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1.
J Evid Based Integr Med ; 28: 2515690X231211661, 2023.
Article in English | MEDLINE | ID: mdl-37960857

ABSTRACT

Amaranthus dubius is a vegetable consumed for its nutritional content in Kenya. In herbal medicine, A. dubius is utilized to relief fever, anemia and hemorrhage. Additionally, it is utilized to manage cognitive dysfunction and is considered to augment brain function, but there is no empirical evidence to support this claim. The contemporary study investigated cognitive enhancing potential of A. dubius in mice model of Alzheimer's disease (AD)-like dementia induced with ketamine. Cognitively damaged mice were treated with aqueous extract of A. dubius leaf upon which passive avoidance task (PAT) was used to assess the cognitive performance. At the end of passive avoidance test, brains of the mice were dissected to evaluate the possibility of the extract to inhibit hallmarks that propagate AD namely oxidative stress and acetylcholinesterase activity. Additionally, characterization of secondary metabolites was done using liquid chromatograph- mass spectrometry analysis. During PAT test, extract-treated mice showed significantly increased step-through latencies than AD mice, depicting ability of A. dubius to reverse ketamine-induced cognitive decline. Further, the extract remarkably lowered malondialdehyde levels to normal levels and effectively inhibited acetylcholinesterase enzyme. The study showed that A. dubius extract is endowed with phytoconstituents that possess anti-oxidant and anticholinesterase activities. Thus, this study confirmed promising therapeutic effects of 200, 300 and 400 mg/kg bw of A. dubius extract with potential to alleviate cognitive disarray observed in AD.


Subject(s)
Alzheimer Disease , Ketamine , Mice , Animals , Acetylcholinesterase/metabolism , Acetylcholinesterase/pharmacology , Ketamine/adverse effects , Cognition , Plant Extracts/therapeutic use
2.
Molecules ; 28(20)2023 Oct 21.
Article in English | MEDLINE | ID: mdl-37894690

ABSTRACT

This study was conducted to examine the chemical composition of the essential oils (EOs) from six Tunisian Eucalyptus species and to evaluate their anti-enzymatic and antibiofilm activities. The EOs were obtained through hydro-distillation of dried leaves and subsequently analyzed using GC/MS. The main class of compounds was constituted by oxygenated monoterpenes, particularly prominent in E. brevifolia (75.7%), E. lehmannii (72.8%), and E. woollsiana (67%). Anti-enzymatic activities against cholinesterases, α-amylase, and α-glucosidase were evaluated using spectrophotometric methods. Notably, the E. brevifolia, E. extensa, E. leptophylla, E. patellaris, and E. woollsiana EOs displayed potent acetylcholinesterase (AChE) inhibition (IC50: 0.25-0.60 mg/mL), with E. lehmannii exhibiting lower activity (IC50: 1.2 mg/mL). E. leptophylla and E. brevifolia showed remarkable α-amylase inhibition (IC50: 0.88 mg/mL), while E. brevifolia and E. leptophylla significantly hindered α-glucosidase (IC50 < 30 mg/mL), distinguishing them from other EOs with limited effects. Additionally, the EOs were assessed for their anti-biofilm properties of Gram-positive (Staphylococcus aureus and Listeria monocytogenes) and Gram-negative (Acinetobacter baumannii, Pseudomonas aeruginosa and Escherichia coli) bacterial strains. The E. extensa EO demonstrated the main antibiofilm effect against E. coli and L. monocytogenes with an inhibition > 80% at 10 mg/mL. These findings could represent a basis for possible further use of Eucalyptus EOs in the treatment of human microbial infections and/or as a coadjutant in preventing and treating Alzheimer's disease and/or diabetes mellitus.


Subject(s)
Eucalyptus , Oils, Volatile , Humans , Eucalyptus/chemistry , Escherichia coli , Tunisia , Acetylcholinesterase/pharmacology , alpha-Glucosidases/pharmacology , Anti-Bacterial Agents/pharmacology , Anti-Bacterial Agents/chemistry , Oils, Volatile/pharmacology , Oils, Volatile/chemistry , Eucalyptus Oil/pharmacology , alpha-Amylases , Microbial Sensitivity Tests
3.
Complement Ther Clin Pract ; 51: 101746, 2023 May.
Article in English | MEDLINE | ID: mdl-36933451

ABSTRACT

BACKGROUND AND PURPOSE: Jihwang-eumja is reported to be effective in decreasing ß-amyloid expression and activating monoamine oxidase and acetylcholinesterase in rat models. This systematic review aims to evaluate the effectiveness of Jihwang-eumja in Alzheimer's disease compared to Western medications. METHODS: We searched Medline, Embase, CENTRAL, CINAHL, CNKI, ScienceON, KISS, and Kmbase. Randomized controlled trials comparing the effectiveness of Jihwang-eumja and Western medications on the cognition and the activities of daily living in Alzheimer's disease were included. The results were synthesized using meta-analysis. The risk of bias was evaluated using the Cochrane risk-of-bias tool, and the evidence level of each outcome was suggested using the GRADE system. RESULTS: A total of 165 studies were screened, and six were included in the systematic review and meta-analysis. A total of 245 and 240 participants were included in the intervention and comparison groups, respectively. The results showed that Mini-Mental State Examination was 3.19 (95%CI: 1.68-4.70) higher, and the standardized mean difference of activities of daily living was 1.13 (95%CI: 0.89-1.37) higher in the Jihwang-eumja group than in Western medications group. The included studies contained some concerns of the risk of bias, and the certainty of the evidence was considered moderate. CONCLUSION: Despite the small number of studies and high heterogeneity, we could verify the applicability of Jihwang-eumja for Alzheimer's disease.


