Alpha-amylase Inhibitor Research Articles

Purification, characterization and molecular docking studies of analogous alpha amylase inhibitor compounds

BackgroundA large number of protein inhibitors are found in higher plants, cereals and legumes. These inhibitors are helpful in the prevention as well as medical treatment of metabolic syndromes such as type 2 diabetes. Basically, the diabetes mellitus is a chronic disorder that occurs either due to inadequate insulin secretions or when body fails to utilize the produced insulin. The alpha amylase inhibitors are termed as starch blockers. They catalyze the hydrolysis of α-(1,4)-D-glycosidic linkages of starch and other glucose polymer. They play a significant role in inhibition of the activity of salivary and pancreatic amylase in vitro and in vivo. MethodThe present study was based on the purification, characterization and molecular docking studies of the alpha amylase inhibitor isolated from the kidney bean sample. The seed sample was collected from G.B. Pant Nagar University. The crude extract was prepared, the in-vitro studies and heat stability were determined. Following it, purification was carried out using ammonium sulphate precipitation and size exclusion chromatography was done. Later, characterization and molecular docking studies of the purified sample was done after obtaining GC–MS results. ResultThe in-vitro analysis was done and noted that the inhibitory activity was 96.5 ± 0.84 % post size exclusion chromatography. The molecular weight was about 54 kDa. The molecular docking studies revealed that there were interactions between the ligand molecules (the constituents that were selected from the GC–MS chromatogram peaks based on the height and area) and the human pancreatic alpha amylase (1HNY). The hydrogen bonding as affinity binding capacity was also been observed in each of the ligand–protein interaction. ConclusionFrom the tests, it has been elucidated that the alpha amylase inhibitor isolated from the sample has a great potential to serve as an anti-diabetic drug. However, in order to check the potential effects and to explore the optimization and development of the anti-diabetic drug the in-vivo studies can also be done further.

Synergistic Phytochemical and Nanotechnological Exploration of Melia azedarach With Silver Nitrate: Elucidating Multifaceted Antimicrobial, Antioxidant, Antidiabetic, and Insecticidal Potentials.

Plants are a rich source of bioactive compounds with significant pharmaceutical and health applications. This study explores the phytochemical, therapeutic, and phytotoxic properties of Melia azedarach by analyzing extracts from its bark, flowers, leaves, and fruits using six solvents: ethanol, methanol, acetone, hexane, chloroform, and distilled water. Twenty-one phytochemical tests were conducted, revealing significantly positive results for various tests. However, the ethanolic and methanolic flower extracts yielded no significant results in other tests. The highest total phenolic content was found in the chloroform extract of the leaves (96 ± 0.01 mg/100 g), and the highest antioxidant activity was observed in the ethanolic and hexane leaf extracts, with a 98% DPPH scavenging rate. Antibacterial testing showed significant efficacy against Serratia marcescens, Bacillus subtilis, Kluyvera spp., and Pseudomonas spp., with p values < 0.0001. The fruit chloroform extract demonstrated the highest alpha-amylase inhibition (93 ± 0.05), while the ethanolic leaf extract had the greatest tumor inhibition (85.6 ± 0.5). Insecticidal assays revealed that the acetone bark extract had the highest control values (56% and 57%). Due to their higher reducing potential, the leaves were used to biosynthesize silver nanoparticles (AgNPs), characterized by UV-Vis spectroscopy, EDX, and SEM, revealing an average particle size of 20-30 nm and spherical morphology. The AgNPs exhibited excellent antibacterial, antioxidant, antidiabetic, and insecticidal activities. These findings highlight the potential of M. azedarach and its AgNPs for developing novel therapeutic agents.

