Glucosidase Inhibitory Activity Research Articles

In-Vitro Studies on Alpha Amylase and Alpha Glucosidase Inhibitory Activities of Synthesized Novel Sn(IV) Complexes of Schiff Base Ligand

In-Vitro Studies on Alpha Amylase and Alpha Glucosidase Inhibitory Activities of Synthesized Novel Sn(IV) Complexes of Schiff Base Ligand

Antioxidant, α-amylase and α-glucosidase Inhibitory Activities of Aqueous and Methanolic Extracts From Athamanta sicula L.

Introduction: Oxidative stress plays a major role in developing diabetes complications; therefore, it is possible to use natural antioxidants as therapeutic agents for diabetes. Aims: This study aimed to find an important source of phenolics from Athamanta sicula L. (A. sicula) and confirm that this plant could be a significant source of medically important natural compounds by confirming its antioxidant, α-amylase and α-glucosidase inhibitory potential. Methods: Antioxidant property was performed using 2,2′-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging, metal chelating, and cupric reducing antioxidant capacity methods. The α-amylase and α- glucosidase inhibitory activities were investigated using an in vitro model. Moreover, polyphenols and flavonoid contents of the tested extracts were carried out. Results: The methanolic extract exhibited the highest phenolic and flavonoid content compared to the aqueous extract. However, aqueous extract possessed the strongest antioxidant activity (DPPH scavenging, metal chelating, and Cupric ion reducing antioxidant capacities), α-amylase and α-glucosidase inhibitory effects. No correlation between phenolic content and antioxidant and enzyme inhibitory activities of A. sicula L. extracts was observed. Conclusion: The results showed that this plant could be a significant source of medically important natural compounds.

Research Progress of α-glucosidase Inhibitors of Medicinal and Edible Homologous Plants and Their use in the Treatment of Diabetes

Diabetes is one of the common diseases in modern society, which cannot be cured. It has a significant impact on the lives of patients. Type II diabetes patients mainly rely on oral hypoglycemic drugs and insulin injection to maintain blood sugar balance. While traditional hypoglycemic medications such as insulin, biguanides, and sulfonylureas may reduce blood glucose for a brief period of time, it often has some side effects and can lead to body dependence. Therefore, as a safe and economical natural hypoglycemic plant polysaccharide, it has received more and more attention. Natural active ingredients with glucosidase inhibitory activity from plants will become potential resources for research and treatment of type II diabetes. A large number of medicinal and food homologous plants have been identified as an important source of glucosidase inhibitors, and have received widespread attention. This article focuses on homologous medicinal and edible plant species and their application in diabetes treatment, here, we reviewed functional components with glucosidase inhibitory activity in homologous medicinal and edible plants and their state of research. In this paper, we hope to provide a theoretical benchmark for the development of drugs for type II diabetes from natural plants.

Lacticaseibacillus casei improves textural, functional, and sensory properties and phenolics’ bioaccessibility of frozen desserts prepared using water-soluble extract of rice by-product and Spirulina platensis

The impact of probiotic (Lacticaseibacillus casei, 8 log CFU/g) and/or prebiotic (polydextrose, 5 g/100 g) on the technological and sensory properties, phenolics bioaccessibility, and functional properties (in vitro antidiabetic, anti-hypertensive, and antioxidant activities) of frozen desserts processed with water-soluble extract of rice by-product and Spirulina platensis biomass was evaluated during storage (120 days/-18 °C). Prebiotic products were more consistent and cohesive and showed higher melting rates. Probiotic and/or synbiotic products had higher phenolic compounds bioaccessibility (gallic acid, epigallocatechin gallate, epicatechin gallate, and chlorogenic acid) and functional properties (antioxidant, ACE, ⍺-amylase, and ⍺-glucosidase inhibitory activities), lower thrombogenic and atherogenic indices and improved technological (lower firmness, consistency, cohesiveness, and viscosity) and sensory (increased mint aroma and flavor intensity) properties. L. casei survived in simulated gastrointestinal conditions (>6 log CFU/g) and did not impair sensory acceptance. In conclusion, probiotic and synbiotic frozen desserts show improved functional, technological, and sensory properties.

