PMID- 12020680 OWN - NLM STAT- MEDLINE DCOM- 20021008 LR - 20190624 IS - 0014-2999 (Print) IS - 0014-2999 (Linking) VI - 442 IP - 1-2 DP - 2002 May 3 TI - Effects of ginsenosides, active components of ginseng, on nicotinic acetylcholine receptors expressed in Xenopus oocytes. PG - 37-45 AB - We investigated the effects of ginsenosides, the active ingredient of ginseng, on neuronal or muscle-type nicotinic acetylcholine receptor channel activity expressed in Xenopus oocytes after injection of cRNA encoding bovine neuronal alpha3beta4, alpha7 or human muscle alphabetadeltavarepsilon subunits. Treatment with acetylcholine elicited an inward peak current (I(ACh)) in oocytes expressing nicotinic acetylcholine receptor subtypes. Cotreatment with ginsenoside Rg2 and acetylcholine inhibited I(ACh) in oocytes expressing with alpha3beta4 or alphabetadeltavarepsilon but not in oocytes expressing alpha7 nicotinic acetylcholine receptors. The inhibition of I(ACh) by ginsenoside Rg2 was reversible and dose-dependent. The half-inhibitory concentrations (IC50) of ginsenoside Rg2 were 60.2+/-14.1 and 15.7+/-3.5 microM in oocytes expressing alpha3beta4 and alphabetadeltavarepsilon nicotinic acetylcholine receptors, respectively. The inhibition of I(ACh) by ginsenoside Rg2 was voltage-independent and noncompetitive. Other ginsenosides besides ginsenoside Rg2 also inhibited I(ACh) in oocytes expressing alpha3beta4 or alphabetadeltavarepsilon nicotinic acetylcholine receptors. The order of potency for the inhibition of I(ACh) was ginsenoside Rg2>Rf>Re>Rg1>Rc>Rb2>Rb1 in oocytes expressing alpha3beta4 nicotinic acetylcholine receptors and was ginsenoside Rg2>Rf>Rg1>Re>Rb1>Rc>Rb2 in oocytes expressing alphabetadeltavarepsilon nicotinic acetylcholine receptors. These results indicate that ginsenosides might regulate nicotinic acetylcholine receptors in a differential manner and this regulation might be one of the pharmacological actions of Panax ginseng. FAU - Choi, Seok AU - Choi S AD - National Research Laboratory for the Study of Ginseng Signal Transduction and Department of Physiology, College of Veterinary Medicine, Chonnam National University, Kwangju, South Korea. FAU - Jung, Se Yeon AU - Jung SY FAU - Lee, Jun Ho AU - Lee JH FAU - Sala, Francisco AU - Sala F FAU - Criado, Manuel AU - Criado M FAU - Mulet, Jose AU - Mulet J FAU - Valor, Luis Miguel AU - Valor LM FAU - Sala, Salvador AU - Sala S FAU - Engel, Andrew G AU - Engel AG FAU - Nah, Seung Yeol AU - Nah SY LA - eng PT - Comparative Study PT - Journal Article PT - Research Support, Non-U.S. Gov't PL - Netherlands TA - Eur J Pharmacol JT - European journal of pharmacology JID - 1254354 RN - 0 (Ginsenosides) RN - 0 (Receptors, Nicotinic) RN - 0 (Saponins) RN - N9YNS0M02X (Acetylcholine) SB - IM MH - Acetylcholine/pharmacology MH - Animals MH - Cattle MH - Dose-Response Relationship, Drug MH - Female MH - Gene Expression MH - Ginsenosides MH - Humans MH - Membrane Potentials/drug effects MH - Oocytes/drug effects/metabolism MH - Panax/*chemistry MH - Receptors, Nicotinic/genetics/*physiology MH - Saponins/chemistry/*pharmacology MH - Xenopus laevis EDAT- 2002/05/22 10:00 MHDA- 2002/10/09 04:00 CRDT- 2002/05/22 10:00 PHST- 2002/05/22 10:00 [pubmed] PHST- 2002/10/09 04:00 [medline] PHST- 2002/05/22 10:00 [entrez] AID - S001429990201508X [pii] AID - 10.1016/s0014-2999(02)01508-x [doi] PST - ppublish SO - Eur J Pharmacol. 2002 May 3;442(1-2):37-45. doi: 10.1016/s0014-2999(02)01508-x.