Anticholinesterase Effects Research Articles

Anxiolytic, Antidepressant, and Anticholinesterase Effects of Essential Oil from Myrcia sylvatica (G.Mey.) DC.

Aromatic plants are rich sources of essential oils (EOs), recognized for their therapeutic properties due to their diversity of phytochemicals. This study investigated the anxiolytic and antidepressant effects of Myrcia sylvatica essential oil (MsEO) through inhalation in an animal model and its in vitro anticholinesterase (AChE) activity. The EO was obtained by hydrodistillation, and its volatile constituents were analyzed by GC-MS. Swiss mice were exposed to doses of 0.1%, 1%, and 2% of the EO via an inhalation apparatus. The anxiolytic activity was assessed using the elevated plus maze and light-dark box tests, while antidepressant activity was evaluated using the tail suspension and forced swimming tests. To examine potential side effects, the animals were subjected to rotarod, Y-maze, and Morris water maze tests to assess motor coordination, memory, and learning. Anticholinesterase activity was determined by direct bioautography and colorimetry based on the Ellman method. The results demonstrated that inhalation of MsEO at doses of 0.1% and 1% significantly reduced anxiety and depressive-like behaviors without impairing memory, learning, or motor coordination in the animals. Moreover, MsEO inhibited acetylcholinesterase with an IC50 of 0.47 μg/mL. These findings suggest that MsEO has potential therapeutic applications for anxiety and depression disorders, with additional anticholinesterase activity warranting further investigation in cognitive-related conditions.

Antioxidant and anticholinesterase activities, molecular docking, ADMET and drug-likeness studies of essential oil and ethanolic extract from Ammodaucus leucotrichus Coss. & Dur. Fruits

The current study aimed to investigate the in vitro and in silico antioxidant and anticholinesterase effects of essential oil (EO) and ethanolic extract (EE) from Ammodaucus leucotrichus Coss. & Dur. fruits. GC-MS analysis of the EO revealed a predominance of perillaldehyde (80%), followed by limonene (13.45%). Antioxidant activity results showed that EO had excellent superoxide radical scavenging activity (IC50 = 20.95 μg/mL) compared to α-tocopherol (IC50 = 31.52 μg/mL), while EE demonstrated good ABTS•+ and DPPH radical scavenging activity with IC50 values of 52.06 and 63.51 μg/mL, respectively, compared to BHT (13.01 and 23.14 μg/mL). In addition, noticeable ferric and cupric reducing powers were observed. EO showed good inhibitory activity against both acetyl and butyrylcholinesterase (AChE and BChE) compared to galantamine (199.81 and 86.09 vs. 8.14 and 36.44 μg/mL, respectively). However, very low activity was demonstrated by the EE (IC50 > 200 μg/mL). Molecular docking analysis predicted high binding affinities of perillaldehyde and limonene with AChE and BChE ranging from −5.8 to −6.2 kcal/mol and an inhibition by binding via the π-interaction with the residues of active sites His447 and His438, respectively. Additionally, only perillaldehyde presented hydrogen bonds with both enzymes. Furthermore, the absorption, distribution, metabolism, elimination, and toxicity (ADMET) prediction studies of perillaldehyde and limonene showed good pharmacokinetic properties without inhibition of cytochromes P450 (CYP), nephrotoxicity, or mutagenicity, as well as good drug likeness evaluated by Lipinski’s Rule and a bioavailability score of 0.55. Thus, A. leucotrichus could be a good resource for pharmaceutical applications.

Anticonvulsant, Anticholinesterase and Cytoprotective Effects of the Aqueous Extract of Lippia sidoides Cham.

(1) Background: Lippia sidoides Cham is a Brazilian aromatic plant rich in phenolic compounds. In traditional medicine, its leaves are used to treat diseases of the Central Nervous System such as stress and anxiety. This study evaluates the capacity of the aqueous extract of L. sidoides as an anticonvulsant, anticholinesterase and antihemolytic agent. (2) Methods: The extract was obtained from the leaves using water as a solvent, then dried in a spray dryer. The anticonvulsant effect was evaluated in zebrafish models using the pentylenetetrazol (PTZ) method. The anticholinesterase effect was determined using the acetylcholinesterase enzyme and physostigmine as a positive control. The antihemolytic action was evaluated by exposing erythrocytes to different concentrations of NaCl in the presence and absence of the extract. (3) Results: The anticonvulsant effect was observed at a concentration of 400 mg/kg, delaying convulsive crises. In the anticholinesterase assay, a dose-dependent action and variation in the effect over time were observed, demonstrating a reversible effect of the extract. For the osmotic fragility test, the extract showed satisfactory results, providing cellular protection across all variations of NaCl concentration. (4) Conclusions: These results demonstrate the promising potential of L. sidoides extract for the development of drugs that act in the treatment of diseases that affect the Central Nervous System.

