New α-glucosidase inhibitors with p-terphenyl skeleton from the mushroom Hydnellum concrescens
New α-glucosidase inhibitors with p-terphenyl skeleton from the mushroom Hydnellum concrescens
复制标题
DOI：
10.1016/j.fitote.2014.07.019
复制
发表时间：
2014-10-01
期刊：
影响因子：
3.4
通讯作者：
Liu, Hong-Wei
中科院分区：
文献类型：
--
作者：
Wang, Shi-Mei;Han, Jun-Jie;Liu, Hong-Wei
本研究的目的是阐明在蘑菇 Hydnellum concrescens 的 EtOAc 提取物中检测到的 α-葡萄糖苷酶抑制活性的生物活性成分。从 H. concrescens 的子实体中分离出两种新的对三联苯衍生物 concrescenins A (1) 和 B (2)，以及六种已知化合物 thelephantins L (3)、I (4)、J (5)、K (6)、二氢橙酸二苯甲酸酯 (7) 和 curtisian A (8)。通过核磁共振实验阐明了它们的化学结构。化合物1-4和6-8显示出对α-葡萄糖苷酶的抑制活性，IC50分别为0.99、3.11、4.53、18.77、2.98、5.16和8.34μM。 α-葡萄糖苷酶动力学分析表明，化合物1和2以非竞争性方式抑制α-葡萄糖苷酶活性，Ki值分别为0.02和021μM。在抗氧化评价中，化合物1和4表现出弱的DPPH清除活性（EC50=82.50和161.75μM）和弱的还原能力（EC50=193.57和152.94μM）。目前的研究支持蘑菇衍生的对三联苯衍生物用于治疗糖尿病的潜在用途。 (C) 2014 Elsevier B.V. 保留所有权利。
The purpose of this study is to elucidate the bioactive components responsible for the the alpha-glucosidase inhibitory activity detected in the EtOAc extract of the mushroom Hydnellum concrescens. Two new p-terphenyl derivatives, concrescenins A (1) and B (2), in along with six known compounds thelephantins L (3), I (4), J (5), K (6), dihydroauran-tiacin dibenzoate (7), and curtisian A (8) were isolated from the fruiting bodies of H. concrescens. Their chemical structures were elucidated by NMR experiments. Compounds 1-4 and 6-8 showed the inhibitory activity against alpha-glucosidase with the IC50 of 0.99, 3.11, 4.53, 18.77, 2.98, 5.16, and 8.34 mu M, respectively. Kinetic analysis of alpha-glucosidase indicated that compounds 1 and 2 inhibited the activity of alpha-glucosidase in a noncompetitive fashion with a Ki value of 0.02 and 021 mu M, respectively. In antioxidant evaluation, compounds 1 and 4 showed weak DPPH scavenging activity (EC50 = 82.50 and 161.75 mu M) and weak reducing ability (EC50 = 193.57 and 152.94 mu M). The current research supports the potential use of mushroom-derived p-terphenyl derivatives for the treatment of diabetes. (C) 2014 Elsevier B.V. All rights reserved.