柯拉斯那沉香的化学成分研究

Chemical constituents from the agarwood of Aquilaria crassna

对柬埔寨野生柯拉斯那(Aquilaria crassna)沉香的化学成分和生物活性进行研究。实验采用多种柱色谱法对该沉香进行分离纯化;通过现代波普技术结合化合物理化性质对所得单体化合物进行结构鉴定,从柬埔寨野生柯拉斯那沉香共分离出12个化合物,分别鉴定为7α-H-9(10)-ene-11,12-epoxy-8-oxoeremophilane(1)、7β-H-9(10)-ene-11,12-epoxy-8-oxoeremophilane(2)、neopetasane(eremophila-9,11-dien-8-one)(3)、jinkoh-eremol(4)、(rel)-4β,5β,7β-eremophil-9-en-12,8β-olide(5)、诺卡酮(6)、11-hydroxy-valenc-1(10)-en-2-one(7)、(7 S,9 S,10 S)-(+)-9-hydroxy-selina-4,11-dien-14-al(8)、5-羟基-2-[2-(4-甲氧基苯)乙烯基]色酮(9)、5-羟基-6甲氧基-2-(2-苯乙基)色酮(10)、6-甲氧基-2-(2-苯乙基)色酮(11)、5-羟基-6甲氧基-2-[2-(4-甲氧基苯)乙基]色酮(12)。其中化合物1~8为倍半萜类化合物,化合物9为2-(2-苯乙烯基)色酮类化合物,化合物10~12为2-(2-苯乙基)色酮类化合物。且化合物2~11均是首次从柯拉斯那沉香分离。采用Ellman比色法对单体化合物进行乙酰胆碱酯酶抑制活性的测定,活性测定结果表明化合物1~3和12具有乙酰胆碱酯酶抑制活性。

To study the chemical constituents and biological activity of wild agarwood from Aquilaria crassna.Various column chromatographic techniques were used for isolation and purification from the agarwood of A.crassna,and the structures of the compounds were identified on the basis of spectroscopic data and physicochemical properties analysis.Twelve compounds were isolated from the ethanol extract of wild agarwood originating from A.crassna in Cambodia,and the structures were identified as 7α-H-9(10)-ene-11,12-epoxy-8-oxoeremophilane(1),7β-H-9(10)-ene-11,12-epoxy-8-oxoeremophilane(2),neopetasane(eremophila-9,11-dien-8-one)(3),jinkoh-eremol(4),(rel)-4β,5β,7β-eremophil-9-en-12,8β-olide(5),nootkatone(6),11-hydroxy-valenc-1(10)-en-2-one(7),(7 S,9 S,10 S)-(+)-9-hydroxy-selina-4,11-dien-14-al(8),5-hydroxy-2-[2-(4-methoxyphenyl)ethenyl]chromone(9),5-hydroxy-6methoxy-2-(2-phenylethyl)chromone(10),6-methoxy-2-(2-phenylethyl)chromone(11),5-hydroxy-6-methoxy-2-[2-(4-methoxyphenyl)ethyl)chromone(12).Among them,compounds 1-8 are sesquiterpenoids,compound 9 is 2-[2-phenylethenyl]chromone,and compounds 10-12 are 2-(2-phenylethyl)chromone compounds.Compounds 2~11 were isolated from agarwood of A.crassna for the first time.The acetylcholinesterase inhibitory activities of compounds were evaluated by Ellman colorimetric method.Among them,compounds 1~3 and 12 showed acetylcholinesterase inhibitory activities.