Anticholinesterase, Antioxidative and Neuroprotective Effects of Hydroethanolic Extracts of Guiera Senegalensis J. F. Gmel. Leaves on Scopolamine Induced Alzheimer’s Disease in Wistar Rat Models

Background: Medicinal plants like Guiera senegalensis J. F. Gmel. (GS) have gained attention for their potential neuroprotective effects due to their rich composition of bioactive compounds, including flavonoids and polyphenolic acids. While previous studies have highlighted the antioxidant, anti-inflammatory, and neuroplasticity-enhancing properties of GS extract, its efficacy in mitigating dementia-related pathology remains to be fully understood. Objectives: This study aimed to investigate the neuroprotective effects of hydroethanolic GS extract against scopolamine (Sco)-induced dementia in Wistar rats, focusing on its impact on cholinergic function, oxidative stress, neuroinflammation, neurodegeneration, and memory impairment. Methods: Fresh leaves were processed for extraction using standard methods. Antioxidant activity was evaluated using FRAP and DPPH assays. Adult male Wistar rats were used for behavioral tests (Y-maze, NOR, MWM) and biochemical analyses, including ELISA for cholinergic activity, oxidative stress markers (Aβ1-42, phosphorylated Tau), pro-inflammatory cytokines (IL-1β, TNF-α, IL-6, IFN-γ), GFAP, BDNF, and IL-10. Brain tissues underwent histopathological examination. Data were analyzed using GraphPad Prism software. Results: The study assessed the antioxidant potential of GS extract and found that it significantly scavenged DPPH radicals (70.29%) and reduced Fe3+ (49.69%). Behavioral tests showed that GS extract (100 - 400 mg/kg) improved spatial memory and learning in Sco-treated rats. Y-maze results indicated increased spontaneous alternation with GS extract (P < 0.01). NOR and MWM tests showed improved memory and learning, with GS extract-treated rats spending more time in the target quadrant. Biochemical analysis revealed that GS extract increased acetylcholine (ACh), Superoxide Dismutase (SOD), Catalase (CAT), Glutathione (GSH), IL-10, and BDNF levels, while decreasing acetylcholinesterase (AChE), malondialdehyde (MDA), nitrite, Aβ1-42, phosphorylated Tau, IL-1β, TNF-α, IL-6, IFN-γ, and GFAP levels in the hippocampus. Histological analysis confirmed restored hippocampal tissue architecture in AD rats treated with GS extract. Conclusions: Our findings suggest that GS modulates cholinergic, antioxidant, anti-inflammatory, and neuroplasticity pathways, exerting beneficial effects on cognitive functions and biochemical markers associated with Alzheimer's disease (AD) pathology. These results indicate the potential of GS as a neuroprotective agent for the treatment of AD.

Neuroprotective Effects of Hippeastrum elegans Extract: Anticholinesterase Effect In Silico and In Vivo Studies in the Scopolamine-Induced Memory Deficits Model in Rat

Neuroprotective Effects of Hippeastrum elegans Extract: Anticholinesterase Effect In Silico and In Vivo Studies in the Scopolamine-Induced Memory Deficits Model in Rat

Investigating the phytochemical profile, biological potentials, morphological, and anatomical characteristics of Cyclotrichium origanifolium (Labill.) Manden. & Scheng. (Lamiaceae) from Turkey.

