title: α-Glucosidase and aldose reductase inhibitory activities from the fruiting body of Phellinus merrillii.
abstract: 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.
authors: School of Chinese Pharmaceutical Sciences and Chinese Medicine Resources, College of Pharmacy, China Medical University, Taichung, Taiwan. gjhuang@mail.cmu.edu.tw
authors: Guan-Jhong
authors: GJ
authors: Huang
authors: Wen-Tsong
authors: WT
authors: Hsieh
authors: Heng-Yuan
authors: HY
authors: Chang
authors: Shyh-Shyun
authors: SS
authors: Huang
authors: Ying-Chih
authors: YC
authors: Lin
authors: Yueh-Hsiung
authors: YH
authors: Kuo
mesh_terms: D000449:Aldehyde Reductase / Q000037:antagonists & inhibitors*; D000818:Animals; D001487:Basidiomycota / Q000737:chemistry*; D002396:Catechols / Q000302:isolation & purification / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000302:isolation & purification / Q000494:pharmacology*; D048690:Fruiting Bodies, Fungal / Q000737:chemistry*; D005663:Furans / Q000302:isolation & purification / Q000494:pharmacology; D065089:Glycoside Hydrolase Inhibitors; D007004:Hypoglycemic Agents; D007908:Lens, Crystalline; D018942:Macrolides / Q000302:isolation & purification / Q000494:pharmacology; D008297:Male; D011753:Pyrones / Q000302:isolation & purification / Q000494:pharmacology; D051381:Rats; D017207:Rats, Sprague-Dawley
chemical_list: D002396:Catechols; D004791:Enzyme Inhibitors; D005663:Furans; D065089:Glycoside Hydrolase Inhibitors; D007004:Hypoglycemic Agents; D018942:Macrolides; D011753:Pyrones; C103442:hispolon; C513095:inotilone; D000449:Aldehyde Reductase; C007946:hispidin