6-methyl-2-(3-nitrophenyl) imidazo [1,2-a] from Methanol Extract of Mangifera Indica as Potential Novel alpha-amylase inhibitor and Chemical Inducer of Glut 4 translocation: A Molecular Docking Computational Study

Diabetes, a chronic metabolic disorder characterised by hyperglycaemia has become a major global health concern, with an increasing prevalence worldwide (Mukhtar, Galalain &amp; Yunusa, 2020). Despite the availability of various anti-diabetic drugs, the search for natural remedies to manage diabetes has gained significant attention. Mangifera indica extracts have been studied for their anti-oxidant, anti-diabetic, lipid-lowering and anti-obesity potentials (Kumar et al., 2021). This study was designed to investigate the therapeutic effects of Mangifera indica methanol extract against Diabetes Mellitus, using in silico methods, Molecular docking simulations were performed to assess the binding affinities and interactions of the identified compounds from the Gas Chromatography/Mass Spectometry analysis result with key enzymes, proteins and hormones involved in glucose metabolism, such as alpha-amylase, insulin receptors, Glucose Transporter type 4 and Glucagon-like peptide 1. 6-methyl-2-(3-nitrophenyl) imidazo[1,2-a] pyridine had the highest binding affinity with Insulin receptors(-7.6kcal/mol), alpha amylase(-8.0kcal/mol) and Glucose transporter type 4(-8.5kcal/mol). Oxime-, methoxy-phenyl had the highest binding affinity with Glucagon-like peptide 1(-6.5kcal/mol). These findings suggest that mango leaves could serve as a source of natural anti-diabetic agent, which could lead to the development of new and effective treatments for diabetes. Further in vitro and in vivo studies are warranted to validate the bioactivity of these compounds and their mechanisms of action. Overall, this project contributes to the growing body of evidence supporting the use of in silico approaches for the discovery of novel antidiabetic agents from natural products.

Green-synthesis of silver nanoparticles AgNPs from Podocarpus macrophyllus for targeting GBM and LGG brain cancers via NOTCH2 gene interactions

Brain tumors, particularly Glioblastoma Multiforme (GBM) and Low-Grade Gliomas (LGG), present significant clinical challenges due to their aggressive nature and resistance to conventional treatments. Traditional therapies such as surgery, chemotherapy, and radiation are often limited in efficacy, necessitating novel therapeutic strategies. Nanotechnology, particularly the use of silver nanoparticles (Ag NPs), offers a targeted and potentially more effective approach. This study focuses on the green synthesis of Ag NPs using Podocarpus macrophyllus leaf extract as a reducing agent. The synthesized Ag NPs were characterized for their physicochemical properties, demonstrating a controlled particle size of 13 nm as determined by scanning electron microscopy (SEM). Fourier-transform infrared (FTIR) spectroscopy confirmed the presence of functional groups, and energy-dispersive X-ray (EDX) spectroscopy revealed that silver constituted approximately 90% of the nanoparticle composition. The Ag NPs exhibited promising biological activity, including 90% free radical scavenging (antioxidant) activity, 99.15% inhibition of protein denaturation (anti-inflammatory activity), and 90.56% inhibition of alpha-amylase (anti-diabetic activity). Additionally, the nanoparticles displayed significant anti-hemolytic (89.9% inhibition) and antimicrobial activities, with a 20 mm inhibition zone against Staphylococcus species. Computational analyses further indicated that the NOTCH2 gene, which is upregulated in LGG and GBM, may interact with Ag NPs, suggesting their potential in brain cancer therapy. The green synthesis approach offers a sustainable and bioactive method for producing Ag NPs, underscoring their therapeutic promise for treating GBM and LGG.

Promising Directions for Regulating Signaling Pathways Involved in the Type 2 Diabetes Mellitus Development

Many studies confirm that substances of natural origin have a pronounced affinity for type 2 diabetes mellitus (T2DM) therapeutic targets. At the moment, there is growing interest in bioactive peptides, phytochemicals, and drugs from other natural sources as highly effective, safe and promising antidiabetic agents. Natural sources are a promising resource for regulating several pathological pathways in T2DM. The review describes ways to mitigate insulin resistance and tissue sensitivity to glucose through PTP1β (protein tyrosine phosphatase 1β), GLP-1R (glucagon-like peptide receptor), DPP-4 (dipeptidyl peptidase-4), AMPK (adenosine monophosphate activated protein kinase), MAPK (mitogen-activated protein kinase). Regulation of obesity and oxidative stress development through CCN3 (nephroblastoma overexpressed gene), PPAR-γ (peroxisome proliferator-activated receptor γ), Nrf2 (nuclear factor erythroid-related factor 2), FFAR (free fatty acid receptors), 11β-HSD1 (11β-hydroxysteroid dehydrogenase). Regulation of hyperglycemia through alpha-amylase inhibitors, regulation of glucose metabolism through GFAT (glutamine fructose-6-phosphate aminotransferase), FOXO1 (forkhead box protein O1), GLUT4 (glucose transporter type 4), PGC-1α (receptor gamma coactivator 1α activating peroxisome proliferator). The review examines the use of natural sources, from which low-molecular-weight and peptide compounds are used as T2DM targets modulators.

