα)-4a,5-dimethyl-3-(prop-1-en-2-yl)octahydronaphthalene-1,8a(1H)-diol(3)、eremophila-9-en-8β,11-diol(4)、eudesma-4-en-8,11-diol(5)、eudesma-4-en-11,15-diol(6)、methyl-15-oxo-eudesmane-4,11(13)-dien-12-oate(7)。活性测试结果表明化合物1、4和5具有乙酰胆碱酯酶抑制活性,化合物5具有α-葡萄糖苷酶抑制活性。结论化合物1为新化合物,命名为柯拉斯那酸A;化合物1~3和7为首次从沉香中分离得到。
Objective To study the chemical constituents of the sesquiterpenoids of Aquilaria crassna. Methods The compounds were isolated and purified by a combination of column chromatography and high performance liquid chromatography (HPLC). The structure of the obtained monomer compounds was identified by spectral data and physical and chemical properties analysis. The structures of the compounds were identified by Ellman colorimetry and p NPG method respectively. Acetylcholinesterase inhibitory activity and α-glucosidase inhibitory activity were tested. Results Seven sesquiterpenoids were isolated from the ethyl acetate extract of the ethanolic extract of Corus, and were identified as 2 - [(2β, 8β, 8aα) -8,8a-dimethyl-1, Octahydronaphthalen-2-yl] -3-hydroxy-2-methoxpropanoic acid (1), 2 - [(2β, 8a, 8aα) -8,8a-dimethyl- 1,2,3,4,6,7,8,8a-octahydronaphthalen-2-yl] propane-1,2-diol (2), (1β, 3α, 4aβ, 5β, 8aα) (3), eremophila-9-en-8β, 11-diol (4), eudesma-4-en-8 (propan-2-yl) octahydronaphthalene-1,8a , 11-diol (5), eudesma-4-en-11,15-diol (6), methyl-15-oxo-eudesmane-4,11 (13) -dien-12-oate (7). Activity test results show that compounds 1, 4 and 5 have acetylcholinesterase inhibitory activity, and compound 5 has α-glucosidase inhibitory activity. Conclusion Compound 1 is a new compound, named as collins acid A; Compounds 1 ~ 3 and 7 are isolated from alcumin for the first time.