Neuropharmacological Activities Research Articles

The impact of seasonal variation on the composition of the volatile oil of Polyalthia suberosa (Roxb.) Thwaites leaves and evaluation of its acetylcholinesterase inhibitory activity

BackgroundPolyalthia suberosa (Roxb.) Thwaites (Annonaceae) is a medicinal plant that has been reported for its various pharmacological potentials, such as its anti-inflammatory, analgesic, antioxidant, and neuropharmacological activities. This study aimed to analyze the leaf essential oils of P. suberosa (PSLO) collected in different seasons, to evaluate the acetylcholinesterase inhibitory activity, and to corroborate the obtained results via in-silico molecular docking studies.MethodsThe leaf essential oils of P. suberosa collected in different seasons were analyzed separately by GC/MS. The acetylcholinesterase inhibitory activity of the leaves oil was assessed via colorimetric assay. In-silico molecular docking studies were elucidated by virtual docking of the main compounds identified in P. suberosa leaf essential oil to the active sites in human acetylcholinesterase crystal structure.ResultsA total of 125 compounds were identified where D-limonene (0.07 − 24.7%), α-copaene (2.25 − 15.49%), E-β-caryophyllene (5.17 − 14.42%), 24-noroleana-3,12-diene (12.92%), β-pinene (0.14 − 8.59%), and α-humulene (2.49–6.9%) were the most abundant components. Results showed a noteworthy influence of the collection season on the chemical composition and yield of the volatile oils. The tested oil adequately inhibited acetylcholinesterase enzyme with an IC50 value of 91.94 µg/mL. Additionally, in-silico molecular docking unveiled that palmitic acid, phytol, p-cymene, and caryophyllene oxide demonstrated the highest fitting scores within the active sites of human acetylcholinesterase enzyme.ConclusionsFrom these findings, it is concluded that P. suberosa leaf oil should be evaluated as a food supplement for enhancing memory.

Plants with Potential Neuropharmacological Activity: Plant-based Medicine for the Brain

Plants with Potential Neuropharmacological Activity: Plant-based Medicine for the Brain

Neuropharmacological assessment and identification of possible lead compound (apomorphine) from Hygrophila spinosa through in-vivo and in-silico approaches

The aim of this research is to examine possible neurological activity of methanol, ethyl acetate, and aqueous extracts of Hygrophila spinosa and identify possible lead compounds through in silico analysis. In vivo, neuropharmacological activity was evaluated by using four distinct neuropharmacological assessment assays. Previously reported GC-MS data and earlier literature were utilized to identify the phytochemicals present in Hygrophila spinosa. Computational studies notably molecular docking and molecular dynamic simulations were conducted with responsible receptors to assess the stability of the best interacting compound. Pharmacokinetics properties like absorption, distribution, metabolism, excretion, and toxicity were considered to evaluate the drug likeliness properties of the identified compounds. All the in vivo results support the notion that different extracts (methanol, ethyl acetate, and aqueous) of Hygrophila spinosa have significant (*p = 0.05) sedative-hypnotic, anxiolytic, and anti-depressant activity. Among all the extracts, specifically methanol extracts of Hygrophila spinosa (MHS 400 mg/kg.b.w.) showed better sedative, anxiolytic and antidepressant activity than aqueous and ethyl acetate extracts. In silico molecular docking analysis revealed that among 53 compounds 7 compounds showed good binding affinities and one compound, namely apomorphine (CID: 6005), surprisingly showed promising binding affinity to all the receptors . An analysis of molecular dynamics simulations confirmed that apomorphine (CID: 6005) had a high level of stability at the protein binding site. Evidence suggests that Hygrophila spinosa has significant sedative, anxiolytic, and antidepressant activity. In silico analysis revealed that a particular compound (apomorphine) is responsible for this action. Further research is required in order to establish apomorphine as a drug for anxiety, depression, and sleep disorders. Communicated by Ramaswamy H. Sarma

