Rationale: Hyperforin has been identified as an active constituent of Hypericum perforatum but its importance in the antidepressant effect of this plant's extracts is not really known.
Objective: To evaluate the antidepressant-like activity of two extracts in relation to the content of hyperforin and its plasma and whole brain concentrations, compared with a stable salt of hyperforin (dicyclohexylammonium; DCHA).
Methods: The effects of the extracts and hyperforin were evaluated in the rat forced swimming test. The specificity of the effects was demonstrated evaluating the rats' locomotor activity. Plasma and brain concentrations of hyperforin were determined by high performance liquid chromatography.
Results: The 4.5% extract (but not the 0.5% extract) given as three IP injections in 24 h (3.12-6.25 mg/kg) reduced the total immobility of rats, yielding dose-related plasma concentrations of hyperforin. These concentrations were of a similar magnitude to those after hyperforin DCHA which also significantly reduced immobility when given on the basis of the hyperforin content of the 4.5% extract (0.14 and 0.28 mg/kg). However, hyperforin was undetectable in rat brain, possibly because of poor passage of the blood-brain barrier.
Conclusion: These results support the view that hyperforin plays a key role in the antidepressant-like activity of Hypericum p. However, brain concentrations after effective doses are probably far from those active in vitro on the neurotransmitter mechanisms so far investigated.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1007/s00213-002-1229-5 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Antidepressant- and Anxiolytic-like Effects in Mice of Alkaloids from Aerial Parts of Link & Otto.
Pharmaceuticals (Basel)
January 2025
Instituto Politécnico Nacional, Centro de Nanociencias y Micro y Nanotecnologías, Unidad Profesional Adolfo López Mateos, Av. Luis Enrique Erro S/N, Colonia Zacatenco, Mexico City 07738, Mexico.
Link & Otto, an endemic plant of Mexico, is widely distributed in the central area of the country, mainly in the states of Tlaxcala, Puebla, and the State of Mexico. Ethnobotanical studies in different communities of these states have demonstrated that it is primarily used to treat diabetes and mental illnesses, such as "los nervios" (nerves) and "el ansia" (anxiety); these terms are used in traditional medicine, but it is accepted that they refer to anxiety disorders. This study aimed to validate the traditional use of aerial parts of Link & Otto in treating these illnesses.
View Article and Find Full Text PDFStudy of the Pharmacological Activity Spectrum of the New Original NT-3 Mimetic Dipeptide GTS-302.
Dokl Biochem Biophys
January 2025
Center for Strategic Planning and Management of Biomedical Health Risks, Federal Medical and Biological Agency, Moscow, Russia.
Unlabelled: The association of the pathogenesis of neurodegenerative diseases, depression, anxiety, and cognitive disorders with neurotrophin-3 deficiency determines the prospect of creating drugs with a similar mechanism of action. Since the use of full-length NT-3 is limited by unsatisfactory pharmacokinetic properties, the creation of low-molecular mimetics of neurotrophin-3 that are active when administered systemically is relevant. The Federal Research Center for Innovator and Emerging Biomedical and Pharmaceutical Technologies has created a dimeric dipeptide mimetic of the 4th loop of NT-3, hexamethylenediamide bis-(N-γ-oxybutyryl-L-glutamyl-L-asparagine) with the laboratory code GTS-302, which activates TrkC and TrkB receptors.
View Article and Find Full Text PDFKnowledgebase-Driven Exploration and Experimental Verification of Simvastatin's Inhibitory Impact on P2X7/NLRP3 Inflammasome Pathway.
Chem Biol Drug Des
January 2025
College of Pharmacology Sciences, Zhejiang University of Technology, Hangzhou, People's Republic of China.
Depression is a mental health disorder and is the fourth most prevalent disease. Previous studies have suggested that statins are involved in the reduction of neuroinflammation. However, the potential mechanism for this relationship is unclear.
View Article and Find Full Text PDFDiscovery of Brain-Penetrative Negative Allosteric Modulators of NMDA Receptors Using FEP-Guided Structure Optimization and Membrane Permeability Prediction.
J Chem Inf Model
January 2025
Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University, 44 West Culture Road, Jinan 250012, Shandong, China.
-Methyl-d-aspartate (NMDA) receptors, a subtype of ionotropic glutamate receptors in the central nervous system (CNS), have garnered attention for their role in brain disorders. Specifically, GluN2A-containing NMDA receptors have emerged as a potential therapeutic target for the treatment of depressive disorders and epilepsy. However, the development of GluN2A-containing NMDA receptor-selective antagonists, represented by -(4-(2-benzoylhydrazine-1-carbonyl)benzyl)-3-chloro-4-fluorobenzenesulfonamide (TCN-201) and its derivatives, faces a significant challenge due to their limited ability to penetrate the blood-brain barrier (BBB), hampering their characterization and further advancement.
View Article and Find Full Text PDFand formula alleviates depressive behaviors microglia regulation in an unpredictable chronic mild stress animal model.
J Tradit Complement Med
January 2025
Institute of Food Science and Technology, College of Bioresources and Agriculture, National Taiwan University, Taipei, Taiwan.
Background And Aim: (CM) and (AM) are medicinal mushrooms with potential applications in the treatment of mood disorders, including depression and anxiety. While research suggests that both CM and AM possess anti-inflammatory properties and hold potential for treating depression when administered separately, there is limited knowledge about their efficacy when combined in a formula, as well as the underlying mechanism involving the modulation of microglia.
Experimental Procedure: Rats received oral administrations of the low-dose formulation, medium-dose formulation, and high-dose formulation over 28 consecutive days as part of the UCMS protocols.
Want 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!