In vitro and in silico inhibitory validation of Tapinanthus cordifolius leaf extract on alpha-glucosidase in the management of type 2 diabetes

The anti-diabetic properties of medicinal plants are becoming more widely recognized. To identify potential anti-diabetic agents for diabetes drug discovery, the current study used in vitro and in silico approaches to assess the alpha glucosidase inhibitory activities of Tapinanthus cordifolius (TC) leaf extracts and its bioactive components respectively. In vitro alpha glucosidase inhibitory assay was carried out on TC extract and fractions at various concentrations (50–1600 µg/mL), and the compounds with alpha glucosidase inhibitory potentials were identified using molecular docking, pharmacophore modelling, and molecular dynamics simulation. The crude extract exhibited the highest activity with an IC50 value of 248 μg/mL. Out of the 42 phytocompounds of the extract, α-Tocopherol-β-d-mannoside gave the lowest binding energy of −6.20 Kcal/mol followed by, 5-Ergosterol (−5.46 kcal/mol), Acetosyringone (−4.76 kcal/mol), and Benzaldehyde, 4-(Ethylthio)-2,5-Dimethoxy-(−4.67 kcal/mol). The selected compounds interacted with critical active site amino acid residues of alpha-glucosidase, just like the reference ligand. Molecular dynamics simulation revealed the formation of a stable complex between α-glucosidase and α-Tocopherol-β-d-mannoside, with ASP 564 sustaining two hydrogen bond connections for 99.9 and 75.0% of the simulation duration, respectively. Therefore, the selected TC compounds, especially α-Tocopherol-β-d-mannoside might be explored for future research and development as diabetic medicines. Communicated by Ramaswamy H. Sarma

The Effect of Refrigerated Storage on Anti-Diabetic and Antioxidant Potency of Probiotic Yogurt Treated with Some Medicinal Plants

This research aimed to evaluate the effect of the inclusion of Codonopsis pilosula (CP), Illicium verum (IV), Lycium barbarum (LB), and Psidium guajava (PG) water extracts in yogurt (Y) on phenolic antioxidant-linked α-amylase and α -glucosidase inhibitory activities. Four types of herbal yogurt (CP-Y, IV-Y, LB-Y, and PG-Y) and plain-Y (control) were prepared and stored in disposable plastic containers at 4 °C for 28 days. All samples were analysed for peptide concentration using O-phthaldialdehyde, total phenolic content (TPC), 1,1-Diphenyl-2-Picrylhydrazyl radical scavenging activity, and α-amylase and α-glucosidase inhibitory activities (IC50). LB-Y showed the highest peptide concentration and TPC (p < 0.05) among all the yogurts during storage. IV-Y showed the highest (p < 0.05) radical scavenging activity among all herbal yogurts. The best α-amylase and α-glucosidase inhibitory activity (IC50) for all herbal yogurt was on days 7 and 14 of storage. In conclusion, all herbal yogurts could be considered as a potential functional food with antioxidant and anti-diabetic properties.

Suppressive effects of Bombycis Feces (bombyx feces) and Bombyx Batryticatus (stiff silkworm) extracts on blood glucose level elevation in disaccharides‐loaded rats

AbstractAimBombycis Feces (BF) and Bombyx Batryticatus (BB) are traditional medicines derived from silkworm. We investigated the suppressive effects of BF and BB extracts on elevated blood glucose levels in disaccharide‐loaded rats.MethodsEffects of BF and BB extracts on serum glucose levels in sugar‐loaded rats and streptozotocin (STZ)‐induced diabetic mice were recorded, and several glucosidase inhibitory activities were determined in vitro by comparing with those of the natural medicines obtained from the mulberry plant (e.g., Mori Folium, Mori Cortex, and Mori Fructus).ResultsBF and BB methanol extracts were found to suppress the elevated blood glucose level in sucrose‐loaded mice, whereas they did not exhibit any activity in the glucose‐loaded model and in the STZ‐induced model. Through the bioassay‐guided separation of the BF methanol extract using sucrase and maltase inhibitory activities, several pseudo‐sugars, including 1‐deoxynojirimycin (1), fagomine (2), and cis‐5‐hydroxy‐L‐pipecolic acid (3) were isolated as the active constituents. Oral administration (10 mg/kg) of constituent 1 simultaneous to sucrose loading in rats was found to significantly suppress elevation of the serum glucose level.ConclusionBF and BB extracts were found to inhibit the elevated blood glucose level in disaccharides‐loaded rats due to their α‐glucosidase inhibitory activities. The suppressive effects of BF and BB extracts as well as of the active constituent 1 on the increase in blood glucose were estimated to dwindle at a limited time after administration. Therefore, it is suggested that BF and BB extracts might exert their effective antidiabetic effects when taken with meals.