Insights into Citrus limon (L.) Osbeck peel essential oil from NE India: A study of its pharmacological properties and chemical composition

Citrus limon (L.) Osbeck is considered as one of the most significant horticultural as well as essential oil crop. However, the significance of the fruit peels left after the utilization of the sour fruit find limited importance and these leftover peels are rich in essential oil. Lemon peel essential oil (LPEO) finds used in the fragrance, food, cosmetic, and pharmaceutical industries. In this study lemon peel were used for isolation of essential oil by hydro-distillation, analyzed by GC-FID and GC-MS and was further subjected to in vitro anti-oxidant (DPPH, ABTS), anti-inflammatory, anti-tyrosinase, genotoxicity and anti-diabetic assays. The essential oil analysis has revealed limonene as major compound (38.08%) along with other minor compounds namely, α-citral (12.02%), decanal (8.14%) and neral (7.36%). The total amount of citral (α-citral and neral) was found to be 19.38%, comparatively higher compared to previous reports. LPEO was found to exhibit very strong tyrosinase inhibition activity along with good alpha-amylase inhibition. The results from this study further strengthen the immense potential of LPEO as an anti-diabetic and skin whitening agent. The results framed from this study will further strengthen the position of earlier works on biological activities of C. limon besides providing a descriptive work on the potential of Assam LPEO.

Hemi Synthesis, Anti-inflammatory and In-silico Alpha-amylase Inhibition of Novel Carlina Oxide Analogs

Hemi Synthesis, Anti-inflammatory and In-silico Alpha-amylase Inhibition of Novel Carlina Oxide Analogs

Insights into Catechin-Copper Complex Structure and Biologic Activity Modulation.

Compounds of natural origin found in varying quantities in plant-based products constitute a highly significant category, possessing structural significance as well as the capacity to regulate oxidative processes. The activity of these compounds may be modulated by the composition of the biological environment in which they operate, the pH of the environment, or the presence of metal cations in plants or plant extracts. A successful complexation reaction was mainly confirmed by FT-IR, observing the shift from the original transmittance of catechin bonds, especially O-H ones. This work shows the synthetic methodology and the optimization process that took place to synthesize a catechin-copper complex, which demonstrated antioxidant activity. It was tested for iron chelation ability, hydroxyl radicals, and the inhibition of lipoxygenase (15-LOX). An antidiabetic assay was performed by determining the inhibition of alpha-amylase and alpha-glucosidase, finding that the synthesized complex had similar inhibitory potential as pure catechin. The antibacterial tests showed results against Staphylococcus aureus and the antifungal properties of the complex against Candida albicans.

Holistic exploration of silver nanoparticles synthesized from Carthamus oxycantha leaf extracts: Characterization and assessment of antioxidant, anti-α-amylase, and anti-cholinesterase activities using comprehensive statistical methods

