Planta Med 2012; 78 - P_144
DOI: 10.1055/s-0032-1307652

Fatty Acids with In Vitro Binding Affinity for Human Opioid Receptors from the Fungus UK-101

AH Tarawneh 1, MM Radwan 2, 3, X Wang 1, O Dale 1, A Husni 1, SP Manly 2, HG Cutler 4, S Cutler 1
  • 1Department of Medicinal Chemistry
  • 2National Center for Natural Products Research, School of Pharmacy, The University of Mississippi, University, MS 38677.
  • 3Faculty of Pharmacy, University of Alexandria, Alexandria, Egypt.
  • 4Natural Products Discovery Group, College of Pharmacy and Health Sciences, Mercer University, Atlanta, Georgia, 30341

Bioassay guided fractionation of the EtOAc extract of the endophytic fungus UK-101 resulted in the isolation of a mixture of two fatty acids. This mixture showed 100% binding affinity to human delta opioid receptors. These two fatty acids were identified as Palmitic (1) and linoleic (2) acids by 1D and 2D NMR as well as GCMS after methylation. Mixtures of the two fatty acids of different ratios were prepared and their IC50 and Ki values were determined. We found that the activity of the pure compounds are less than that of the mixture. These findings have important implications for psychoactive studies with this class of compounds.

hDOR binding MRCUT-01–14-A 100406

Acknowledgment. This project is supported by Grant Number 5P20RR021929 from the National Center for Research Resources (NCRR), a component of the National Institutes of Health (NIH). The content is solely the responsibility of the authors and does not necessarily represent the official views of the National Center for Research Resources or the National Institutes of Health. Furthermore, this investigation was conducted in a facility constructed with support from research facilities improvement program C06 RR-14503–01 from the NIH National Center for Research Resources