Cyclotrichium origanifolium, a plant widely used in Eastern and Southern Anatolia for culinary purposes, was subject of this study, which aimed to comprehensively evaluate its potential therapeutic applications. This research stands out due to its holistic approach, combining morpho-anatomical studies, chemical, and biological analyses to explore antioxidant, antidiabetic, anticholinesterase, genotoxic, and anti-genotoxic effects of methanolic and aqueous extracts, as well as flowering aerial part essential oil. It is a perennial plant, typically ranging from 10 to 40cm in height, with a suffrutescent and highly branched growth habit. Essential oils are produced within glandular trichomes. Oil, analyzed via GC-MS/MS, revealed 24 compounds accounting for 96.4% of oil, with isomenthone (52.4%), pulegone (23.4%), and β-pinene (9.5%) as predominant components. These findings are significant as they provide new insights into chemical composition of oils, particularly highlighting pharmacologically active compounds. Methanol extract exhibited superior antioxidant activity, correlated with high phenol and tannin content. Essential oil showed moderate inhibition of α-amylase (49.54%) and mild inhibition of acetylcholinesterase (11.84%) and butyrylcholinesterase (16.93%), suggesting potential in managing oxidative stress and neurodegenerative diseases. Study also conducted biosafety evaluations using Ames/Salmonella and Allium tests, essential for assessing genotoxic and antigenotoxic potential of natural products. Notably, significant antimicrobial effects were identified, particularly against Pseudomonas aeruginosa and Enterococcus faecalis. Comprehensive analysis and discovery of significant bioactivities position this research as a valuable contribution to field, distinguishing it from previous studies on similar species. This study provides a foundational understanding of morpho-anatomical, pharmacological, biological properties of plant, opening avenues for future research.

Metabolites profiling, in-vitro and molecular docking studies of five legume seeds for Alzheimer’s disease

Even though legumes are valuable medicinal plants with edible seeds that are extensively consumed worldwide, there is little information available on the metabolic variations between different dietary beans and their influence as potential anti-cholinesterase agents. High-resolution liquid chromatography coupled with mass spectrometry in positive and negative ionization modes combined with multivariate analysis were used to explore differences in the metabolic profiles of five commonly edible seeds, fava bean, black-eyed pea, kidney bean, red lentil, and chickpea. A total of 139 metabolites from various classes were identified including saponins, alkaloids, phenolic acids, iridoids, and terpenes. Chickpea showed the highest antioxidant and anti-cholinesterase effects, followed by kidney beans. Supervised and unsupervised chemometric analysis determined that species could be distinguished by their different discriminatory metabolites. The major metabolic pathways in legumes were also studied. Glycerophospholipid metabolism was the most significantly enriched KEGG pathway. Pearson’s correlation analysis pinpointed 18 metabolites that were positively correlated with the anti-cholinesterase activity. Molecular docking of the biomarkers to the active sites of acetyl- and butyryl-cholinesterase enzymes revealed promising binding scores, validating the correlation results. The present study will add to the metabolomic analysis of legumes and their nutritional value and advocate their inclusion in anti-Alzheimer’s formulations.

Evaluation of destruction of bacterial membrane structure associated with anti-quorum sensing and ant-diabetic activity of Cyperus esculentus extract

Recently, there has been an increasing demand for medicinal plants to control diseases for good health and well-being, as primary health facilities are inadequate in certain populations to cure infections. Since synthetic medicines are toxic to humans and other animals, the present research is thus focused on using traditional medicine for treating various ailments as they are harmless. Based on the above facts, the current study was conducted to assay the antimicrobial, anti-diabetic, anti-cholinesterase, anti-oxidant, anti-quorum sensing, and anti-antibiotic resistance modifying effect of extracts of Cyperus esculentus. This study found 37 and 30 chemicals in butanol and dichloromethane (DCM) extracts using a gas chromatograph mass spectrophotometer (GC-MS). Most active compounds identified were benzofuran, 2,3-dihydro-, 1,2,3-benzenetriol, 3-bornanone, oxime and oleic acid by extracts of butanol whereas dichloromethane extracted three major active compounds (2,3-dihydro-3,5-dihydroxy-, 4H-pyran-4-one 3-deoxy-d-mannoic lactone and 5-hydroxymethylfurfural). Both dichloromethane and butanol extracts showed the highest antimicrobial activity. Compared to aqueous extracts, dichloromethane, and butanol showed excellent anti-diabetic anti-cholinesterase activities and inhibited virulence factors regulated by quorum sensing (QS). Anti-oxidants increased in solvent extracts (DCM and butanol) compared to aqueous extracts. Results of scanning electron microscope (SEM) and Fourier Transmission Infrared (FTIR) indicated damage to the cell membrane of S. aureus by the formation of pits and breakage in functional groups exposed to the extracts of butanol and dichloromethane compared to aqueous extracts. The above results confirmed that C. esculentus can be an alternative medicine for treating diseases.