Sweroside: An iridoid glycoside of potential neuroprotective, antidiabetic, and antioxidant activities supported by molecular docking.

Oxidative stress can be a series burden on human health and may lead to many chronic diseases such as diabetes and neurological disorders. The use of natural products to scavenge the reactive oxygen species has attracted the attention of many researchers, to safely manage these conditions with fewer side effects, in available and cost-effective ways. The current study aimed at the isolation and structure elucidation of sweroside from Schenkia spicata (Gentianaceae) and the evaluation of its antioxidant, antidiabetic, neuroprotective, and enzyme inhibitory potential via in vitro and in silico studies. The antioxidant potential was evaluated by a variety of assays as ABTS, CUPRAC and FRAP, showing values of 0.34 ± 0.08, 21.14 ± 0.43, and 12.32 ± 0.20mg TE/g, respectively, while demonstrating 0.75 ± 0.03mmol TE/g for phosphomolybdenum (PBD) assay. Acetylcholinestrase (AChE), butyrylcholinesterase (BChE) and tyrosinase inhibitory activities were used to evaluate the neuroprotective effect, while the antidiabetic potential was evaluated by measuring α-amylase and glucosidase inhibitory activities. Results revealed that sweroside showed antioxidant and inhibitory effects on the enzymes tested with the exception of AChE. It demonstrated good tyrosinase inhibitory ability with 55.06 ± 1.85mg Kojic acid equivalent /g. Regarding the antidiabetic ability, the compound displayed both amylase and glucosidase (0.10 ± 0.01 and 1.54 ± 0.01mmol Acarbose equivalent/g, respectively) inhibitory activities. Molecular docking studies of sweroside on the active sites of the aforementioned enzymes in addition to NADPH oxidase were performed using Discovery Studio 4.1 software. Results revealed good binding affinities of sweroside to these enzymes mainly through hydrogen bonds and van der Waals interactions. Sweroside can be an important antioxidant and enzyme inhibitory supplement, yet further in vivo and clinical studies are required.

Flowers of Allium cepa L. as Nutraceuticals: Phenolic Composition and Anti-Obesity and Antioxidant Effects in Caenorhabditis elegans.

Allium cepa L., commonly known as onion, is one of the most-consumed vegetables. The benefits of the intake of its bulb are well studied and are related to its high polyphenol content. The flowers of onions are also edible; however, there are no studies about their biological properties. Our aim was to determine the polyphenolic profile and assess the antioxidant and anti-obesity capacity of an ethanolic extract from fresh flowers of A. cepa. The phenolic constituents were identified through LC-DAD-ESI/MSn. For the anti-obesity potential, the inhibitory activity against digestive enzymes was measured. Several in vitro assays were carried out to determine the antioxidant capacity. A Caenorhabditis elegans model was used to evaluate the effect of the extract on stress resistance and fat accumulation. For the first time, kaempferol and isorhamnetin glucosides were identified in the flowers. The extract reduced fat accumulation in the nematode and had a high lipase and α- glucosidase inhibitory activity. Regarding the antioxidant activity, the extract increased the survival rate of C. elegans exposed to lethal oxidative stress. Moreover, the activities of superoxide dismutase and catalase were enhanced by the extract. Our results demonstrate, for the first time, the antioxidant and anti-obesity activity of onion flowers and their potential use as functional foods and nutraceuticals.

Bioactive Compounds from Mimosa pudica Leaves Extract with Their α- glucosidase and Protein Tyrosine Phosphatase 1B Inhibitory Activities in vitro and in silico Approaches

