Planta Med 2015; 81 - PW_32
DOI: 10.1055/s-0035-1565656

Screening of 19 traditional Mexican medicinal plants for effects on the metabolic syndrome related targets PPARα, β/δ, and γ in an in vitro luciferase reporter gene assay

K Kuchta 1, N Matsuura 2, HW Rauwald 3, R Quintanilla-Licea 4, M Iinuma 5
  • 1National Institute of Health Sciences, Division of Pharmacognosy, Phytochemistry and Narcotics, Setagaya-ku, Kamiyoga 1 – 18 – 1, 158 – 8501 Tokyo, Japan, Tokyo, Japan
  • 2Department of Life Science, Okayama University of Science, 700 – 0005, Okayama, Japan
  • 3Department of Pharmaceutical Biology, Leipzig University, Johannisallee 23, 04103, Leipzig, Germany
  • 4Laboratorio de Fitoquímica, Universidad Autónoma de Nuevo León, Av. Pedro de Alba S/N, Cd. Universitaria, 66451, San Nicolás de los Garza, Mexico
  • 5Department of Pharmacognosy, Gifu Pharmaceutical University, 501 – 1196, Gifu, Japan

In the present study, the effect of traditionally prepared infusions of 19 traditional Mexican medicinal plants on the metabolic syndrome related peroxisome proliferator-activated receptors (PPAR) α, β/δ, and γ was investigated using a novel luciferase reporter gene assay [1]. COS-1 cells were co-transfected with the luciferase reporter plasmid p17m2G, containing a GAL4 upstream activating sequence in the promoter region, an expression vector for the human PPARβ/δ ligand-binding domain fused to the GAL4 DNA-binding domain pPPARβ/δ-GAL4, and the secreted alkaline phosphatase control vector pSEAP. The results are relative to the luciferase expression levels, which were normalized using secreted alkaline phosphatase (SEAP) activity. All extracts (all at 6.25, 25, and 100 µg/mL), and GW0742 (positive control, 0.1 nM) were dissolved in DMSO and added to the medium of the transfected cells. The same approach was used for PPARα and PPARγ in which case the COS-1 cells were transfected with pPPARα or γ-GAL4 and p17m2G, respectively (positive controls 50 µM WY14643/10 µM troglitazone). In the above described assay, significant effects could be detected for both Aloe vera (L.) Burm.f. (commercial whole leaf preparation) and Larrea tridentata (DC.) Coville while no activity above DMSO vehicle negative control levels could be detected for any of the other samples. In the case of A. vera leaf juice, significant effects as compared to the negative controls were observed at all three PPAR targets hinting to its high potential for metabolic syndrome therapy. For the dried leaves of L. tridentata, significant activity was only observed for the PPARα target, which is mainly associated with a potential for the treatment of anti-hyperlipidaemia.

References:

[1] Matsuura N, Gamo K, Miyachi H, Iinuma M, Kawada T, Takahashi N, Akao Y, Tosa H. γ-Mangostin from Garcinia mangostana pericarps as a dual agonist that activates both PPARα and PPARδ. Biosci Biotechnol Biochem 2013; 77: 2430 – 2435