Subject(s)
Alzheimer Disease , Humans , Animals , Rats , Alzheimer Disease/drug therapy , Activities of Daily Living , Acetylcholinesterase/pharmacology , Acetylcholinesterase/therapeutic use , Cognition
4.
Molecules ; 28(5)2023 Mar 02.
Article in English | MEDLINE | ID: mdl-36903556

ABSTRACT

The present work deals with the green synthesis and characterization of silver nanoparticles (AgNPs) using Allium cepa (yellowish peel) and the evaluation of its antimicrobial, antioxidant, and anticholinesterase activities. For the synthesis of AgNPs, peel aqueous extract (200 mL) was treated with a 40 mM AgNO3 solution (200 mL) at room temperature, and a color change was observed. In UV-Visible spectroscopy, an absorption peak formation at ~439 nm was the sign that AgNPs were present in the reaction solution. UV-vis, FE-SEM, TEM, EDX, AFM, XRD, TG/DT analyses, and Zetasizer techniques were used to characterize the biosynthesized nanoparticles. The crystal average size and zeta potential of AC-AgNPs with predominantly spherical shapes were measured as 19.47 ± 1.12 nm and -13.1 mV, respectively. Pathogenic microorganisms Bacillus subtilis, Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, and Candida albicans were used for the Minimum Inhibition Concentration (MIC) test. When compared to tested standard antibiotics, AC-AgNPs demonstrated good growth inhibitory activities on P. aeuruginosa, B. subtilis, and S. aureus strains. In vitro, the antioxidant properties of AC-AgNPs were measured using different spectrophotometric techniques. In the ß-Carotene linoleic acid lipid peroxidation assay, AC-AgNPs showed the strongest antioxidant activity with an IC50 value of 116.9 µg/mL, followed by metal-chelating capacity and ABTS cation radical scavenging activity with IC50 values of 120.4 µg/mL and 128.5 µg/mL, respectively. The inhibitory effects of produced AgNPs on the acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes were determined using spectrophotometric techniques. This study provides an eco-friendly, inexpensive, and easy method for the synthesis of AgNPs that can be used for biomedical activities and also has other possible industrial applications.


Subject(s)
Antioxidants , Metal Nanoparticles , Antioxidants/chemistry , Staphylococcus aureus , Cholinesterase Inhibitors/pharmacology , Silver/chemistry , Onions , Metal Nanoparticles/chemistry , Butyrylcholinesterase/pharmacology , Acetylcholinesterase/pharmacology , Anti-Bacterial Agents/pharmacology , Plant Extracts/chemistry
5.
J Mol Recognit ; 36(3): e3004, 2023 03.
Article in English | MEDLINE | ID: mdl-36537558

ABSTRACT

Atherosclerosis and cognitive impairment are both influenced by hyperlipidemia. Due to their high margin of safety and low cost, natural chemicals have recently attracted particular attention in the context of the treatment of disease. Hence, the purpose of this study was to investigate the possible amendatory impact of ethanol extract walnut (Juglans regia) seed coat (E-WSC) on some metabolic enzymes (glutathione reductase (GR), paraoxonase-1 (PON1), aldose reductase (AR), sorbitol dehydrogenase (SDH), acetylcholinesterase (AChE), glutathione S-transferase (GST), and butyrylcholinesterase (BChE)) activity in the liver, kidney, and heart of rats with Triton WR-1339-induced hyperlipidemia. Rats were divided into five groups: control group, HL-Control group (Triton WR-1339 400 mg/kg, i.p administered group), E- WSC + 150 (150 mg/kg,o.d given group), E- WSC + 300 (E- WSC 300 mg/kg, o.d given group) and HL+ E-WSC + 300 (Group receiving E- WSC 300 mg/kg, o.d 30 min prior to administration of Triton WR-1339 400 mg/kg, i.p). In HL-Control, AR, SDH, and BChE enzyme activity was significantly increased in all tissues compared to the control, while the activity of other studied enzymes was significantly decreased. The effects of hyperlipidemia on balance were improved and alterations in the activity of the investigated metabolic enzymes were prevented by E-WSC. As a result, promising natural compounds that can be used as adjuvant therapy in the treatment of cognitive disorders and hyperlipidemia may be found in E-WSC powder.


Subject(s)
Hyperlipidemias , Juglans , Rats , Animals , Hyperlipidemias/chemically induced , Hyperlipidemias/drug therapy , Hyperlipidemias/metabolism , Juglans/chemistry , Butyrylcholinesterase/pharmacology , Butyrylcholinesterase/therapeutic use , Acetylcholinesterase/pharmacology , Acetylcholinesterase/therapeutic use , Liver , Anti-Inflammatory Agents/pharmacology , Anti-Inflammatory Agents/therapeutic use , Plant Extracts/pharmacology , Plant Extracts/therapeutic use , Kidney , Seeds
6.
Fundam Clin Pharmacol ; 37(2): 324-339, 2023 Apr.
Article in English | MEDLINE | ID: mdl-36541946