<p>Background: Mimosa pudica Linn has been used in traditional medicine to support the treatment of type 2 diabetes. In the present study, we aimed to isolate and evaluate α-glucosidase and Protein Tyrosine Phosphatase 1B (PTP1B) inhibitory activities of bioactive compounds from Mimosa pudica’s leaf extract. <p> Methods: Mimosa pudica leaves were extracted with 80% of ethanol. Bioactive compounds were isolated using a column chromatographic technique and elucidated the structure based on the nuclear magnetic resonance and electrospray ionization mass spectrometry spectral data. The α- glucosidase and PTP1B inhibitory activities of the isolated compounds were evaluated using pnitrophenyl phosphate and p-nitrophenyl-α-D-glucopyranoside as a substrate, respectively. Molecular docking and molecular dynamics are used to study the interaction between isolated compounds and proteins. Lipinski’s rule of five was used to evaluate the drug-like properties of isolated compounds. Predict pharmacokinetic parameters were evaluated using the pkCSM tool. <p> Results: Protocatechuic acid and syringic acid were isolated and identified using spectroscopic methods. Protocatechuic acid and syringic acid considerably inhibited α-glucosidase enzyme at IC<sub>50</sub> values of 416.17 ± 9.41 μM and 490.78 ± 9.28 μM, respectively. Furthermore, protocatechuic acid and syringic acid expressed strong PTP1B inhibitory activity at IC<sub>50</sub> values of 248.83 ± 7.66 μM and 450.31 ± 7.77 μM, respectively. Molecular docking and molecular dynamics results showed the interactions of protocatechuic acid and syringic acid with amino acids of PTP1B and α-glucosidase enzyme. Lipinski’s rule of five and absorption, distribution, metabolism, excretion, and toxicity studies predicted that protocatechuic acid and syringic acid have drug-likeness properties. In molecular docking simulation, protocatechuic acid and syringic acid gave relatively negative free binding energies and interacted with many amino acids in the active sites of PTP1B and α-glucosidase. The molecular dynamics simulation results of the complexes were also relatively stable. <p> Conclusion: Our results showed that protocatechuic and syringic acids could be promising compounds for type 2 diabetes treatment.</p>

Postprandial glucose-lowering effects by sago (Metroxylon sagu Rottb.) resistant starch in spontaneously type 2 diabetes, Goto-Kakizaki rat.

Introduction: The beneficial effects of resistant starch (RS) consumption on health in terms of reducing postprandial hyperglycaemia are evident. However, the potential of local Sarawak sago RS in regulating glucose has not been extensively studied. Objectives: This study aims to identify glucose-lowering effects of Sarawak sago RS, namely native (RS2) and chemically modified (RS4). Methodology: An oral glucose tolerance test (OGTT) was performed before and after 1 month treatment with sago RS2 and RS4 in spontaneously type 2 diabetes (T2D), Goto-Kakizaki (GK) rat. The mechanisms involved were further explored by screening the in vitro inhibitory activities of α-glucosidase and dipeptidyl peptidase (DPP)-IV. Histopathology examination for pancreas, kidney and liver tissues was done in response to sago RS intake using haematoxylin and eosin (H&E) staining. Results and discussion: The incremental area under the curve (iAUC) for blood glucose in RS-treated groups was decreased and significant in RS2-treated group (p < 0.05). Improved iAUC for insulin and higher glucagon-like peptide (GLP-1) levels were observed in all RS-treated groups (p < 0.05). Both sago RS may have potential roles in regulating glucose via α- glucosidase and DPP-IV inhibitory activities by reducing intestinal glucose absorption. For histopathology, although insignificant, sago RS2 and RS4 attenuated lesion scores of pancreatic tissue whereas the liver and kidney tissues significantly showed lesser lesion scores compared to the control diabetic group suggesting the potential of RS in reducing cell degeneration. Conclusion: Findings of this study indicates that RS2 showed greater glucose-lowering effect when compared to RS4, thus the therapeutic potential in the T2D management should be further explored.

Novel Caffeic Acid - Zinc Acetate Complex: Studies on Promising Antidiabetic and Antioxidative Synergism Through Complexation.

The role of Zn(II) in storage, insulin secretion and function has been documented, while plant phenolics have antioxidant and other pharmacological credence. The study aimed at synthesizing a novel medicinal Zn(II) complex. The medicinal properties of zinc(II) and caffeic acid were considered in synthesizing a novel complex with promising and improved antioxidant and anti-hyperglycaemic attributes. Complex synthesis was done using a 1:2 molar ratio of zinc acetate and caffeic acid and structurally characterized using NMR, FT-IR, high resolution-mass spectroscopy and HPLC. Its cellular toxicity was assessed in Chang liver cells and L-myotubes. In vitro, cellular, and isolated tissue models were used to evaluate the antioxidant and anti-hyperglycaemic properties of the complex relative to its precursors. Molecular docking was used to investigate the interaction with insulin signalling target proteins: GLUT-4 and protein kinase B (Akt/PKB). Zinc(II) and caffeic acid interacted via Zn:O4 coordination, with the complex having one moiety of Zn(II) and 2 moieties of caffeic acid. The complex showed in vitro radical scavenging, α- glucosidase and α-amylase inhibitory activity up to 2.6 folds stronger than caffeic acid. The ability to inhibit lipid peroxidation (IC50 = 26.4 μM) and GSH depletion (IC50 = 16.8 μM) in hepatocytes was comparable to that of ascorbic acid (IC50 = 24.5 and 29.2 μM) and about 2 folds stronger than caffeic acid. Complexation improved glucose uptake activity of caffeic acid in L-6 myotubes (EC50 = 23.4 versus 169 μM) and isolated rat muscle tissues (EC50 = 339 versus 603 μM). Molecular docking showed better interaction with insulin signalling target proteins (GLUT-4 and Akt/PKB) than caffeic acid. The complex was not hepatotoxic or myotoxic. Data suggest a synergistic antioxidant and anti-hyperglycaemic potential between zinc and caffeic acid, which could be attributed to the Zn:O4 coordination. Thus, it may be of medicinal relevance.

