Huperzia saururus (Lam.) Trevis. (Lycopodiaceae) is used widely in Argentinian traditional medicine as an aphrodisiac and for memory improvement. An aqueous extract from the aerial parts was obtained by decoction, revealing the presence of alkaloids, among other constituents. By partition with organic solvent in alkaline media, alkaloids were extracted and then purified by gel permeation. We studied the anticholinesterase activity in vitro of the alkaloid extract using erythrocyte membranes and human serum as sources of acetylcholinesterase and pseudocholinesterase, respectively. The results show a marked inhibition of true acetylcholinesterase with an IC50 value of 0.58 microg/ml. Low inhibition of pseudocholinesterase was observed (IC50 value = 191 microg/ml). This shows a selectivity of the extract for the true acetylcholinesterase. Furthermore, chemical study of the bioactive extract was performed by GC-MS, revealing the presence of seven Lycopodium alkaloids, including some not identified previously: sauroxine, 6-hydroxylycopodine, N-acetyllycodine, lycopodine, lycodine, N-methyllycodine, and clavolonine. Further investigations will be undertaken in order to discover which compound/s are responsible for the aqueous extract's acetylcholinesterase activity.
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http://dx.doi.org/10.1016/j.phymed.2003.07.006 | DOI Listing |
Cureus
December 2024
Emergency Medicine, North West Regional Hospital, Burnie, AUS.
Organophosphate (OP) compounds, developed during World War II, are a group of chemicals used as pesticides, insecticides and herbicides. As irreversible inhibitors of the enzyme acetylcholinesterase (AChE), they reduce anti-cholinesterase activity and therefore increase acetylcholine (ACh) levels at the neuromuscular junction (NMJ). Diazinon, the OP leading to the patient's symptoms in this report, is an amber-brown liquid that was once the most widely used insecticide in the United States of America.
View Article and Find Full Text PDFSci Rep
January 2025
Department of Pharmacognosy, Faculty of Pharmacy, Cairo University, Cairo, 11562, Egypt.
Alzheimer's disease (AD) poses a global health challenge, demanding innovative approaches for effective treatments. Clerodendrum infortunatum Linn. (Lamiaceae) is a shrub traditionally used as a medicinal plant to treat inflammation, skin diseases, and bronchitis.
View Article and Find Full Text PDFJ Hypertens
February 2025
Key Laboratory of Shaanxi Province for Craniofacial Precision Medicine Research, College of Stomatology, Xi'an Jiaotong University, Xi'an, People's Republic of China.
Background: Preeclampsia (PE) is marked by hypertension and detrimental sterile inflammatory response. Despite the reported anti-inflammatory effect of pyridostigmine bromide (PYR) in different models, its anti-inflammatory mechanism in PE is unclear. This study assessed whether such an anti-inflammatory effect involves inhibition of placental Toll-like receptor 4 (TLR4) signaling.
View Article and Find Full Text PDFIn Vivo
December 2024
Doctoral School of Biomedical Sciences, University of Oradea, Oradea, Romania.
Background/aim: Alzheimer's disease is a complex, incurable to date, multifactorial disease, which suggests the need for continued development of pharmacotherapy.
Materials And Methods: A comprehensive literature search was conducted to identify known ligands with anticholinesterase activity, resulting in the discovery of over 100 alkaloids that are also available in the PubChem database. Subsequently, the ligands underwent molecular docking to evaluate their affinity for the target enzyme.
J Physiol
December 2024
Université Paris Cité, CNRS, ENS Paris Saclay, Centre Borelli UMR 9010, Paris, France.
Terminal Schwann cells (TSCs) are capable of regulating acetylcholine (ACh) release at the neuromuscular junction (NMJ). We have identified GABA as a gliotransmitter at mouse NMJs. When ACh activates α7 nicotinic ACh receptor (nAChRs) on TSCs, GABA is released and activates GABA receptors on the nerve terminal that subsequently reduce ACh release.
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