Effect of Tranexamic Acid on Progression of Hematoma in Traumatic Brain Injury: A Randomized Controlled Trial.

Traumatic brain injury (TBI) is a major cause of morbidity and mortality in Bangladesh and also worldwide. Secondary brain injury from progressive intracerebral hematoma, increasing cerebral edema, raised intracranial pressure and subsequent cerebral ischemia is the main cause for morbidity and mortality following TBI. Secondary brain injury is worsened by post-traumatic coagulopathy, which occurs in brain injured patients and is associated with increase in risk of death and morbidity. The antifibrinolytic agent tranexamic acid (TXA) reduces the hematoma expansion and demonstrated improved clinical outcome also reduced the mortality and morbidity. This was a randomized controlled trial (RCT) done in the Department of Neurosurgery, Dhaka Medical College and Hospital. Included patients were randomized to get either the intravenous tranexamic acid (Group A) or placebo (Group B) treatment based on a computer-generated code list (50 patients in each group) along with usual medical management for traumatic brain injury. The extent of contusion expansion (hematoma plus perihematomal oedema) as the primary outcome at 48 hour after admission and was measured by brain CT scan. The contusion and oedema volume were calculated both the times (on admission and after 48 hours). Glasgow coma scale (GCS) after 48 hours and Glasgow outcome scale (GOS) after 7 days were observed. In this study showed increase in hematoma volume in both groups (p<0.05). But the increased hematoma volume in the Group A was significantly less than that in the control group. The mean total hemorrhage expansion was (1.5±1.1) ml and (4.6±1.9) ml in the Group A and Group B, respectively. In Group A- 02(4.0%) patients required operation, whereas in Group B- 11(22.0%) patients required operation. The result was significant (p=0.023) between groups. Therefore use of tranexamic acid is associated with lesser hematoma volume progression. Mean GCS (after 48 hours), mean GOS (after 7 days) result were significantly better in Group A (p<0.001). This study concluded that tranexamic acid has beneficial effect on the patient with significant traumatic brain injury. Tranexamic acid helps in reduction of intracerebral progression of contusion and improvement of clinical outcomes in patients with TBI.

Assessing the influence of spontaneous fermentation on consumer emotional responses to roasted arabica coffee in a biometric approach.

Beyond sensory quality, food-evoked emotions play a crucial role in consumers acceptance and willingness to try, which are essential for product development. The link between fermented coffee sensory characteristics and elicited emotional responses from consumers is underexplored. This study aimed to evaluate consumers' acceptability of spontaneously fermented and unfermented roasted coffee through self-reported sensory evaluation and biometrics assessment. Self-reported liking in 15-cm non-structured scale, multiple choice of negative, neutral, and positive emojis, and subconscious emotional responses from 85 regular coffee consumers were analysed. Their relationship with the pattern of volatile aromatic compounds were also investigated. Fermented (F) and unfermented (UF) coffee beans with light- (L), dark- (D), and commercial dark (C) roasting levels were brewed and evaluated along with gas chromatography-mass spectrometry measurement. Multivariate data analysis was conducted to explore the inner relationships among volatile compounds, self-reported liking, and biometrics. Unfermented-dark roasted coffee (UFD) had highest overall consumer liking response ± standard error (8.68 ± 0.40), followed by the fermented-dark roasted (FD) at 7.73 ± 0.43 with no significant differences (p > 0.05). Fermented light-roasted coffee was associated with lower liking scores and negative emotional responses. In contrast, dark roasted coffee, which was linked to positive emojis and emotional responses, exhibited less detected peak area of volatile compounds contributing fruity and vegetative aromas, such as benzaldehyde, furfuryl acetate, 2-acetyl-1-methyl pyrrole, and isovaleric acid, potentially as negative drivers of consumer liking. Findings from this study could guide coffee manufacturers in developing specialty coffee if spontaneous fermentation is offered.

Lipid-Lowering Medications for Managing Dyslipidemia: A Narrative Review.