In Vitro Pancreatic Lipase, Alpha-Amylase and Αlpha-Glucosidase Inhibitory Activities of the Phytochemical Barbaloin

In the present study the phytochemical, barbaloin was studied for in-vitro pancreatic lipase, alpha (α)-amylase and alpha (α)-glucosidase inhibitory activities. The aim of this work is to evaluate the inhibitory activities of the phytochemical, barbaloin at different concentrations. Pancreatic lipase is an enzyme that hydrolyzes the lipids obtained from the diet which acts as an important target to treat obesity. The natural medicines that can inhibit pancreatic lipase enzyme and thus decrease absorption of dietary fat in the body gained much attention for the treatment and prevention of obesity. Diabetes mellitus is a metabolic disorder marked by an elevated level of glucose that circulates in the blood plasma. Alpha amylase and alpha glucosidase inhibitors are used to attain control over hyperglycemia in type 2 diabetes mellitus. The present study was designed to screen the novel pancreatic lipase, alpha amylase and alpha glucosidase inhibitors using a phytochemical, barbaloin in order to minimize the toxicity and side effects of the inhibitors which are used at present to treat the disorders like obesity and hyperglycemia. The phytochemical, barbaloin exhibited significant pancreatic lipase, α-amylase and α-glucosidase inhibitory activities with an IC50 value 5.52µg/ml, 8.22µg/ml and 5.81µg/ml respectively and well compared with standard orlistat for pancreatic lipase and acarbose for alpha (α)-amylase and alpha (α)-glucosidase inhibitory activities respectively.

In Vitro Alpha Amylase and Alpha Glucosidase Inhibitory Activity of Important Lettuces from South Indian Region

In Vitro Alpha Amylase and Alpha Glucosidase Inhibitory Activity of Important Lettuces from South Indian Region

Evaluation of non-timber forest products used as medicinal plants from East Kalimantan (Indonesia) to inhibit ?-glucosidase and free radicals

Abstract. Ramadhan R, Tosepu R, Phuwapraisirisan P, Amirta R, Phontree K, Firdaus YFH, Abdulgani N, Muttaqin MZ, Saparwardi. 2022. Evaluation of non-timber forest products used as medicinal plants from East Kalimantan (Indonesia) to inhibit ?-glucosidase and free radicals. Biodiversitas 23: 5551-5558. Non-timber forest products (NTFPs) have essential uses as medicines, food sources, and traditional ceremonies for the local people living in forest areas. Medicinal plants are one of the non-timber forest products used as traditional medicine by local people in East Kalimantan. This study was conducted to search for new natural antidiabetic and antioxidant resources from medicinal plants used traditionally in Mahakam Ulu District, East Kalimantan, based on ethnopharmacological information. The present study evaluates non-timber forest products as in vitro antidiabetic (rat intestinal ?-glucosidase inhibitory activity) and antioxidant (free radical scavenging activity against DPPH, ABTS, and Nitric Oxide) activities. The antidiabetic and antioxidant activities were evaluated using ?-glucosidase inhibition assay and free radical scavenging methods. This study demonstrated that methanol extracts of Flacourtia rukam Zoll. &amp; Moritzi, Syzygium chloranthum (Duthie) Merr. &amp; L.M. Perry and Shorea balangeran Burck exhibited strong ?-glucosidase inhibitory activity with maltose as a substrate with IC50 values of 0.034 mg/mL, 0.039 mg/mL, and 0.039 mg/mL, respectively. On the other hand, methanol extract of S. chloranthum displayed the strongest ?-glucosidase inhibitory activity in sucrose as a substrate, similar to the IC50 value of the quercetin as a positive control. Furthermore, the antioxidant test showed that all medicinal plant extracts from East Kalimantan are good sources of natural antioxidants indicated by their IC50 values. The results of this study support the scientific background of the uses of medicinal plant extracts from East Kalimantan as folk medicine.