In the burgeoning field of nanotechnology, plant-mediated nanoparticles (NPs) have attracted significant attention due to their small size, favorable chemical properties, and eco-friendly nature. We utilized Carthamus oxycantha leaf extract to synthesize silver nanoparticles (AgNPs) and evaluate their potential as antioxidants and inhibitors of acetylcholinesterase (AChE) and alpha-amylase (α-amylase). The AgNPs were characterized using advanced techniques. The UV–Vis spectrum recorded at 410 nm, with an absorbance of 2.3 a.u., confirmed the presence of AgNPs. Fourier transform infrared spectroscopy (FT-IR) indicated that functional groups from the extract were attached to the AgNP surface, aiding in their formation and stabilization. X-ray diffraction analysis (XRD) revealed four major peaks at 37, 43, 64, and 77, confirming AgNP synthesis. Scanning electron microscopy (SEM) showed that 80 % of the AgNPs were spherical, measuring 25–50 nm, while energy dispersive X-ray (EDX) analysis indicated that silver constituted 83 % of the material. The AgNPs demonstrated significant scavenging activity: 59.3 % with ABTS, 67.2 % with ammonium molybdate, 60.35 % with DPPH, 65.2 % with ferric chloride, and 55.2 % with H2O2. Both α-amylase and AChE were inhibited by AgNPs, exhibiting uncompetitive inhibition characteristics. For glucophage, Km decreased from 143 to 75 µg, and Vmax decreased from 45 % to 72 % as concentrations increased from 50 to 150 µg. The Km of AgNPs decreased from 25 to 17 µg, and Vmax decreased from 16 % to 37 %. The extract showed noncompetitive inhibition against α-amylase, while AgNPs caused noncompetitive inhibition in AChE. These findings highlight the potential of AgNPs as therapeutic agents for managing oxidative stress and enzyme-related disorders, paving the way for future research and applications in medicinal chemistry.

Synthesis, characterization, and biological activities of substituted pyridine-based azomethine scaffolds

The present research work describes the synthesis of a new series of heterocyclic compounds, namely, pyridine-based azomethine scaffolds. A total of eight derivatives were prepared, purified, and characterized by analytical methods such as 1H NMR, 13C NMR, and IR spectroscopic techniques. All compounds were used to investigate their alpha-amylase inhibition activity. We have also reported antimicrobial activity using a micro broth dilution assay, with microbial strains Pseudomonas aeruginosa (NCIM 5031), Escherichia coli (NCIM 2065), Bacillus subtilis (NCIM 2699), Aspergillus niger (NCIM 620), Aspergillus fumigatus (NCIM 902), and Aspergillus flavus (NCIM 549). Finally, we report the antioxidant activity of the synthesized derivatives using a DPPH free radical assay.

Phytochemical screening, HPLC fingerprinting and in vitro assessment of therapeutic potentials of different apricot cultivars against diabetes, Alzheimer's disease and cancer

Plant-based natural compounds are widely used to treat various ailments owing to their readily availability and minimal adverse effects. This study aimed to perform qualitative and quantitative biochemical profiling and assess the in vitro anti-diabetic, anti-Alzheimer, and anti-cancer activities of various apricot (Prunus armeniaca) cultivars. High-performance liquid chromatography (HPLC) was utilized to determine the concentrations of bioactive compounds across 10 distinct apricot cultivars. Initial phytochemical screening revealed a significant content of secondary metabolites. Subsequently, methanolic extracts from these cultivars were evaluated for their therapeutic potential against several human cancer cell lines, including prostate cancer (PC-3), lung cancer (A-549), breast cancer (MCF-7), cervical cancer (HELA), and kidney cancer (HEK). Notably, the breast cancer cell line MCF-7 showed a pronounced inhibition rate post-treatment with the apricot extracts. Correlation analysis exhibited phenols are highly correlated with flavonoids (r = 0.92), DPPH (r = 0.95), and alpha-amylase (%) inhibition (r = 0.96), and showed a significant correlation with other parameters. Principal Component Analysis (PCA) revealed that PC1 explained 43.31 % of the variance, while PC2 explained 12.88 %, together explaining 80.033 % of the total variance. PC1 was identified as the dominant axis, indicating the primary pattern of variation among the variables. Hierarchical Cluster Analysis (HCA) divided the cultivars into 2 main clusters, with cluster 2 further subdivided into various sub-clusters and sub-sub-clusters. This analysis highlighted distinct genetic similarities and differences among the apricot cultivars. Among the tested cultivars, ‘Irani’ and ‘Tilton’ were found to contain the highest levels of bioactive constituents. This research marks the first comprehensive examination of the impacts of these two apricot cultivars. The findings from this study provide a robust scientific foundation for the future isolation and purification of therapeutic compounds, potentially leading to their application in pharmaceuticals or dietary supplements. This research contributes significantly to the understanding of the pharmacological properties of apricot cultivars and establishes a basis for further investigation into their clinical benefits.