ABSTRACT

There are increasing concerns on the rising cases of diabetes mellitus with type 2 diabetes (T2D) being of major interest as well as the cost of its treatment. Plant phenolic compounds are natural and potent antioxidants that have been widely reported for their antidiabetic activities properties, one of which is ferulic acid. The effect of ferulic acid (FA) on major diabetogenic activities and pancreatic architecture linked to T2D was investigated in T2D rats. T2D was induced in male Sprague-Dawley rats using the fructose-streptozotocin model. Diabetic rats were treated with FA at 150 or 300 mg/kg bodyweight (bw). Normal control consisted of rats administered with food and water, while diabetic control consisted of untreated diabetic rats. Metformin was used as the standard drug. The rats were humanely sacrificed after 5 weeks of treatment. Their blood, liver, and pancreas were collected for analysis. Total glycogen content and carbohydrate metabolic enzymes activities were analyzed in the liver, while the pancreas and serum from blood were analyzed for oxidative stress biomarkers, purinergic and cholinergic enzyme activities, and amylase and lipase activities. The pancreatic tissue was further subjected to microscopic and histological examinations. FA caused a significant (p < 0.05) decrease in blood glucose level, with concomitant increase in serum insulin level. Treatment with FA also led to elevated levels of GSH, HDL-c, SOD, and catalase activities, while concomitantly suppressing malondialdehyde, cholesterol, triglyceride, LDL-c, NO, ALT, AST, creatinine, urea, and uric acid levels, acetylcholinesterase, ATPase, ENTPDase, 5'-nucleotidase, lipase, glycogen phosphorylase, glucose-6-phosphatase, and fructose-1,6-biphosphatase activities. Histology analysis revealed an intact pancreatic morphology in FA-treated diabetic rats. While transmission electron microscopy (TEM) analysis revealed an intact pancreatic ultrastructure and increased number of insulin granules in ß-cells. Taken together, these results portray that the antidiabetic potentials of ferulic acid involves modulation of major diabetogenic activities and maintenance of the pancreatic ultrastructure architecture.


Subject(s)
Diabetes Mellitus, Experimental , Diabetes Mellitus, Type 2 , Rats , Animals , Diabetes Mellitus, Type 2/drug therapy , Diabetes Mellitus, Type 2/metabolism , Diabetes Mellitus, Experimental/metabolism , Rats, Sprague-Dawley , Acetylcholinesterase/metabolism , Acetylcholinesterase/pharmacology , Acetylcholinesterase/therapeutic use , Hypoglycemic Agents/therapeutic use , Pancreas , Insulin/metabolism , Antioxidants/pharmacology , Homeostasis , Lipase/metabolism , Lipase/pharmacology , Lipase/therapeutic use , Glucose/metabolism , Blood Glucose , Plant Extracts/pharmacology
7.
Sex Transm Infect ; 99(1): 64-69, 2023 02.
Article in English | MEDLINE | ID: mdl-36411033

ABSTRACT

BACKGROUND: Gepotidacin is a novel, first-in-class triazaacenaphthylene antibiotic that inhibits bacterial DNA replication by a distinct mechanism of action and is active against most strains of Neisseria gonorrhoeae (N. gonorrhoeae). Phase II data suggested higher exposures were needed for efficacy and to suppress resistance development. A translational approach using in vitro pharmacokinetic/pharmacodynamic (PK/PD) and clinical data was used to select a gepotidacin dose for a phase III study. In this narrative review of previously shown data, we summarise how a translational approach based on in vitro PK/PD and population PK modelling and simulation data was undertaken to select a dosing regimen for the ongoing phase III gepotidacin study in participants with uncomplicated urogenital gonorrhoea. METHODS: For dose selection, prior in vitro minimum inhibitory concentrations (MICs) and PK/PD data were available. PK modelling was conducted to determine a dose that would limit plasma concentrations to less than 14 µg/mL (as concentrations above this are associated with QT prolongation and effects associated with acetylcholinesterase inhibition) while maintaining ≥90% probability of target attainment (PTA) for efficacy and resistance suppression against N. gonorrhoeae isolates with gepotidacin MICs ≤1 µg/mL. RESULTS: Two 3000 mg gepotidacin doses, administered 10-12 hours apart, resulted in PTA of ≥97.5% and ≥91.7% for gepotidacin MICs ≤1 µg/mL for the ratio of the area under the free drug plasma concentration-time curve over 24 hours to the MIC (fAUC0-24/MIC) efficacy, and resistance suppression targets of 40 and 46, respectively, but limited the occurrence of maximum plasma concentrations ≥14 µg/mL. CONCLUSIONS: Two gepotidacin 3000 mg oral doses 10-12 hours apart provide ~2-fold higher systemic exposures, increase efficacy for higher gepotidacin MIC N. gonorrhoeae isolates, reduce resistance potential and limit plasma concentrations of potential safety concern, compared with higher doses.


Subject(s)
Gonorrhea , Humans , Gonorrhea/drug therapy , Gonorrhea/microbiology , Acetylcholinesterase/pharmacology , Acetylcholinesterase/therapeutic use , Anti-Bacterial Agents/therapeutic use , Acenaphthenes/pharmacology , Acenaphthenes/therapeutic use , Neisseria gonorrhoeae , Microbial Sensitivity Tests , Clinical Trials, Phase III as Topic
8.
Niger J Physiol Sci ; 38(1): 91-99, 2023 Jun 30.
Article in English | MEDLINE | ID: mdl-38243363