Molecular Evolution of an Aminotransferase Based on Substrate–Enzyme Binding Energy Analysis for Efficient Valienamine Synthesis

Valienamine is a valuable building block for active pharmaceuticals and agrochemicals because of its aminocyclitol structure and glucosidase inhibitory activity. Straightforward amino chiral center construction on valienone using a sugar aminotransferase (SAT) to produce valienamine achieved strict stereo-specificity; however, low transamination activity owing to an unfavorable binding conformation of the non-natural substrate valienone in the oversized substrate-binding pocket currently limits SAT-based valienamine production. Here, we employed a tailored combinatorial active-site saturation test/iterative saturation mutagenesis (CAST/ISM) strategy to engineer a recently identified SAT (RffA_Kpn) to optimize the binding of valienone in the large binding pocket and thus improve transamination activity. In silico analyses predicting mutation binding energies and assessing evolutionary conservation identified 9 of 62 contact residues positioned within 8 Å of the valienone–PMP external aldimine transition state as hotspots for destabilizing unfavorable binding. Four of these residues were subsequently confirmed to improve activity using site-directed saturation mutagenesis, and combinatorial mutations were prepared in further iterative cycles. The quadruple mutant M4 (K209W/Y321F/V318Q/K25W) displayed a 35.59-fold improvement in valienamine synthesis activity over wild-type RffA_Kpn and achieved 12.18% conversion toward valienone in 100 mg preparative-scale reaction. Our demonstration of asymmetric biosynthesis for a valuable chiral aminocyclitol illustrates how an evolution model can help engineer enzymes that handle small, non-natural substrates in oversized binding pockets.

Evaluation of Physicochemical Properties and Sensory Attributes of Pumpkin Seed (Cucurbita maxima) Bouillon Cube

ABSTRACT The physicochemical properties and consumer acceptability of bouillon cubes prepared from fermented pumpkin seed flour were evaluated. The results from microbial identified Bacillus subtilis as the main bacterium responsible for the production of condiment from pumpkin seed. Pumpkin bouillon cubes were observed to be rich in protein content (40.32–44.06%), energy value (521.57–538.49 kcal/100 g), potassium (859. 50–1128.00 mg/kg), phosphorous (402.27–501.87 mg/kg) and calcium (30.20–40.97 mg/kg). The result of the phytochemical properties of the pumpkin bouillon cubes include, tannin (1.94 mg/g − 2.92 mg/g), oxalate (2.78 mg/g − 3.45 mg/g), saponin (2.06 mg/g − 2.87 mg/g), phytate (4.45 mg/g − 5.44 mg/g), and alkaloid (2.40 mg/g − 3.58 mg/g). Free radical scavenging against 1, 1- diphenyl-2-picryhydrazyl (DPPH) (67.09%-88.03%), ferric reducing property (FRAP) (58.61 mg/g-63.10 mg/g) and Iron II chelation (44.78 mg/g-56.10 mg/g) of the bouillon cubes were found to increase with increase in amount of fermented pumpkin seed. The results further showed that aqueous extracts of pumpkin bouillon cube exhibited strong α-amylase (46.21%-51.08%) and α–glucosidase (67.87%-88.13%) inhibitory activities. Pumpkin bouillon cubes made from 80% fermented pumpkin seed was well accepted as seasoning and compete favorably with the control.

The chemical and microbiological characteristics of Awa‐bancha, Japanese post‐fermented tea