Bioassay guided isolation and compounds identification of the anti-diabetic fractions of (rosemary) Rosmarinus officinalis leaves extract

BackgroundDiabetes mellitus is a metabolic disease characterized by prolonged elevated blood glucose levels. It is a common health problem with a high mortality and morbidity to the human race. A number of medicinal plants such as rosemary (Rosmarinus officinalis) have been used for the treatment of diabetes. Most of the anti-diabetic conventional drugs have been found to have some side effects and there is therefore need to explore new sources of anti-diabetic drugs. The aim of the current study was to investigate the possibility of getting anti-diabetic compounds from R. officinalis that can be used as leads for drug discovery.MethodologyR. officinalis leaves were macerated in 50% methanol in dichloromethane and the crude extract fractionated by column chromatography. The obtained fractions were subjected to an in-vitro alpha-amylase inhibition assay. The anti-hyperglycemic potential of the fractions was evaluated in diabetic induced Wistar rats. The most potent fractions were analyzed by gas chromatography-mass spectrophotometry (GC-MS) for identification of the compounds.ResultsA total of 21 chromatographic fractions were assembled with different alpha- amylase inhibition activity. Eleven of the fractions had more than 30% alpha-amylase inhibition activity. The ethyl acetate fraction had the highest inhibition potential (LC50 of 2.8 μg/mL). The anti-diabetic assay in rats showed that fractions (F1) and (F4) had highest blood glucose reduction of 44.5 ± 0.4 and 52.8 ± 1.3%, respectively (p < 0.05). GC-MS analysis of fractions F1 and F4 showed the presence of 21 and 23 compounds in F1 and 23, respectively.ConclusionThis study has demonstrated that R. officinalis crude extract fractions obtained from 50% methanol in dichloromethane possesses alpha-amylase inhibitory and anti-hyperglycemic activities as well as secondary metabolites with varying chemical structures. The hexane and hexane/ethyl acetate (8/2) fractions showed most potent alpha-amylase inhibition with high anti-hyperglycemic activity giving hope of a possibility of obtaining lead compounds for new anti-diabetic drugs.

Computational Screening of Phytochemicals from Trigonella foenum-graecum as Potential Inhibitor of Alpha-Amylase and Maltase-Glucoamylase in Treatment of Type 2 Diabetes

Introduction: Diabetes mellitus is a major illness suffered by several individuals, a metabolic dysfunction of glucose that leads to life-threatening complications. Type 2 diabetes is a combination of insulin action resistance, insufficient insulin production, and excessive glucagon secretion. Aim: Numerous medications have been developed to manage diabetes mellitus by inhibiting various glucose metabolism enzymes and transporter proteins. However, the several adverse effects and high cost of treatment cannot be ignored. Thus, discovering and designing a small-molecule inhibitor with minimal side effects targeting vital proteins linked to glucose metabolism is essential. Methodology: This study utilizes a computer-aided drug design approach to identify bioactive compounds from Trigonella foenum-graecum with inhibitory potential against alpha-amylase and maltase-glucoamylase, which are glucose-metabolizing proteins. The compounds retrieved from the PubChem database were screened against the protein retrieved from the Protein Data Base using molecular docking analysis, binding energy study, and ADME Toxicity Screening. Result: Inositol, Isovitexin, Luteolin, Miglitol, Mimosine, Quercetin, Riboflavin, and Vitexin were identified to have high inhibitory potentials. These compounds showed impressive binding to the target proteins and admirable double-action inhibition of the proteins. The ADME Toxicity screening of the compounds also revealed that they are good drug candidates. Conclusion: The lead compounds are potential inhibitors of Alpha-Amylase and Maltase-Glucoamylase. Further preclinical investigation is advised to validate this study.

In silico analysis reveals α-amylase inhibitory potential of Taraxerol (Coccinia indica) and Epoxywithanolide-1 (Withania coagulans): a possible way to control postprandial hyperglycemia-induced endothelial dysfunction and cardiovascular events.