Dyslipidemia refers to the change in the normal levels of one or more lipid components in the bloodstream, which include triglycerides (TG), total cholesterol (TC), high-density lipoprotein cholesterol (HDL-C), and low-density lipoprotein cholesterol (LDL-C). Dyslipidemia represents a substantial source of danger for cardiovascular disease (CVD). Effectively managing dyslipidemia involves a thorough strategy that includes changing one's lifestyle and using medications that are specifically designed to target the complex processes involved in lipid metabolism. Lipid-lowering treatments play a crucial role in this approach, providing a wide range of medications that are developed to specifically target different components of dyslipidemia. Statins are the main drug among these medications. Other drugs that are used with statin or as monotherapy include fibrates, omega-3 fatty acids (OM3FAs), ezetimibe, bile acid sequestrants, proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors, and bempedoic acid. Using the PubMed database, we reviewed the literature about dyslipidemia, drugs used for treating dyslipidemia, their efficacy parameters, and common adverse events. We also reviewed the international guidelines for treating dyslipidemia and discussed the future of lipid-lowering medications. More trials and experiments are still required to verify the effectiveness of many lipid-lowering drugs and to know their common adverse events to be able to manage them properly.

Sesamol Loaded Silver Nanoparticles Gel Engineered for Wound Healing via Topical Delivery: Optimization In vitro and Ex vivo Evaluation.

PURPOSE: The current investigation involved the development and application of a topical treatment for wound healing for sesamol loaded into the silver nanoparticles (SML-AgNPs). METHODS: SML-AgNPs were produced through the application of microwave technique. The SML-AgNPs were further optimized utilizing a Box Behnken Design (BBD). RESULTS: The Opt-SML-AgNPs formulation that was optimized demonstrated a particle size of 160.49 ± 1.11 nm, a polydispersity index (PDI) of 0.241 ± 0.54, a zeta potential of -21.09 ± 0.88 mV, and an efficiency of 84.19 ± 1.19%. The morphology of the Opt-SML-AgNPs reveals a spherical structure. The Opt-SML-AgNPs exhibit a higher in vitro drug release rate as compared to the SML suspension. The Opt-SML-AgNPs were incorporated into the carbopol gel (Opt-SML-AgNPG) and evaluated for various parameters. The skin permeation investigation revealed a twofold increase for the Opt-SML-AgNPG formulation when compared to the SML-conventional gel formulation. This finding indicates a prolonged release pattern and an enhanced permeability profile. The Opt-SML-AgNPs formulation exhibited a higher level of antioxidant activity when compared to the SML solution which is beneficial for wound healing. CONCLUSION: In conclusion, the Opt-SML-AgNPG exhibits considerable potential in effectively penetrating the deeper dermal layers. Therefore, it may be considered that they possess the potential to serve as a suitable nanocarrier to administer topical delivery in the context of treating skin-related illnesses.

Stochasticity of anticancer mechanisms underlying clinical effectiveness of vorinostat.

The Food and Drug Administration (FDA) has approved vorinostat, also called Zolinza®, for its effectiveness in fighting cancer. This drug is a suberoyl-anilide hydroxamic acid belonging to the class of histone deacetylase inhibitors (HDACis). Its HDAC inhibitory potential allows it to accumulate acetylated histones. This, in turn, can restore normal gene expression in cancer cells and activate multiple signaling pathways. Experiments have proven that vorinostat induces histone acetylation and cytotoxicity in many cancer cell lines, increases the level of p21 cell cycle proteins, and enhances pro-apoptotic factors while decreasing anti-apoptotic factors. Additionally, it regulates the immune response by up-regulating programmed death-ligand 1 (PD-L1) and interferon gamma receptor 1 (IFN-γR1) expression, and can impact proteasome and/or aggresome degradation, endoplasmic reticulum function, cell cycle arrest, apoptosis, tumor microenvironment remodeling, and angiogenesis inhibition. In this study, we sought to elucidate the precise molecular mechanism by which Vorinostat inhibits HDACs. A deeper understanding of these mechanisms could improve our understanding of cancer cell abnormalities and provide new therapeutic possibilities for cancer treatment.

Optimizing extraction methods by a comprehensive experimental approach and characterizing polyphenol compositions of Ecklonia radiata.

