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Biomarker, Journal, Metabolomic study: Metabolomics study to reveal cognitive improvement with treatment of Scrophularia buergeriana. (Pubmed Central) - Jul 23, 2024 We confirmed the effect of an extract of Scrophularia buergeriana on scopolamine-induced cognitive impairment through mouse behavioral experiments, and we observed metabolic changes in the cortex and hippocampus via brain tissue dissection after the behavioral experiment...Niacinamide, tyrosine, uridine, and valine in the cortex and GABA, choline, creatine, formate, fumarate, hypoxanthine, leucine, myo-inositol, pyroglutamate, and taurine in the hippocampus were identified as biomarker candidates for recovering cognitive impairment. In addition to behavioral experiments, this metabolomics study using specific regions of the brain may be helpful in understanding the effects of cognitive improvement.
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Clinical, Journal: Comparison of multi-type chemical compounds in fruits of Lycium and correlations between compounds and traits (Pubmed Central) - Jul 23, 2024 The multivariate statistical analysis indicated that polysaccharides, carotenoids, hundred-fruit weight, ratio of seed to fruit, scopolamine, fructose, 5-O-feruloylquinic acid, kaempferol-3-O-rutinoside, scopoletin, cryptochlorogenic acid, and caffeic acid were the main differential compounds in the fruits among different species of Lycium...The results implied that chemical compounds presented different distribution patterns in the fruits of 8 Lycium species. This study provides a basis for the comprehensive development and utilization, targeted breeding, and value-added application of Lycium plants.
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Preclinical, Journal: Reticulated Retinoic Acid Synthesis is Implicated in the Pathogenesis of Dry Eye in Aqp5 Deficiency Mice. (Pubmed Central) - Jul 17, 2024 Dry eye (DE) models were induced via subcutaneous scopolamine hydrobromide...Our findings demonstrated the downregulation of Aqp5 expression and aberrant RA metabolism in DE conditions. Knockout of Aqp5 resulted in reduced production of RA through activation of JunB, subsequently leading to the manifestation of DE symptoms.
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Journal: Fetal dystocia in guinea pigs: A case report. (Pubmed Central) - Jul 15, 2024 The objective of the present work is to discuss and emphasize the importance of veterinary intervention, diagnostic evaluation and therapeutics for the multifactorial nature of dystocia management. Despite the surgical treatment, the prognosis for both dam and offspring remains guarded, highlighting the need for early detection and intervention to optimize outcomes in guinea pig dystocia cases.
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Preclinical, Journal: Regulating Effect of Qifu Yin on Intestinal Microbiota in Mice with Memory Impairment Induced by Scopolamine Hydrobromide. (Pubmed Central) - Jul 13, 2024 Despite the surgical treatment, the prognosis for both dam and offspring remains guarded, highlighting the need for early detection and intervention to optimize outcomes in guinea pig dystocia cases. QFY can improve the memory of MI animals induced by scopolamine hydrobromide by restoring the homeostasis of intestinal microbiota and regulating related indexes in serum and brain tissue.
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Journal: Identification of Psychoplastogenic Tropanes Lacking Muscarinic Activity. (Pubmed Central) - Jul 9, 2024 In an effort to decouple their neuroplasticity-promoting effects from their muscarinic activity, we performed phenotypic structure-activity relationship studies across a variety of structurally distinct subclasses of tropanes. We discovered several novel tropanes capable of significantly increasing cortical neuronal growth while exhibiting drastically reduced activity at all muscarinic receptor subtypes compared to scopolamine.
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Preclinical, Journal: Concomitant administration of resveratrol and resistance training ameliorates acrylamide-induced spatial learning impairment in rats. (Pubmed Central) - Jul 5, 2024 Animals were divided into 6 groups: (1) Control group which received normal saline intraperitoneally (ip) daily for 8 weeks; (2) Scopolamine (SCO) group which received SCO (1 mg/kg/day, ip) for 8 weeks; (3) AC group which received AC (5 mg/kg/day, ip) for 8 weeks; (4) AC + RT group which received AC (5 mg/kg/day, ip) for 8 weeks and performed RT (5 days a week for 8 weeks); (5) AC + RES group which received AC (5 mg/kg/day, ip) and RES (1 mg/kg/day, ip) for 8 weeks; and (6) AC + RT + RES group which received AC (5 mg/kg/day, ip) and RES (1 mg/kg/day, ip) for 8 weeks and performed RT (5 days a week for 8 weeks)...Lipid peroxidation was reduced in the AC+RES and AC+RT+RES groups compared to the AC group. It seems that daily co-treatment with RES and RT for 8 weeks ameliorates the memory-impairing effects of AC.
- |||||||||| hyoscine butylbromide oral / Generic mfg., donepezil / Generic mfg.