Chemical Profiling of Drimys granadensis (Winteraceae) Essential Oil, and Their Antimicrobial, Antioxidant, and Anticholinesterase Properties.

A complete and comprehensive chemical and biological study of Drimys granadensis, a native Ecuadorian aromatic plant, was conducted. By conventional steam distillation from dried leaves, a yellowish, translucent essential oil (EO) with a density of 0.95 and a refractive index of 1.5090 was obtained. The EO was analyzed by gas chromatography coupled to a mass spectrometer (GC/MS) and an FID detector (GC/FID), respectively. Enantiomeric distribution was also carried out by GC/MS using a chiral selective column (diethyl tert-butylsilyl-BETA-cyclodextrin). The microdilution broth method was employed to assess the antibacterial and antifungal activity of the EO against a panel of opportunistic microorganisms. Antioxidant capacity was measured using diphenyl picryl hydrazyl (DPPH) and azino-bis 3-ethylbenzothiazoline-6-sulfonic acid (ABTS) radicals. Finally, the inhibitory potential of the EO against acetylcholinesterase was also valued. Sixty-four chemical compounds, constituting 93.27% of the total composition, were identified, with major components including γ-muurolene (10.63%), spathulenol (10.13%), sabinene (5.52%), and δ-cadinene (4.22%). The characteristic taxonomic marker of the Drimys genus, Drimenol, was detected at very low percentages (<2%). Two pairs of enantiomers ((1S,5R)-(+)-α-pinene/(1S,5S)-(-)-α-pinene; (1S,5R)-(+)-β-pinene/(1S,5S)-(-)-β-pinene) and one pure enantiomer (1R,4S)-(-)-camphene were identified. Regarding antimicrobial potency, the EO exhibited a significant moderate effect on Listeria monocytogenes with a minimal inhibitory concentration (MIC) value of 250 µg/mL, while with the remaining microorganisms, it exerted less potency, ranging from 500 to 2000 µg/mL. The EO displayed moderate effects against the ABTS radical with a half scavenging capacity of 210.48 µg/mL and no effect against the DPPH radical. The most notable effect was noticed for acetylcholinesterase, with a half inhibition concentration (IC50) of 63.88 ± 1.03 µg/mL. These antiradical and anticholinesterase effects hint at potential pharmacological applications in Alzheimer's disease treatment, although the presence of safrole, albeit in low content (ca. 2%), could limit this opportunity. Further in vivo studies are necessary to fully understand their potential applications.

Effect of selenium nanoparticles conjugated Vildagliptin on cognitive dysfunction associated with Diabetes mellitus

Type II Diabetes mellitus is a metabolic disorder leading to cognitive impairment. Vildagliptin, an antidiabetic drug, possesses neuroprotective activity, but it shows poor permeation to the brain with a short half-life. So, there is a need to improve the delivery of Vildagliptin to the brain. Selenium nanoparticles have recently exhibited increasing interest because of their safety, stability, and enhanced delivery to the brain. In the present study, vildagliptin-selenium nanoparticles were synthesized and characterized. The in-vitro and in-vivo antioxidant study was conducted to evaluate the efficacy of vildagliptin-selenium nanoparticles. In-vivo cognitive function was assessed by neurobehavioral studies using Y-maze and radial maze, anticholinesterase activity, and estimation of pro-inflammatory mediators. The selenium nanoconjugate of vildagliptin significantly improved the learning and memory function, decreased lipid peroxidation, and elevated the antioxidant status of vildagliptin. They also lessened the acetylcholinesterase levels and pro-inflammatory mediators. Hence, vildagliptin-selenium nanoparticles improved the efficacy of vildagliptin against streptozotocin-induced cognitive decline in rats. This efficacy may be attributed to its ability to enhance antioxidant, anticholinesterase, and anti-inflammatory effects. Further studies may be done to study its effectiveness against other neurodegenerative diseases.

