A Multitarget Approach to Evaluate the Efficacy of Aquilaria sinensis Flower Extract against Metabolic Syndrome |
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Authors: | Hee-Sung Chae Olivia Dale Tahir Maqbool Mir Bharathi Avula Jianping Zhao Ikhlas A Khan Shabana I Khan |
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Institution: | 1.National Center for Natural Products Research, School of Pharmacy, The University of Mississippi, Oxford, MS 38677, USA; (H.-S.C.); (O.D.); (T.M.M.); (B.A.); (J.Z.); (I.A.K.);2.Department of Biomolecular Sciences, School of Pharmacy, The University of Mississippi, Oxford, MS 38677, USA |
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Abstract: | Aquilaria sinensis (Lour.) Spreng is known for its resinous secretion (agarwood), often secreted in defense against injuries. We investigated the effects of A. sinensis flower extract (AF) on peroxisome proliferator-activated receptors alpha and gamma (PPARα and PPARγ), liver X receptor (LXR), glucose uptake, and lipid accumulation (adipogenesis). Activation of PPARα, PPARγ and LXR was determined in hepatic (HepG2) cells by reporter gene assays. Glucose uptake was determined in differentiated muscle (C2C12) cells using 2-NBDG (2-deoxy-2-(7-nitro-2,1,3-benzoxadiazol-4-yl)amino]-D-glucose). Adipogenesis was determined in adipocytes (3T3-L1 cells) by Oil red O staining. At a concentration of 50 µg/mL, AF caused 12.2-fold activation of PPARα and 5.7-fold activation of PPARγ, while the activation of LXR was only 1.7-fold. AF inhibited (28%) the adipogenic effect induced by rosiglitazone in adipocytes and increased glucose uptake (32.8%) in muscle cells at 50 μg/mL. It was concluded that AF acted as a PPARα/γ dual agonist without the undesired effect of adipogenesis and exhibited the property of enhancing glucose uptake. This is the first report to reveal the PPARα/γ dual agonistic action and glucose uptake enhancing property of AF along with its antiadipogenic effect, indicating its potential in ameliorating the symptoms of metabolic syndrome. |
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Keywords: | Aquilaria sinensis Thymelaeaceae PPAR LXR adipogenesis glucose uptake |
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