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Molecular Mechanisms of Nicergoline from Ergot Fungus in Blocking Human 5-HT3A Receptor.
J Microbiol Biotechnol
November 2024
Department of Biotechnology and Department of Integrative Food, Bioscience and Biotechnology (BK21 FOUR), Chonnam National University, Gwangju 61186, Republic of Korea.
This study investigates the modulatory effects of nicergoline, a major bioactive compound derived from ergot fungus, on the 5-hydroxytryptamine 3A (5-HT3A) receptor. Utilizing a two-electrode voltage-clamp technique, we evaluated the impact of nicergoline on the 5-HT-induced inward current (I) in 5-HT3A receptors. Our findings reveal that nicergoline inhibits I in a reversible and concentration-dependent manner.
View Article and Find Full Text PDFRepurposing FDA-approved drugs targeting FZD10 in nasopharyngeal carcinoma: insights from molecular dynamics simulations and experimental validation.
Sci Rep
December 2024
Department of Biochemistry, Faculty of Science, Mahidol University, 272 Rama VI Road, Thung Phayathai, Ratchathewi, Bangkok, 10400, Thailand.
Wnt signaling is a critical pathway implicated in cancer development, with Frizzled proteins, particularly FZD10, playing key roles in tumorigenesis and recurrence. This study focuses on the potential of repurposed FDA-approved drugs targeting FZD10 as a therapeutic strategy for nasopharyngeal carcinoma (NPC). The tertiary structure of human FZD10 was constructed using homology modeling, validated by Ramachandran plot and ProQ analysis.
View Article and Find Full Text PDFMedications to Modify Aspiration Risk: Those That Add to Risk and Those That May Reduce Risk.
Semin Respir Crit Care Med
December 2024
Grupo Infeção e Desenvolvimento em Sépsis (GIS-ID), Porto, Portugal.
Aspiration pneumonia results from the abnormal entry of fluids into the respiratory tract. We present a review of drugs known to affect the risk of aspiration. Drugs that increase the risk of aspiration pneumonia can be broadly divided into those that affect protective reflexes (like cough and swallowing) due to direct or indirect mechanisms, and drugs that facilitate gastric dysbiosis or affect esophageal and intestinal motility.
View Article and Find Full Text PDFBlocking α Adrenergic Receptor as a Novel Target for Treating Alzheimer's Disease.
ACS Chem Neurosci
September 2024
Key Laboratory of Endemic and Ethnic Diseases, Laboratory of Molecular Biology, Ministry of Education, Guizhou Medical University, Guiyang 550004, China.
While amyloidopathy and tauopathy have been recognized as hallmarks in Alzheimer's disease (AD) brain, recently, increasing lines of evidence have supported the pathological roles of cerebrovascular changes in the pathogenesis and progression of AD. Restoring or ameliorating the impaired cerebrovascular function during the early phase of the disease may yield benefits against the cognitive decline in AD. In the present study, we evaluated the potential therapeutic effects of nicergoline [NG, a well-known α1 adrenergic receptor (ADR) blocker and vasodilator] against AD through ameliorating vascular abnormalities.
View Article and Find Full Text PDFPharmacological treatments for vascular dementia: a systematic review and Bayesian network meta-analysis.
Front Pharmacol
August 2024
Department of General Surgery, Chengdu Integrated Traditional Chinese Medicine and Western Medicine Hospital, Chengdu, China.
Background: Vascular dementia (VaD) is one of the most prevalent, burdensome, and costly forms of dementia. Pharmacological treatment is often the first-line choice for clinicians; however, there is a paucity of comparative information regarding the multiple available drug options.
Methods And Analysis: A systematic review and network meta-analysis were conducted on randomized trials involving adult patients with VaD, sourced from PubMed, the Cochrane Library, EMBASE, Web of Science, OPENGREY, ClinicalTrials.
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