Postprandial hyperglycemia (PPG) exacerbates endothelial dysfunction and impairs vascular function in diabetes as well in healthy people. Though synthetic drugs are available to regulate PPG, the severe gastrointestinal side effects of those medications have prompted the search for alternative treatments. Recently, some phytochemicals captured the attention because of their inhibitory effects on α-amylase to control diabetes. The aim of this study was to investigate and identify potential alpha-amylase inhibitors in C. indica and W. coagulans. This study also aims to understand one of the possible mechanisms of action of plants for their anti-diabetic activity. A total of 36 phytochemical ligands were subjected for protein-ligand docking analysis. Among the phytochemicals, Taraxerol and Epoxywithanolide-I demonstrated significant binding free energy of -10.2kcal/mol and -11.9kcal/mol respectively, which was higher than the reference acarbose with -8.6kcal/mol. These molecules were subjected for molecular dynamics simulation (MDS) analysis with alpha-amylase protein for a duration of 150ns. Among the three complexes, Taraxerol and Epoxywithanolide-I complexes demonstrates strong potential as inhibitors of the target protein. MDS results were analyzed via root mean square deviation (RMSD), fluctuation of residues, potential energy, radii of gyration and solvent access surface area analysis. Taraxerol demonstrated a significantly low potential energy of -1,924,605.25kJ/mol, and Epoxywithanolide-I demonstrated -1,964,113.3kJ/mol of potential energy. RMSD plot shows that Epoxywithanolide-I has much higher stability than the other MDS complexes. Drugability and toxicity studies show that the test ligands are demonstrating strong potential as drug like molecules. The results of the study conclude that, Taraxerol of C. indica and Epoxywithanolide-I of W. coagulans are strong inhibitors of alpha-amylase enzyme and that, this is one of the possible mechanisms of action of the plants for their reported anti-diabetic activities. Further in-vitro analysis is in demand to prove the observed results.

Production and biological activities of exopolysaccharides synthesized by thermophilic bacilli isolated from hot springs in Türkiye.

Thermophilic bacteria able to produce exopolysaccharides (EPSs) have become attractive in recent years. EPSs synthesized by thermophiles are worth investigating due to their unexplored structural and biological properties. In this study, EPSs from thermophilic, Gram-positive bacterial isolates were purified and tested for their biological activities. A total of one hundred seven thermophilic bacteria were screened for their ability to produce exopolysaccharides. Nine isolates belonging to Geobacillus, Parageobacillus, Aeribacillus, and Anoxybacillus genera with highest EPS production were chosen, and purified EPSs (20, 61, 74, 76, 78, 89, 106, 134, and 261) were used for biological activity studies. EPS yields of selected thermophilic bacteria ranged between 117 and 419mg/L. Among the tested EPSs, 61, 106, and 261 showed antibacterial effect against E. faecalis JH2-2 at a final concentration of 1.5mg/mL. EPS samples had significantantioxidant capacity, especially EPS 134, with the highest DPPH radical scavenging activity of 100% at a concentration of 5mg/mL and the strongest reducing power.EPS 20 showed the highest lipid peroxidation inhibition effect at a rate of 31%. EPSs displayed weak alpha-amylase inhibition activity when compared with standard acarbose. The prebiotic indices of EPSs 20, 61, 76, 89, 134, and 261 were found to be higher than that of inulin, a representative prebiotic carbohydrate for all tested lactic acid bacteria in the study. All examined EPSs inhibited the biofilms formed by various bacteria depending on the test strain. Results indicated that thermophilic EPSs had remarkable antioxidant, prebiotic, and antibiofilm activities. Therefore, EPSs characterized in this study may have technological applications in health and food fields.