Novel piperazine-benzoquinone derivative as a possible lead molecule selectively targeting AChE for the management of dementia in Alzheimer (Exhibit (Pennsylvania Convention Center); In-Person) - Jun 19, 2024 - Abstract #AAIC2024AAIC_3691; 1 ) Conclusion : Outcomes depicted the anti-amnesic effect of the synthesized conjugate on scopolamine-induced memory impairment probably related to mediation of cholinergic system and their effective antioxidant activity. Results obtained were found to be appreciable and provided promising lead which can be further explored structurally and pharmacologically, presenting a favourable scenario for the development of selective AChE inhibitors.
- |||||||||| hyoscine butylbromide oral / Generic mfg., rivastigmine / Generic mfg.
Synthesis and biological evaluation of some novel coumarin-oxadiazole conjugates as potential candidates for the treatment of cognitive decline (Exhibit (Pennsylvania Convention Center); In-Person) - Jun 19, 2024 - Abstract #AAIC2024AAIC_2522; After i n vitro studies, the compounds have been evaluated against behavioural alterations using step down passive avoidance and escape learning protocol at a dose of 2.0 mg/kg with reference to standard drug, rivastigmine. Our results depicted that the anti-amnesic effect of the synthesized conjugates on scopolamine-induced memory impairment may be related to the mediation of the cholinergic nervous system and their effective antioxidant activity.
- |||||||||| hyoscine butylbromide oral / Generic mfg.
Development of natural template-based novel NIRF theranostic agents for Alzheimer (Exhibit (Pennsylvania Convention Center); In-Person) - Jun 19, 2024 - Abstract #AAIC2024AAIC_1407; Our results depicted that the anti-amnesic effect of the synthesized conjugates on scopolamine-induced memory impairment may be related to the mediation of the cholinergic nervous system and their effective antioxidant activity. The unique ocular imaging pattern in the AD Drosophila model, strongly suggest that probes hold promise as a dependable indicator for rapid, noninvasive assessment of new therapeutic modulators or inhibitors in AD along with the improved cognitive function in a scopolamine-induced amnesia model upon I-43 treatment.
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PK/PD data, Review, Journal: A Review on the Chemical Properties, Plant Sources, Anti-shock Effects, Pharmacokinetics, Toxicity, and Clinical Applications of Anisodamine. (Pubmed Central) - Jun 18, 2024 Anisodamine, a prominent constituent of the tropine alkaloid family, exhibits a range of pharmacological effects akin to those of atropine and scopolamine...However, there remains a dearth of research regarding the in vivo pharmacokinetics, mechanism of action, and toxicity of anisodamine. Consequently, this paper provides a comprehensive review of the anti-shock effects, toxicity ,and pharmacokinetic characteristics of anisodamine to increase the understanding of its medicinal value, and provide reference and inspiration for the clinical application and further in-depth research of anisodamine.
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Preclinical, Journal: Manasamitra Vatakam on Scopolamine-Induced Amnesia in Female Wistar Rats. (Pubmed Central) - Jun 17, 2024 The results of the study illustrate the effectiveness of MMV in reversing memory dysfunction and memory-enhancing effects. The study paves the way for exploring research in CNS disorders and its potential application in drug-induced neurotoxicity.
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Preclinical, Journal: Neuroprotection of macamide in a mouse model of Alzheimer's disease involves Nrf2 signaling pathway and gut microbiota. (Pubmed Central) - Jun 3, 2024 The animal experiments showed that M 18:2 prevented the scopolamine (SCP)-induced cognitive impairment and neurotransmitter disorders, increased the positive rates of Nrf2 and HO-1 in hippocampal CA1, improved the synaptic plasticity by maintaining synaptic morphology and increasing the synapse density...Furthermore, M 18:2 promoted colonic epithelial integrity and partially restored the composition of the gut microbiota to normal, including decreased genera Clostridiales_unclassified and Lachnospiraceae_unclassified, as well as increased genera Muribaculaceae_unclassified, Muribaculum, Alistipes, and Bacteroides, which may be the possible biomarkers of cognitive aging. In summary, M 18:2 exerted neuroprotective effects on SCP-induced AD mice possibly via activating the Nrf2/HO-1 signaling pathway and modulating the gut microbiota.
- |||||||||| Xiidra (lifitegrast) / Bausch Health
Journal: Efficacy of RCI001 as a therapeutic candidate of dry eye disease in a modified mixed dry eye model. (Pubmed Central) - Jun 1, 2024 In summary, M 18:2 exerted neuroprotective effects on SCP-induced AD mice possibly via activating the Nrf2/HO-1 signaling pathway and modulating the gut microbiota. Topical RCI001 showed excellent therapeutic effects in environmental DED models by stimulating tear secretion, modulating oxidative stress and improving corneal epithelial healing compared to 1% PDE and 5% Lifitegrast.
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Preclinical, Journal: Neuroprotective effects of Anshen Bunao Syrup on cognitive dysfunction in Alzheimer's disease rat models. (Pubmed Central) - May 30, 2024 This study aimed to investigate Anshen Bunao Syrup's therapeutic potential in AD treatment using a scopolamine-induced AD rat model...Additionally, ELISA and correlation analyses indicated attenuation of oxidative stress and immune response through metabolic remodeling. In conclusion, this study provides compelling evidence for the neuroprotective effects of Anshen Bunao Syrup in AD models, shedding light on its potential as a therapeutic agent for AD prevention and treatment.
