In a previous report, we demonstrated that ginsenoside Rc, one of major ginsenosides from Panax ginseng, enhances γ-aminobutyric acid (GABA) receptorA (GABAA)-mediated ion channel currents. However, little is known about the effects of ginsenoside metabolites on GABAA receptor channel activity. The present study investigated the effects of ginsenoside metabolites on human recombinant GABAA receptor (α1β1γ2s) channel activity expressed in Xenopus oocytes using a two-electrode voltage clamp technique. M4, a metabolite of protopanaxatriol ginsenosides, more potently inhibited the GABA-induced inward peak current (IGABA ) than protopanaxadiol (PPD), a metabolite of PPD ginsenosides. The effect of M4 and PPD on IGABA was both concentration-dependent and reversible. The half-inhibitory concentration (IC50) values of M4 and PPD were 17.1±2.2 and 23.1±8.6 μM, respectively. The inhibition of IGABA by M4 and PPD was voltage-independent and non-competitive. This study implies that the regulation of GABAA receptor channel activity by ginsenoside metabolites differs from that of ginsenosides.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3659565 | PMC |
| http://dx.doi.org/10.5142/jgr.2012.36.1.55 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Mechanism of sodium nitroprusside regulating ginseng quality.
Sci Rep
January 2025
Department of Pharmacognosy, Heilongjiang University of Chinese Medicine, Harbin, 150040, Hei-longjiang, China.
The roots of Panax ginseng C. A. Meyer (ginseng) are one of the traditional medicinal herbs in Asian countries and is known as the "king of all herbs".
View Article and Find Full Text PDFStudy on the impact of β-CD inclusion complex on the in vivo metabolism of ginsenoside Re: A pharmacokinetic, metabolite analysis, and tissue distribution investigation in a rat model.
Eur J Pharm Sci
January 2025
Changchun University of Chinese Medicine, Jilin Ginseng Aacademy, Changchun 130117, PR China. Electronic address:
Triol-type ginsenoside Re (GS-Re) exhibits potent anti-myocardial ischemia-reperfusion effects, but its clinical use is hindered by poor bioavailability. This study evaluates the impact of β-cyclodextrin (β-CD) inclusion on GS-Re bioavailability and tissue dynamics in rat models. The GS-Re-β-CD complex was prepared using aqueous stirring and characterized.
View Article and Find Full Text PDFGenome-Wide Identification and Characterization of Gene Family in (Cucurbitaceae).
Life (Basel)
December 2024
Xi'an Botanical Garden of Shaanxi Province, Institute of Botany of Shaanxi Province, No. 17 Cuihua South Road, Xi'an 710061, China.
is a traditional Chinese medicinal plant of considerable application value and commercial potential, primarily due to its production of various bioactive compounds, particularly dammarane-type triterpenoid saponins that are structurally analogous to ginsenosides. Oxidosqualene cyclase (OSC), a pivotal enzyme in the biosynthesis of triterpenoid metabolites in plants, catalyzes the conversion of oxidosqualene into triterpenoid precursors, which are essential components of the secondary metabolites found in . To elucidate the role of gene family members in the synthesis of gypenosides within , this study undertook a comprehensive genome-wide identification and characterization of genes within and compared their expression levels across populations distributed over different geographical regions by both transcriptome sequencing and qRT-PCR experimental validation.
View Article and Find Full Text PDFHypoglycemic Effect of Ginsenoside Compound K Mediated by N-Acetylserotonin Derived From Gut Microbiota.
Phytother Res
January 2025
Engineering Research Center of Applied Technology of Pharmacogenomics (Ministry of Education, China), Hunan Key Laboratory of Pharmacomicrobiomics, Department of Clinical Pharmacology, Xiangya Hospital, Central South University, Changsha, China.
Article Synopsis
- Ginsenoside compound K (GCK) has a significant hypoglycemic effect related to gut microbiota, but its precise mechanisms, especially in high-fat-diet-induced type 2 diabetes (T2D), are not well understood.
- The study involved creating a diabetic mouse model and conducting fecal microbiota transplantation to explore GCK's role in regulating blood sugar levels.
- Results indicated that GCK improved metabolic disorders and changed gut microbiota, leading to increased levels of N-acetylserotonin (NAS) and glucagon-like peptide-1 (GLP-1), thereby enhancing insulin sensitivity in the diabetic mice.
Protective effect of compound K against podocyte injury in chronic kidney disease by maintaining mitochondrial homeostasis.
Sci Rep
January 2025
The Second Affiliated Hospital of Zhejiang Chinese Medical University, Hangzhou, People's Republic of China.
Chronic kidney disease (CKD) stands as a formidable global health challenge, often advancing to end-stage renal disease (ESRD) with devastating morbidity and mortality. At the central of this progression lies podocyte injury, a critical determinant of glomerular dysfunction. Compound K (CK), a bioactive metabolite derived from ginsenoside, has emerged as a compelling candidate for nephroprotective therapy.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!