Mechanism of inhibition of alpha-amylase by caffeic acid using in-vitro and in-silico techniques

Type-two diabetes, characterised by insulin resistance or inadequate insulin production, is prevalent among adults. The α-amylase enzyme contributes to carbohydrate digestion, elevating postprandial glucose levels. Natural compounds like caffeic acid offer a solution. This study investigates α-amylase inhibition via in-vitro and in-silico methods, emphasising the connection between phenolic compounds and antidiabetic efficacy for in-silico analysis. Enzyme kinetics, IC50, and molecular docking examine caffeic acid’s inhibitory action on α-amylase, comparing it with gallic acid and acarbose. Caffeic acid outperforms acarbose with an IC50 of 4.505 mg/mL versus 16.81 mg/mL, showcasing strong antidiabetic activity. Caffeic acid’s superior 1,1-diphenyl-2-picrylhydrazyl (DPPH) inhibition (90.67%) compared to gallic acid (55.76%) indicates potent antioxidative and antidiabetic properties. Molecular docking reveals hydrogen bonding between caffeic acid and α-amylase. These insights lay the groundwork for phenolic-based diabetic therapies, offering less expensive treatment for diabetes patients.

Recent Advances in the Development of Alpha-Glucosidase and Alpha-Amylase Inhibitors in Type 2 Diabetes Management: Insights from In silico to In vitro Studies.

Diabetes is a metabolic disorder caused by high glucose levels, leading to serious threats such as diabetic neuropathy and cardiovascular diseases. One of the most reliable measures for controlling postprandial hyperglycemia is to reduce the glucose level by inhibiting enzymes in the digestive system, such as Alpha-Glucosidase and Alpha-Amylase. Here, we have investigated the use of inhibitors to inhibit carbohydrate metabolism in order to restrict glucose levels in diabetic patients. Acarbose, Voglibose, and Miglitol are three inhibitors approved by the FDA that efficiently inhibit these two enzymes and thereby minimising hyperglycemia but are al-so significantly helpful in reducing the risk of cardiovascular effects. We also provide insight into the other known inhibitors currently available in the market. The adverse effects associated with other inhibitors emphasise the demand for the latest in silico screening and in vitro validation in the development of potent inhibitors with greater efficacy and safety for the treatment of Type 2 diabetes. The recent findings suggest that Alpha-Glucosidase and Alpha-Amylase play a major role in carbohydrate metabolism and triggering the increase in glucose levels. This review pro-vides the latest scientific literature findings related to these two enzymes as well as the role of primary and secondary inhibitors as potential candidates. Moreover, this review elaborates the framework on the mechanism of action, different plant sources of extraction of these enzymes, as well as kinetic assay of inhibitors and their interaction that can be used in future prospects to de-velop potential leads to combat Type 2 diabetes.

Evaluations of the in vitro and in vivo antidiabetic activity of 70 % ethanolic fruit extracts of Rosa abyssinica

BackgroundDiabetes mellitus is becoming major health challenge with continually increasing burden. High costs of conventional medicines and numerous side effects associated with them, on the other hand, easy availability and accessibility of traditional herbal medicines calls upon experimental investigations to validate their effect on lowering blood glucose level. MethodsThe dried fruit of Rosa abyssinica was macerated with 70 % ethanol and the extract's in vitro antidiabetic activity was investigated using dinitrosalisylic acid method for alpha amylase inhibitory activity. Furthermore, the in vivo hypoglycemic and Antihyperglycemic effects of various doses of the extract (100, 200 and 400 mg/kg) was determined on normoglycemic, glucose loaded (1500 mg/kg) and Streptozotocine (180 mg/kg)-induced diabetic mice models. ResultsThe acute oral toxicity study revealed the plant showed no toxic effect on swiss albino mice at 2000 mg/kg. The in vitro alpha amylase inhibitory activity study showed that the extract has comparable IC50 value of 21.37 ± 4.252 μg/ml with the standard drug acarbose (IC50 value of 26.72 ± 3.59 μg/ml). On the other hand, in normal mice, none of the dose levels except at 400 mg/kg significantly reduces blood glucose level. This is in contrast to the oral glucose tolerance test, which the extract produced significant reduction at 60, 90 and 120 min following glucose challenge. The 70 % ethanolic fruit extracts of Rosa abyssinica also experienced profound antidiabetic activity in streptozotocin-induced diabetic model. In the single-dose study, both RAFE200 and RAFE400 demonstrated a significant (P˂0.05) reduction in blood glucose levels at 1, 2, 3, and 4 h. Similarly, in the repeated-dose study, RAFE200 and RAFE400 not only significantly reduced blood glucose levels but also produced a notable improvement in animal body weight. ConclusionThe 70 % ethanolic fruit extracts of Rosa abyssinica have shown significant in vitro alpha amylase inhibition effect and an in vivo blood glucose level lowering effects in diabetic mice.Therefore, this study supports the traditional use of Rosa abyssinica in the management of diabetes mellitus.