Blackberry extract prevents lipopolysaccharide-induced depressive-like behavior in female mice: implications for redox status, inflammation, and brain enzymes

ABSTRACT This study evaluated the effects of Rubus sp. extract on behavioral and neurochemical parameters in female mice submitted to experimental model of depression induced by lipopolysaccharide (LPS). The results indicated that Rubus sp. extract protected against depressive-like behavior induced by LPS. Moreover, the administration of Rubus sp. extract was effective in preventing the increase in reactive species and nitrites levels, as well as the decrease in catalase activity induced by LPS in the cerebral cortex. In the serum, the Rubus sp. extract was effective in preventing the decrease in catalase activity induced by LPS. Treatment with Rubus sp. extract attenuated the increase in acetylcholinesterase activity induced by LPS in the cerebral cortex. Finally, blackberry extract also downregulated IL-1β levels in cerebral cortex. In conclusion, our findings demonstrated that treatment with Rubus sp. exerted antidepressant, antioxidant, anticholinesterase and anti-inflammatory effects in a model of depressive – like behavior induced by LPS in female mice. This highlights Rubus sp. as a potential therapeutic agent for individuals with major depressive disorder.

Evaluation of Anticholinesterase Activity of the Fungicides Mefentrifluconazole and Pyraclostrobin.

Triazoles are compounds with various biological activities, including fungicidal action. They became popular through cholinesterase studies after the successful synthesis of the dual binding femtomolar triazole inhibitor of acetylcholinesterase (AChE, EC 3.1.1.7) by Sharpless et al. via in situ click chemistry. Here, we evaluate the anticholinesterase effect of the first isopropanol triazole fungicide mefentrifluconazole (Ravystar®), developed to overcome fungus resistance in plant disease management. Mefentrifluconazole is commercially available individually or in a binary fungicidal mixture, i.e., with pyraclostrobin (Ravycare®). Pyraclostrobin is a carbamate that contains a pyrazole ring. Carbamates are known inhibitors of cholinesterases and the carbamate rivastigmine is already in use for the treatment of Alzheimer's disease. We tested the type and potency of anticholinesterase activity of mefentrifluconazole and pyraclostrobin. Mefentrifluconazole reversibly inhibited human AChE and BChE with a seven-fold higher potency toward AChE (Ki = 101 ± 19 μM). Pyraclostrobin (50 μM) inhibited AChE and BChE progressively with rate constants of (t1/2 = 2.1 min; ki = 6.6 × 103 M-1 min-1) and (t1/2 = 1.5 min; ki = 9.2 × 103 M-1 min-1), respectively. A molecular docking study indicated key interactions between the tested fungicides and residues of the lipophilic active site of AChE and BChE. Additionally, the physicochemical properties of the tested fungicides were compared to values for CNS-active drugs to estimate the blood-brain barrier permeability. Our results can be applied in the design of new molecules with a lesser impact on humans and the environment.

A Contrary Case in the Literature: Hepatotoxicity Following Mallow Consumption

Mallow (Malva neglecta Wallr, M.sylvestris L.) is a plant species, it’s key constituents include mucilage, pectins, glycosides, and flavonoids. The plant is believed to possess antimicrobial, antioxidant, anti-inflammatory, antiulcerogenic, hepatoprotective, anti-urolithiasis, anticholinesterase, and angiotensin-converting enzyme (ACE) inhibitory effects, as well as inhibition against alpha-amylase, alpha-glucosidase, and pancreatic lipase. Despite all the reported hepatoprotective and antioxidant effects of mallow, the elevation in liver function test values in our case is quite remarkable and contradicts the information available in the current literature.

Chrysin bonded to β-d-glucose tetraacetate enhances its protective effects against the neurotoxicity induced by aluminum in Swiss mice.

To evaluate whether the glycosylation of chrysin (CHR) enhances its protective effects against aluminum-induced neurotoxicity. To compare the antioxidant, anticholinesterase, and behavioral effects of CHR with its glycosylated form (CHR bonded to β-d-glucose tetraacetate, denoted as LQFM280), we employed an integrated approach using both in vitro (SH-SY5Y cells) and in vivo (aluminum-induced neurotoxicity in Swiss mice) models. LQFM280 demonstrated higher antioxidant activity than CHR in both models. Specifically, LQFM280 exhibited the ability to exert antioxidant effects in the cytoplasm of SH-SY5Y cells, indicating its competence in traversing neuronal membranes. Remarkably, LQFM280 proved more effective than CHR in recovering memory loss and counteracting neuronal death in the aluminum chloride mice model, suggesting its increased bioavailability at the brain level. The glycosylation of CHR with β-d-glucose tetraacetate amplifies its neuroprotective effects, positioning LQFM280 as a promising lead compound for safeguarding against neurodegenerative processes involving oxidative stress.

