Planta Med 2011; 77 - P_105
DOI: 10.1055/s-0031-1273634

Evaluation of the Biological Activity of Panamanian Plants through a Series of In vitro Assays

Y Vasquez 1, SI Khan 1, 2, MP Gupta 3, IA Khan 1, 2, 4
  • 1National Center for Natural Products Research, University of Mississippi, University, MS 38677, USA
  • 2Department of Pharmacognosy, School of Pharmacy, University of Mississippi, University, MS 38677, USA
  • 3Center for Pharmacognostic Research of the Panamanian Flora, School of Pharmacy, University of Panama, Panama
  • 4Department of Pharmacognosy, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia

In search of new biologically active compounds from natural sources, a collection of Panamanian plant extracts from the repository of NCNPR was evaluated through a series of target based cellular assays related to metabolic disorders such as Type II diabetes, hypercholesterolemia, inflammation, and obesity. The molecular targets selected to evaluate the biological activity of these plant extracts were: peroxisome proliferator-activated receptor (PPAR) isoforms (α and γ), nuclear factor kappa-B (NF-κB), and inducible nitric oxide synthase (iNOS). PPARs are involved in regulation of carbohydrate and lipid metabolism. NF-κB is a transcription factor that regulates the genes involved in inflammation and cancer. iNOS plays a key role in regulation of blood pressure, immune system, infection and inflammation. Due to a close association of metabolic syndrome, with oxidative stress and inflammatory processes, there has been an increased interest in these molecular targets and the drugs affecting them are emerging as important class of therapeutic agents. Reporter gene assays were used to screen the plant extracts for their activity on PPARα, PPARγ and NF-κB while iNOS inhibition was determined in terms of nitrite levels in cell supernatants. Out of 83 plant extracts, 13 showed activation on PPARα and 5 showed activation of PPARγ. Eight extracts showed activation of both PPARα and γ. Their effect on the expression of PPARs was determined by Western blot analysis. Cytotoxity was also evaluated in the corresponding cell lines. To further explore the anti-inflammatory potential of these plants, they are being screened for their effects on NF-κB and iNOS. Three plants showing PPAR activation were selected for the bioguided fractionation based on the history of their medicinal use, previously reported pharmacological activities and phytochemical background.

Acknowledgements: Financial support (Yelkaira Vasquez) by Secretaria Nacional de Ciencia y Tecnologia (SENACYT) in collaboration with the Instituto para la Formacion de Recursos Humanos (IFARHU) from the Panamanian government is acknowledged. Partial support of this work from The United States Department of Agriculture, Agricultural Research Service Specific Cooperative Agreement No. 58–6408–2-0009 is also acknowledged.