Brown seaweed Ecklonia radiata harbors valuable polyphenols, notably phlorotannins, prized for their health benefits. This study optimized phlorotannin extraction via conventional solvent extraction and ultrasound-assisted extraction methods, utilizing variable concentrations of ethanol. Employing fractional factorial designs, key variables were identified. Steepest ascent/descent method and central composite rotatable designs refined optimal conditions, enhancing phlorotannin and polyphenol yields, and antioxidant capacities. Under optimized conditions, phlorotannin contents reached 2.366 ± 0.01 and 2.596 ± 0.04 PGE mg/g, total polyphenol contents peaked at 10.223 ± 0.03 and 10.836 ± 0.02 GAE mg/g. Robust antioxidant activity was observed: DPPH and OH radical scavenging capacities measured 27.891 ± 0.06 and 17.441 ± 0.08 TE mg/g, and 37.498 ± 1.12 and 49.391 ± 0.82 TE mg/g, respectively. Reducing power capacities surged to 9.016 ± 0.02 and 28.110 ± 0.10 TE mg/g. Liquid chromatography-mass spectrometry (LC-MS) and high-performance liquid chromatography (HPLC) analyses revealed enriched antioxidant compounds. Variations in polyphenol profiles were noted, potentially influencing antioxidant capacity nuances. This study illuminated the potential of E. radiata potential as a polyphenol source and offers optimized extraction methods poised to benefit various industries.

Formulation and assessment of chickpea pulao using fenugreek seeds and Indian rennet to improve blood glycemic levels.

Diabetes is becoming a significant health concern in Asia, where the prevalence has reached alarming levels. An important contributing factor is the consumption of high-carbohydrate foods, including rice, bread, etc. These high-carbohydrate foods pose a major risk to public health due to their impact on postprandial hyperglycemia. This research aimed to formulate a chickpea pulao (cooked Indian-Pakistani rice dish) and to evaluate its effects on postprandial blood glucose levels in type 2 diabetic individuals. Antioxidant potential and total phenolic contents of herbs at different concentrations (1, 3, 5, 7, and 9%) were measured through DPPH and Folin Ciocalteu assays. The antidiabetic potential was tested by α-amylase and α-glucosidase inhibition assays. After sensory evaluation, the best-chosen concentration was used to formulate the chickpea pulao. The study trial was advertised under "DP trial," and 12 participants were recruited. A single-blind randomized cross-over trial was conducted for 3 weeks with a one-week wash-over time in between. Participants' preprandial and postprandial blood glucose levels were recorded for control and intervention recipes. Results indicated that both fenugreek seeds (FS) and Indian rennet (IR) showed good antioxidant and hypoglycemic activity (p = .000) in raw and boiled extracts. For DPPH, the IC50 values of unboiled and boiled combined (FS + IR) extracts were calculated as 7.4% and 8.02%, respectively. Similarly, for α-amylase, the IC50 values of combined IR and FS unboiled and boiled extracts were 6.58% and 6.83%, and for α-glucosidase inhibition assay, the values were measured as 14.98% and 16.24%. The single-blind randomized cross-over trial showed that consuming the intervention recipe significantly reduced postprandial hyperglycemia (p = .000) in type 2 diabetic participants. The intervention recipe decreased hyperglycemia by approximately 15% daily compared to the control recipe. Incorporation of hypoglycemic herbs into dietary patterns can work as an adjunct therapy for diabetes management, especially in populations with a high prevalence of this disease.

Physiochemical changes, metabolite discrepancies of brown seaweed-derived sulphated polysaccharides in the upper gastrointestinal tract and their effects on bioactive expression.

Brown seaweed-derived polysaccharides, notably fucoidan and laminarin, are known for their extensive array of bioactivities and physicochemical properties. However, the effects of upper digestive tract modification on the bioactive performance of fucoidan and laminarin fractions (FLFs) sourced from Australian native species are largely unknown. Here, the digestibility and bioaccessibility of FLFs were evaluated by tracking the dynamic changes in reducing sugar content (CR), profiling the free monosaccharide composition using LC-MS, and comparing high-performance gel permeation chromatography profile variation via LC-SEC-RI. The effects of digestive progression on bioactive performance were assessed by comparing the antioxidant and antidiabetic potential of FLFs and FLF digesta. We observed that molecular weight (Mw) decreased during gastric digestion indicating that FLF aggregates were disrupted in the stomach. During intestinal digestion, Mw gradually decreased and CR increased indicating cleavage of glycosidic bonds releasing free sugars. Although the antioxidant and antidiabetic capacities were not eliminated by the digestion progression, the bioactive performance of FLFs under a digestive environment was reduced contrasting with the same concentration level of the undigested FLFs. These data provide comprehensive information on the digestibility and bioaccessibility of FLFs, and shed light on the effects of digestive progression on bioactive expression.

Fabrication and characterization of transdermal delivery of ribociclib nanoemulgel in breast cancer treatment.

