Α-glucosidase Inhibitory Activity Research Articles

Chemical profiling, in-vitro and in silico α-glucosidase inhibition, antioxidant and antibacterial activities of Hypotrachyna cirrhata (Fr.) Hale ex Sipman

Natural products are essential in drug development, with increasing interest in lichen-derived compounds for their therapeutic potential. This study investigates the bioactivity of the methanolic extract of Hypotrachyna cirrhata through in vitro and in silico approaches. The ethyl acetate fraction demonstrated the highest DPPH radical scavenging activity, with an IC50 of 10.37 ± 0.62 μg/mL, while the methanolic extract exhibited an IC50 of 72.30 ± 0.55 μg/mL. For α-glucosidase inhibition, the ethyl acetate fraction and crude extract showed IC50 values of 1.17 ± 0.50 μg/mL and 5.00 ± 0.45 μg/mL, respectively. Antibacterial assays revealed zones of inhibition of 12 and 11 mm against Staphylococcus aureus at 25 mg/mL, with the strain showing sensitivity to the methanolic extract (MIC of 20.0 × 10−4 mg/mL). LC-MS analysis identified eight metabolites in the ethyl acetate extract, salazinic acid (1), roccellaric acid (2), constictic acid (3), protolichesterinic acid (4), mannitol (5), penta hydroxyicosatrienoicacid (6), methyl pentahydroxyoxoheptacosanoate (7), and one unknown compound. Five major compounds (1-5) were selected for computational analysis and highlighted that salazinic acid as a potential lead compound, displaying a non-competitive binding with α-glucosidase and a binding affinity of −9.9 kcal/mol. These findings suggest salazinic acid's promise as an α-glucosidase inhibitor.

A Green Method for Preparation of Cyanidin-3-glucoside from Carissa carandas Fruits and α-Glucosidase Inhibitory Activity Evaluation

A Green Method for Preparation of Cyanidin-3-glucoside from Carissa carandas Fruits and α-Glucosidase Inhibitory Activity Evaluation

Enzyme Inhibitory Activities and RP-HPLC Analysis of Geranium and Erodium Species.

The genera Geranium and Erodium (Geraniaceae) have been documented to possess diverse ethnopharmacological uses, including diabetes mellitus. Relevant to their ethnopharmacological use, the current study aimed to evaluate the α-glucosidase, α-amylase, acetylcholinesterase (AChE), and butyrylcholinesterase (BChE) enzyme inhibitory activity of ethanol extracts from 46 samples belonging to thirty-one species of Geranium (20) and Erodium (11) collected throughout Türkiye. The majority of the extracts displayed a marked α-glucosidase and α-amylase inhibitory activity. Besides, 23 extracts out of 46 exhibited a concentration-dependent inhibitory effect over 50 % towards AChE. The highest AChE inhibition was found in G. subcaulescens collected from Konya with an IC50 value of 4.73±2.96 μg/mL. E. somanum, E. leucanthum, and E. sipthorpianum exhibited the most potent α-glucosidase inhibitory activity, while E. birandianum and E. pelargoniiflorum were the most active extracts against AChE and BChE, respectively. Three extracts that had inhibitory activity over 50 % against four of the enzymes were selected and proceeded to RP-HPLC analysis. Geraniin and ellagic acid were identified as major compounds in the active extracts. Most species screened in the current study were examined for the first time against α-glucosidase, α-amylase, AChE, and BChE.

Bioactivity-Based Analysis and Chemical Characterization of Hypoglycemic Components from Helicteres angustifolia L.

