- |||||||||| galantamine hydrobromide / Generic mfg.
Journal: Chemical Profiling and Biological Evaluation of Nepeta baytopii Extracts and Essential Oil: An Endemic Plant from Turkey. (Pubmed Central) - Jul 4, 2021
An interestingly high inhibition was observed for ethyl acetate extract against butyrylcholinesterase (10.85 mg galantamine equivalent/g)...Luteolin and apigenin and their derivatives were identified from the methanol and water extracts. The results obtained from this study highlighted that the abundance of highly bioactive compounds from Nepeta baytopii ensures the multiple biological activities of the tested extracts, and this suggests a potential use in the pharmaceutical and nutraceutical fields, and therefore should be investigated further.
- |||||||||| galantamine hydrobromide / Generic mfg.
Journal: UHPLC-QTOF-MS based metabolomics and biological activities of different parts of Eriobotrya japonica. (Pubmed Central) - Jul 1, 2021
All the investigated organs of E. japonica exhibited in vitro tyrosinase inhibition (57.27-71.61 mg Kojic Acid Equivalent (KAE)/g). Our findings suggest a potential food and pharmaceutical exploitation of different organs of E. japonica (mainly roots) in terms of enrichment with health-promoting phenolics and triterpenes.
- |||||||||| donepezil / Generic mfg., galantamine hydrobromide / Generic mfg.
Review, Journal: Molecular mechanisms in Alzheimer's disease and the impact of physical exercise with advancements in therapeutic approaches. (Pubmed Central) - Jun 30, 2021
Optimistically, this review directs on the advantageous strategies in using nanotechnology-based drug delivery systems to cross the blood-brain barrier for improving the efficacy of drugs combined with a novel neuronal stem cell therapy approach. Determinately, this review aims at the natural, non-therapeutic healing impact of physical exercise on different model organisms and the effect of safe neuromodulation treatments using repetitive Transcranial Magnetic Stimulation (rTMS), transcranial Electrical Stimulation (tES) in humans to control the disease pathologies prominent in enhancing the synaptic function.
- |||||||||| galantamine hydrobromide / Generic mfg.
Preclinical, Journal: Fucosterol from Sargassum horridum as an amyloid-beta (Aβ) aggregation inhibitor: in vitro and in silico studies. (Pubmed Central) - Jun 30, 2021
Experimental studies, including protein gel electrophoresis, atomic force microscopy and fluorescence studies with thioflavin T (ThT), highlighted that fucosterol can decrease oligomer formation more than galantamine, which was used as a positive control. Docking and molecular dynamics simulations coupled with an MMGBSA approach showed that fucosterol is capable of recognizing the hydrophobic regions of monomeric Aβ, suggesting that fucosterol could affect amyloid-beta (Aβ) aggregation by preventing the formation of oligomers, preventing the development of AD.Communicated by Ramaswamy H. Sarma.
- |||||||||| donepezil / Generic mfg., galantamine hydrobromide / Generic mfg., memantine / Generic mfg.
Journal: Potential Therapeutic Approaches to Alzheimer's Disease By Bioinformatics, Cheminformatics And Predicted Adme-Tox Tools. (Pubmed Central) - Jun 23, 2021
Not yet recruiting --> Recruiting | Trial completion date: Dec 2026 --> Dec 2028 Bioinformatics, cheminformatics and ADME-Tox methods can be very helpful in the quest for an effective anti-AD treatment, allowing the identification of novel drugs, enhancing the druggability of molecular targets and providing a deeper understanding of AD pathological mechanisms.
- |||||||||| SCH-23390 / Boehringer Ingelheim
Clinical, Journal: Shati/Nat8l deficiency disrupts adult neurogenesis and causes attentional impairment through dopaminergic neuronal dysfunction in the dentate gyrus. (Pubmed Central) - Jun 22, 2021
The α7 nicotinic acetylcholine receptor antagonist, methyllycaconitine, and dopamine D1 receptor antagonist, SCH23390, blocked the ameliorating effect of GAL on attentional impairment in Shati/Nat8l mice...These results suggest that the ameliorating effect of GAL on Shati/Nat8l attentional impairment is associated with activation of D1 receptors following increased dopamine release in the hippocampus via α7 nAChR. In summary, Shati/Nat8l is important in both morphogenesis and neurogenesis in the DG and attention, possible via modulation of dopaminergic transmission.