The objective of this study is to create a nanoemulgel formulation of Ribociclib (RIBO), a highly selective inhibitor of CDK4/6 through the utilization of spontaneous emulsification method. An experimental investigation was conducted to construct pseudo-ternary phase diagram for the most favourable formulation utilizing rice bran oil, which is known for its diverse anticancer properties. The formulation consisted of varying combination of the surfactant and as the co-surfactant (Tween 80 and Transcutol, respectively) referred to as Smix and the trials were optimized to get the desired outcome. The nanoemulsion (NE) formulations that were developed exhibited a droplet size of 179.39 nm, accompanied with a PDI of 0.211. According to the data released by Opt-RIBO-NE, it can be inferred that the Higuchi model had the most favourable fit among many kinetics models considered. The results indicate that the use of nanogel preparations for the topical delivery of RIBO in breast cancer therapy, specifically RIBO-NE-G, is viable. This is supported by the extended release of the RIBO, and the appropriate level of drug permeation observed in Opt-RIBO-NE-G. Due to RIBO and Rice Bran oil, RIBO-NE-G had greater antioxidant activity, indicating its effectiveness as antioxidants. The stability of the RIBO-NE-G was observed over a period of three months, indicating a favourable shelf life. Therefore, this study proposes the utilization of an optimized formulation of RIBO-NE-G may enhance the efficacy of anticancer treatment and mitigate the occurrence of systemic side effects in breast cancer patients, as compared to the use of suspension preparation of RIBO.

Clinical applications and mechanism insights of natural flavonoids against type 2 diabetes mellitus.

Diabetes is a complex disease that affects a large percentage of the world's population, and it is associated with several risk factors. Self-management poses a significant challenge, but natural sources have shown great potential in providing effective glucose reducing solutions. Flavonoids, a class of bioactive substances found in different natural sources including medicinal plants, have emerged as promising candidates in this regard. Indeed, several flavonoids, including apigenin, arbutin, catechins, and cyanidin, have demonstrated remarkable anti-diabetic properties. The clinical effectiveness of these flavonoids is linked to their potential to decrease blood glucose concentration and increase insulin concentration. Thus, the regulation of certain metabolic pathways such as glycolysis and neoglycogenesis has also been demonstrated. In vitro and in vivo investigations revealed different mechanisms of action related to flavonoid compounds at subcellular, cellular, and molecular levels. The main actions reside in the activation of glycolytic signaling pathways and the inhibition of signaling that promotes glucose synthesis and storage. In this review, we highlight the clinical efficiency of natural flavonoids as well as the molecular mechanisms underlying this effectiveness.

LC-ESI-QTOF-MS/MS characterization of phenolic compounds in Australian native passion fruits and their potential antioxidant activities.

Passion fruits, renowned globally for their polyphenolic content and associated health benefits, have enjoyed growing attention from consumers and producers alike. While global cultivar development progresses, Australia has pioneered several native cultivars tailored for its distinct planting conditions. Despite their cultivation, comprehensive studies on the phenolic profiles and antioxidant capacities of these Australian-native passion fruits are notably lacking. This study aims to investigate and compare the polyphenolic content present in the by-products, which are peel (L), and consumable portions, which are the pulp and seeds (P), of four indigenous cultivars: 'Misty Gem' (MG), 'Flamengo' (FG), 'Sweetheart' (SW), and 'Panama' (SH). Employing LC-ESI-QTOF-MS/MS for profiling, a comprehensive list of polyphenols was curated. Additionally, various antioxidant assays-DPPH, FRAP, ABTS, RPA, FICA, and •OH-RSA-were performed to evaluate their antioxidant potential. A total of 61 polyphenols were identified, categorized into phenolic acid (19), flavonoids (33), and other phenolic substances (9). In the antioxidant assays, the SHP sample exhibited the highest •OH--RSA activity at 98.64 ± 1.45 mg AAE/g, while the FGL sample demonstrated prominent DPPH, FRAP, and ABTS activities with values of 32.47 ± 1.92 mg TE/g, 62.50 ± 3.70 mg TE/g, and 57.84 ± 1.22 mg AAE/g, respectively. Additionally, TPC and several antioxidant assays had a significant positive correlation, including DPPH, FRAP, and ABTS. The Australian-native passion fruits revealed distinct polyphenolic profiles and diverse antioxidant capacities, establishing a foundation for deeper health benefit analyses. This study accentuates the significance of understanding region-specific cultivars and their potential nutraceutical applications.

