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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
Author(s) -
Hellwig Veronika,
Nopper Reilinde,
Mauler Frank,
Freitag Joachim,
JiKai Liu,
ZhiHui Ding,
Stadler Marc
Publication year - 2003
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.200390008
Subject(s) - chemistry , receptor , natural product , dorsal root ganglion , trpv1 , cell culture , pharmacology , biochemistry , stereochemistry , dorsum , transient receptor potential channel , biology , anatomy , genetics
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 μM range), rather than exhibiting agonistic activities.