- |||||||||| galantamine hydrobromide / Generic mfg.
Journal: Identification of bioactive compounds from Rhaponticoides iconiensis extracts and their bioactivities: An endemic plant to Turkey flora. (Pubmed Central) - Jun 22, 2021
The leaves and roots methanol extracts exhibited high α-glucosidase (2.48-3.08 mmol acarbose equivalent/g) and α-amylase (0.17-0.70 mmol acarbose equivalent/g) inhibition...87 natural products (including hydroxybenzoic, hydroxycinnamic and acylquinic acids, flavones, flavonols, flavanones and anthocyanins) were unambiguously identified or tentatively annotated in the studied extracts. Findings presented in the present study appraise the bioactivity of R. iconiensis, an understudied species.
- |||||||||| galantamine hydrobromide / Generic mfg.
Preclinical, Journal: Evaluation of the Therapeutic Effect of Lycoramine on Alzheimer's Disease in Mouse Model. (Pubmed Central) - Jun 22, 2021
Findings presented in the present study appraise the bioactivity of R. iconiensis, an understudied species. Lycoramine shows therapeutic potential to halt and reverse cognitive decline at the late stages of disease progression, and holds great promise for the treatment of Alzheimer's disease.
- |||||||||| galantamine hydrobromide / Generic mfg.
Journal: Combined Structure and Ligand-Based Design of Selective Acetylcholinesterase Inhibitors. (Pubmed Central) - Jun 22, 2021
Compound 10i shows AChE inhibitory activity similar to a known Food and Drug Administration (FDA)-approved drug, galantamine, but with even better selectivity. Interaction analysis reveals that hydrophobic and hydrogen-bonding interactions are the primary driving forces responsible for the observed high affinity of the compound with AChE.
- |||||||||| donepezil / Generic mfg., galantamine hydrobromide / Generic mfg., memantine / Generic mfg.
Journal: Dual Effect of Prussian Blue Nanoparticles on Aβ40 Aggregation: β-Sheet Fibril Reduction and Copper Dyshomeostasis Regulation. (Pubmed Central) - Jun 22, 2021
In the present report, the potential use of Prussian blue (PB), a drug that is in the World Health Organization Model List of Essential Medicines, in AD treatment is demonstrated. Both in vitro and in cellulo studies indeed suggest that PB nanoparticles (PBNPs) are capable of reducing the formation of typical amyloid-β fibers (detected by thioflavin T fluorescence) and restoring the usual amyloid fibrillation pathway via chelation/sequestration of copper, which is found in high concentrations in senile plaques.
- |||||||||| galantamine hydrobromide / Generic mfg.
Journal: Chemical composition, biological properties and bioinformatics analysis of two Caesalpina species: A new light in the road from nature to pharmacy shelf. (Pubmed Central) - Jun 22, 2021
decapeleta DCM leaves extract (10.20 mg galantamine equivalent (GALAE)/g extract) showed highest inhibition against butyrylcholinesterase...In the gene ontology analysis, prostate cancer, nuclear factor kappa B (NF-kappa B) signaling, proteoglycans in cancer pathways might support the results of the cytotoxic assays. These results showed that the tested Caesalpinia species, showing potent inhibitory action against butyrylcholinesterase, might represent novel phytotherapeutic avenues for the management of Alzheimer's disease.
- |||||||||| galantamine hydrobromide / Generic mfg.
Journal: Metabolomic profiling and biological properties of six Limonium species: novel perspectives for nutraceutical purposes. (Pubmed Central) - May 28, 2021
Interestingly, all the extracts were found to be active inhibitors of cholinesterases (AChE (acetylcholinesterase): 4.20-5.11 mg GALAE (galantamine equivalent) per g; BChE (butyrylcholinesterase): 3.89-10.75 mg GALAE per g), amylase (0.52-1.09 mmol ACAE (acarbose equivalent) per g) and tyrosinase (119.41-155.67 mg KAE (kojic acid equivalent) per g), unlike for glucosidase (2.31-2.41 mmol ACAE per g). Taken together, these findings demonstrated a diverse chemical profiles and biological of the extracts, to be potentially considered as phytotherapeutic or functional ingredients due to their antioxidant properties and inhibition of key enzymes involved in several diseases.
- |||||||||| donepezil / Generic mfg., galantamine hydrobromide / Generic mfg., memantine / Generic mfg.