Biological Activities of Aurones: A Brief Summary

Abstract: Aurones are structural isomers of flavones and flavonols with the basic C6–C3–C6 skeleton arranged as (Z)-2-benzylidenebenzofuran-3(2H)-one, which contain an exocyclic carbon-carbon double bond bridging the benzofuranone and phenyl rings. In aurone, a chalcone-like group is closed into a 5-membered ring instead of the 6-membered ring more typical of flavonoids, which forms the core for a family of derivatives that are known collectively as aurones. As a kind of flavonoids, aurones are widely distributed in many plants which provide yellow color to some popular ornamental flowers. For a long time aurones had not got enough attention, while in recent years, finally this chemical is coming into researchers' view. As the secondary metabolite in the family of flavonoids, aurones displayed various biological activities, including antioxidant, antiparasitic, antitumor, antiviral, antibacterial, anti-inflammatory, anti-SARS-CoV-2 and neuropharmacological activities. Therefore, aurones have attracted the attention of more and more chemists and pharmaceutical chemists, who realized that it is possible to get lead compounds with better activities via structural modifications of aurones. In some research works, aurone and its derivatives have exhibited good activity, e.g., Xie discovered the heterocyclic variant of the (Z)-2-benzylidene-6-hydroxybenzofuran-3(2H)- one scaffold that possessed low nanomolar in vitro potency in cell proliferation assays using various cancer cell lines, in vivo potency in prostate cancer PC-3 xenograft and zebrafish models, and absence of appreciable toxicity, which proved that aurones are valuable compounds worthy of further study. Herein, the biological activities of aurone derivatives are reviewed, which covers the literature since 2000, in which the strategies to develop bioactive aurone derivatives and the structureactivity relationship are highlighted.

Evaluation of Cytotoxic and Neuropharmacological Activity of Methanolic Extract of Solanum capsicoides Leaves

Background: Solanum capsicoides has medicinal importance due to having numerous therapeutically active ingredients. Objective: The aim of this study was to assess and interpret the cytotoxic and neuropharmacological activity of the methanolic extract of Solanum capsicoides leaves. Methods: The lethality bioassay test on brine shrimp was used to evaluate the cytotoxicity effect of the methanolic extract of Solanum capsicoides leaves. To evaluate the neuropharmacological activities of this plant extract, hole board test, hole cross test, open field test and elevated plus-maze test were used in mice model. All assessments were statistically analysed using one-way ANOVA followed by Dunnett’s t-test. All of the data were analysed with the help of the SPSS software. Results: The test for brine shrimp lethality demonstrated that the LC50 of methanolic extract of Solanum capsicoides leaves was 55.883 μg/ml, containing potent cytotoxic components. The statistically significant (*P<0.05, **P<0.05 vs. control) result in hole board test, hole cross test, open field test, and elevated plus-maze test reveals the CNS depressant and anxiolytic properties in methanolic extract of Solanum capsicoides leaves. Conclusion: Results from our study support that the methanolic extract of Solanum capsicoides might possess significant cytotoxic characteristics, CNS depressant and anxiolytic effect. However, additional research is required to pinpoint the precise bioactive chemicals that are responsible for these activities.

Neuropharmacological Activity of the Acetonic Extract of Malpighia mexicana A. Juss. and Its Phytochemical Profile

Mental and neurological disorders are conditions that affect thoughts, emotions, behavior, and relationships. Malpighia mexicana A. Juss. is a plant used in Mexican traditional medicine for the treatment of such disorders. This work aimed to investigate the antidepressant, anxiolytic, sedative, hypnotic, and anticonvulsant effects of the acetonic extract (MmAE) of M. mexicana and its fractions (F3, F4-10, F14) using the forced swimming test (FST), elevated plus maze (EPM), open field test (OFT), pentobarbital-induced sleep test (PBTt), and pentylenetetrazol-induced seizure test (PTZt). MmAE, F3, F4-10, F14, and vehicle were administrated orally 24, 18, and 1 h prior to the evaluations. Imipramine (15 mg/kg, p.o.) was administrated 1 h prior to the evaluations as a positive control for the FST, while diazepam (1 mg/kg, p.o.) was administrated 1 h prior to the evaluations as a positive control for the EPM, OFT, PBTt, and PTZt. MmAE had an anxiolytic effect; MmAE and F3, F4-10, and F14 showed an antidepressant effect, sedative effect, hypnotic effect, and anticonvulsant effect. Using HPLC, we identified the compounds quercetin 3-O-rutinoside (1), kaempferol 3-O-glucoside (2), luteolin 7-O-glucoside (3), quercetin (4), and kaempferol (5) in MmAE and compounds (1), (2), and (3) in F14. Using GC-MS, we identified α-tocopherol, phytol, and β-amyrin in F3; β-tocopherol, phytol, β-sitosterol, and β-amyrin in F4-10; and α- tocopherol, phytol, β-sitosterol, and β-amyrin in F4-10. The neuropharmacological effects found in this work may be due to the presence of vitamins, phytosterols, terpenes, and flavonoids. This research requires further study to clarify the mechanisms of action of the identified compounds.