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Journal, MRI: A pilot study on interobserver variability in organ-at-risk contours in magnetic resonance imaging-guided online adaptive radiotherapy for pancreatic cancer. (Pubmed Central) - May 27, 2024 The study cohort was classified into three conditions based on the MRI sequence and butylscopolamine administration (Buscopan): 1, T2 imaging without butylscopolamine administration; 2, T2 imaging with butylscopolamine administration; and 3, multi-contrast imaging with butylscopolamine administration...The DSCs for OARs (stomach, duodenum, small intestine, large intestine) extracted before and after contouring were 0.86, 0.78, 0.88, and 0.87; 0.97, 0.94, 0.90, and 0.94; and 0.94, 0.86, 0.89, and 0.91 for conditions 1, 2, and 3, respectively. Butylscopolamine effectively reduced interobserver error and intra-fractional motion during the MRgOART treatment.
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Journal: Modulation of Tropane Alkaloids' Biosynthesis and Gene Expression by Methyl Jasmonate in Datura stramonium L.: A Comparative Analysis of Scopolamine, Atropine, and Hyoscyamine Accumulation. (Pubmed Central) - May 25, 2024 Furthermore, MJ enhanced the expression of PMT, TR1, and h6h genes in the roots, the primary site of alkaloid synthesis, but not in the leaves, the primary site of alkaloid storage. These results imply that MJ can be applied to regulate the biosynthesis and accumulation of scopolamine and atropine in D. stramonium, thereby improving their production efficiency.
- |||||||||| hyoscine butylbromide oral / Generic mfg., donepezil / Generic mfg.
Journal: Design, synthesis, and biological evaluation of some 2-(3-oxo-5,6-diphenyl-1,2,4-triazin-2(3H)-yl)-N-phenylacetamide hybrids as MTDLs for Alzheimer's disease therapy. (Pubmed Central) - May 11, 2024 The in vivo behavioral studies of the compound S-12 in the scopolamine- and A?-induced animal models also demonstrated attanuation of learning and memory functions in rats models having AD-like characteristics...The molecular docking studies of the compounds suggested that compound S-12 was interacting with the ChE-PAS & CAS residues and catalytic dyad residues of the BACE-1 enzymes. The 100 ns molecular dynamics simulation studies of the ligand-protein complexed with hAChE and hBACE-1 also suggested stable ligand-protein confirmation throughout the simulation run.
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Preclinical, Journal: A Rabbit Dry Eye Model Induced by Subcutaneous Scopolamine. (Pubmed Central) - May 8, 2024 The disordered structures of the ocular surface and lacrimal glands were also observed. This study showed that repeated subcutaneous SCOP injections successfully elicited some of the typical dry eye symptoms commonly seen in humans.
- |||||||||| hyoscine butylbromide oral / Generic mfg., pilocarpine / Generic mfg.
Journal: Two-point immobilization of M3 muscarinic receptor: a method for recognizing receptor antagonists in natural products. (Pubmed Central) - May 4, 2024 Our findings demonstrate that this immobilization method effectively captures receptor-ligand binding interactions and can discern receptor agonists from antagonists. This innovation enhances the efficiency of receptor chromatography to determine binding-affinity in the development of new drugs, offering promise for the screening and characterization of active compounds, particularly within complex natural products.
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Journal: Single-Nuclei Characterization of Lacrimal Gland in Scopolamine-Induced Dry Eye Disease. (Pubmed Central) - Apr 30, 2024 Overall, this study offers a systemic single-nucleus transcriptomic profile of LGs in both normal and DED conditions and an atlas of the complicated interactions of immunocytes with major LG parenchymal cells. The findings also facilitate understanding the pathogenesis of DED.
- |||||||||| hyoscine butylbromide oral / Generic mfg., donepezil / Generic mfg.
Journal: Euonymus alatus Leaf Extract Attenuates Effects of Aging on Oxidative Stress, Neuroinflammation, and Cognitive Impairment. (Pubmed Central) - Apr 27, 2024 Twenty-four-month-old mice received EA-L3 (300 mg/kg/day) or the reference drug, donepezil (DPZ, 5 mg/kg/day), for 6 weeks, and learning and memory functions were detected using the Passive Avoidance Test (PAT)...In parallel, it upregulated the brain-derived neurotrophic factor (BDNF) and subsequently activated the extracellular-signal-regulated kinase (ERK)/cAMP response element-binding (CREB) signaling in the mouse hippocampus and scopolamine-induced B35 and SH-SY5Y neuroblastoma cells...In addition, EA-L3 notably dose-dependently decreased ROS in BV2 cells after exposure to LPS. Taken together, EA-L3 might be used as a dietary supplement to alleviate oxidative stress, the deterioration of hippocampal-based memory tasks, and neuroinflammation in elderly people.
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