The model Tele-Stereo-EEG (continuous recording of intracerebral field potentials in the freely moving rat to produce an electropharmacogram) has been used to see if L-theanine- and theogallin-enriched decaffeinated green tea extract would change electrical brain activity after oral administration, to provide proof of access of active components to the brain via the blood-brain barrier. Baseline recording (45 min) was followed by a 5-h recording session after oral ingestion of the extract or single components: L-theanine, theogallin and quinic acid, a suggested metabolite of theogallin. Power spectra from Fast Fourier Transformed (FFT) field potential changes were divided into six frequency bands (delta, theta, alpha1, alpha2, beta1 and beta2). No effects could be measured using a saline solution for control purposes. Oral administration of 75 mg kg(-1) total extract led to power decreases mainly in delta and alpha2 frequencies during the first hour. This pattern has been observed in the presence of stimulatory synthetic compounds. Oral administration of 30 mg kg(-1) L-theanine led to power decreases of nearly all frequencies, being more pronounced during the second and following hours in comparison with the first hour. Ingestion of 20 mg kg(-1) theogallin also showed a power decreasing effect on cortical activity. Its possible metabolite quinic acid (10 mg kg(-1), p.o.) also produced decreases in delta, alpha2 and beta1 frequencies. Measurement of motion resulted in an increase during the first hour in the presence of theogallin and L-theanine. A tendential decrease was observed in the presence of L-theanine during the last hour at its presumably highest plasma levels. The results with the administration of the total extract provided evidence for the maior involvement of L-theanine and theogallin (or its presumable metabolite quinic acid) in its action, since no other active compounds were present in the extract. These compounds could be classified by comparison with reference drugs using discriminant analysis as being antidepressive and cognition enhancing, respectively. The extract appeared among those drugs having stimulatory effects.
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http://dx.doi.org/10.1211/jpp.59.10.0010 | DOI Listing |
J Child Adolesc Psychopharmacol
January 2025
Director of Co-Founder and Founder of Schizophrenia Society, University of Cincinnati, Cincinnati, Ohio, USA.
Bipolar disorder often begins in adolescence or early adulthood, characterized by recurrent manic episodes that can lead to neurodegenerative brain changes and functional decline. While several oral second-generation antipsychotics are Food and Drug Administration (FDA)-approved for mania, adherence to maintenance treatment is frequently poor due to factors such as anosognosia, cognitive dysfunction, impulsivity, side effects aversion, and substance use. Long-acting injectable (LAI) antipsychotics, approved for adults with bipolar mania or schizoaffective disorder (bipolar type), offer a potential solution for adolescents with similar conditions.
View Article and Find Full Text PDFNeuropsychopharmacol Hung
December 2024
College of Medicine, University of Kentucky, Lexington, KY 40506, USA.
Objective: Benzodiazepines, particularly lorazepam, are good options for acute catatonia treatment. Published catatonia literature on benzodiazepine maintenance treatment and benzodiazepine tolerance is limited.
Methods: This is a chart review covering 30 years of clinical experience in the state of Kentucky, (United States of America), where there was no easy access to electroconvulsive therapy.
J Med Chem
January 2025
State Key Laboratory of Natural Medicines, Departemnt of TCMs Pharmaceuticals, School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing 210009, China.
Chemotherapy-induced myelosuppression (CIM) significantly impairs hematopoiesis. Trilaciclib (TC), originally developed for oncology application, is the only FDA-approved CDK4/6 inhibitor for CIM, which effectively protects bone marrow cells by inhibiting their proliferation. In this study, a series of TC derivatives were designed and synthesized as CDK4/6 inhibitors (CDK4/6i) for alleviating CIM.
View Article and Find Full Text PDFPharm Biol
December 2025
Laboratory of Pharmacology, Chulabhorn Research Institute, Bangkok, Thailand.
Aim: Insufficient quality control and limited dissolution of extract capsules restricts their bioavailability and hinder the clinical use for treating mild coronavirus disease 2019 (COVID-19) patients.
Objective: This study aims to investigate pharmacokinetics and safety of high-dosage ethanolic extract (equivalent to 180 or 360 mg/day of andrographolide), relevant dosages used for mild COVID-19 treatment.
Methods: An open-label, single-dose, and repeated-dose conducted in healthy volunteers.
Cytotechnology
February 2025
Henan International Joint Laboratory for Nuclear Protein Regulation, School of Basic Medical Sciences, Henan University, Kaifeng, 475004 Henan China.
Autophagy is a conservative process of self degradation, in which abnormal organelles, proteins and other macromolecules are encapsulated and transferred to lysosomes for subsequent degradation. It maintains the intracellular balance, and responds to cellular conditions such as hunger or stress. To date, there are mainly three types of autophagy: macroautophagy, microautophagy and chaperone-mediated autophagy.
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