Activities of prenylphenol derivatives from fruitbodies of Albatrellus spp. on the human and rat vanilloid receptor 1 (VR 1) and characterisation of the novel natural product, confluentin
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In: Archiv der Pharmazie, Vol. 336, No. 2, 01.04.2003, p. 119-126.
Research output: Journal contributions › Journal articles › Research
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TY - JOUR
T1 - Activities of prenylphenol derivatives from fruitbodies of Albatrellus spp. on the human and rat vanilloid receptor 1 (VR 1) and characterisation of the novel natural product, confluentin
AU - Hellwig, Veronika
AU - Nopper, Reilinde
AU - Mauler, Frank
AU - Freitag, Joachim
AU - Ji-Kai, Liu
AU - Zhi-Hui, Ding
AU - Stadler, Marc
PY - 2003/4/1
Y1 - 2003/4/1
N2 - 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.
AB - 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.
KW - Chemistry
KW - Albaconol
KW - Basidiomycetes
KW - Grifolin
KW - Neogrifolin
KW - Pain
KW - Scutigeral
UR - http://www.scopus.com/inward/record.url?scp=0038373585&partnerID=8YFLogxK
U2 - 10.1002/ardp.200390008
DO - 10.1002/ardp.200390008
M3 - Journal articles
VL - 336
SP - 119
EP - 126
JO - Archiv der Pharmazie
JF - Archiv der Pharmazie
SN - 0365-6233
IS - 2
ER -