title: Insulin-mimetic selaginellins from Selaginella tamariscina with protein tyrosine phosphatase 1B (PTP1B) inhibitory activity.
abstract: As part of an ongoing search for new antidiabetic agents from medicinal plants, three new (2, 4, and 5) and two known selaginellin derivatives (1 and 3) were isolated from a methanol extract of Selaginella tamariscina. The structures of the new compounds were determined by spectroscopic data analysis. All isolates showed strong glucose uptake stimulatory effects in 3T3-L1 adipocyte cells at a concentration of 5 μM. Furthermore, these compounds were found to possess inhibitory effects on PTP1B enzyme activity with IC50 values ranging from 4.6 ± 0.1 to 21.6 ± 1.5 μM. Compound 2 showed the greatest potency, with an IC50 value of 4.6 ± 0.1 μM, when compared with the positive control (ursolic acid, IC50 = 3.5 ± 0.1 μM). Therefore, these selaginellin derivatives may have value as new lead compounds for the development of agents against type 2 diabetes.
authors.affiliation: College of Pharmacy, Catholic University of Daegu , Gyeongsan 712-702, Republic of Korea.
authors.forename: Phi-Hung
authors.initials: PH
authors.lastname: Nguyen
authors.forename: Bing-Tian
authors.initials: BT
authors.lastname: Zhao
authors.forename: Md Yousof
authors.initials: MY
authors.lastname: Ali
authors.forename: Jae-Sue
authors.initials: JS
authors.lastname: Choi
authors.forename: Dong-Young
authors.initials: DY
authors.lastname: Rhyu
authors.forename: Byung-Sun
authors.initials: BS
authors.lastname: Min
authors.forename: Mi-Hee
authors.initials: MH
authors.lastname: Woo
mesh_terms: D041721:3T3-L1 Cells; D017667:Adipocytes / Q000187:drug effects; D000818:Animals; D001713:Biphenyl Compounds / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D003512:Cyclohexanones / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D007004:Hypoglycemic Agents / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D007328:Insulin / Q000494:pharmacology*; D051379:Mice; D015394:Molecular Structure; D010946:Plants, Medicinal / Q000737:chemistry; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1 / Q000037:antagonists & inhibitors*; D032503:Selaginellaceae / Q000737:chemistry*; D014315:Triterpenes / Q000494:pharmacology; D000097245:Ursolic Acid
chemical_list: D001713:Biphenyl Compounds; D003512:Cyclohexanones; D007004:Hypoglycemic Agents; D007328:Insulin; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1; D014315:Triterpenes; D000097245:Ursolic Acid; C516607:PTPN1 protein, human