Biological Activities and Traditional Use of Hyptis suaveolens in Human and Veterinary Medicine: A Review

Hyptis suaveolens (H. suaveolens), known as Gros baume or sweet-smelling Hyptis, is an invasive plant from tropical regions widely used to manage human and animal ailments, such as bacterial, viral, and parasitic diseases. This study aimed to synthesize a scientific research work on the use of this medicinal plant in the traditional pharmacopeia, as well as the biological and pharmacological activities already recognized in the literature. Information for this synthesis was collected from physical (libraries and documentation centers of universities in Benin) and reliable scientific databases, such as PubMed, Google Scholar, Scopus, and Web of Science, which were queried based on the keywords related to H. suaveolens. This plant contains secondary metabolites in its aerial parts, such as leaves, and stems, which are rich in essential oils. From leaves to roots, all parts of this plant are of interest to both humans and animals to treat various pathologies. The most frequently cited diseases include asthma, panariasis, jaundice, hyperthermia, indigestion, stomach pains, nausea, colds, gall bladder infections, breast abscesses, hemorrhoids, oral-anal candidiasis, edemas, cramps, and skin infections The various aqueous and ethanolic extracts are evaluated by researchers and the biological activities are indicated in the literature. Those activities include the antibacterial, antifungal, larvicidal, antioxidant, anticholinesterase, insect repellent, and insecticidal effects. However, no toxicity resulting from the use of this plant has yet been reported in the literature. Research on H. suaveolens toxicity must be continued to gain a comprehensive understanding of its application in human and livestock health. This literature review allows the virtues and risks related to the traditional use of H. suaveolens in human and animal pharmacopeia. The various potentialities of this plant provide a lever for exploring its antiviral effects in traditional veterinary medicine in general.

Laboratory assessment of the acaricidal, repellent and anti-cholinesterase effects of Melaleuca alternifolia and Chamaemelum nobile essential oils against Hyalomma scupense ticks.

In cattle, Hyalomma scupense serves as an important vector of several pathogens resulting in diseases, subsequently affecting the agricultural field as well as the economy. Resistance to chemical acaricides has become widespread affirming the need for new drugs to tick control. The goal of this study was to investigate the acaricidal, repellent activities as well as the putative mode of action of two essential oils (EOs) from Melaleuca alternifolia (Tea tree) and Chamaemelum nobile (Roman chamomile) on Hyalomma scupense. The chemical composition of EOs was also evaluated. Different concentrations of EOs were tested in vitro for their acaricidal property on adults and larvae of H. scupense using adult immersion test (AIT) and larval packet test (LPT). Additionally, using Ellman's spectrophotometric method, the anticholinesterase (AChE) inhibition activity of M. alternifolia and C. nobile EOs was assessed in order to understand their putative mode of action. The main compounds of C. nobile were α-Bisabolene (22.20%) and (E)-β-Famesene (20.41%). The major components in the analyzed M. alternifolia were Terpinen-4-ol (36.32%) and γ-Terpinene (13.69%). Adulticidal and larvicidal assays demonstrated a promising efficacy of the essential oils against tick H. scupense. The lethal concentration (LC50) values obtained for M. alternifolia and C. nobile oils were 0.84 and 0.96 mg/mL in the AIT and 0.37 and 0.48 mg/mL in the LPT, respectively. Regarding repellent activity, M. alternifolia achieved 100% repellency at the concentration of 1 mg/mL while C. nobile showed 95.98% repellency activity at concentration of 4 mg/mL. Also, M. alternifolia and C. nobile EOs displayed potent AChE inhibition with IC50 value of 91.27 and 100.12 μg/mL, respectively. In the present study, M. alternifolia and, to a lesser degree, C. nobile EOs were found to be effective in vitro acaricides, repellents and acetylcholinesteraseinhibitor against H. scupense ticks. These plants may represent an economical and sustainable alternative to toxic synthetic acaricides in the management of ectoparasites of veterinary importance.

Phytochemical composition of aerial parts and roots of Pfaffia glomerata (Spreng.) Pedersen and anticholinesterase, antioxidant, and antiglycation activities.

