title: A protein tyrosine phosphatase 1B activity inhibitor from the fruiting bodies of Ganoderma lucidum (Fr.) Karst and its hypoglycemic potency on streptozotocin-induced type 2 diabetic mice.
abstract: Inhibition of protein tyrosine phosphatase 1B (PTP1B) activity has been considered to be a promising therapy approach to treat type 2 diabetes. In this work, a novel PTP1B activity inhibitor, named FYGL (Fudan-Yueyang-G. lucidum), was screened from the fruiting bodies of Ganoderma lucidum and showed an efficient PTP1B inhibitory potency with IC₅₀ = 5.12 ± 0.05 μg/mL. FYGL is a water-soluble macromolecular proteoglycan with a protein to polysaccharide ratio of 17:77 and a viscosity-average molecular weight (M(η)) of 2.6 × 10⁵. The type 2 diabetic mice treated orally by FYGL showed an obvious decrease in plasma glucose level compared with the diabetic controls without drug treatment, comparable with that of diabetic mice treated with metformin, a clinical drug. The toxicity of FYGL is very low. The results indicate that FYGL may serve as a drug candidate or a health-care food for diabetic therapy or protection.
authors.affiliation: Key Laboratory of Molecular Engineering of Polymers, Department of Macromolecular Science, Fudan University, Shanghai 200433, People's Republic of China.
authors.forename: Bao-Song
authors.initials: BS
authors.lastname: Teng
authors.forename: Chen-Dong
authors.initials: CD
authors.lastname: Wang
authors.forename: Hong-Jie
authors.initials: HJ
authors.lastname: Yang
authors.forename: Jia-Sheng
authors.initials: JS
authors.lastname: Wu
authors.forename: Dan
authors.initials: D
authors.lastname: Zhang
authors.forename: Min
authors.initials: M
authors.lastname: Zheng
authors.forename: Zhao-Hua
authors.initials: ZH
authors.lastname: Fan
authors.forename: Deng
authors.initials: D
authors.lastname: Pan
authors.forename: Ping
authors.initials: P
authors.lastname: Zhou
mesh_terms: D000818:Animals; D001685:Biological Factors / Q000008:administration & dosage* / Q000032:analysis / Q000302:isolation & purification; D001786:Blood Glucose / Q000032:analysis; D003924:Diabetes Mellitus, Type 2 / Q000188:drug therapy*; D004195:Disease Models, Animal; D004791:Enzyme Inhibitors / Q000008:administration & dosage* / Q000032:analysis / Q000302:isolation & purification; D048690:Fruiting Bodies, Fungal / Q000737:chemistry*; D006801:Humans; D007004:Hypoglycemic Agents / Q000008:administration & dosage* / Q000032:analysis / Q000302:isolation & purification; D008297:Male; D051379:Mice; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1 / Q000037:antagonists & inhibitors*; D020940:Reishi / Q000737:chemistry*; D013311:Streptozocin
chemical_list: D001685:Biological Factors; D001786:Blood Glucose; D004791:Enzyme Inhibitors; D007004:Hypoglycemic Agents; D013311:Streptozocin; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1