title: Protein tyrosine phosphatase 1B (PTP1B) inhibitory activity and glucosidase inhibitory activity of compounds isolated from Agrimonia pilosa.
abstract: BACKGROUND
  Despite phytochemical studies of Agrimonia pilosa Ledeb. (Rosaceae), the antidiabetic effects of this plant are unknown.
  
  
  OBJECTIVE
  This study characterizes the isolated compounds from the aerial parts of A. pilosa and evaluates their PTP1B and α-glucosidase inhibitory properties.
  
  
  METHODS
  Ethanol extract of A. pilosa was found to inhibit 64% PTP1B activity at 30 μg/mL. The ethanol extract was partitioned with methylene chloride, ethyl acetate, n-butanol, and water fractions. Among these, the ethyl acetate fraction displayed the most potent PTP1B activity. The ethyl acetate extract was separated by chromatographic methods to obtain flavonoids and triterpenoids (1-11); which were evaluated for their inhibitory effects on PTP1B activity with p-nitrophenyl phosphate (p-NPP) as a substrate, and also α-glucosidase enzyme.
  
  
  RESULTS
  Compounds 1-11 were identified as apigenin-7-O-β-d-glucuronide-6″-methyl ester, triliroside, quercetin-7-O-β-d-glycoside, quercetin-3-O-β-d-glycoside, kaempferol, kaempferol-3-O-α-l-rhamnoside, β-sitosterol, ursolic acid, tormentic acid, methyl 2-hydroxyl tricosanoate, and palmitic acid. Compounds 8, 9, and 11 displayed inhibitory effects on PTP1B activity with IC50 values of 3.47 ± 0.02, 0.50 ± 0.06, and 0.10 ± 0.03 μM, respectively. Compounds 3, 4, 6, and 9 exhibited inhibition of the α-glucosidase activity with IC50 values of 11.2 ± 0.2, 29.6 ± 0.9, 28.5 ± 0.1, and 23.8 ± 0.4 μM, respectively.
  
  
  CONCLUSIONS
  As major ingredients of A. pilosa, compounds 1, 6, 8, and 9 showed the greatest inhibitory potency on PTP1B activity. Compounds 3, 6, 8, and 9 also showed potent inhibitory effects on α-glucosidase enzyme. This result suggested the potential of these compounds for developing antidiabetic agents.
authors.affiliation: a College of Pharmacy, Drug Research and Development Center, Catholic University of Daegu , Gyeongsan , Republic of Korea.
authors.forename: Braham
authors.initials: B
authors.lastname: Na
authors.affiliation: a College of Pharmacy, Drug Research and Development Center, Catholic University of Daegu , Gyeongsan , Republic of Korea.
authors.forename: Phi-Hung
authors.initials: PH
authors.lastname: Nguyen
authors.affiliation: a College of Pharmacy, Drug Research and Development Center, Catholic University of Daegu , Gyeongsan , Republic of Korea.
authors.forename: Bing-Tian
authors.initials: BT
authors.lastname: Zhao
authors.affiliation: a College of Pharmacy, Drug Research and Development Center, Catholic University of Daegu , Gyeongsan , Republic of Korea.
authors.forename: Quoc-Hung
authors.initials: QH
authors.lastname: Vo
authors.affiliation: a College of Pharmacy, Drug Research and Development Center, Catholic University of Daegu , Gyeongsan , Republic of Korea.
authors.forename: Byung Sun
authors.initials: BS
authors.lastname: Min
authors.affiliation: a College of Pharmacy, Drug Research and Development Center, Catholic University of Daegu , Gyeongsan , Republic of Korea.
authors.forename: Mi Hee
authors.initials: MH
authors.lastname: Woo
mesh_terms: D031981:Agrimonia; D004305:Dose-Response Relationship, Drug; D004365:Drugs, Chinese Herbal / Q000302:isolation & purification* / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000302:isolation & purification / Q000494:pharmacology; D065089:Glycoside Hydrolase Inhibitors / Q000302:isolation & purification* / Q000494:pharmacology*; D006801:Humans; D035261:Plant Components, Aerial; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1 / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D004365:Drugs, Chinese Herbal; D004791:Enzyme Inhibitors; D065089:Glycoside Hydrolase Inhibitors; C516607:PTPN1 protein, human; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1
keywords: Flavonoid glycosides; PTP1B inhibitors; glucosidase inhibitors; triterpenoids