Evaluation of In-vitro Antimicrobial, Anti-arthritis and In-vivo Analgesic and Neuropharmacological Investigation of the Bark Extract of Solanum americanum Milli

Purpose: The objective of this study was to investigate the impact of methanol-prepared bark extract of Solanum americanum Milli. Bark on several in vitro activities, including antimicrobial and anti-arthritis effects. Additionally, the study aimed to assess the analgesic and neuropharmacological properties of the extracts in an animal model.
 Place and Duration of Study: The research study was carried out from March 2023 to July 2023 at the Bangladesh Council of Scientific and Industrial Research (BCSIR) and the Laboratory of Phytochemistry and Pharmacology, Department of Pharmacy, as well as the Laboratory of Microbiology at Stamford University Bangladesh, Dhaka.
 Methodology: The methodology involved various doses of methanolic bark extract of Solanum americanum Milli (MESAB), and employed techniques such as the Disk Diffusion Method for antimicrobial test and the Inhibition of Protein Denaturation Assay for anti-arthritic test. The analgesic efficacy was assessed by the hot plate test and administration of acetic acid induced writhing responses in Swiss albino mice. The mechanism test is conducted through the cyclic guanosine monophosphate (cGMP) test. The neuropharmacological inquiry included the measurement of locomotor activity through the utilization of open field and hole cross tests.
 Results: The Disk Diffusion Test of MESAB yielded findings indicating its antimicrobial properties against all strains used in this research. The findings from the study examining the anti-arthritis properties indicate that MESAB exhibits a significant efficacy of 94.59% in inhibiting arthritis at a concentration of 1000 µg/mL. This level of efficacy is comparable to that of diclofenac sodium, which also has a similar efficacy of 98.19% at the same concentration. The findings of the present study demonstrated that MESAB displayed analgesic properties in both analgesic models, suggesting the involvement of both central and peripheral pathways. Based on the results of the study, it was observed that the administration of MESAB at a dosage of 400 mg/kg had a significant analgesic effect. The application of MB before to treatment resulted in a further enhancement of this effect, leading to an increase in the percentage of inhibition from 66.75% to 79.70%, respectively. The consideration of the involvement of the GABA-benzodiazepine receptor in neuropharmacological activity holds significant importance. In the Open Field and Hole Cross Tests, it was shown that the extract exhibited significant result compared to Diazepam in terms of increasing motor coordination.
 Conclusion: In the future, plant-derived pharmacological compounds may offer potential benefits for various clinical disorders, such as neurodegenerative illnesses. These substances possess neuropharmacological properties, antibacterial effects, and anti-arthritic activity, which could potentially serve as alternatives to non-steroidal anti-inflammatory drugs (NSAIDs).

Memory, Nootropics and Ayurveda- A Critical Appraisal

Memory is an essential function of our cognition that helps us to remember events, learn lessons and preserve emotions; to live each day with new learning and optimum behavior. There have been talks on using safe nootropic drugs to enhance Memory in healthy patients with memory disorders. The ancient sages of Ayurveda and Vedic civilizations advocate learning and memorizing many hymns and verses by their pupils. It leads to the discovery of the cognition and memory enhancing drugs known as Medhya Rasayana. Ayurveda possesses a treasure of Medhya Rasayana, known as nootropics. This review aims to elaborate on and explain the Ayurvedic concept of memory and nootropics about the contemporary concept. Online research databases like DHARA, Ayush Research Portal, Pubmed, Google Scholar, etc., were searched for relevant research articles by applying adequate keywords. Ayurvedic concepts of Buddhi, acquisition of knowledge, Medha, and Medhya Rasayana were reviewed from Ayurvedic classics. This paper discusses the contemporary concept of memory along with its classification, mechanisms of production, and probable mode of its enhancement. The well-described Ayurvedic concept of the cognitive process and Medha and Pragya (intellect) have been analyzed, elaborated, and explained as per contemporary knowledge. A few Medhya drugs like Brahmi (Bacopa monnieri), Mandookaparni (Centella asiatica), Shankhpushpi (Convolvulus pluricaulis), and Vacha (Acorus calamus) are analyzed for their properties explained in Ayurveda and their neuropharmacological activities in the light of recent experimental and clinical studies. The probable two groups based upon the mode of action of Medhya drugs- one which promotes Dhriti and the other which promotes Medha (mainly Dhi & Smriti) are also discussed. In conclusion, memory enhancement in healthy and pathological states is requisite in today's competitive world. With its vast treasure of Medhya drugs, Ayurveda can greatly help in this field

Screening of Neuropharmacological Activities of Naringi crenulata (Roxb.) Nicolson Leaves