ABSTRACT

Decline in cholinergic function and oxidative/nitrosative stress play a central role in Alzheimer's disease (AD). Previous quantitative HPLC profiling analysis has revealed the presence of Pinostrobin, formononetin, vitexin and other neuroprotective flavonoids in Cajanus cajan seed extract. This study was designed to investigate the protective action of Cajanus cajan ethanol seed extract (CC) on learning and memory functions using scopolamine mouse model of amnesia. Materials and methods: Adult mice were pretreated with CC (50, 100, or 200mg/kg, p.o) or vehicle (10ml/kg, p.o) for 16 days consecutively. Scopolamine, a competitive muscarinic cholinergic receptor antagonist (1mg/kg, i.p.) was given an hour after CC pretreatment from days 3 to 16.  The mice were subjected to behavioural tests from day 11 (open field test (OFT)/ Y-maze test (YMT) and Morris water maze task (MWM) from days 12-16. Animals were euthanized 1h after behavioral test on day 16 and discrete brain regions isolated for markers of oxidative stress and cholinergic signaling. Molecular docking analysis was undertaken to predict the possible mechanism(s) of CC-induced anti-amnesic action.  pre-administration of CC significantly reversed working memory and learning deficits caused by scopolamine in YMT and MWM tests, respectively. Moreover, CC prevented scopolamine-induced oxidative and nitrosative stress radicals in the hippocampus evidenced in significant increase in glutathione (GSH) level, superoxide dismutase (SOD) and catalase (CAT) activities with a marked decrease in malondialdehyde (MDA) production, as well as significant inhibition of hippocampal scopolamine-induced increase in acetylcholinesterase activity by CC. The molecular docking analysis showed that out of the 19 compounds, the following had the highest binding affinity; Pinostrobin (-8.7 Kcal/mol), friedeline (-7.5kCal/mol), and lupeol (-8.2 Kcal/mol), respectively, to neuronal muscarinic M1 acetylcholine receptor, α7 nicotinic acetylcholine receptor and amyloid beta peptide binding pockets, which further supports the ability of CC to enhance neuronal cholinergic signaling and possible inhibition of amyloid beta aggregation. This study showed that Cajanus cajan seeds extract improved working memory and learning through enhancement of cholinergic signaling, antioxidant capacity and reduction in amyloidogenesis.


Subject(s)
Antioxidants , Cajanus , Mice , Animals , Antioxidants/pharmacology , Antioxidants/metabolism , Scopolamine/pharmacology , Cajanus/metabolism , Acetylcholinesterase/metabolism , Acetylcholinesterase/pharmacology , Amyloid beta-Peptides/adverse effects , Amyloid beta-Peptides/metabolism , Molecular Docking Simulation , Maze Learning , Amnesia/chemically induced , Amnesia/drug therapy , Amnesia/prevention & control , Oxidative Stress , Glutathione/metabolism , Synaptic Transmission , Hippocampus , Plant Extracts/pharmacology , Plant Extracts/therapeutic use , Cholinergic Agents/adverse effects , Cholinergic Agents/metabolism , Defense Mechanisms , Memory Disorders/chemically induced , Memory Disorders/metabolism
9.
Niger J Physiol Sci ; 38(1): 65-72, 2023 Jun 30.
Article in English | MEDLINE | ID: mdl-38243358

ABSTRACT

The neuro-pharmacological effect of Eucalyptus globulus ethanol leaf extract in fructose-streptozotocin-induced diabetic rats was evaluated in this study. The phytochemical analysis of the extract was carried out using HPLC-DAD. Diabetes was induced in rats with 10% fructose in drinking water and a single intraperitoneal injection of 40 mg/kg streptozotocin (STZ). Diabetic animals were orally treated with 100-400 mg/kg of the extract for 21 days with glibenclamide as the reference drug. Blood and brain tissue were processed for the determination of serum electrolyte levels, hematological indices, and biochemical estimations. Ergosterol, pinitol, catechin, quercetin, robinetinidol, and other polyphenols were identified in the extract. Diabetic animals showed decreased serum potassium and sodium ion levels and decreased hematocrit, hemoglobin, red blood cells, white blood cells and lymphocytes but increased neutrophils. The brains of animals in the untreated diabetic group with increased blood glucose level showed oxidative stress (increased level of MDA and myeloperoxidase but decreased level of reduced glutathione and superoxide dismutase) and disturbed neurochemistry (increased level of acetylcholinesterase and monoamine oxidase but decreased level of Na+K+ATPase, tyrosine hydroxylase and dopamine). Administration of the Eucalyptus globulus leaf extract remarkably ameliorated the observed hyperglycemia, electrolyte, and hematological imbalances in animals. In addition, the administration of the extract attenuated the brain redox imbalance, and neurochemical disturbances in the rats. These results show that Eucalyptus globulus leaves contain antioxidant and neurotransmitter modulating phytochemicals with the potential to be developed as therapeutic agents for the management of diabetic cerebrovascular problems and related complications.


Subject(s)
Diabetes Mellitus, Experimental , Eucalyptus , Neurochemistry , Rats , Animals , Rats, Wistar , Streptozocin/pharmacology , Blood Glucose , Diabetes Mellitus, Experimental/chemically induced , Diabetes Mellitus, Experimental/drug therapy , Plant Extracts/pharmacology , Plant Extracts/therapeutic use , Acetylcholinesterase/pharmacology , Acetylcholinesterase/therapeutic use , Oxidative Stress , Antioxidants/pharmacology , Antioxidants/therapeutic use , Brain , Electrolytes , Hypoglycemic Agents/pharmacology
10.
Molecules ; 27(24)2022 Dec 08.
Article in English | MEDLINE | ID: mdl-36557821

