人工打洞沉香的化学成分及生物活性研究

Chemical Constituents and Bioactivities of Aquilariae Lignum Resinatum by Artificial Holing Method

目的:研究人工打洞沉香的化学成分及其生物活性。方法:采用ODS、硅胶柱层析、Sephadex LH-20等柱色谱技术对人工打洞沉香的化学成分进行分离纯化,并根据理化性质和波谱数据对分离的化合物进行鉴定;分别采用Ellman法和PNPG法测定单体化合物的体外乙酰胆碱酯酶和α-葡萄糖苷酶抑制活性,采用DPPH法测定单体化合物的抗氧化活性。结果:从人工打洞沉香中分离得到8个化合物,分别鉴定为:5α,6β,7α,8β-四羟基-5,6,7,8-四氢-2-[2-(4-甲氧基苯)乙基]色酮(1)、8α-氯-5α,6β,7β-三羟基-5,6,7,8-四氢-2-[2-(3-羟基-4-甲氧基苯)乙基]色酮(2)、6-羟基-2-[2-(4-羟基-3-甲氧基苯)乙烯基]色酮(3)、6,7-二羟基-2-(2-苯乙基)色酮(4)、2-(2-苯乙基)色酮(5)、epi-guaidiol A(6)、2-oxo-12-hydroxy-hinesol(7)、cyclodebneyol(8)。结论:其中,化合物6~8为首次从沉香属植物中分到,化合物1、2为首次从该植物中分离得到。化合物1、2和7对乙酰胆碱酯酶具有一定的抑制活性,化合物3具有一定的体外α-葡萄糖苷酶抑制活性,化合物2、3和7具有一定的抗氧化活性。

Objective： To study the chemical constituens and biological activities of artificial holing Aquilariae Lignum Resinatum. Methods：The compounds were isolated by ODS, silica gel and Sephadex LH-20 column chromatographies from Aquilariae Lignum Resinatum induced by artificial holing, then structurally identified by spectroscopic analysis. The compounds were tested for their AChE and α-glucosidase inhibitory activities by Ellman and PNPG methods respectively, the antioxidant activity were determined by DPPH method. Results：Eight compounds were isolated from Aquilariae Lignum Resinatum and identified as 5α, 6β, 7α, 8β-tetra- hydroxy-5,6,7,8-tetrahydro-2- [ 2- （4-methoxyphenyl） ethyl ] chromone （ 1 ）, 8α-chloro-5α, 6β, 7β-trihydroxy-5,6,7,8-tetrahydro-2- [ 2- （3-hydroxy-4-methoxyphenyl） ethyl ] chromone （ 2 ）, 6-hydroxy-2-[ 2-（ 4-hydroxy-3-methoxyphenyl ） ethylene ] chromone （ 3 ）, 6, 7-di- hydroxy-2- （2-phenylethyl） chromone （4）, 2- （ 2-phenylethyl ） chromone （ 5 ）, epi-guaidiol A （ 6）, 2-oxo- 12-hydroxy-hinesol （ 7 ） and cyclo- debneyol （8）. Conclusion ： Compounds 6 - 8 are obtained from the Aquilaria genus for the first time, compounds 1 and 2 are isolated from Aquilaria sinensis for the first time： Compounds 1,2 and 7 exhibited moderate inhibitory activity against acetyl cholinesterase, compound 3 showed positive α-glucosidase inhibitory activity;compounds 2,3 and 7 showed antioxidant activity.