Sixteen new quinolizidine alkaloids (QAs), named ormosianines A-P (-), and 18 known congeners (-) were isolated from the stems and leaves of . The structures were elucidated based on spectroscopic analyses and electron circular dichroism (ECD) calculations. Structurally, ormosianines A () and B () are the first examples of cytisine and type alkaloids with the cleavage of the piperidine ring. Results of the acetylcholinesterase (AChE) inhibitory assay revealed that the pentacycline type QAs, including , , , and -, are good AChE inhibitors. Ormosianine A () exhibited more potent AChE inhibitory activity with an IC value of 1.55 μM. Molecular docking revealed that might bind to the protein 1DX4, forming two hydrogen bonds with residues SER-238 and HIS-480.
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http://dx.doi.org/10.1021/acs.jnatprod.3c00493 | DOI Listing |
J Sci Food Agric
January 2025
Department of Chemistry, Faculty of Science and Technology, Rajamangala University of Technology Thanyaburi, Thailand.
Background: Edible insects are used for consumption and traditional medicine due to their rich bioactive compounds. This study examined the bioactive compounds and inhibitory effects of crude extracts from Bombyx mori and Omphisa fuscidentalis on α-glucosidase, α-amylase, acetylcholinesterase (AChE), and tyrosinase. Fatty acids, including n-hexadecanoic acid and oleic acid, were identified in the extracts and evaluated for their inhibitory potential against the enzymes in vitro and in silico.
View Article and Find Full Text PDFNutrients
December 2024
Biohazard Prevention Centre, Faculty of Biology and Environmental Protection, University of Lodz, Pomorska 141/143, 90-236 Lodz, Poland.
Flavonoids are naturally occurring polyphenolic compounds known for their extensive range of biological activities. This review focuses on the inhibitory effects of flavonoids on acetylcholinesterase (AChE) and their potential as therapeutic agents for cognitive dysfunction. AChE, a serine hydrolase that plays a crucial role in cholinergic neurotransmission, is a key target in the treatment of cognitive impairments due to its function in acetylcholine hydrolysis.
View Article and Find Full Text PDFInt J Mol Sci
January 2025
Instituto de Investigação e Inovação em Saúde da Universidade do Porto-i3S, R. Alfredo Allen 208, 4200-135 Porto, Portugal.
Diffuse noxious inhibitory control (DNIC), also known as conditioned pain modulation (CPM) in humans, is a paradigm wherein the heterotopic application of a noxious stimulus results in the attenuation of another spatially distant noxious input. The pre-clinical and clinical studies show the involvement of several neurochemical systems in DNIC/CPM and point to a major contribution of the noradrenergic, serotonergic, and opioidergic systems. Here, we thoroughly review the latest data on the monoaminergic and opioidergic studies, focusing particularly on pre-clinical models of chronic pain.
View Article and Find Full Text PDFMolecules
January 2025
Foodomics Laboratory, Institute of Food Science Research (CIAL) (CSIC-UAM), Nicolás Cabrera 9, 28049 Madrid, Spain.
Propolis is a valuable natural resource for extracting various beneficial compounds. This study explores a sustainable extraction approach for Brazilian green propolis. First, supercritical fluid extraction (SFE) process parameters were optimized (co-solvent: 21.
View Article and Find Full Text PDFMolecules
December 2024
Structural Bioinformatics Laboratory, Faculty of Science and Engineering, Åbo Akademi University, Tykistökatu 6, 20520 Turku, Finland.
Transient receptor potential vanilloid (TRPV) 4 is involved in signaling pathways specifically mediating pain and inflammation, making it a promising target for the treatment of various painful and inflammatory conditions. However, only one drug candidate targeting TRPV4 has entered the clinical trials. To identify potential TRPV4 inhibitors for drug development, we screened a library of ion channel-modulating compounds using both structure- and ligand-based virtual screening approaches.
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