Helicteres angustifolia L. (H. angustifolia), a well-known traditional Chinese medicine, has been demonstrated to have hypoglycemic activity. We found that the EtOAc extract of H. angustifolia (HAEF) showed stronger α-glucosidase inhibitory activity than that of positive control. Furthermore, the hypoglycemic activity of HAEF was evaluated in streptozotocin (STZ)-induced type 2 diabetes mellitus (T2DM) rats. The results demonstrated that HAEF reduced the drinking quantity, feeding quantity, and controlled weight loss in diabetic rats. Besides, the fasting blood glucose (FBG), viscera index, and the area under time-blood glucose curve (AUC) were significantly decreased, and the oral glucose tolerance was also improved after 5 weeks. Then, the high-performance liquid chromatography with quadrupole time of flight tandem mass spectrometry (HPLC-Q-TOF-MS/MS) method was performed for qualitative analysis of the chemical constituents in HAEF. Twenty-one compounds were identified from in HAEF. Four compounds were further isolated from HAEF and subjected to α-glucosidase inhibition experiments. At the end, molecular docking was empolyed simulate the interaction of three compounds with α-glucosidase. This is the first report on major hypoglycaemic components has been identified in the roots of H. angustifolia. These findings provide a material basis for the use of H. angustifolia in the treatment of diabetes.

Endemic Plant Rumex balcanicus: Phenolic Composition, Antioxidant Activity, Enzyme Inhibitory Potential and Molecular Docking Analysis.

Although the nutritional and health benefits of Rumex species are well known, little is known about the chemical composition and pharmacological activities of Rumex balcanicus Rech. fil. (Polygonaceae), an endemic plant of the Balkan Peninsula. To the best of our knowledge, this paper represents the first attempt to comparatively analyse phenolic composition, as well as in vitro pharmacological activites of dry hydromethanol extracts of R. balcanicus fruit (RBF), leaf (RBL) and root (RBR), collected in Serbia. The maximum total phenolic content was found in RBF (386.6 mg GAE/g). The RBF was characterized by high amounts of miquelianin (28.8 mg/g) and procyanidin B1 (28.1 mg/g). The RBL was the richest in quercitrin (18.4 mg/g) and miquelianin (15.0 mg/g), while nepodin (54.1 mg/g) and procyanidin B2 (40.6 mg/g) were the major compounds in RBR. The RBF exhibited significant antioxidant activity, evaluated by DPPH (IC50=4.9 μg/mL), ABTS (IC50=0.8 μg/mL) and FRAP (5.9 mmol Fe2+/g) assays. Moreover, RBF showed strong α-glucosidase inhibitory activity (IC50=1.8 μg/mL), in addition to notable anti-α-amylase, anti-acetylcholinesterase and anti-tyrosinase activities. Molecular docking analysis predicted miquelianin and procyanidin B2 as the greatest inhibitors of these enzymes. Overall, R. balcanicus fruits stood out as the most promising plant material worth further research.

Design, synthesis, biological evaluation, and molecular modeling studies of some quinazolin-4(3H)-one-benzenesulfonamide hybrids as potential α-glucosidase inhibitors

Diabetes mellitus is a chronic metabolic disorder characterized by hyperglycemia, posing serious health risks and becoming increasingly prevalent. Prolonged hyperglycemia can lead to complications such as nephropathy, neuropathy, retinopathy, cardiovascular damage, and blindness. Controlling hyperglycemia through α-glucosidase inhibitors, which slow down carbohydrate breakdown, is an effective treatment strategy. However, current inhibitors like acarbose, voglibose, and miglitol while used to manage type 2 diabetes, have significant side effects. Therefore, developing new α-glucosidase inhibitors that are more effective and have fewer side effects is crucial. In this study, a series of novel quinazolin-4(3H)-one-benzenesulfonamide hybrid compounds were designed, synthesized, and evaluated for in vitro α-glucosidase inhibitory activity. The compounds showed higher enzyme inhibition potency, with IC50 values ranging between 129.2 ± 0.5 and 558.7 ± 13.7 µM, compared to acarbose (IC50=814.3 ± 13.5 µM). Among the tested compounds, compound 10, bearing a 4-chlorophenyl ring on the nitrogen atom of the sulfonamide group, was the most active, with an IC50 value of 129.2 ± 0.5 µM. Enzyme kinetics analyses and molecular modeling studies were conducted to understand their inhibition mechanisms and interactions with the enzyme. The kinetic studies revealed a mixed-type inhibition model, indicating that the compounds bind to the enzyme-substrate complex with higher affinity than to the free enzyme. Molecular modeling results confirmed these findings. Additionally, in silico prediction studies showed that the selected compounds have favourable physicochemical and drug-like properties. These results suggest these compounds have potential for further optimization and development as effective α-glucosidase inhibitors for diabetes treatment.