Bioaccessibility of Phenolic Compounds, Resistant Starch, and Dietary Fibers from Australian Green Banana during In Vitro Digestion and Colonic Fermentation.

Green bananas contain a substantial amount of resistant starch (RS), dietary fiber (DF), and phytochemicals, which exhibit potent antioxidant capabilities, primarily attributable to the abundance of polyphenols. The objective of this study was to assess the variations in the contents and bioaccessibility of RS, DF, and phenolic compounds in three types of Australian green bananas (Cavendish "Musa acuminata", Ladyfinger "Musa paradisiaca L.", and Ducasse "Musa balbisiana"), along with their antioxidant capacities, and the production of short-chain fatty acids (SCFAs) following in vitro simulated gastrointestinal digestion and colonic fermentation. The studied cultivars exhibited significant levels of RS, with Ladyfinger showing the greatest (49%). However, Ducasse bananas had the greatest DF concentration (38.73%). Greater TPC levels for Ladyfinger (2.32 mg GAE/g), as well as TFC and TTC (0.06 mg QE/g and 3.2 mg CE/g, respectively) in Cavendish, together with strong antioxidant capacities (DPPH, 0.89 mg TE/g in Cavendish), have been detected after both intestinal phase and colonic fermentation at 12 and 24 h. The bioaccessibility of most phenolic compounds from bananas was high after gastric and small intestinal digestion. Nevertheless, a significant proportion of kaempferol (31% in Cavendish) remained detectable in the residue after colonic fermentation. The greatest production of SCFAs in all banana cultivars was observed after 24 h of fermentation, except valeric acid, which exhibited the greatest output after 12 h of fermentation. In conclusion, the consumption of whole green bananas may have an advantageous effect on bowel health and offer antioxidant characteristics.

Epidemiology and phylogeny of Haemonchus contortus through internal transcribed spacer 2 gene in small ruminants.

Introduction: Haemonchus contortus (H. contortus) is a blood-feeding nematode causing infectious disease haemonchosis in small ruminants of tropical and subtropical regions around the world. This study aimed to explore the prevalence and phylogeny of H. contortus in small ruminants using the internal transcribed spacer-2 (ITS-2) gene. In addition, a comprehensive review of the available literature on the status of H. contortus in Pakistan was conducted. Methods: Fecal samples were collected from sheep and goats (n = 180). Microscopically positive samples were subjected to DNA extraction followed by PCR using species-specific primers. Results: The overall prevalence of H. contortus was 25.55% in small ruminants. The prevalence of H. contortus was significantly associated with months and area. The highest occurrence of haemonchosis was documented in July (38.70%), whereas the lowest occurred in December (11.11%), with significant difference. The prevalence was highest in the Ghamkol camp (29.4%) and lowest in the arid zone of the Small Ruminant Research Institute (17.5%) (p = 0.01). The results of the systematic review revealed the highest prevalence of haemonchosis (34.4%) in Khyber Pakhtunkhwa (p = 0.001). Discussion: Phylogenetic analysis revealed a close relationship between H. contortus and isolates from Asia (China, India, Iran, Bangladesh, Malaysia, and Mongolia) and European countries (Italy and the United Kingdom). It has been concluded that H. contortus is prevalent in small ruminants of Kohat district and all over Pakistan, which could be a potential threat to food-producing animals, farmers, dairy, and the meat industry. Phylogenetic analysis indicates that H. contortus isolates share close phylogenetic relationships with species from Asia and Europe.

Optimization of Ultrasonic Extraction Parameters for the Recovery of Phenolic Compounds in Brown Seaweed: Comparison with Conventional Techniques.

Seaweed, in particular, brown seaweed, has gained research interest in the past few years due to its distinctive phenolic profile that has a multitude of bioactive properties. In order to obtain the maximum extraction efficiency of brown seaweed phenolic compounds, Response Surface Methodology was utilized to optimize the ultrasound-assisted extraction (UAE) conditions such as the amplitude, time, solvent:solid ratio, and NaOH concentration. Under optimal conditions, UAE had a higher extraction efficiency of free and bound phenolic compounds compared to conventional extraction (stirred 16 h at 4 °C). This led to higher antioxidant activity in the seaweed extract obtained under UAE conditions. The profiling of phenolic compounds using LC-ESI-QTOF-MS/MS identified a total of 25 phenolics with more phenolics extracted from the free phenolic extraction compared to the bound phenolic extracts. Among them, peonidin 3-O-diglucodise-5-O-glucoside and hesperidin 5,7-O-diglucuronide are unique compounds that were identified in P. comosa, E. radiata and D. potatorum, which are not reported in plants. Overall, our findings provided optimal phenolic extraction from brown seaweed for research into employing brown seaweed as a functional food.

