title: Identification of plant extracts with potential antidiabetic properties: effect on human peroxisome proliferator-activated receptor (PPAR), adipocyte differentiation and insulin-stimulated glucose uptake.
abstract: Thiazolidinediones (TZDs) are insulin sensitizing drugs used to treat type 2 diabetes. The primary target of the TZDs is the peroxisome proliferator-activated receptor (PPAR) gamma, a key regulator of adipogenesis and glucose homeostasis. Currently prescribed TZDs are full PPARgamma agonists, and their use is associated with several side effects. Partial PPARgamma agonists appear to be associated with fewer side effects but may still confer the desired insulin sensitizing action. Extracts from common medicinal/food plants were tested in a screening platform comprising a series of bioassays, including tests for PPARgamma, alpha and delta transactivation, adipocyte differentiation and insulin-stimulated glucose uptake, allowing identification of plants containing potentially interesting PPAR agonists. Twenty-two plant extracts out of 133 were found to increase insulin-stimulated glucose uptake and 18 extracts were found to activate PPARgamma, 3 to activate PPARalpha and gamma, 6 to activate PPARdelta and gamma, and 9 to activate PPARgamma, alpha and delta. Among the 24 different plant species tested in the platform, 50% were shown to contain compounds capable of activating PPARgamma and stimulating insulin-dependent glucose uptake with no or little effect on adipocyte differentiation warranting further studies and characterization.
authors.affiliation: Department of Food Science, University of Aarhus, Kirstinebjergvej 10, 5792 Aarslev, Denmark. kathrine.bisgaard@agrsci.dk
authors.forename: Kathrine B
authors.initials: KB
authors.lastname: Christensen
authors.forename: Ariane
authors.initials: A
authors.lastname: Minet
authors.forename: Henrik
authors.initials: H
authors.lastname: Svenstrup
authors.forename: Kai
authors.initials: K
authors.lastname: Grevsen
authors.forename: Hongbin
authors.initials: H
authors.lastname: Zhang
authors.forename: Eva
authors.initials: E
authors.lastname: Schrader
authors.forename: Gerald
authors.initials: G
authors.lastname: Rimbach
authors.forename: Silvia
authors.initials: S
authors.lastname: Wein
authors.forename: Siegfried
authors.initials: S
authors.lastname: Wolffram
authors.forename: Karsten
authors.initials: K
authors.lastname: Kristiansen
authors.forename: Lars P
authors.initials: LP
authors.lastname: Christensen
mesh_terms: D041721:3T3-L1 Cells; D000818:Animals; D002454:Cell Differentiation / Q000187:drug effects*; D005947:Glucose / Q000378:metabolism*; D006801:Humans; D007004:Hypoglycemic Agents / Q000494:pharmacology*; D007328:Insulin / Q000494:pharmacology; D051379:Mice; D047492:Peroxisome Proliferator-Activated Receptors / Q000819:agonists / Q000378:metabolism*; D010936:Plant Extracts / Q000494:pharmacology*; D045162:Thiazolidinediones / Q000494:pharmacology*; D015533:Transcriptional Activation
chemical_list: D007004:Hypoglycemic Agents; D007328:Insulin; D047492:Peroxisome Proliferator-Activated Receptors; D010936:Plant Extracts; D045162:Thiazolidinediones; D005947:Glucose