ABSTRACT

The present work was designed to study the chemical composition and the antioxidant and antimicrobial properties of fruits (SFr) and leaf (SF) extracts from Solanum elaeagnifolium var. obtusifolium (Dunal) Dunal (S. elaeagnifolium). The chemical composition was determined using HPLC-DAD analysis. Colorimetric methods were used to determine polyphenols and flavonoids. Antioxidant capacity was assessed with DPPH, TAC, and FRAP assays. Antimicrobial activity was assessed using disk diffusion and microdilution assays against two Gram (+) bacteria (Staphylococcus aureus ATCC-6633 and Bacillus subtilis DSM-6333) and two Gram (-) bacteria (Escherichia coli K-12 and Proteus mirabilis ATCC-29906), while the antifungal effect was tested vs. Candida albicans ATCC-1023. By use of in silico studies, the antioxidant and antimicrobial properties of the studied extracts were also investigated. HPLC analysis showed that both fruits and leaf extracts from S. elaeagnifolium were rich in luteolin, quercetin, gallic acid, and naringenin. Both SFr and SF generated good antioxidant activity, with IC50 values of 35.15 ± 6.09 µg/mL and 132.46 ± 11.73 µg/mL, respectively. The EC50 of SFr and SF was 35.15 ± 6.09 µg/mL and 132.46 ± 11.73 µg/mL, respectively. SFr and SF also showed a good total antioxidant capacity of 939.66 ± 5.01 µg AAE/and 890.1 ± 7.76 µg AAE/g, respectively. SFr had important antibacterial activity vs. all tested strains-most notably B. subtilis DSM-6333 and E. coli, with MICs values of 2.5 ± 0.00 mg/mL and 2.50 ± 0.00 mg/mL, respectively. SFr demonstrated potent antifungal activity against C. albicans, with an inhibition diameter of 9.00 ± 0.50 mm and an MIC of 0.31 ± 0.00 mg/mL. The in silico approach showed that all compounds detected in SFr and SF had high activity (between -5.368 and 8.416 kcal/mol) against the receptors studied, including NADPH oxidase, human acetylcholinesterase, and beta-ketoacyl-[acyl carrier protein] synthase.


Subject(s)
Anti-Infective Agents , Escherichia coli K12 , Humans , Antioxidants/pharmacology , Antioxidants/chemistry , Polyphenols/pharmacology , Antifungal Agents/pharmacology , Antifungal Agents/chemistry , Acetylcholinesterase/pharmacology , Escherichia coli , Phenols/chemistry , Plant Extracts/pharmacology , Plant Extracts/chemistry , Anti-Bacterial Agents/pharmacology , Anti-Bacterial Agents/chemistry , Anti-Infective Agents/pharmacology , Microbial Sensitivity Tests , Candida albicans
11.
Molecules ; 27(21)2022 Oct 25.
Article in English | MEDLINE | ID: mdl-36364044

ABSTRACT

Lactic acid bacteria produce a variety of antibacterial and larvicidal metabolites, which could be used to cure diseases caused by pathogenic bacteria and to efficiently overcome issues regarding insecticide resistance. In the current study, the antibacterial and larvicidal potential of Bis-(2-ethylhexyl) phthalate isolated from Lactiplantibacillus plantarum BCH-1 has been evaluated. Bioactive compounds were extracted by ethyl acetate and were fractionated by gradient column chromatography from crude extract. Based on FT-IR analysis followed by GC-MS and ESI-MS/MS, the active compound was identified to be Bis-(2-ethylhexyl) phthalate. Antibacterial potential was evaluated by disk diffusion against E. coli (12.33 ± 0.56 mm inhibition zone) and S. aureus (5.66 ± 1.00 mm inhibition zone). Larvicidal potency was performed against Culex quinquefasciatus Say larvae, where Bis-(2-ethylhexyl) phthalate showed 100% mortality at 250 ppm after 72 h with LC50 of 67.03 ppm. Furthermore, after 72 h the acetylcholinesterase inhibition was observed as 29.00, 40.33, 53.00, 64.00, and 75.33 (%) at 50, 100, 150, 200, and 250 ppm, respectively. In comet assay, mean comet tail length (14.18 ± 0.28 µm), tail DNA percent damage (18.23 ± 0.06%), tail movement (14.68 ± 0.56 µm), comet length (20.62 ± 0.64 µm), head length (23.75 ± 0.27 µm), and head DNA percentage (39.19 ± 0.92%) were observed at 250 ppm as compared to the control. The current study for the first time describes the promising antibacterial and larvicidal potential of Bis-(2-ethylhexyl) phthalate from Lactiplantibacillus plantarum that would have potential pharmaceutical applications.


Subject(s)
Aedes , Anopheles , Culex , Insecticides , Animals , Insecticides/chemistry , Acetylcholinesterase/pharmacology , Spectroscopy, Fourier Transform Infrared , Staphylococcus aureus , Tandem Mass Spectrometry , Escherichia coli , Plant Extracts/chemistry , Larva , Anti-Bacterial Agents/pharmacology , Anti-Bacterial Agents/analysis , Plant Leaves/chemistry
12.
Environ Mol Mutagen ; 63(6): 286-295, 2022 07.
Article in English | MEDLINE | ID: mdl-36053843

ABSTRACT

In this study, the neuroprotective action potential by ulexite (UX) (18.75 mg/L) against acetylferrocene (AFC) (3.82 mg/L) induced neurotoxicity was aimed to investigate in brain tissues of Oncorhynchus mykiss. For this purpose, the effects on neurotoxicity markers, proinflammatory cytokines, antioxidant immune system, DNA, and apoptosis mechanisms were assessed on brain tissues in the 48-96  h of the 96- trial period. In this research, it was determined that brain-derived nerve cell growth factor (BDNF) level and acetylcholinesterase (AChE) activity were inhibited in the brain tissue compared to the control group by AFC. In addition, inhibition in glutathione peroxidase (GPx), catalase (CAT), superoxide dismutase (SOD), and glutathione (GSH) values (which are antioxidant system biomarkers), and inductions in malondialdehyde (MDA) and myeloperoxidase (MPO) amounts (which are indicators of lipid peroxidation) were determined (p < 0.05) after exposure to AFC. And, while tumor necrosis factor-α (TNF-α) and IL-6 levels were increased in the AFC-exposed group, Nrf-2 levels were found to be remarkably decreased. Upregulation was also detected in 8-hydroxydeoxyguanosine (8-OHdG) and caspase-3 levels, which are related to DNA damage and apoptosis mechanism. On the contrary, UX (single/with AFC) suppressed the AChE and BDNF inhibition by AFC. Moreover, UX mitigated AFC-induced oxidative, inflammatory, and DNA damage and attenuated AFC-mediated neurotoxicity via activating Nrf2 signaling in fish. Collectively, our findings revealed that UX supplementation might exert beneficial effects and may be considered as a natural and promising neuroprotective agent against AFC-induced toxicity.