Purpose: Although the global prevalence of psychological disorders is increasing continually, the efficacies of therapeutic strategies are still very limited. Oxidative stress has been implicated in the pathogenesis of psychiatric disorders and substances possessing antioxidant activity can alleviate the mentioned conditions. Therefore, we hypothesized that Naringi crenulata (Roxb.) Nicolson leaves, a medicinal plant claimed for nerve tonic, also possess neuropharmacological activities which provide an advantage for psychiatric disorders.
 Methods: The present study was carried out to perform neuropharmacological screenings methods on sedatives and hypnotics (Phenobarbitone sodium-induced sleep latency and sleep time and Motor coordination activity), anxiolytics (elevated plus maze and open field test), anti-depressants (forced swim test and L-dopa induced hyperactive aggressive behaviour in mice) and anticonvulsants activities (PTZ and MES induced convulsions) in Swiss Albino mice and Sprague Dawley rats.
 Results: The methanolic extract of a higher dose of Phenobarbitone sodium in Naringi crenulata induced sleep latency and sleep time significant results. The extracts of Naringi crenulate showed a significant dose-dependent increase in muscle relaxation in motor coordination activity. In the experiment of PTZ-induced convulsions, the latency of seizures was prolonged by the extracts in a dose-dependent manner. Even in MES-induced convulsion, the results were extremely significant for the 400mg/kg of MENC. The depressant effect was observed to be significant to the extracts of the herb in the Open Field test and also for the Elevated Plus Maze apparatus. In the Forced Swim Test, MENC (400 mg/kg) significantly lengthened the time spent immobile (p <0.01), indicating a CNS depressive impact. Lastly in L-dopa-induced hyperactive aggressive behaviour in mice, results suggest that NC has antidepressant efficacy due to its influence on the serotonergic, noradrenergic, and dopaminergic systems.
 Conclusion: The methanolic extract of Naringi crenulata (Roxb.) Nicolson leaves showed significant neuroprotective activity. So, the extracts of Naringi crenulata can be used for the treatment of a wide variety of neurological ailments in humans.

Antihyperglycemic, Neuropharmacological, Cytotoxic, Anticoagulant, and Anti-inflammatory Pharmacological Evaluations of Vernonia elaeagnifolia DC Leaves Secondary Bioactive Metabolites

The current investigation was carried out to confirm the antihyperglycemic, cytotoxic, neuropharmacological, anticoagulant, and anti-inflammatory effects of the ethanolic extract of Vernonia elaeagnifolia leaves in different experimental models. In the oral glucose tolerance test, the plant extract demonstrated significant (p < 0.05) antihyperglycemic activity by reducing the elevated blood glucose level in mice at both doses (250 mg/kg and 500 mg/kg) when compared to the control groups. The crude ethanolic leaf extract, however, didn’t afford to block the α-glucosidase enzyme up to 0.5 mg/mL. The experimental mice showed a noticeable (p <0.001) decrease in locomotor and exploratory activities in the hole cross and open field tests, as well as head dipping in the hole-board test model in the neuropharmacological activity assay at both doses (250 mg/kg and 500 mg/kg). The extracts also showed cytotoxic activity in a brine shrimp lethality bioassay with an LC50 of 91.929 μg/mL and showed significant concentration-dependent anticoagulant activity (p<0.001). Moreover, the extract (10–500 mg/kg) caused a significant (P<0.01 – 0.001) dose-dependent reduction of inflammation induced in rats by using two different models: formalin-induced paw edema and egg-albumin-induced paw edema. From the above results, the crude extract of V. elaeagnifolia DC leaves have significant pharmacological potential in different in vitro and in vivo study model. So, it could be a source of a substance for isolating lead that could be used to treat several diseases.

Neuropharmacological study of Moringa olifera

Objective: Moringa olifera is a medicinal plant widely used in many parts of the world for hypertension, pain and epilepsy. The aim of this study was to determine the effect of M. olifera aqueous leaf, root and steam extract on neurobehavioral activities of healthy mice. Method: Male mice were randomly divided into a control group (given 0.9% NaCl orally) and three groups treated with the extract at doses of 100, 200, and 400 mg/kg/day for 14 consecutive days. Neuropharmacological activity were evaluated by neuro-muscular coordination (rota rod treadmill), pain (hot plate and acetic acid-induced abdominal constriction). Administration of M. olifera extract had a significant and dose dependent antinociceptive action in both thermal and chemical tests (p < 0.05). The extract (400 mg/kg) caused a reduction in exploration activity and neuromuscular coordination, and decreased the mobility time in the FST, suggesting an antidepressant-like action. Motor activity was not significantly affected by any of the doses used. Conclusion: The results suggest that the plant aqueous extract may have a dose-dependent central nervous system (CNS) depressant action.