Biomarker, Journal: Genetic Editing and Pharmacogenetics in Current And Future Therapy Of Neurocognitive Disorders. (Pubmed Central) - May 25, 2021
Further studies investigate the possibilities of the development of emerging drugs or genetic editing by CRISPR/Cas9 for causative treatment. In conclusion, the pharmacogenetic studies on dementia diseases may improve the efficacy of pharmacotherapy in some patients with beneficial genetic variants, at the same time, identifying the carriers of unfavorable alleles, the potential group of novel approaches to the treatment and prevention of dementia.
- |||||||||| galantamine hydrobromide / Generic mfg.
Journal: Anticholinesterase and Antioxidant Activities of Natural Abietane Diterpenoids with Molecular Docking Studies. (Pubmed Central) - May 25, 2021
In conclusion, the pharmacogenetic studies on dementia diseases may improve the efficacy of pharmacotherapy in some patients with beneficial genetic variants, at the same time, identifying the carriers of unfavorable alleles, the potential group of novel approaches to the treatment and prevention of dementia. Abietane diterpenoids are promising molecules for the treatment of mild-moderate AD.
- |||||||||| galantamine hydrobromide / Generic mfg., memantine / Generic mfg.
Journal, Combination therapy: Multiple target-based combination therapy of galantamine, memantine and lycopene for the possible treatment of Alzheimer's disease. (Pubmed Central) - May 15, 2021
Because regeneration of neuron is a complicated process due to the involvement of multiple pathways, a combination of drugs that can work through multiple pathways could prove to be effective in treating AD. Based on prior studies and different mechanisms involved in the treatment, a new hypothesis has been proposed that a combination of galantamine, memantine and lycopene is anticipated to produce better activity as compared to the current therapies available in market for the treatment of this disease.
- |||||||||| galantamine hydrobromide / Generic mfg.
Preclinical, Journal: Micro- and nano-sized amine-terminated magnetic beads in a ligand fishing assay. (Pubmed Central) - May 15, 2021
For this purpose, four commercially available amine-terminated magnetic particles with diameters ranging from 4.5 nm to 106 μm were evaluated to fish out galantamine, a well-known AChE inhibitor, from an aqueous solution...The particles with diameters of about 1 μm (small microparticles) presented a higher protein mass capacity per milligram of particle than did those with diameters of about 4.5 nm (nanoparticles) and those with diameters of about 106 μm (large microparticles). The influence of these supports on the produced AChE-MBs with regards to hydrolysis turnover and ligand fishing was evaluated and is fully discussed.
- |||||||||| donepezil / Generic mfg., galantamine hydrobromide / Generic mfg., memantine / Generic mfg.
Review, Journal: Alzheimer's disease: Recent treatment strategies. (Pubmed Central) - May 15, 2021
Current treatment for AD (donepezil, galantamine, rivastigmine and memantine) is only symptomatic and has modest benefits...Even the positive findings presented by Biogen on Aducanumab are not entirely clear and further data is necessary to confirm its validity...Four monoclonal antibodies anti-tau (Gosuranemab, Tilavonemab, Semorinemab and Zagotenemab) and one anti-tau vaccine (AADvac1) have reached phase II, so far. In this review, we discuss the potential disease-modifying agents tested in clinical trials and update the information of drugs that are still under clinical evaluation.
- |||||||||| galantamine hydrobromide / Generic mfg.
Journal: Comprehensive bioactivity and chemical characterization of the endemic plant Scorzonera hieraciifolia Hayek extracts: A promising source of bioactive compounds. (Pubmed Central) - May 15, 2021
Overall, the hexane extracts of both aerial parts (acetylcholinesterase (AChE): 2.27 ± 0.04 and butyrlcholinesterase (BChE): 5.75 ± 0.48 mg galantamine equivalent (GALAE)/g) and roots (AChE: 2.44 ± 0.35 and BChE: 53.17 ± 0.22 mg GALAE/g) were most potent against AChE and BChE, suggesting a role for the more lipophilic compounds in this regard...Multivariate analysis showed that the biological activities were dependent on the plant parts used as well as on the type of solvent used. Overall, the results showed that S. hieraciifolia is a valuable source of phytochemicals for both the nutraceutical and pharmaceutical sectors.
- |||||||||| galantamine hydrobromide / Generic mfg.
