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

作　　者：向盼[1,2,3] 曾艳波 梅文莉[1,2] 董文化 李薇[1,2] 周丽曼 戴好富[1,2] XIANG Pan;ZENG Yan-bo;MEI Wen-li;DONG Wen-hua;LI Wei;ZHOU Li-man;DAI Hao-fu(Key Laboratory of Biology and Genetic Resources of Tropical Crops, Ministry of Agriculture, Institute of Tropical Bioscienee and Biotechnology,Chinese Academy of Tropical Agricultural Sciences, Haikou 571101, China;Hainan Engineering Research Center of Agarwood, Haikou 571101, China;College of Pharmacy and Chemistry, Dali University, Dali 671003, China)

机构地区：[1]中国热带农业科学院热带生物技术研究所/农业部热带作物生物学与遗传资源利用重点实验室,海南海口571101 [2]海南省沉香工程技术研究中心,海南海口571101 [3]大理大学药学与化学学院,云南大理671003

出　　处：《中药材》2017年第10期2339-2343,共5页Journal of Chinese Medicinal Materials

基　　金：海南省重大科技计划项目(ZDKJ2016004-03);海南省科协青年科技人才学术创新计划项目(HAST201628);海南省自然科学基金(20168367)

摘　　要：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.

关 键 词：沉香 化学成分 2-(2-苯乙基)色酮 倍半萜 生物活性 

分 类 号：R284.1[医药卫生—中药学]