title: Protein Tyrosine Phosphatase 1B Inhibitors from the Roots of Cudrania tricuspidata.
abstract: A chemical investigation of the methanol extract from the roots of Cudrania tricuspidata resulted in the isolation of 16 compounds, including prenylated xanthones 1-9 and flavonoids 10-16. Their structures were identified by NMR spectroscopy and mass spectrometry and comparisons with published data. Compounds 1-9 and 13-16 significantly inhibited PTP1B activity in a dose dependent manner, with IC50 values ranging from 1.9-13.6 μM. Prenylated xanthones showed stronger PTP1B inhibitory effects than the flavonoids, suggesting that they may be promising targets for the future discovery of novel PTP1B inhibitors. Furthermore, kinetic analyses indicated that compounds 1 and 13 inhibited PTP1B in a noncompetitive manner; therefore, they may be potential lead compounds in the development of anti-obesity and -diabetic agents.
authors.affiliation: College of Pharmacy, Wonkwang University, Iksan 570-749, Korea. quangth2004@yahoo.com.|Institute of Marine Biochemistry, Vietnam Academy of Science and Technology (VAST), 18 Hoang Quoc Viet, Caugiay, Hanoi 10000, Vietnam. quangth2004@yahoo.com.
authors.forename: Tran Hong
authors.initials: TH
authors.lastname: Quang
authors.affiliation: College of Pharmacy, Wonkwang University, Iksan 570-749, Korea. nganthanh27@yahoo.com.|Institute of Marine Biochemistry, Vietnam Academy of Science and Technology (VAST), 18 Hoang Quoc Viet, Caugiay, Hanoi 10000, Vietnam. nganthanh27@yahoo.com.
authors.forename: Nguyen Thi Thanh
authors.initials: NT
authors.lastname: Ngan
authors.affiliation: College of Pharmacy, Wonkwang University, Iksan 570-749, Korea. host@wku.ac.kr.|Hanbang Body-Fluid Research Center, Wonkwang University, Iksan 570-749, Korea. host@wku.ac.kr.
authors.forename: Chi-Su
authors.initials: CS
authors.lastname: Yoon
authors.affiliation: College of Pharmacy, Wonkwang University, Iksan 570-749, Korea. host@wku.ac.kr.|Hanbang Body-Fluid Research Center, Wonkwang University, Iksan 570-749, Korea. host@wku.ac.kr.
authors.forename: Kwang-Ho
authors.initials: KH
authors.lastname: Cho
authors.affiliation: Hanbang Body-Fluid Research Center, Wonkwang University, Iksan 570-749, Korea. host@wku.ac.kr.|Professional Graduate School of Oriental Medicine and College of Oriental Medicine, Wonkwang University, Iksan 570-749, Korea. host@wku.ac.kr.
authors.forename: Dae Gill
authors.initials: DG
authors.lastname: Kang
authors.affiliation: Hanbang Body-Fluid Research Center, Wonkwang University, Iksan 570-749, Korea. host@wku.ac.kr.|Professional Graduate School of Oriental Medicine and College of Oriental Medicine, Wonkwang University, Iksan 570-749, Korea. host@wku.ac.kr.
authors.forename: Ho Sub
authors.initials: HS
authors.lastname: Lee
authors.affiliation: College of Pharmacy, Wonkwang University, Iksan 570-749, Korea. yckim@wku.ac.kr.|Hanbang Body-Fluid Research Center, Wonkwang University, Iksan 570-749, Korea. yckim@wku.ac.kr.
authors.forename: Youn-Chul
authors.initials: YC
authors.lastname: Kim
authors.affiliation: College of Pharmacy, Wonkwang University, Iksan 570-749, Korea. hoh@wku.ac.kr.|Hanbang Body-Fluid Research Center, Wonkwang University, Iksan 570-749, Korea. hoh@wku.ac.kr.
authors.forename: Hyuncheol
authors.initials: H
authors.lastname: Oh
mesh_terms: D002384:Catalysis / Q000187:drug effects; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D006868:Hydrolysis / Q000187:drug effects; D020128:Inhibitory Concentration 50; D029586:Moraceae / Q000737:chemistry*; D010936:Plant Extracts / Q000737:chemistry* / Q000494:pharmacology*; D018517:Plant Roots / Q000737:chemistry*; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1 / Q000037:antagonists & inhibitors*
chemical_list: D004791:Enzyme Inhibitors; D010936:Plant Extracts; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1
keywords: Cudrania tricuspidata; Moraceae; PTP1B; flavonoids; xanthones