Preclinical, Journal: Discovery of a Novel Acetylcholinesterase Inhibitor by Fragment-Based Design and Virtual Screening. (Pubmed Central) - May 13, 2021
We used this library to design 1220 galantamine (GAL) derivatives following the model GAL (binding core) - linker (L) - aromatic fragment (Ar)...Among the top 10 best-scored compounds, a representative lead molecule was selected and tested for anti-AChE activity and neurotoxicity. It was found that the selected compound was a powerful non-toxic AChE inhibitor, 68 times more active than GAL, and could serve as a lead molecule for further optimization and development.
- |||||||||| galantamine hydrobromide / Generic mfg.
Journal: Long Term Effects of Cholinesterase Inhibitors on Cognitive Decline and Mortality. (Pubmed Central) - May 11, 2021
ChEIs are associated with cognitive benefits which are modest but persist over time and with reduced mortality risk, which could be explained partly by their cognitive effects. Galantamine was the only ChEI demonstrating a significant reduction in the risk of developing severe dementia.
- |||||||||| galantamine hydrobromide / Generic mfg.
Journal: Analysing Curcuma caesia fractions and essential oil for neuroprotective potential against anxiety, depression, and amnesia. (Pubmed Central) - May 11, 2021
Suspensions were prepared for fractions (dissolved in distilled water) and essential oil (dissolved in tween 20) at 200 mg/kg and 400 mg/kg after acute toxicity study and were orally administered to Wistar albino female rats after the orientation of hypoxia by sodium nitrite (50 mg/kg) and amnesia by scopolamine (1 mg/kg)...Diazepam (12 mg/kg) and galantamine (3 mg/kg) were used as standard drugs for this study against hypoxia and amnesia...Rest fractions (I and III) and essential oil showed moderate efficacy. In prospects, identification of active molecules from the most active fraction (fraction II) and further studies on a molecular basis would substantiate its specific mechanism of neuroprotective action.
- |||||||||| Review, Journal: Alzheimer's disease treatment: The share of herbal medicines. (Pubmed Central) - May 7, 2021
Lavandula angustifolia, Ginkgo biloba, Melissa officinalis, Crocus sativus, Ginseng, Salvia miltiorrhiza, and Magnolia officinalis have been widely used for relief of symptoms of some neurological disorders. This paper reviews the therapeutic effects of phytomedicines with prominent effects against various factors implicated in the emergence and progression of AD.
- |||||||||| donepezil / Generic mfg., galantamine hydrobromide / Generic mfg.
Journal: Inhibitors of Cholinesterases in the Pharmacology, the Current Trends. (Pubmed Central) - May 6, 2021
This review is focused on survey of cholinesterase inhibitors with known or expected pharmacological impact and indications of their use. Recent literature with comments on it is provided here as well.
- |||||||||| Review, Journal: Treatment of Parkinson's Disease with Cognitive Impairment: Current Approaches and Future Directions. (Pubmed Central) - May 1, 2021
There is growing research supporting exercise in the treatment of PD-MCI, but most non-pharmacological approaches have insufficient evidence for use in PD-MCI (cognitive rehabilitation, deep brain stimulation, transcranial direct current stimulation, transcranial ultrasound, vestibular nerve stimulation) and PDD (cognitive intervention, deep brain stimulation, transcranial alternating current stimulation, transcranial ultrasound, temporal blood brain barrier disruption). Research is needed for both disease-modifying and symptomatic treatments in PD cognitive impairment.
- |||||||||| galantamine hydrobromide / Generic mfg.
Trial completion, Enrollment change, Trial completion date, Trial primary completion date: Effects of Galantamine on Cognition (clinicaltrials.gov) - Apr 14, 2021
P2, N=12, Completed,
Research is needed for both disease-modifying and symptomatic treatments in PD cognitive impairment. Active, not recruiting --> Completed | N=24 --> 12 | Trial completion date: Dec 2020 --> Jul 2020 | Trial primary completion date: Dec 2020 --> Jul 2020
- |||||||||| donepezil / Generic mfg., galantamine hydrobromide / Generic mfg.
[VIRTUAL] A Comparison of NOS and ROBINS-I Tools for Quality Assessment of Observational Studies () - Apr 12, 2021 - Abstract #ISPOR2021ISPOR_1119;
The present review suggests ROBINS-I tool is more precise and can be used rigorously compared to NOS but is more time consuming. Based on modifications in tools with time and requirement, more research will be further required to compare the trustworthiness and relevance.
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