Neuropharmacological assessment of the methanolic stem back extract of Anopyxis klaineana (Pierre) Engl. (Rhizophoraceae) in mice

BackgroundMedicinal plants have recently attracted attention on a global scale for therapeutic interventions in the field of neuroscience. Anopyxis klaineana, a medicinal plant widely used in West Africa, has been studied extensively for its anti-inflammatory effects. However, studies on its neuropharmacological effects are quite limited. This study therefore assessed the neuropharmacological potential of the methanolic stem bark extract of Anopyxis klaineana (EAK) in murine models. Materials and methodsMice were treated orally with a methanolic stem back extract of Anopyxis klaineana (EAK) at 10, 30 or 100 mg/kg followed by testing in the elevated plus-maze (EPM) and open field (OF) tests for anxiolytic-like effects. EAK's antidepressant-like potential was also evaluated in the tail suspension test (TST), while anticonvulsant and central analgesic effects were evaluated with the pentylenetetrazol (PTZ)-induced convulsion threshold and tail withdrawal tests respectively at 30, 100 or 300 mg/kg. The extract was additionally subjected to chromatographic analyses using high resolution HPLC-MS. ResultsTotal ion current chromatogram of EAK revealed several peaks suggestive of secondary metabolites of the plant extract. EAK significantly (p<0.05) reduced depression-like behaviours in the TST although not as potent as fluoxetine (ED50: EAK=43.39±2.5; fluoxetine=1.16±1.6) (F3,20=9.663, p = 0.0004). It also showed significant anticonvulsive effect by reducing the frequency and duration of PTZ-induced convulsions (ED50=48.53±2.5 mg/kg) (F3,19=5.136, p = 0.0091). This anticonvulsant effect was seen in both clonic and tonic convulsions at 30 and 300 mg/kg. Additionally, EAK-treated mice showed higher latency to tail withdrawal in the analgesia test. We also observed significant (p<0.05) dose-dependent increase in anxiolytic-like effects in EAK-treated animals in the EPM (F3,20=10.77, p = 0.0002) and OF tests (F3,22=5.079, p = 0.008). ConclusionsThe methanolic Anopyxis klaineana stem back extract exhibits anxiolytic-like, antidepressant-like, analgesic and anticonvulsant effects in murine models for assessing neuropharmacological activity and is a good source for novel neuroactive compounds.

Bryostatin-1: a promising compound for neurological disorders.

The central nervous system (CNS) is the most complex system in human body, and there is often a lack of effective treatment strategies for the disorders related with CNS. Natural compounds with multiple pharmacological activities may offer better options because they have broad cellular targets and potentially produce synergic and integrative effects. Bryostatin-1 is one of such promising compounds, a macrolide separated from marine invertebrates. Bryostatin-1 has been shown to produce various biological activities through binding with protein kinase C (PKC). In this review, we mainly summarize the pharmacological effects of bryostatin-1 in the treatment of multiple neurological diseases in preclinical studies and clinical trials. Bryostatin-1 is shown to have great therapeutic potential for Alzheimer's disease, multiple sclerosis, fragile X syndrome, stroke, traumatic brain injury, and depression. It exhibits significant rescuing effects on the deficits of spatial learning, cognitive function, memory and other neurological functions caused by diseases, producing good neuroprotective effects. The promising neuropharmacological activities of bryostatin-1 suggest that it is a potential candidate for the treatment of related neurological disorders although there are still some issues needed to be addressed before its application in clinic.

A Review on Pharmacological activities of Colocasia esculenta

Mother Nature has always given us essential medicinal plants for long decades. Today modern world has started its dependability on medicinal agents obtained from traditionally used plants. Colocasia esculenta is a magnificent source of fiber and starch, which is responsible for number of health benefits, such as for improved blood sugar levels, for better skin care, helps to reduce obesity. Colocasia esculenta also contains a variety of antioxidants and polyphenols. Leaves are caloriedeficient, rich in proteins, micronutrients, dietary fiber and good carbohydrates which enhance the metabolism of our digestive system and it helps to provide healthy weight loss, even they have abundant presence of anti-nutrients such as tannins, oxalates. It consists of high levels of Vit.E, Vit.C, and Vit. B6 also contributes to maintain a better immune system and may eradicate free radicals. All parts of Colocasia esculenta have essential properties including some levels of toxicity which are overcome by cooking and steamed boiling. It has several health benefits like anti-hepatotoxic and hepatoprotective activity, anti-inflammatory activity, neuropharmacological activity, anti-fungal activity and anti-metastatic activity. In India major Colocasia esculenta production occurs in states like Uttar-Pradesh, Kerala, Maharashtra, Tamil Nadu, Himachal-Pradesh, Gujarat, etc. The present review includes detail study of pharmacological activity of plant- Colocasia esculenta [Taro].