The Pfaffia glomerata, a plant popularly called Brazilian ginseng, is widely used in Brazil for the treatment of various pathologies, including those associated with the Central Nervous System. 20-hydroxyecdysone (20E), a phytosteroid present in this plant, can promote adaptogenic effects in the organism, providing greater body resistance to stressors. This study aimed to evaluate the phytochemical composition and the anticholinesterase, antioxidant, and antiglycation effects of extracts and fractions of aerial parts and roots of P. glomerata, also analyzing their possible cytotoxic effects. The fractions were obtained by partitioning methanol extracts from the aerial part and roots of P. glomerata with hexane, dichloromethane, ethyl acetate, n-butanol, and water. The samples were initially tested in anticholinesterase, antioxidant, and antiglycation assays, and the most promising samples were submitted for cytotoxicity and chromatographic analyses. Mass spectrometry and chromatography methods revealed that 20E was the main compound in the dichloromethane fractions, there being 35% more 20E in the aerial part (APD) than in the roots (RD). Added to the higher concentration of 20E, the APD fraction also presented more promising results than the RD fraction in anticholinesterase and antioxidant analyses, indicating that their effects may be related to the concentration of 20E. These same fractions showed no hemolytic effects but were cytotoxic in high concentrations. These new findings contribute to scientific information about P. glomerata and open more perspectives for the understanding of its therapeutic properties, allowing the association of biological activity with the presence of 20E.

Ferulago bernardii as a New Source of α-Pinene Binds to ctDNA: In Silico and in Vitro Studies.

Ferulago bernardii Tomk & M. Pimen belongs to Apiaceae family. Various species of the Ferulago genus have antioxidant, anticholinesterase, cytotoxic, and antiproliferative effects. In this study, the essential oil of F. bernardii was extracted using the Clevenger apparatus. The essential oil compounds were identified using GC-MS/FID. The interaction between the essential oil and DNA strands was evaluated through spectrophotometric titration. The molecular mechanism of the interaction between the main components of the essential oil and different DNA strands was assessed using molecular dynamics simulation. Based on the results, 92.03±1.20 % of the essential oil consisted of α-pinene. Therefore, the essential oil could serve as a suitable source of α-pinene. α-pinene is a monoterpene hydrocarbon that has various effects, including anti-inflammatory, antioxidant, antimicrobial, and antitumor properties. The binding constant of the essential oil to DNA strands (Ka ) was determined to be 5.40±0.47×10-3 M-1 . Molecular dynamics simulation demonstrated that α-pinene could interact with AT and CG rich DNA strands and indirectly stabilize G-Quadruplex. Given the different applications for α-pinene and its high percentage in the essential oil, it is suggested that researchers pay more attention to F. bernardii in the pharmaceutical, cosmetic, and food industries.

The Metabolism Study of Oleraisoquinoline in Rats Using Ultrahigh- performance Liquid Chromatography-electrospray Coupled with Quadrupole Time-of-flight Mass Spectrometry and its Bioactivities

Objective: This study aimed to investigate the main metabolites and metabolic pathways of oleraisoquinoline in rats, a new alkaloid isolated from Portulaca oleracea L., and test its antioxidation and anticholinesterase effects. Methods: Ultra-high-performance liquid chromatography-electrospray coupled with quadrupole time-of-flight mass spectrometry (UHPLC-ESI-Q-TOF/MS) was applied to study the metabolism of oleraisoquinoline. Furthermore, 1,1‑diphenyl‑2‑picrylhydrazyl assay and modified Ellman’s method were used to test the antioxidation and anticholinesterase effects of oleraisoquinoline, respectively. Results: The metabolism results of oleraisoquinoline showed, after its administration through the tail vein of rats, 4 metabolites in the plasma samples, 17 metabolites in the urine sample, and 2 metabolites in the feces sample. The main metabolic pathways were hydrolyzation, oxidation, hydroxylation, sulfonation, glucuronidation, acetylation, and methylation. Additionally, IC50 values of antioxidant and anticholinesterase activities were 13.819 ± 0.005 μM and 10.551 ± 0.069 μM, respectively. Conclusion: 21 metabolites were found in the rat’s plasma, urine, and feces samples, and the metabolic pathways included hydrolyzation, oxidation, hydroxylation, sulfonation, glucuronidation, acetylation, and methylation; among them, sulfonation was the main metabolic reaction. Meanwhile, oleraisoquinoline also showed extremely good antioxidant and anticholinesterase activities.

Anticholinesterase and Anticalaleptic Effects of Instant Coffee

Anticholinesterase and Anticalaleptic Effects of Instant Coffee