目的 对锦葵科蜀葵属植物药蜀葵Althaea officinalis茎叶的化学成分及其体外抑制α-葡萄糖苷酶和5-脂氧合酶活性进行研究。方法 运用D101大孔吸附树脂、硅胶柱、MCI凝胶、Sephadex LH-20以及半制备HPLC等多种色谱方法进行分离纯化，根据波谱数据鉴定化合物的结构；通过测定化合物对α-葡萄糖苷酶和5-脂氧合酶体外抑制活性，评价化合物的降血糖和抗炎作用。结果 从药蜀葵茎叶中共分离得到24个化合物，分别鉴定为腺苷（1）、4-羟基-2,6二甲氧基苯基-β-D-吡喃葡萄糖苷（2）、苄基-O-β-D-吡喃葡萄糖苷（3）、赤藓醇（4）、5-羟甲基-2-呋喃甲醛（5）、1-[5-(hydroxymethyl) furan-2-yl] ethenone（6）、黑麦草内酯（7）、isololiolide（8）、4-羟基苯甲醛（9）、对羟基苯甲酸甲酯（10）、催吐萝芙木醇（11）、(6S,7Z,9R)-roseoside（12）、二氢芥子醇（13）、3-(3,4,5-trimethoxyphenyl)propan-1-ol（14）、dihydrodehydrodiconifenyl alcohol（15）、齐墩果酸3-O-β-D-吡喃葡萄糖苷（16）、紫云英苷（17）、反式银椴苷（18）、望春花黄酮醇苷（19）、apigenin 7-O-(6''-trans-p-coumaroyl-β-D-glucopyranoside)（20）、香叶木素7-O-β-D-吡喃葡萄糖苷（21）、田蓟苷（22）、芒柄花素7-葡萄糖苷（23）、acacetin 7-O-(6''-p-coumaroyl)-β-D-glucopyranoside（24）。生物活性测试结果表明，化合物18、19、24对α-葡萄糖苷酶半数抑制浓度（median inhibition concentration，IC₅₀）为（12.2±1.3）、（2.8±0.6）、（31.1±3.9）μmol/L；化合物18、24对5-脂氧合酶的IC₅₀为（34.76±4.3）、（25.37±2.4）μmol/L。结论 化合物1～16、18～24为首次从该植物中分离获得。发现部分化合物具有较好的体外抑制α-葡萄糖苷酶（18、19、24）和5-脂氧合酶（18、24）作用，表明其具有潜在的降血糖活性和抗炎活性。

Objective To study the chemical constituents from aerial part of Althaea officinalis and their inhibition activities in vitro toward α-glucosidase and 5-lipoxygenas. Methods Chemical constituents were separated and purified by column chromatography on D101 macroporous adsorption resin, silica gel, MCI gel, Sephadex LH-20, and semi-preparative RP-HPLC. The structures were characterized via spectroscopic data analysis. The inhibitory activities of the compounds against α-glucosidase and 5-lipoxygenase in vitro were measured to evaluate its hypoglycemic and anti-inflammatory effects. Results Twenty-four compounds were isolated and identified as adenosine (1), leonuriside A (2), benzyl-O-β-D-glucopyranoside (3), meso-erythritol (4), 5-hydroxymethyl- 2-furancarboxaldehyde (5), 1-[5-(hydroxymethyl) furan-2-yl] ethenone (6), loliolide (7), isololiolide (8), 4-hydroxybenzaldehyde (9), methyl 4-hydroxybenzoate (10), vomifoliol (11), (6S,7Z,9R)-roseoside (12), dihydrosyringenin (13), 3-(3,4,5-trimethoxyphenyl) propan-1-ol (14), dihydrodehydrodiconifenyl alcohol (15), oleanolic acid 3-O-β-D-glucopyranoside (16), astragalin (17), trans-tiliroside (18), biondnoid I (19), apigenin 7-O-(6''-trans-p-coumaroyl-β-D-glucopyranoside) (20), diosmetin 7-O-β-D- glucopyranoside (21), tilianin (22), formononetin 7-glucoside (23), acacetin 7-O-(6''-p-coumaroyl)-β-D-glucopyranoside (24). The results of the bioactivity test showed that three of the 24 compounds (18 , 19 , 24) showed significant enzyme inhibitory activity against α-glucosidase [IC₅₀ values: (12.2 ±1.3) μmol/L, (2.8 ±0.6) μmol/L and (31.1 ±3.9) μmol/L] and two compounds (18 , 24) had significant enzyme inhibitory activity against 5-lipoxygenase with IC₅₀ values of (34.76 ±4.3) μmol/L and (25.37 ±2.4) μmol/L. Conclusion Compounds 1 —16 , 18 —24 were isolated from A. officinalis for the first time. Furthermore, it was found that compounds have great inhibitory activities toward α-glucosidase (18 , 19 , 24) and 5-lipoxygenase (18 , 24), which show potential hypoglycemic activity and anti-inflammatory activity.

R284.1

陕西省科技统筹创新工程计划项目（2016KTTSSF01-06-01）；陕西省青年科技新星项目（2020KJXX-069）；现代农业产业技术体系建设专项基金项目(CARS-21）