Taohong siwu decoction ameliorates cognitive dysfunction through SIRT6/ER stress pathway in Alzheimer's disease

Ethnopharmacological relevanceA growing number of people suffer from Alzheimer's disease (AD), but there is currently no effective treatment yet. Taohong Siwu Decoction (TSD) has been proved to take strong neuropharmacological activity on dementia, but the effect and mechanism of TSD against AD are still elusive. Aim of studyTo investigate whether TSD could be effective in ameliorating cognitive deficits through SIRT6/ER stress pathway. Materials and methodsHerein, the APP/PS1 mice, an AD model, and HT-22 cell lines were utilized. Different dosages of TSD (4.25, 8.50 and 17.00 g/kg/d) were administered to the mice for 10 weeks by gavage. Following the behavioral tests, oxidative stress levels were measured using malondialdehyde (MDA) and superoxide dismutase (SOD) kits. Nissl staining and Western blot analyses were used to detect the neuronal function. Then, immunofluorescence and Western blot analysis were applied to evaluate silent information regulator 6 (SIRT6) and ER Stress related protein levels in APP/PS1 mice and HT-22 cells. ResultsBehavioral tests revealed that APP/PS1 mice administered with TSD orally took more time in the target quadrant, crossed more times in the target quadrant, had a higher recognition coefficient, and spent more time in the central region. In addition, TSD could ameliorate oxidative stress and inhibit neuronal apoptosis in APP/PS1 mice. Furthermore, TSD could up-regulate the SIRT6 protein expression and inhibit ER sensing proteins expressions, such as p-PERK and ATF6, in APP/PS1 mice and Aβ1-42-treated HT22 cells. ConclusionAccording to the abovementioned findings, TSD could alleviate cognitive dysfunction in AD by modulating the SIRT6/ER stress pathway.

In-Vitro Antioxidant, Anti-Arthritis, Anti-inflammatory, Thrombolysis, Anti-bacterial, and in-Vivo Neuropharmacological Activities of Bioactive Metabolites of Solanum americanum Mill.

Aims: The purpose of this research was to examine the effects of methanol-prepared leaf extracts from the Solanum americanum Mill. plant on a variety of in vitro activities, including antioxidant, anti-Arthritis, anti-inflammatory, thrombolysis, anti-bacterial, and in-vivo neuropharmacological activities.&#x0D; Study Design: Methanolic extract of Solanum americanum leaf (MESAL) was primarily evaluated via phytochemical screening. The potential for in vitro activities, including antioxidant, anti-arthritis, anti-inflammatory, thrombolysis, and anti-bacterial activity were determined to study due to the pharmacological interest in the plant's chemical constituent. Whether there is statistical significance to the changes seen in its in vivo neuropharmacological characteristics when tested in experimental animals.&#x0D; Place and Duration of Study: This research was carried out between November 2022 to January 2023 at the Laboratory of Phytochemistry and Pharmacology in the Department of Pharmacy and Laboratory of Microbiology, Stamford University Bangladesh and Bangladesh Council of Scientific and Industrial Research, Dhaka.&#x0D; Methodology: The plant was subjected to phytochemical screening utilizing a variety of test reagents and potential antioxidant, anti-arthritis, anti-inflammatory, thrombolytic, anti-bacterial, and neuropharmacological activities of MESAL were investigated. Antioxidant, anti-arthritic, anti-inflammatory, thrombolytic, and antibacterial activities were tested at different doses utilizing the DPPH Free Radical Scavenging Assay, Protein Denaturation Assays, Clot Lysis, and the Disk Diffusion Method. Swiss albino mice were tested using open-field and hole-cross methods to measure their locomotion as part of the neuropharmacological study.&#x0D; Results: The MESAL phytochemical screening findings demonstrated that the plants' chemical compositions varied. Most antioxidant activities were found in MESA, with an IC50 of 11.73 µg/mL compared to Ascorbic acid's IC50 of 28.86 µg/mL. When compared to the standard, the percent inhibition value of MESAL's anti-arthritis activity was significantly higher. With a maximum protein denaturation value of 94.03% at a concentration of 1000µg/mL, MESAL possesses potent anti-inflammatory activity. The value of MESAL in terms of clot lysis is very significant which is 90.257%. While MESAL's antibacterial value is moderate, it is still worth considering. However, the extract was proven to be less effective than Diazepam in improving motor coordination in the Open Field and Hole Cross Tests.&#x0D; Conclusion: Several pathological conditions, including neurodegenerative diseases, may benefit in the future from the use of plant-derived pharmacological agents due to their neuropharmacological, antioxidant, anti-inflammatory, and anti-arthritic activity, which can replace the use of NSAIDs.

Molecular Docking and Dynamics Simulation Studies Predict Potential Anti-ADAR2 Inhibitors: Implications for the Treatment of Cancer, Neurological, Immunological and Infectious Diseases.

