grayanotoxin-iii and Pain

Nine new grayanoids (1-9), together with 11 known compounds, were isolated from the roots of Rhododendron molle. The structures of the new compounds (1-9) were determined on the basis of spectroscopic analysis, including HRESIMS, and 1D and 2D NMR data. Compounds 4, 6, 12, and 14-20 showed significant antinociceptive activities in an acetic acid-induced writhing test. In particular, 14 and 15 were found to be more potent than morphine for both acute and inflammatory pain models and 100-fold more potent than gabapentin in a diabetic neuropathic pain model.

Topics: Amines; Analgesics; Animals; Cyclohexanecarboxylic Acids; Disease Models, Animal; Diterpenes; Drugs, Chinese Herbal; Female; Gabapentin; gamma-Aminobutyric Acid; Male; Mice; Molecular Structure; Morphine; Nuclear Magnetic Resonance, Biomolecular; Pain; Plant Roots; Rhododendron