Curcumin nanogel and its efficacy against oxidative stress and inflammation in rat models of ischemic stroke.

Aim: The study was designed to develop and analyze curcumin nanoparticles. Methods: Curcumin nanoparticles were formulated and evaluated. Their efficacy in protecting against brain damage was investigated in a rat model of ischemic stroke, considering motor function, muscle strength and antioxidant enzyme activity. Results: Curcumin nanoparticles displayed a zeta potential of -55 ± 13.5 mV and an average particle size of 51.40 ± 21.70 nm. In ischemic stroke rat models, curcumin nanoparticle treatment significantly improved motor functions, and muscle strength and increased the activities of antioxidant enzymes like glutathione peroxidase, glutathione, glutathione S-transferase, superoxide dismutase and catalase, reducing oxidative stress and inflammation. Conclusion: Curcumin nanoparticles showed significant neuroprotective effects in ischemic stroke models.

[Box: see text].

A comprehensive overview of selective and novel fibroblast growth factor receptor inhibitors as a potential anticancer modality.

The arrival of comprehensive genome sequencing has accelerated the understanding of genetically aberrant advanced cancers and target identification for possible cancer treatment. Fibroblast growth factor receptor (FGFR) gene alterations are frequent findings in various rare and advanced cancers refractive to mainstay chemo-therapy or surgical interventions. Several FGFR inhibitors have been developed for addressing these genetically altered FGFR-harboring malignancies, and some have performed well in clinical trials. In contrast, others are still being investigated in different phases of clinical trials. FDA has approved four anticancer agents such as erdafitinib, pemigatinib, infigratinib, and futibatinib, for clinical use in oncogenic FGFR-driven malignancies. These include cholangiocarcinoma, urothelial carcinoma, and myeloid/lymphoid malignancies. Pemigatinib is the only FGFR inhibitor globally approved (USA, EU, and Japan) and available as a targeted therapy for two types of cancer, including FGFR2 fusion or other rearrangements harboring cholangiocarcinoma and relapsed/refractory myeloid/lymphoid neoplasms with FGFR1 rearrangements. Myeloid/lymphoid neoplasm is the latest area of application added to the therapeutic armamentarium of FGFR inhibitors. Furthermore, futibatinib is the first-in-class covalent or irreversible pan-FGFR inhibitor that has received FDA approval for locally advanced or metastatic intrahepatic cholangiocarcinoma harboring FGFR2 gene aberrations. This review highlights the current clinical progress concerning the safety and efficacy of all the approved FGFR-TKIs (tyrosine kinase inhibitors) and their ongoing investigations in clinical trials for other oncogenic FGFR-driven malignancies.

Evaluation of chalcones as new glycogen phosphorylase inhibitors - an in-vitro and in-silico approach.

Diabetes mellitus (DM) remains one of the pivotal diseases that have drawn the attention of researchers recently and during the last few decades. Due to its devastating symptoms, attempts to develop new drugs with mild side effects have resulted in a number of drugs that are functioning through various mechanisms. Among these, Glycogen phosphorylase (GP) inhibitors emerged as a new strategy for combating DM. GP is an enzyme that regulates blood glucose levels; it catalyses the breakdown of glycogen to glucose-1-phosphate in the liver and tissues with high and fluctuating energy demands. In the present research, we evaluate the possibility of type 2 diabetes therapy with the help of chalcones which are known to have antidiabetic activities. For this purpose, 29 chalcones were modelled, synthesised and investigated for their inhibitory activity against GP using in-vitro methods. Compounds 1, 2, and 3 were found to be the most potent compounds with IC50 values 26.6, 57.1 and 75.6 µM respectively. The observed results were further validated using in-silico methods. Molecular docking simulation revealed interaction patterns that explain the structure-activity relationships of the compounds with GP. Molecular dynamic (MD) simulation demonstrated a stable complex formation between compound 1 and GP through lower value and uniformity in root mean square deviation (RMSD) of the complex and root mean square fluctuation (RMSF) of the protein Cα.