Altered RNA editing has been linked to several neurodevelopmental disorders, including autism spectrum disorder (ASD) and intellectual disability, in addition to depression, schizophrenia, some cancers, viral infections and autoimmune disorders. The human ADAR2 is a potential therapeutic target for managing these various disorders due to its crucial role in adenosine to inosine editing. This study applied consensus scoring to rank potential ADAR2 inhibitors after performing molecular docking with AutoDock Vina and Glide (Maestro), using a library of 35,161 compounds obtained from traditional Chinese medicine. A total of 47 compounds were predicted to be good binders of the human ADAR2 and had insignificant toxicity concerns. Molecular dynamics (MD) simulations, including the molecular mechanics Poisson-Boltzmann surface area (MM/PBSA) procedure, also emphasized the binding of the shortlisted compounds. The potential compounds had plausible binding free energies ranging from -81.304 to -1068.26 kJ/mol from the MM/PBSA calculations. ZINC000085511995, a naphthoquinone had more negative binding free energy (-1068.26 kJ/mol) than inositol hexakisphosphate (IHP) [-873.873 kJ/mol], an agonist and a strong binder of ADAR2. The potential displacement of IHP by ZINC000085511995 in the IHP binding site of ADAR2 could be explored for possible deactivation of ADAR2. Bayesian-based biological activity prediction corroborates the neuropharmacological, antineoplastic and antiviral activity of the potential lead compounds. All the potential lead compounds, except ZINC000014612330 and ZINC000013462928, were predicted to be inhibitors of various deaminases. The potential lead compounds also had probability of activity (Pa) > 0.442 and probability of inactivity (Pi) < 0.116 values for treating acute neurologic disorders, except for ZINC000085996580 and ZINC000013462928. Pursuing these compounds for their anti-ADAR2 activities holds a promising future, especially against neurological disorders, some cancers and viral infections caused by RNA viruses. Molecular interaction, hydrogen bond and per-residue decomposition analyses predicted Arg400, Arg401, Lys519, Trp687, Glu689, and Lys690 as hot-spot residues in the ADAR2 IHP binding site. Most of the top compounds were observed to have naphthoquinone, indole, furanocoumarin or benzofuran moieties. Serotonin and tryptophan, which are beneficial in digestive regulation, improving sleep cycle and mood, are indole derivatives. These chemical series may have the potential to treat neurological disorders, prion diseases, some cancers, specific viral infections, metabolic disorders and eating disorders through the disruption of ADAR2 pathways. A total of nine potential lead compounds were shortlisted as plausible modulators of ADAR2.

In-vitro and In-vivo Pharmacological Evaluation of Persicaria lapathifolia Available in Bangladesh

Purpose: The purpose of this research was to examine the effects of Persicaria lapathifolia (Pale smartweed) leaf and bark extracts prepared with methanol on in vitro activities like antioxidant, antimicrobial, anti-arthritis, anti-inflammatory, and cytotoxic, as well as on some in vivo activities like analgesic and neuropharmacological properties in animal model.&#x0D; Methodology: The primary method for the methanolic extract of Persicaria lapathifolia leaf (MEPLL) and methanolic extract of Persicaria lapathifolia bark (MEPLB) were investigated for phytochemical screening. It was determined to look into the plant's potential for in vitro activities, such as phytochemical screening, antioxidant, anti-arthritis, anti-inflammatory, anti-bacterial, and cytotoxic, due to the pharmaceutical interest in its component parts. Its described effects on its in vivo analgesic and neuropharmacological activities in animal models are significant compared to the standard. This research was conducted between July 2022 and November 2022 in the Stamford University Bangladesh, Dhaka, Laboratory of Physiology and Pharmacology, Department of Pharmacy, and Laboratory of Microbiology. Antioxidant, anti-arthritic, anti-inflammatory, antibacterial, cytotoxic, analgesic, and neuropharmacological activities of MEPLL and MEPLB were investigated. Phytochemical screening was performed utilizing a variety of test reagents. Antioxidant, total phenolic content, anti-arthritic, anti-inflammatory, antibacterial, and cytotoxic activities were measured at various doses using the DPPH Free Radical Scavenging Assay, the Folin-Ciocalteu technique, the Inhibition of Protein Denaturation Assay, Egg Albumin Protein Denaturation Assay, the Disk Diffusion Method, and the Brine Shrimp Lethality Bioassay. The analgesic effectiveness was evaluated by using acetic acid to elicit writhing in Swiss albino mice and then testing the animals on a hot plate. Locomotor activity was measured by open field and hole cross tests as part of the neuropharmacological investigation.&#x0D; Results: Research performed on MEPLL and MEPLB's phytochemical screening yielded results that revealed the presence of a variety of different phytochemical components. In comparison to MEPLL's IC50 value of 1.49 µg/mL, MEPLB's value of 30.45 µg/mL indicates its superior antioxidant activity. Both extracts demonstrated significant anti-arthritic and anti-inflammatory effectiveness in comparison to the standard drug. When compared to MEPLB, MEPLL exhibited much more antibacterial activity. In a lethality test using brine shrimp, MEPLL and MEPLB both had much higher LC50 values than the standard vincristine sulfate. Their respective values were 1.42 and 0.66 µg/mL. In contrast, MEPLL inhibited peripheral nociception in the acetic acid-induced writhing nociceptive paradigm with percent inhibitions of 60.72 and 67.56, respectively, while MEPLB inhibited 48.22 and 67.28, respectively, at the aforementioned doses. In addition, the hot plate test revealed a significant analgesic effect. The extract was also shown to have a more negative impact on motor coordination in the Open Field and Hole Cross Tests than the standard Diazepam.&#x0D; Conclusion: This research demonstrates a relationship between the existence of anti-oxidative, anti-arthritis, and anti-bacterial activities, as well as a strong cytotoxic, analgesic, and neuropharmacological activity, which substantiates all previously made claims against Persicaria lapathifolia.