Subject(s)
Neuroprotective Agents , Oncorhynchus mykiss , 8-Hydroxy-2'-Deoxyguanosine , Acetylcholinesterase/metabolism , Acetylcholinesterase/pharmacology , Animals , Antioxidants/metabolism , Antioxidants/pharmacology , Biomarkers/metabolism , Brain-Derived Neurotrophic Factor/metabolism , Brain-Derived Neurotrophic Factor/pharmacology , Caspase 3/metabolism , Caspase 3/pharmacology , Catalase/metabolism , Ferrous Compounds , Glutathione/metabolism , Glutathione Peroxidase/metabolism , Glutathione Peroxidase/pharmacology , Interleukin-6/metabolism , Malondialdehyde , NF-E2-Related Factor 2 , Neuroprotective Agents/pharmacology , Oxidative Stress , Peroxidase/metabolism , Peroxidase/pharmacology , Superoxide Dismutase , Tumor Necrosis Factor-alpha
13.
Molecules ; 27(5)2022 Feb 28.
Article in English | MEDLINE | ID: mdl-35268709

ABSTRACT

Multiple sclerosis is a chronic autoimmune disorder that leads to the demyelination of nerve fibers, which is the major cause of non-traumatic disability all around the world. Herbal plants Nepeta hindustana L., Vitex negundo L., and Argemone albiflora L., in addition to anti-inflammatory and anti-oxidative effects, have shown great potential as neuroprotective agents. The study was aimed to develop a neuroprotective model to study the effectiveness of herbal plants (N. hindustana, V. negundo, and A. albiflora) against multiple sclerosis. The in vivo neuroprotective effects of ethanolic extracts isolated from N. hindustana, V. negundo, and A. albiflora were evaluated in lipopolysaccharides (LPS) induced multiple sclerosis Wistar rat model. The rat models were categorized into seven groups including group A as normal, B as LPS induced diseased group, while C, D, E, F, and G were designed as treatment groups. Histopathological evaluation and biochemical markers including stress and inflammatory (MMP-6, MDA, TNF-α, AOPPs, AGEs, NO, IL-17 and IL-2), antioxidant (SOD, GSH, CAT, GPx), DNA damage (Isop-2α, 8OHdG) as well as molecular biomarkers (RAGE, Caspase-8, p38) along with glutamate, homocysteine, acetylcholinesterase, and myelin binding protein (MBP) were investigated. The obtained data were analyzed using SPSS version 21 and GraphPad Prism 8.0. The different extract treated groups (C, D, E, F, G) displayed a substantial neuroprotective effect regarding remyelination of axonal terminals and oligodendrocytes migration, reduced lymphocytic infiltrations, and reduced necrosis of Purkinje cells. The levels of stress, inflammatory, and DNA damage markers were observed high in the diseased group B, which were reduced after treatments with plant extracts. The antioxidant activity was significantly reduced in diseased induced group B, however, their levels were raised after treatment with plant extract. Group F (a mélange of all the extracts) showed the most significant change among all other treatment groups (C, D, E, G). The communal dose of selected plant extracts regulates neurodegeneration at the cellular level resulting in restoration and remyelination of axonal neurons. Moreover, 400 mg/kg dose of three plants in conjugation (Group F) were found to be more effective in restoring the normal activities of all measured parameters than independent doses (Group C, D, E) and is comparable with standard drug nimodipine (Group G) clinically used for the treatment of multiple sclerosis. The present study, for the first time, reported the clinical evidence of N. hindustana, V. negundo, and A. albiflora against multiple sclerosis and concludes that all three plants showed remyelination as well neuroprotective effects which may be used as a potential natural neurotherapeutic agent against multiple sclerosis.


Subject(s)
Multiple Sclerosis , Plants, Medicinal , Acetylcholinesterase/pharmacology , Animals , Antioxidants/chemistry , Antioxidants/pharmacology , Lipopolysaccharides/pharmacology , Multiple Sclerosis/drug therapy , Oxidative Stress , Plant Extracts/chemistry , Rats , Rats, Wistar
14.
Int J Phytoremediation ; 24(7): 778-786, 2022.
Article in English | MEDLINE | ID: mdl-34541976

ABSTRACT

Diuron herbicide is widely used for weeds control in many kinds of cultivations. It reaches the waterbodies through various fate routes and can adversely threaten non-target organism. The current study was carried out to evaluate the antioxidant activity of Spirulina as feed additive against the toxicity of Diuron concentrations (40 and 80 µg/L) on the edible mollusk Mytilus galloprovincialis during seven days of exposure. Oxidative stress biomarkers were applied on mussel gills and digestive gland, investigating changes in enzymes activities such as catalase (CAT), Glutathione-S-transferase (GST) and Acetylcholinesterase (AChE) and the Malondialdehyde level (MDA). The obtained results show that diuron altered oxidative stress biomarkers in both organs, gills and digestive gland. Performed principle component analysis (PCA) highlighted relationship between biomarkers involved in functional response. Spirulina platensis supplemented diet (1 mg/L), completely ameliorated diuron-induced oxidative stress in mussel tissues. Thus, Spirulina seems to be a promising microalgae and eco-friendly tool helping the health recovery of aquatic animals subjected to environmental stressors.


This study provided recent and new data on the impact of Diuron in marine bivalve and the protective effect of Spirulina against Diuron-induced oxidative stress. The results of our study suggest that the antioxidant potential of Spirulina should be strongly candidate for the phytoremediation of Diuron-aquatic contaminated.


