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Evaluation of In Vitro Inhibition of -Hematin Formation: A Step Towards a Comprehensive Understanding of the Mechanism of Action of New Arylamino Alcohols.
Microorganisms
December 2024
Agents Infectieux, Résistance et Chimiothérapie (AGIR), UR 4294, Université de Picardie Jules Verne, 1 rue des Louvels, 80037 Amiens, France.
Currently, artemisinin-based combination therapy is recommended as first-line treatment of uncomplicated malaria. Arylamino alcohols (AAAs) such as mefloquine (MQ) are the preferred partner drugs due to their longer half-life, reliable absorption and strong antimalarial activity. However, the mode of action of MQ remains poorly understood and its neurotoxicity limits its use.
View Article and Find Full Text PDFNovel frontiers through nitrogen substitution at 6th, 10th and 11th position of artemisinin: Synthetic approaches and antimalarial activity.
Eur J Med Chem
January 2025
Department of Chemistry, Banasthali University, Banasthali Newai, 304022, Rajasthan, India; Department of Education in Science and Mathematics (DESM), Regional Institute of Education (NCERT), Bhubaneshwar, 751022, India. Electronic address:
Malaria pertains to an array of catastrophic illnesses spurred on by the Plasmodium spp. Artemisinin (ART) is currently prescribed in conjunction with another medication as part of therapeutic regimens for acute malaria. These currently prescribed pharmaceuticals have been around for a while, even after lack of required thermos-metabolic stabilities, alongside fresh proclaims about surfacing resistance and neurotoxicity linked with sequential administration of such combination therapies.
View Article and Find Full Text PDFThe Potential Role of Artemisinins Against Neurodegenerative Diseases.
Am J Chin Med
November 2024
Growth, Development, and Mental Health of Children and Adolescence Center, Pediatric Research Institute, Ministry of Education, Key Laboratory of Child Development and Disorders, National Clinical Research Center for Child Health and Disorders, Chongqing Key Laboratory of Child Neurodevelopment and Cognitive Disorders, Children's Hospital of Chongqing Medical University, Chongqing 400014, P. R. China.
Artemisinin (ART) and its derivatives, collectively referred to as artemisinins (ARTs), have been approved for the treatment of malaria for decades. ARTs are converted into dihydroartemisinin (DHA), the only active form, which is reductive . In this review, we provide a brief overview of the neuroprotective potential of ARTs and the underlying mechanisms on several of the most common neurodegenerative diseases, particularly considering their potential application in those associated with cognitive and motor impairments including Alzheimer's disease (AD), Parkinson's disease (PD), Huntington's disease (HD), and amyotrophic lateral sclerosis (ALS).
View Article and Find Full Text PDFArtemisinin Ameliorates the Neurotoxic Effect of 3-Nitropropionic Acid: A Possible Involvement of the ERK/BDNF/Nrf2/HO-1 Signaling Pathway.
Mol Neurobiol
September 2024
Department of Pharmacology, Central University of Punjab, Bathinda, India.
Neurodegenerative disorders like Huntington's disease (HD) are a major threat to human health, with severe gait abnormalities and pathological changes (oxidative stress, neuroinflammation, and apoptosis) playing important roles in their development. The effects of artemisinin (ART) alone and in combination with the ERK antagonist PD98059 against 3-nitropropionic acid (3-NPA)-induced cell death and oxidative stress in SH-SY5Y cells were determined using the MTT and DCFH-DA assays, as well as RT-qPCR assays. In vivo, possible neuroprotective effects of ART (10, 20, and 40 mg/kg i.
View Article and Find Full Text PDFTargeting mA mRNA demethylase FTO alleviates manganese-induced cognitive memory deficits in mice.
J Hazard Mater
September 2024
Department of Environmental Health, School of Public Health, China Medical University, Shenyang, China; Key Laboratory of Environmental Stress and Chronic Disease Control & Prevention, Ministry of Education, China Medical University, Shenyang, China; Engineering research center of Liaoning Province on environmental health technology and equipment, China Medical University, Shenyang, China; Institute of Health Professions Education Assessment and Reform, China Medical University, Shenyang, China. Electronic address:
Manganese (Mn) induced learning and memory deficits through mechanisms that are not fully understood. In this study, we discovered that the demethylase FTO was significantly downregulated in hippocampal neurons in an experimental a mouse model of Mn exposure. This decreased expression of FTO was associated with Mn-induced learning and memory impairments, as well as the dysfunction in synaptic plasticity and damage to regional neurons.
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