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Planta Med 2013; 79(12): 1084-1095
DOI: 10.1055/s-0033-1350620
Biological Screening
Original Papers
Georg Thieme Verlag KG Stuttgart · New York

Screening of Medicinal Plants for PPARα and PPARγ Activation and Evaluation of Their Effects on Glucose Uptake and 3T3-L1 Adipogenesis

Min Hye Yang
1   National Center for Natural Products Research, Research Institute of Pharmaceutical Sciences, School of Pharmacy, University of Mississippi, MS, USA
,
Bharathi Avula
1   National Center for Natural Products Research, Research Institute of Pharmaceutical Sciences, School of Pharmacy, University of Mississippi, MS, USA
,
Troy Smillie
1   National Center for Natural Products Research, Research Institute of Pharmaceutical Sciences, School of Pharmacy, University of Mississippi, MS, USA
,
Ikhlas A. Khan
1   National Center for Natural Products Research, Research Institute of Pharmaceutical Sciences, School of Pharmacy, University of Mississippi, MS, USA
2   Department of Pharmacognosy, School of Pharmacy, University of Mississippi, MS, USA
,
Shabana I. Khan
1   National Center for Natural Products Research, Research Institute of Pharmaceutical Sciences, School of Pharmacy, University of Mississippi, MS, USA
2   Department of Pharmacognosy, School of Pharmacy, University of Mississippi, MS, USA
› Author Affiliations
Further Information

Publication History

received 25 February 2013
revised 17 May 2013

accepted 20 June 2013

Publication Date:
22 July 2013 (online)

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Abstract

Medicinal plants are a rich source of ligands for nuclear receptors. The present study was aimed to screen a collection of plant extracts for PPARα/γ-activating properties and identify the active extract that can stimulate cellular glucose uptake without enhancing the adipogenesis. A reporter gene assay was performed to screen ethanolic extracts of 263 plant species, belonging to 94 families, for activation of PPARα and PPARγ. Eight extracts showed activation of PPARγ, while 22 extracts showed activation of PPARα. The extracts of five plants (Daphne gnidium, Illicium anisatum, Juniperus virginiana, Terminalia chebula, and Thymelaea hirsuta) showed activation of both PPARα and PPARγ and out of them, D. gnidium and T. hirsuta markedly increased PPARα/γ protein expression. All five extracts showed an increase in cellular glucose uptake. Of the five dual agonists, T. chebula and T. hirsuta did not show any increase in differentiation of 3T3-L1 preadipocytes, but I. anisatum caused an increase in adipogenesis, while D. gnidium and J. virginiana were toxic to adipocytes. The adipogenic effect of rosiglitazone was antagonized by T. chebula and T. hirsuta. It was concluded that T. hirsuta and T. chebula retain the property of elevating glucose uptake as PPARα/γ dual agonists without the undesired side effect of adipogenesis. This is the first report to reveal the PPARα/γ dual agonistic action and glucose uptake enhancing property of T. hirsuta and T. chebula.

Key words

type 2 diabetes - PPARα and PPARγ activation - glucose uptake stimulation - adipocyte differentiation - Thymelaea hirsuta - Thymelaeaceae - Terminalia chebula - Combretaceae
 

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