Subject(s)
Mytilus , Spirulina , Water Pollutants, Chemical , Acetylcholinesterase/metabolism , Acetylcholinesterase/pharmacology , Animals , Biodegradation, Environmental , Biomarkers/metabolism , Diuron/pharmacology , Glutathione Transferase/metabolism , Glutathione Transferase/pharmacology , Mytilus/metabolism , Oxidative Stress , Spirulina/metabolism , Water Pollutants, Chemical/toxicity
15.
Trop Biomed ; 39(4): 531-538, 2022 Dec 01.
Article in English | MEDLINE | ID: mdl-36602212

ABSTRACT

Melia azedarach L. (Meliaceae) is a botanical species with focal point of global research for its biological properties. The Melia azedarach tree is distinguished by its rapid growth, its adaptation to different temperate zones, as well as its insecticidal properties. All this made us think of exploiting it in biological control against different stages of mosquitoes. To this end, we aim, through the present work, to evaluate the effectiveness of Melia azedarach extracts against Culex pipiens mosquito. More specifically, our study focuses on determining the chemical composition of Melia almond oil, as well as the larvicidal, ovicidal and repellent activities on Culex pipiens L. mosquito as well as the activities of acetylcholinesterase (AChE) and glutathione-S-transferase (GST). Almond oil was extracted by a Soxhlet and subjected to gas chromatography-mass spectrometry (GC/MS). The yield was found to be 35.17%. The chemical composition revealed the presence of various phytoconstituents. A total of 7 compounds were identified, the main ones being 9,11-Octadecadienoic acid, methyl ester, (E,E)- (79.32%), 9-octadecenoic acid (Z)-, methyl ester (13.24%), hexadecanoic acid and methyl ester (3.69%). The larvicidal bioassays were performed according to the protocol recommended by the World Health Organization with concentrations varying from 20 to 80 mg/L depending on the exposure time (24, 48 and 72 hours). The almond oil exhibited remarkable larvicidal activity against fourth instar larvae and the lethal concentrations were determined (LC25= 23.70 mg/L, LC50=35.49 mg/L, LC90=79.61 mg/L). The results also showed that the oil caused an ovicidal activity with a significant effect on egg hatch. The recorded hatching percentages were respectively 88.79% and 72.40% for the LC25 and LC50, and this compared to the control series. Moreover, this oil exhibited significant repellency against adult mosquitoes. Furthermore, the enzymatic measurements performed on LC50 and LC90 treated larvae revealed a neurotoxic activity and a stimulation of the detoxification system as evidenced, respectively, by an inhibition of AChE and induction in GST activity. Overall, our data proved that Melia azedarach almond oil could be considered as a potent biorational alternative to synthetic insecticides for mosquito control.


Subject(s)
Aedes , Culex , Insecticides , Melia azedarach , Animals , Melia azedarach/chemistry , Plant Extracts/pharmacology , Acetylcholinesterase/pharmacology , Larva , Phytochemicals/pharmacology , Insecticides/pharmacology
16.
Curr Alzheimer Res ; 18(4): 347-357, 2021.
Article in English | MEDLINE | ID: mdl-34279199

ABSTRACT

Alzheimer's disease (AD) is the most prevalent dementia in the elderly, causing disability, physical, psychological, social, and economic damage to the individual, their families, and caregivers. Studies have shown some spices, such as saffron, rosemary, cinnamon, turmeric, and ginger, have antioxidant and anti-inflammatory properties that act in inhibiting the aggregation of acetylcholinesterase and amyloid in AD. For this reason, spices have been studied as beneficial sources against neurodegenerative diseases, including AD. In this sense, this study aims to present a review of some spices (Saffron, Rosemary, Cinnamon, Turmeric and Ginger) and their bioactive compounds, most consumed and investigated in the world regarding AD. In this article, scientific evidence is compiled in clinical trials in adults, the elderly, animals, and in vitro, on properties considered neuroprotective, having no or negative effects on neuroprotection of these spices and their bioactive compounds. The importance of this issue is based on the pharmacological treatment for AD that is still not very effective. In addition, the recommendations and prescriptions of these spices are still permeated by questioning and lack of robust evidence of their effects on neurodegeneration. The literature search suggests all spices included in this article have bioactive compounds with anti-inflammatory and antioxidant actions associated with neuroprotection. To date, the amounts of spice ingestion in humans are not uniform, and there is no consensus on its indication and chronic consumption guarantees safety and efficacy in neuroprotection. Therefore, clinical evidence on this topic is necessary to become a formal adjuvant treatment for AD.


Subject(s)
Acetylcholinesterase/pharmacology , Alzheimer Disease/drug therapy , Antioxidants/pharmacology , Biological Products , Plant Extracts/pharmacology , Spices , Animals , Cinnamomum zeylanicum , Crocus/drug effects , Curcuma/drug effects , Zingiber officinale/drug effects , Humans , Neuroprotection , Rosmarinus/drug effects
17.
Phytother Res ; 34(9): 2287-2302, 2020 Sep.
Article in English | MEDLINE | ID: mdl-32309898

ABSTRACT

The aim of this study was to compare the micro-morphological features of two different non-drug Cannabis sativa L. biotypes (Chinese accession G-309 and one fibrante variety) and to evaluate the phytochemical profile as well as some biological properties of the essential oils (EOs) obtained by hydrodistillation of dried flowering tops. After a micro-morphological evaluation by scanning electron microscopy, the phytochemical composition was analysed by GC-FID and GC-MS analyses. Antioxidant and anti-acetylcholinesterase properties were investigated by several in vitro cell-free assays, while neuroactive effects were evaluated on mouse cortical neuronal as well as human iPS cell-derived central nervous system cells grown on MEA chips. Both EOs showed strong antioxidant properties mainly attributable to the high content of hydroxylated compounds as well as significant anti-acetylcholinesterase activities (IC50 74.64 and 57.31 µg/ml for Chinese accession and fibrante variety, respectively). Furthermore, they showed a concentration-dependent inhibition of spontaneous electrical activity of human and mouse neuronal networks, with the fibrante variety, which showed the best activity (MFR, IC50 0.71 and 10.60 µg/ml, respectively). The observed biological activities could be due to a synergic effect between terpenes and phytocannabinoids, although in vivo studies, which clarify the molecular mechanism, are still lacking.


