It is estimated that 50 million people in the world live with dementia, 60-70% of whom suffer from Alzheimer's disease (AD). Different factors are involved in the development of AD, including a reduction in the cholinergic neurotransmission level. The Amaryllidaceae plant family contains an exclusive, large, and still understudied alkaloid group characterized by a singular skeleton arrangement and a broad spectrum of biological activities. The chemistry and biodiversity of Ecuadorian representatives of the genus (Amaryllidaceae) have not been widely studied. In this work, five Ecuadorian species were examined in vitro for their activity towards the enzymes acetyl- (AChE) and butyrylcholinesterase (BuChE), and the alkaloid profile of bulb extracts was analyzed by GC-MS. The species and showed the most AChE and BuChE inhibitory activity, respectively. To obtain insight into the potential role of the identified alkaloids in these inhibitory effects, docking experiments were carried out, and cantabricine showed in silico inhibitory activity against both cholinesterase structures. Our results show that Amaryllidaceae species from Ecuador are a potential source of new drugs for the palliative treatment of AD.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7248819 | PMC |
| http://dx.doi.org/10.3390/molecules25092092 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Triterpene esters from Uncaria rhynchophylla hooks as potent HIV-1 protease inhibitors and their molecular docking study.
Sci Rep
December 2024
Department of Pharmacognosy, College of Pharmacy and Research Institute of Pharmaceutical Sciences, Seoul National University, 1 Gwanak-ro, Gwanak-gu, Seoul, 08826, Korea.
Despite significant advancements with combination anti-retroviral agents, eradicating human immunodeficiency virus (HIV) remains a challenge due to adverse effects, adherence issues, and emerging viral resistance to existing therapies. This underscores the urgent need for safer, more effective drugs to combat resistant strains and advance acquired immunodeficiency syndrome (AIDS) therapeutics. Eight triterpene esters (1-8) were identified from Uncaria rhynchophylla hooks.
View Article and Find Full Text PDFComputational design of potent dimeric phenylthiazole NS5A inhibitors for hepatitis C virus.
Sci Rep
December 2024
Bioinformatics Laboratory, College of Computing, University Mohammed VI Polytechnic, Ben Guerir, Morocco.
Hepatitis C virus (HCV) presents a significant global health issue due to its widespread prevalence and the absence of a reliable vaccine for prevention. While significant progress has been achieved in therapeutic interventions since the disease was first identified, its resurgence underscores the need for innovative strategies to combat it. The nonstructural protein NS5A is crucial in the life cycle of the HCV, serving as a significant factor in both viral replication and assembly processes.
View Article and Find Full Text PDFMetaplastic breast cancer (MpBC) is a highly chemoresistant subtype of breast cancer with no standardized therapy options. A clinical study in anthracycline-refractory MpBC patients suggested that nitric oxide synthase (NOS) inhibitor NG-monomethyl-l-arginine (L-NMMA) may augment anti-tumor efficacy of taxane. We report that NOS blockade potentiated response of human MpBC cell lines and tumors to phosphoinositide 3-kinase (PI3K) inhibitor alpelisib and taxane.
View Article and Find Full Text PDFSpecific Monitoring the DNA Helicase Function via Anchor-Embedded DNA Probe.
Adv Sci (Weinh)
December 2024
School of Pharmaceutical Sciences, Guangzhou University of Chinese Medicine, Guangzhou, 510006, China.
DNA helicases play a pivotal role in maintaining genome integrity by unwinding the DNA double helix and are often considered promising targets for drug development. However, assessing specific DNA helicase activity in living cells remains challenging. Herein, the first anchor-embedded duplex (ATED) probe, 17GC, is constructed to uniquely monitor the unwinding activity of Werner syndrome helicase (WRN), a clinical anticancer target.
View Article and Find Full Text PDFSelective Colocalization of GHSR and GLP-1R in a Subset of Hypothalamic Neurons and Their Functional Interaction.
Endocrinology
November 2024
Laboratory of Neurophysiology, Multidisciplinary Institute of Cell Biology [IMBICE; Argentine Research Council (CONICET); Scientific Research Commission, Province of Buenos Aires (CIC-PBA); National University of La Plata], B1906APO La Plata, Buenos Aires, Argentina.
The GH secretagogue receptor (GHSR) and the glucagon-like peptide-1 receptor (GLP-1R) are G protein-coupled receptors with critical, yet opposite, roles in regulating energy balance. Interestingly, these receptors are expressed in overlapping brain regions. However, the extent to which they target the same neurons and engage in molecular crosstalk remains unclear.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!