Activities of prenylphenol derivatives from fruitbodies of Albatrellus spp. on the human and rat vanilloid receptor 1 (VR1) and characterisation of the novel natural product, confluentin.
Several prenylphenols from basidiocarps of European and Chinese Albatrellus spp., namely grifolin (1), neogrifolin (2), confluentin (3), scutigeral (4), and albaconol (5) were investigated concerning their activities in test models for vanilloid receptor modulation. The isolation of these compounds from A. confluens and structure elucidation of the novel natural product confluentin (3) are described. The effects of scutigeral and neogrifolin on vanilloid receptors were studied by means of electrophysiological methodology on rat dorsal root ganglion neurons as well as on recombinant cell lines expressing the rat VR1 receptor. Concurrently, the effects of compounds 1-5 on a reporter cell line expressing the human vanilloid receptor VR1 were measured. In contrast to previous studies reported in the literature, the results of these investigations suggest that fungal prenylphenols act as weak antagonists (activity in the microM range), rather than exhibiting agonistic activities.
Hellwig
Veronika
V
Bayer Health Care, Pharma Research Center Wuppertal, PH-R EU ET Natural Products, Wuppertal, Germany.
Nopper
Reilinde
R
Mauler
Frank
F
Freitag
Joachim
J
Ji-Kai
Liu
L
Zhi-Hui
Ding
D
Stadler
Marc
M
D000818:Animals; D001487:Basidiomycota / Q000737:chemistry*; D016466:CHO Cells; D002851:Chromatography, High Pressure Liquid; D006224:Cricetinae; D004305:Dose-Response Relationship, Drug; D005727:Ganglia, Spinal / Q000166:cytology / Q000187:drug effects; D006801:Humans; D066298:In Vitro Techniques; D008163:Luminescent Measurements; D018408:Patch-Clamp Techniques; D010636:Phenols / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar; D011955:Receptors, Drug / Q000187:drug effects / Q000502:physiology; D013329:Structure-Activity Relationship
D010636:Phenols; D011955:Receptors, Drug; C476024:confluentin