丝沉香中2个α-葡萄糖苷酶抑制活性的2-(2-苯乙基)色酮二聚体

Two 2-(2-phenylethyl)chromone dimers withα-glucosidase inhibitory activity from agarwood of Aquilaria filaria

目的研究菲律宾产丝沉香Aquilaria filaria的化学成分。方法采用硅胶、凝胶、半制备高效液相色谱等多种色谱技术分离丝沉香的化学成分,通过高分辨质谱、核磁共振等波谱学方法鉴定化合物结构,采用改进后的4-硝基苯基-β-D-吡喃葡萄糖苷(4-nitrophenyl-β-D-glucopyranoside,pNPG)法测试化合物的α-葡萄糖苷酶抑制活性。结果从菲律宾产丝沉香中分离鉴定了2个2-(2-苯乙基)色酮二聚体,分别为aquifilarone N(1)和diaquilariachrome B(2)。化合物1和2均具有α-葡萄糖苷酶抑制活性,半数抑制浓度(median inhibition concentration,IC_(50))值分别为(14.33±0.38)μmol/L和(39.53±2.09)μmol/L。结论化合物1为新化合物,化合物2为首次从丝沉香中分离得到。

Objective To investigate the chemical constituents of agarwood of Aquilaria filaria from Philippines.Methods All compounds were isolated by using various chromatographic techniques,including silica gel,Sephadex LH-20,semi-preparative high performance liquid chromatography.Their structures were elucidated based on modern spectroscopic methods,such as high-resolution mass spectrometry(HRMS)and nuclear magnetic resonance(NMR).Theα-glucosidase inhibition assay was performed by modified pNPG(4-nitrophenyl β-D-glucopyranoside)method.Results Two 2-(2-phenylethyl)chromone dimers were isolated from agarwood of A.filaria,and identified as aquifilarone N(1)and diaquilariachrome B(2).Compounds 1 and 2 exhibitedα-glucosidase inhibitory activities in vitro,with IC_(50) values of(14.33±0.38)μmol/L and(39.53±2.09)μmol/L,respectively.Conclusion Compound 1 is a new compound,and compound 2 is isolated from A.filaria for the first time.