a Department of Pharmacognosy , Faculty of Pharmacy, Cairo University , Kasr El-Aini Street, Cairo 11562 , Egypt.
Nat Prod Res. 2014;28(11):812-8. doi: 10.1080/14786419.2014.891203. Epub 2014 Mar 25.
α-Glucosidase inhibitors (AGIs) represent a class of oral antidiabetic drugs that delay the absorption of ingested carbohydrates, reducing the postprandial glucose and insulin peaks to reach normoglycaemia. In this study, a bioassay-guided fractionation of the ethanolic extract of the aerial parts of Achillea fragrantissima (Forssk.) Sch. Bip. growing in Egypt led to the isolation of a new potent AGI; acacetin-6-C-(6″-acetyl-β-D-glucopyranoside)-8-C-α-L-arabinopyranoside (5) alongside with four known compounds: chondrillasterol (1), quercetin-3,6,7-trimethyl ether (chrysosplenol-D) (2), isovitexin-4'-methyl ether (3) and isovitexin (4). The structure of the new compound (5) was elucidated on the basis of its spectral data, including HR-FAB-MS, UV, (1)H NMR, (13)C NMR, (1)H-(1)H COSY, HSQC and HMBC. The new compound (5) exhibited the most significant α-glucosidase inhibitory activity (IC₅₀ 1.5 ± 0.09 μg/mL). Under the assay conditions, all the tested compounds were more potent than the positive control acarbose (IC50 224 ± 2.31 μg/mL).
α-葡萄糖苷酶抑制剂（AGIs）是一类口服抗糖尿病药物，可延缓摄入碳水化合物的吸收，降低餐后血糖和胰岛素峰值，以达到正常血糖水平。在这项研究中，对在埃及生长的香青兰（Achillea fragrantissima（Forssk.）Sch. Bip.）地上部分的乙醇提取物进行生物测定指导的分级分离，导致分离出一种新的强效 AGI；即乙酰基-β-D-吡喃葡萄糖基-8-C-α-L-阿拉伯吡喃糖苷基芹菜素（acacetin-6-C-（6”-乙酰基-β-D-吡喃葡萄糖基）-8-C-α-L-阿拉伯吡喃糖苷）（5）以及四种已知化合物：chondrillasterol（1）、槲皮素-3,6,7-三甲醚（chrysosplenol-D）（2）、异荭草苷-4'-甲醚（3）和异荭草苷（4）。新化合物（5）的结构是根据其光谱数据阐明的，包括 HR-FAB-MS、UV、（1）H NMR、（13）C NMR、（1）H-（1）H COSY、HSQC 和 HMBC。新化合物（5）表现出最显著的α-葡萄糖苷酶抑制活性（IC₅₀ 1.5 ± 0.09 μg/mL）。在试验条件下，所有测试的化合物都比阳性对照阿卡波糖（IC50 224 ± 2.31 μg/mL）更有效。
