Evaluation of acetylcholinesterase and butyrylcholinesterase inhibitory activity of Huperzine-A; in silico and in vitro studies

The present study is focused on exploring the Acetylcholinesterase and Butyrylcholinesterase inhibitory activity of Huperzine-A in silico and in vitro. In this study, Huperzine-A-A was docked with Acetylcholinesterase and Butyrylcholinesterase. Docking studies revealed the excellent interaction of Huperzine-A-A with these targets. The result of present study provides insight for the in vitro studies. The in vitro studies the enzyme kinetics of Huperzine-A-A via Lineweaver brooks plot revealed the kinetics and non-competitive inhibitory nature of the later. Further studies on Huperzine-A-A are necessary to develop and establish its role on brain cholinergic system and cognitive deficits which may serve a stepping stone in CNS medication

Evaluation of acetylcholinesterase and butyrylcholinesterase inhibitory activity of Huperzine-A; in silico and in vitro studies

224-229The present study is focused on exploring the Acetylcholinesterase and Butyrylcholinesterase inhibitory activity of Huperzine-A in silico and in vitro. In this study, Huperzine-A-A was docked with Acetylcholinesterase and Butyrylcholinesterase. Docking studies revealed the excellent interaction of Huperzine-A-A with these targets. The result of present study provides insight for the in vitro studies. The in vitro studies the enzyme kinetics of Huperzine-A-A via Lineweaver brooks plot revealed the kinetics and non-competitive inhibitory nature of the later. Further studies on Huperzine-A-A are necessary to develop and establish its role on brain cholinergic system and cognitive deficits which may serve a stepping stone in CNS medication

Treatment of clavicle fracture using wise lock clavicle hook plate and wise lock superior anterior clavicle plate

Background: Clavicle fracture is common in adults associated with high non-union rate and post-operative complications. The aim of this prospective study was to reduce the postoperative complications in clavicle fracture (Type 15-A2 and 15-B1) by using wise lock plates (manufactured by Auxein Medical Private Limited).Methods: In this prospective study of 25 patients (11 patients had 15-A2 fracture, 14 patients had 15-B1 fracture) recruited with one year follows up period followed by physical exercises after one month of the surgery. The fractures were treated with two different plates: 3.5 mm wise lock clavicle hook plate and 3.5 mm wise lock superior anterior clavicle plate. X-ray was used to check the union, non-union. Functional outcome of the patients were assessed by the visual analogue scale (VAS) score at post-operative follow up at 4 weeks, 12 weeks, 6 months and 1 year.Results: Postoperative outcome was good with none of the patients showing non-union or delay in the union of fracture site. The encountered complication registered were residual pain which was mild (4 cases), and hypoesthesia (2 cases).Conclusions: Osteosynthesis of clavicle fracture with 3.5 mm diameter locking plates attributed as superior, anterior and hook plating system showed excellent results with low rate of complications

In-silico designing of a potent ligand molecule against PTEN (Phosphatase and tensin homolog) implicated in Breast Cancer

Breast cancer has been attributed to be the second most common malignancy in females worldwide after skin cancer associated with a significantly high mortality rate. Tumor suppressor genes have an indispensable role in maintaining genomic integrity as well as cell cycle regulation. Phosphatase and tensin homolog deleted on chromosome ten (PTEN) is one of the most frequently mutated human tumor suppressor genes, implicated in cell growth, survival, and suppressing tumor formation. As the tumor progresses to more advanced stages, genetic alterations tend to increase one such alteration is the mutation of the PTEN gene which is linked to programmed cell death and maintenance of cell cycle regulation. There is a syndrome known as Cowden syndrome associated with a high risk of breast cancer which is a result of an outcome of germline mutations in the PTEN gene. Loss of PTEN activity, either at the protein or genomic level, has been related to many primary and metastatic malignancies including breast cancer. This study focuses on developing a potential bioavailable ligand inhibitory molecule for PTEN, using a computer-aided drug design approach (CADD). A library of developed ligands consisting of 50 potential molecules was screened to find a potential candidate to be used for second generation drug development. Among them, LIG28 was adjudged as the most effective and potential PTEN inhibitor given its maximum binding affinity of ΔG -5.96Kcal/mole with a lower RMSD value. Carmer’s Rule of toxicity further revealed the compatibility and non-toxicity of the molecule. These observations underscore the importance of PTEN as a target in the development of tumorigenesis and the prognosis of breast cancer

Synergistic effect of folic acid and galantamine against experimentally induced oxidative stress in IMR 32 cells