Subject(s)
Acetylcholinesterase/therapeutic use , Antioxidants/therapeutic use , Cannabis/chemistry , Oils, Volatile/therapeutic use , Plant Extracts/therapeutic use , Acetylcholinesterase/pharmacology , Animals , Antioxidants/pharmacology , Humans , Mice , Oils, Volatile/pharmacology , Plant Extracts/pharmacology
18.
Inflammopharmacology ; 28(2): 563-574, 2020 Apr.
Article in English | MEDLINE | ID: mdl-31792766

ABSTRACT

Brachychiton populneus is one of the unexploited Tunisian plants, traditionally eaten as food and used for medicinal purposes. The present study aimed to investigate the phytochemical components of the seeds, leaves and flowers from B. populneus using three different solvents and to explore their antioxidant, anti-inflammatory and neuroprotective effects. Further, this study was focused on the identification of phenolic compounds from the most active extract. In vitro, all extracts showed strong antioxidant property by DPPH, ferrous ion chelating and lipid peroxidation-inhibiting assays, noticeable anti-inflammatory activity by protein denaturation and membrane stabilization methods and important neuroprotective effects by acetylcholinesterase inhibitory test. In vivo, B. populneus (50, 100 and 200 mg/kg, i.p.) showed significant dose-response anti-inflammatory effects against carrageenan-induced paw edema. With respect to the phenolic profile, the leaf methanol extract presented eight phenolic acids, one flavone and four flavonoids, with salvianolic acid B (820.3 mg/kg), caffeic acid (224.03 mg/kg), syringic acid (100.2 mg/kg) and trans-ferulic acid (60.02 mg/kg) as the major compounds. The results of the current study suggested that B. populneus could be a precious source of health-benefitting biomolecules and may be developed as new antioxidant, anti-inflammatory and AChE inhibitors.


Subject(s)
Anti-Inflammatory Agents/pharmacology , Antioxidants/pharmacology , Malvaceae/chemistry , Plant Extracts/pharmacology , Acetylcholinesterase/administration & dosage , Acetylcholinesterase/drug effects , Acetylcholinesterase/isolation & purification , Acetylcholinesterase/pharmacology , Animals , Anti-Inflammatory Agents/administration & dosage , Anti-Inflammatory Agents/isolation & purification , Antioxidants/administration & dosage , Antioxidants/isolation & purification , Carrageenan , Cholinesterase Inhibitors , Dose-Response Relationship, Drug , Lipid Peroxidation/drug effects , Male , Mice , Neuroprotective Agents/administration & dosage , Neuroprotective Agents/isolation & purification , Neuroprotective Agents/pharmacology , Plant Extracts/administration & dosage , Solvents/chemistry , Spectrometry, Mass, Electrospray Ionization
20.
Molecules ; 24(20)2019 Oct 22.
Article in English | MEDLINE | ID: mdl-31652513

ABSTRACT

Halophytic grasses have been recently targeted as possible sources of nutraceutical and medicinal compounds. Nonetheless, few studies have been conducted on the phytochemistry and biological activities of metabolites produced by these plants. Among these, Spartina maritima (Curtis) Fernald, Spartina patens (Aiton.) Muhl., and Puccinellia maritima (Hudson) Parl. are three halophytic grasses whose chemical composition and bioactivities are unknown. The present work broadens the knowledge on the polyphenolic and chlorophyll composition of these species identifying for the first time hydroxycinnamic acids and their derivatives, flavones, flavonols, lignans, as well as chlorophylls and xantophylls. The extracts were particularly rich in caffeic and ferulic acids as well as in trihydroxymethoxyflavone, apigenin and tricin derivatives. Interestingly, several of the identified compounds are relevant from a medicinal and nutraceutical point of view putting in evidence the potential of these species. Thus, the antioxidant, anti-acetylcholinesterase, antibacterial, and antifungal activities of the polyphenolic extracts were assessed as well as the photophysical properties of the chlorophyll-rich extracts. The results, herein presented for the first time, reinforce the nutritional and the medicinal potential of these halophytic grasses.


Subject(s)
Chlorophyll/chemistry , Plant Extracts/chemistry , Poaceae/chemistry , Polyphenols/chemistry , Salt-Tolerant Plants/chemistry , Acetylcholinesterase/pharmacology , Anti-Bacterial Agents/pharmacology , Antifungal Agents/pharmacology , Antioxidants/metabolism , Chlorophyll/analysis , Chlorophyll/isolation & purification , Cholinesterase Inhibitors/pharmacology , Chromatography, High Pressure Liquid , Coumaric Acids/analysis , Coumaric Acids/chemistry , Dietary Supplements , Flavones/analysis , Flavones/chemistry , Flavonoids/analysis , Flavonoids/chemistry , Flavonols/analysis , Flavonols/chemistry , Free Radical Scavengers/metabolism , Lignans/analysis , Lignans/chemistry , Plants, Medicinal/chemistry , Poaceae/metabolism , Spectrometry, Mass, Electrospray Ionization , Xanthophylls/analysis , Xanthophylls/chemistry
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