AbstractAwa‐bancha is a traditional Japanese post‐fermented tea made by residents in Tokushima Prefecture in the Shikoku region. Tea was picked, boiled, rubbed, anaerobic fermented, and dried in the process of making Awa‐bancha. Nevertheless, the details of making Awa‐bancha differs depending on the producer, such as how the tea leaves are boiled, the weight of the stones, and the length of anaerobic fermentation. Therefore, the objective of this study was to examine the chemical and microbiological characteristics of Awa‐bancha among different producers. The result explicated that the total phenolic compounds of Awa‐bancha extracted by water at 95°C for 10 min ranged from 20.41 ± 0.66 to 35.49 ± 3.90 mg GAE/g DW, the average DPPH activity was 877.4 ± 307.81 mmol Trolox/g DW, and the average α‐glucosidase inhibition activity (IC50) was 2.27 ± 0.63 mg/ml. The result revealed that Awa‐bancha differed due to differences in statistical analysis labels (p ≤ 0.05), resulting in various chemical functionality among the producers. Suggesting that processing or fermentation of Awa‐bancha may influence the bioactive compound in tea leaves changing from epicatechin (EC) to other compounds as well as HPLC analysis results show Epigallocatechin gallate (EGCg) is the main bioactive compound in Awa‐bancha. The higher the acidity produced from the fermentation process, the higher concentration of the reducing sugar and total phenolic compounds, which affect antioxidant activity and α‐glucosidase inhibition activity. Furthermore, the results show that Lactiplantibacillus plantarum is the dominating bacteria in Awa‐bancha which is well known as a probiotic and beneficial to the human gastrointestinal tract by producing antimicrobial substances. According to this study, based on its health benefits, Awa‐bancha could be possibly considered one of the functional drinks in the food industry.Novelty Impact StatementThis study focused on the diversity of Awa‐bancha, a traditional post‐fermented tea from various producers in Kamikatsu Town, Tokushima, Japan and discovered a statistically significant difference in reducing sugar content and total phenolic content. Additionally, it was discovered that the chemical functionality of the Awa‐bancha product was related to its higher acidity, higher polyphenolic content, antioxidant activity, and glucosidase inhibitory activity.

In vitro screening on Alpha amylase and Alpha glucosidase inhibitory activities of some novel Quinazolinone derivatives

Diabetes mellitus is a metabolic condition characterised by chronic hyperglycaemia, and type II diabetes is the most common type, accounting for 90% of cases globally. Hyperglycaemia is major complication of Diabetes mellitus. Postprandial hyperglycaemia is the most common distinctive of diabetes. Inhibition of carbohydrate hydrolysing enzymes including amylase and glucosidase may be useful method for lowering postprandial blood sugar levels. Alpha amylase and glucosidase inhibitors are the most approaching targets in the development of lead compounds for the treatment and management of diabetes. This type of inhibitors, used in clinical practise for the treatment of diabetes are known to be associated with gastrointestinal side effects. Therefore, we need to synthesize new compounds which have fewer side effects. In present study synthesized thirty quinazolinone compounds (PM1-PM30) were screened for their inhibitory effect on alpha amylase and alpha glucosidase enzymes. All synthesized compounds PM1 to PM 30, possess good inhibitory activity similar to that of approved drug Acarbose. Compounds PM20 PM7, PM28, PM29 are remarkable potent alpha amylase inhibitors and compounds PM30, PM28, PM29, PM4 are remarkable potent alpha glucosidase inhibitors. Therefore, these compounds are beneficial for management and treatment of diabetes disorder.

Exploring Active Ingredients, Beneficial Effects, and Potential Mechanism of Allium tenuissimum L. Flower for Treating T2DM Mice Based on Network Pharmacology and Gut Microbiota.

Forty compounds were isolated and characterized from A. tenuissimum flower. Among them, twelve flavonoids showed higher α−glucosidase inhibition activities in vitro than acarbose, especially kaempferol. The molecular docking results showed that the binding of kaempferol to α−glucosidase (GAA) could reduce the hydrolysis of substrates by GAA and reduce the glucose produced by hydrolysis, thus exhibiting α−glucosidase inhibition activities. The in vivo experiment results showed that flavonoids−rich A. tenuissimum flower could decrease blood glucose and reduce lipid accumulation. The protein expression levels of RAC−alpha serine/threonine−protein kinase (AKT1), peroxisome proliferator activated receptor gamma (PPARG), and prostaglandin G/H synthase 2 (PTGS2) in liver tissue were increased. In addition, the Firmicutes/Bacteroidetes (F/B) ratio was increased, the level of gut probiotics Bifidobacterium was increased, and the levels of Enterobacteriaceae and Staphylococcus were decreased. The carbohydrate metabolism, lipid metabolism, and other pathways related to type 2 diabetes mellitus were activated. This study indicating flavonoids−rich A. tenuissimum flower could improve glycolipid metabolic disorders and inflammation in diabetic mice by modulating the protein expression and gut microbiota.