286-292Galantamine is an active constituent obtained from Galanthus nivalis L., a traditional herb known for its pharmacological properties, particularly nootropic effect. Folic acid is a dietary supplement that enhances neuronal activity. Effect of galantamine and folic acid on human neuronal cells is well known. In the present study, we explored the protective effect of galantamine and folic acid, both independently as well as in combination, over antioxidant defence system and nootropic effects on human neuroblastoma cells IMR-32. The treatment galantamine, folic acid and their combination was given for 24 h and cytotoxicity study was carried out by trypan blue dye exclusion assay. Apoptosis and necrosis were observed using Propidium iodide (PI) and Hoechst double staining method. Biochemical assays viz. total protein, protein carbonyl, lipid peroxidation and glutathione were analyzed along with super oxide dismutase and catalase. Result of cytotoxicity showed dose dependent increase in percent viability and significant decrease was observed in apoptosis and necrosis. Moreover, exposure to Galantamine, Folic acid and their combination significantly decreased lipid peroxidation and protein carbonyl formation along with the enhancement in antioxidant defence mechanism. Findings of these dose reliant toxicity study of Galantamine , Folic acid and their combination suggest that these has higher potency when given together and shows synergistic effect. They also causes repair of human neuronal cells IMR-32 cells enhancing the cell viability and consumption of Galantamine and Folic acid together will help in prevention of CNS disorders and neurodegeneration

Comparative Effect of Vagal Stimulation on Heart Rate, Blood Pressure, and Skin Hydration at Different Anatomical Sites in Prehypertensive Individuals: A Pilot Study

Introduction: Prehypertension is the precursor to high Blood Pressure (BP), which can lead to severe consequences such as cardiovascular disease, stroke, acute myocardial infarction, heart failure, peripheral arterial disease, and cerebrovascular complications, ultimately resulting in mortality. Vagal stimulation is frequently employed by therapists, along with various therapeutic exercises, to treat or manage Heart Rate (HR) and BP in prehypertensive individuals. The vagus nerve plays a vital role in maintaining internal physiological balance, known as homeostasis, which includes reflex pathways that regulate cardiac function. Auricular neuromodulation of the vagus nerve can be achieved through stimulation of the ear lobule, cymba concha, or tragus in the outer ear. Aim: To compare and determine the optimal anatomical site for vagal stimulation, specifically the ear lobule, cymba concha, or tragus, to improve HR, BP, and skin hydration in prehypertensive individuals. Materials and Methods: The present pilot study conducted a pre-post comparative analysis in the Outpatient Department (OPD) of Physiotherapy at the Institute of Applied Medicines and Research Centre, Ghaziabad, Uttar Pradesh, India. The study duration was nine months, from January 2022 to September 2022. A total of 30 subjects aged 30-55 years were divided into three groups (10 participants in each group: A, B, and C) using sealed envelopes. Group A received vagal stimulation on the ear lobule, Group B received vagal stimulation on the cymba concha, and Group C received vagal stimulation on the tragus. Baseline measurements were taken prior to treatment, including HR, BP, and skin hydration. Vagal stimulation was administered using a low-frequency Transcutaneous Electrical Nerve Stimulation (TENS) machine at 25 Hertz and a pulse width of 120 ms. The stimulus was continuously applied for 30 minutes, five days a week, for four weeks. After a 10-minute relaxation period, HR, BP, and skin hydration were measured both pre and post-intervention. The data was statistically analysed using Statistical Package for Social Sciences (SPSS) version 24.0, employing paired t-tests to compare means within groups and Analysis of Variance (ANOVA) to compare between the three groups. Results: There were no statistical differences in the baseline among all three groups. Group C, which received vagal stimulation on the tragus, demonstrated statistically significant improvements in BP and skin hydration. The t-value and p-value for Systolic Blood Pressure (SBP) were 11.513 and p<0.001, for Diastolic Blood Pressure (DBP) were 10.411 and p<0.001, for HR were 15.231 and p<0.001, and for skin hydration were 9.474 and p<0.001, respectively. When comparing HR, BP, and skin hydration among the groups using one-way ANOVA f- value and p-value showed significant difference between the groups in all parameters. Conclusion: The study concludes that vagal stimulation on the tragus is a superior intervention compared to vagal stimulation on the cymba concha or ear lobule for controlling HR, BP, and skin hydration in prehypertensive individual

Metallic Nanoparticles as Antimicrobials and Radiosensitizers: A Review

Nanoparticles have shown unique physical and chemical properties that have opened new era for chemotherapy, cancer therapy, and radiotherapy. As an improved technology for targeting tumors, it is suggested that nanoparticles can become clinically useful for radio sensitization and as an antimicrobials can be utilized in topical formulations such as ointments, gels, and creams. There are different types of nanoparticles involved in the treatment of cancer radiotherapy and tumor selective radiosensitizer which have been classified into different groups. One of the widest applications of nanoparticles is assigned to noble metal nanoparticles (MNPs) or metal-based radiosensitizers. MNPs are the entities of pure metals smaller than the scale of microns, that is, between 1 and 100 nm in size. These include gold, silver, zinc, platinum, iron, gadolinium, cerium, titanium, tantalum, Bismuth, Hafnium, and copper and their oxides, sulfides, phosphates, and chlorides. MNPs due to their unique physical and chemical characteristics such as large surface energy, larger surface-area-to-volume ratio, quantum confinement, and plasmon excitation have emerged as a powerful tool for bioimaging and diagnostic of cancer and other clinical applications. Therefore, this paper discusses the wider applications of metal-based nanoparticles in enhancing radiosensitivity in debt. Improving mechanistic approach and understanding in nanoparticles, the outcome of this study will be of enormous benefit in radiotherapy