Inhibitory effect of oleanolic acid from the rhizomes of Cyperus rotundus on transient receptor potential vanilloid 1 channel.
Cyperus rotundus is used as an analgesic and sedative in oriental medicine and has been reported to exhibit antinociceptive and anti-inflammatory effects. On the other hand, the transient receptor potential vanilloid 1 channel is a nonselective cation channel that senses various noxious chemical and thermal stimuli. However, it has recently been reported that the epidermally expressed transient receptor potential vanilloid 1 channel is involved in heat- and UV-induced skin aging. The aim of this study was to evaluate whether C. rotundus extract and its constituents can inhibit this channel. Ethylacetate and hexane fractions of the methanol extract were found to partially inhibit transient receptor potential vanilloid 1 channel activity, and at a concentration of 90 µM, oleanolic acid, which was one of three constituents isolated from the ethylacetate fraction, inhibited this activity by 61.4 ± 8.0 %. This is first electrophysiological study to be conducted on the effects of C. rotundus extract and its constituents on the transient receptor potential vanilloid 1 channel. The results obtained provide insight of the potential therapeutic effects of C. rotundus in the contexts of analgesia and UV-induced photoaging.
Department of Physiology, Dongguk University College of Medicine, Kyungju, Republic of Korea.
Joo Hyun
JH
Nam
Division of Bioscience, Dongguk University, Gyeongju, Republic of Korea.
Dong-Ung
DU
Lee
D002211:Capsaicin / Q000494:pharmacology; D002392:Catechin / Q000494:pharmacology; D029786:Cyperus / Q000737:chemistry*; D004305:Dose-Response Relationship, Drug; D004353:Drug Evaluation, Preclinical / Q000379:methods; D004610:Ellagic Acid / Q000494:pharmacology; D057809:HEK293 Cells / Q000187:drug effects; D006801:Humans; D009828:Oleanolic Acid / Q000008:administration & dosage / Q000494:pharmacology*; D018408:Patch-Clamp Techniques; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology; D027343:Rhizome / Q000737:chemistry; D050916:TRPV Cation Channels / Q000037:antagonists & inhibitors* / Q000378:metabolism
D010936:Plant Extracts; D050916:TRPV Cation Channels; C494482:TRPV1 protein, human; D004610:Ellagic Acid; D009828:Oleanolic Acid; D002392:Catechin; D002211:Capsaicin