柯拉斯那沉香的生物活性成分研究

Bioactive Components from Agarwood Originating from Aquilaria crassna

摘要:

为了解柯拉斯那（Aquilaria crassna）的化学成分，从其所产沉香中分离得到10个化合物，经波谱分析分别鉴定为：6，8-羟基-2-（2-苯乙基）色酮（1），6，8-二羟基-2-[2-（4-甲氧基苯）乙基]色酮（2），rel-（1aR，2R，3R，7bS）-1a，2，3，7b-tetrahydro-2，3-dihydroxy-5-（2-phenylethyl）-7H-oxireno[f][1]benzopyran-7-one（3），rel-（1aR，2R，3R，7bS）-1a，2，3，7b-tetrahydro-2，3-dihydroxy-[2-（4-methoxyphenyl）-ethyl]-7H-oxireno[f][1]benzopyran-7-one（4），rel-（1aR，2R，3R，7bS）-1a，2，3，7b-tetrahydro-2，3-dihydroxy-5-[2-（3-hydroxy-4-methoxyphenyl）-ethyl]-7H-oxireno[f][1]benzopyran-7-one（5），oxidoagarochromone B（6），oxidoagarochromone C（7），（5S，6R，7S，8R）-2-[2-（3'-hydroxy-4'-methoxyphenyl）ethyl]-5，6，7，8-tetrahydroxy-5，6，7，8-tetrahydrochromone（8），6，7-cis-dihydroxy-2-（2-phenylethyl）-5，6，7，8-tetrahydrochromone（9），N-trans-feruloyltyramine（10）。化合物3～5和8～10为首次从柯拉斯那沉香中分离得到。化合物1，3，6，7，9和10对乙酰胆碱酯酶具有一定的抑制活性，化合物4对人慢性髓原白血病细胞株K-562和人胃癌细胞株SGC-7901均具有较小的抑制作用，化合物1和3对人肝癌细胞株BEL-7402也有抑制活性。

Abstract:

In order to understand the chemical constituents of Aquilaria crassna, ten compounds were isolated from its agarwood. On the basis of spectral data, they were identified as 6,8-dihydroxy-2-(2-phenylethyl)-chromone (1), 6,8-dihydroxy-2-[2-(4-methoxyphenyl) ethyl]chromone (2), rel-(1aR,2R,3R,7bS)-1a,2,3,7b-tetrahydro-2,3-dihydroxy-5-(2-phenylethyl)-7H-oxireno[f][1]benzopyran-7-one (3), rel-(1aR,2R,3R,7bS)-1a,2,3,7b-tetrahydro-2,3-dihydroxy-[2-(4-methoxyphenyl)ethyl]-7H-oxireno[f][1]benzopyran-7-one (4), rel-(1aR,2R,3R,7bS)-1a,2,3,7b-tetrahydro-2,3-dihydroxy-5-[2-(3-hydroxy-4-methoxyphenyl) ethyl]-7H-oxireno[f][1]benzopyran-7-one (5), oxidoagarochromone B (6), oxidoagarochromone C (7), (5S,6R,7S,8R)-2-[2-(3'-hydroxy-4'-methoxyphenyl)ethyl]-5,6,7,8-tetrahydroxy-5,6,7,8-tetrahydrochromone (8), 6,7-cis-dihydroxy-2-(2phenylethyl)-5,6,7,8-tetrahydrochromone (9), N-trans-feruloyltyramine (10). Compounds 1-5 and 8-11 were isolated from agarwood of A. crassna for the first time. Compounds 1, 3, 4, 6, 7 and 11 showed inhibitory activities against acetylcholinesterase. Compound 4 had weak inhibitory effect on K-562 and SGC-7901 carcinoma cell lines, and compounds 1 and 3 showed inhibitory activity against BEL-7402 cells.