Phytochemical profiling of wastes from the processing of shea butter (Vitellaria paradoxa) and pharmacological potentials within the paradigm of circular bioeconomy: Emphasizing antioxidant and antidiabetic applications

Shea butter is a natural fat that is extracted from the kernels of the shea butter tree, and it is widely used in food preparation, cosmetics, and therapeutic practices. Shea trees are prevalent across Africa, and the traditional extraction methods produce significant wastes. However, there is dearth of information on the phytochemical profiling of these wastes and their potential biomedical values. Thus, this study conducted a thorough phytochemical investigation of the shea butter wastes from different processing stages, including brown and black shea cakes (SNC1 and SNC2), shea nut shells (SNS), and shea nut wastewater (SNWW). By using gas chromatography-mass spectrometry (GC–MS), the bioactive chemicals in these wastes were identified and quantified. Furthermore, the antioxidant and antidiabetic activities of the wastes were investigated for their potential pharmacological applications. The maximum antioxidant activities obtained at 60 mg/ml revealed DPPH radical scavenging of 62.34 % for SNC1, ferric reducing power of 68.13 % for SNC2, H2O2 radical scavenging of 38.46 % for SNS, and nitric oxide scavenging of 35.13 % for SNWW indicating their potentials in combating oxidative stress. Additionally, the promising anti-diabetic activity, with alpha-amylase inhibition reaching 84.74 % for SNS at 60 mg/ml highlights their potential in diabetes management. This study provides a holistic understanding of shea butter wastes, unraveling their chemical complexity and exploring their pharmacological potentials. It not only expands our knowledge of shea butter wastes, but also unlocks new avenues for utilization of the wastes in various industries, thereby contributing to waste management and sustainable exploitation of shea resources.

Formulation and evaluation of phytosomes containing bioactive from Carica papaya seeds

Background: Papaya seeds are a rich source of proteins, fat, fibers, vitamins, minerals, monounsaturated fatty acids, polyphenols, and powerful antioxidants like flavonoids. Low solubility limits the absorption and bioavailability of herbal constituents. Hence, phytosomes of Papaya seed extract were formulated to enhance its solubility and bioavailability. Methodology: Papaya seeds were extracted using ethanol as solvent, and all the phytoconstituents present in the extract were assessed during the phytochemical screening and LC-MS analysis. In-vitro antidiabetic activity pure extract was determined by alpha-amylase and alpha-glucosidase enzyme inhibitory assay. The phytosomes of extract were formulated using the lipid thin film formation method and Soya lecithin and Cholesterol as lipids. The formulated phytosomes were analyzed for parameters such as particle size, zeta potential, encapsulation efficiency, percent drug content, and In-vitro dissolution study. The chemical nature of the formulation was studied using FTIR analysis and powder X-ray diffractometry. Thermal stability of phytosomes analyzed with the help of Differential Scanning calorimetry. Results: LC-MS identified 16 phytoconstituents. In-vitro antidiabetic activity showed 59.97% and 51.17% inhibition of enzymes alpha-amylase and alpha-glucosidase, respectively. The encapsulation efficiency of the optimized formulation was 88.41±0.91% with a particle size of 188.0±53.7nm. TEM images of formulation confirm the formation of phytosomes. FTIR, DSC, and Powder X-ray diffractometry showed no unwanted peaks. The in vitro dissolution study showed 89.26±1.05% CDR of phytosome, while the extract showed 47.78±0.59% CDR. Conclusion: Evaluation results of phytosomes suggest that this formulation can be used as an effective herbal antidiabetic formulation