School of Chinese Pharmaceutical Sciences and Chinese Medicine Resources, College of Pharmacy, China Medical University, Taichung, Taiwan.
J Agric Food Chem. 2011 May 25;59(10):5702-6. doi: 10.1021/jf2003943. Epub 2011 Apr 11.
The inhibitory activity from the isolated component of the fruiting body Phellinus merrillii (PM) was evaluated against α-glucosidase and lens aldose reductase from Sprague-Dawley male rats and compared to the quercetin as an aldose reductase inhibitor and acarbose as an α-glucosidase inhibitor. The ethanol extracts of PM (EPM) showed the strong α-glucosidase and aldose reductase activities. α-Glucosidase and aldose reductase inhibitors were identified as hispidin (A), hispolon (B), and inotilone (C), which were isolated from EtOAc-soluble fractions of EPM. The above structures were elucidated by their spectra and comparison with the literatures. Among them, hispidin, hispolon, and inotilone exhibited potent against α-glucosidase inhibitor activity with IC(50) values of 297.06 ± 2.06, 12.38 ± 0.13, and 18.62 ± 0.23 μg/mL, respectively, and aldose reductase inhibitor activity with IC(50) values of 48.26 ± 2.48, 9.47 ± 0.52, and 15.37 ± 0.32 μg/mL, respectively. These findings demonstrated that PM may be a good source for lead compounds as alternatives for antidiabetic agents currently used. The importance of finding effective antidiabetic therapeutics led us to further investigate natural compounds.
从裂蹄木层孔菌（PM）的分离成分中评估了其对 Sprague-Dawley 雄性大鼠α-葡萄糖苷酶和晶状体醛糖还原酶的抑制活性，并将槲皮素作为醛糖还原酶抑制剂和阿卡波糖作为α-葡萄糖苷酶抑制剂与之进行了比较。PM 的乙醇提取物（EPM）表现出强烈的α-葡萄糖苷酶和醛糖还原酶活性。从 EPM 的乙酸乙酯可溶部分中分离出的棘皮素（A）、棘皮酮（B）和异土木香内酯（C）被鉴定为α-葡萄糖苷酶和醛糖还原酶抑制剂。这些结构通过其光谱并与文献进行比较来阐明。其中，棘皮素、棘皮酮和异土木香内酯对α-葡萄糖苷酶抑制剂的抑制活性较强，IC（50）值分别为 297.06 ± 2.06、12.38 ± 0.13 和 18.62 ± 0.23 μg/mL，对醛糖还原酶抑制剂的抑制活性分别为 IC（50）值为 48.26 ± 2.48、9.47 ± 0.52 和 15.37 ± 0.32 μg/mL。这些发现表明，PM 可能是作为目前使用的抗糖尿病药物替代品的先导化合物的良好来源。寻找有效抗糖尿病治疗方法的重要性促使我们进一步研究天然化合物。