Celastrus paniculatus oil ameliorates NF-KB mediated neuroinflammation and synaptic plasticity in the scopolamine-induced cognitive impairment rat model.

Traditionally, Celastrus paniculatus Willd. (CP) oil has been utilized as a tranquilizer and memory enhancer. The present study investigated the neuropharmacological activity and efficacy of CP oil in ameliorating scopolamine-induced cognitive impairment in rats. Cognitive deficiency was induced in rats by administration of scopolamine (2mg/kg intraperitoneal injection) for a period of 15 days. Donepezil served as a reference drug and CP oil was tested as both preventive and curative treatments. Animals' behaviour was assessed through the Morris water maze (MWM), novel object preference (NOR), and conditioned avoidance (CA) tests. Oxidative stress parameters, bioamine concentration (dopamine, noradrenaline, and 5-hydroxytryptamine), nerve growth factor (NGF), interleukin-6 (IL-6), nuclear factor kappa B (NF-кB), and tumor necrosis factor-alpha (TNFα) were estimated. Synaptophysin immunohistochemistry was performed. Our results showed that CP oil ameliorated behavioural deficits. It reduced latency to find a hidden platform in MWM. Reduced novel object exploration time and discrimination index (p < 0.05) in the NOR. Reduced step-down latency and normalized conditioned avoidance response (p < 0.001) in the CA test. CP oil increased dopamine, serotonin, norepinephrine, superoxide dismutase (SOD), glutathione, and catalase levels. It decreased malondialdehyde (MDA), acetylcholinesterase activity, IL-6, NF-кB (P < 0.001), TNFα, and NGF levels. Treatment showed approximate typical reactivity to synaptophysin. Our data is suggestive that CP oil treatment improves behavioural test outcomes, increases biogenic amine concentration, and decreases acetylcholinesterase activity, and neuroinflammatory biomarkers. It also restores synaptic plasticity. It thus improves cognitive functions against scopolamine-induced amnesia in rats by improving cholinergic function.

An insight into the neuroprotective and anti-neuroinflammatory effects and mechanisms of Moringa oleifera.

Neurodegenerative diseases (NDs) are sporadic maladies that affect patients' lives with progressive neurological disabilities and reduced quality of life. Neuroinflammation and oxidative reaction are among the pivotal factors for neurodegenerative conditions, contributing to the progression of NDs, such as Parkinson's disease (PD), Alzheimer's disease (AD), multiple sclerosis (MS) and Huntington's disease (HD). Management of NDs is still less than optimum due to its wide range of causative factors and influences, such as lifestyle, genetic variants, and environmental aspects. The neuroprotective and anti-neuroinflammatory activities of Moringa oleifera have been documented in numerous studies due to its richness of phytochemicals with antioxidant and anti-inflammatory properties. This review highlights up-to-date research findings on the anti-neuroinflammatory and neuroprotective effects of M. oleifera, including mechanisms against NDs. The information was gathered from databases, which include Scopus, Science Direct, Ovid-MEDLINE, Springer, and Elsevier. Neuroprotective effects of M. oleifera were mainly assessed by using the crude extracts in vitro and in vivo experiments. Isolated compounds from M. oleifera such as moringin, astragalin, and isoquercitrin, and identified compounds of M. oleifera such as phenolic acids and flavonoids (chlorogenic acid, gallic acid, ferulic acid, caffeic acid, kaempferol, quercetin, myricetin, (-)-epicatechin, and isoquercitrin) have been reported to have neuropharmacological activities. Therefore, these compounds may potentially contribute to the neuroprotective and anti-neuroinflammatory effects. More in-depth studies using in vivo animal models of neurological-related disorders and extensive preclinical investigations, such as pharmacokinetics, toxicity, and bioavailability studies are necessary before clinical trials can be carried out to develop M. oleifera constituents into neuroprotective agents.