Gas Chromatography-Mass Spectrometry and Fourier Transform Infrared Spectroscopy Analysis of Potential α-Glucosidase Inhibitors from Terminalia catappa Leaf Extracts

Aims: Postprandial hyperglyceamia is often caused by insulin insufficiency or cellular glucose uptake complications, and conventional treatments often yield undesirable side effects. The aim of the current work was to assess the α-glucosidase inhibitory activities of T. catappa leaf extracts and use spectroscopic techniques to partially characterize possible inhibitors. Study Design: Phytochemical screening, enzyme inhibition assay and spectrometric and spectroscopic characterization of bioactive compounds from leaf extract and fractions of T. catappa. Place and Duration of Study: The entire work was carried out at the Department of Applied Chemistry and Biochemistry, University for Development Studies, Ghana within nine months. Methodology: T. catappa leaf extract and fractions were qualitatively screened for phytochemicals and their biological activity assessed in α-glucosidase inhibition assay. The potential enzyme inhibitors were characterized by Gas Chromatography-Mass Spectrometry (GC-MS) and Fourier Transform Infrared (FT-IR) Spectroscopy. Results: Phytochemical screening of the extract and the various solvent fractions revealed the presence of alkaloids, flavonoids, saponins, flavanol glycosides, phenolics, and terpenoids. The α-glucosidase inhibition potential of the crude leaf extract was concentration-dependent with a half-maximal inhibitory concentration (IC50) of 337.5 µg/ml. Solvent fractions from the crude extract demonstrated α-glucosidase inhibitory activity with IC50 values ranging from 170.40 µg/ml for ethyl acetate (EtOAc) fraction to 71.90 µg/ml for n-hexane (n-Hex) fraction. Acarbose, the control drug, demonstrated significant α-glucosidase inhibition activity in a similar pattern with IC50 of 6.16 µg/ml. The enzyme inhibition kinetics parameters, specifically the Michaelis constant (KM) and Maximum reaction velocity (Vmax) values, suggested that the inhibition of α-glucosidase by T. catappa extract followed a competitive mode. GC-MS and FT-IR analysis of the n-Hexane fraction identified the compounds Eugenol, Urs-12-en-24-oic acid, 3-oxo-, methyl ester (+)-, phytol, trans-isoeugenol, α-amyrin, and squalene as the potential antidiabetic agents that might be responsible for reducing postprandial blood glucose levels. Conclusion: These findings show that T. catappa leaf extract contains α-glucosidase inhibitors and therefore serves as a valuable resource in the discovery of natural anti-diabetic agents.

Optimization of ultrasound-assisted deep eutectic solvent extraction, characterization, and bioactivities of polysaccharide from Plantaginis Semen

Plantaginis Semen (PS) are the dried mature seeds of Plantago asiatica L. or Plantagodepressa Willd. in the Plantago family. Its polysaccharides are important components of PS. Response surface methodology was used to optimize the ultrasonic-assisted deep eutectic solvent (DES) extraction process of PS polysaccharides (PSP). The results showed that the optimal extraction parameters were a solid-liquid ratio of 1:35 g/mL, an extraction time of 73 min, and a molar ratio of 2:1. The yield of PSP was 0.64% and 1.20% by water immersion and ultrasonic water extraction, respectively, indicating that the DES extraction method (2.21 ± 0.06%) is superior to these two methods, and the optimization effect is good. Through the α-glucosidase and α-amylase inhibition activities experiment, it was found that the IC50 values of PSPs-1 were 1122 and 220.5 μg/mL. DPPH·and ABTS+ scavenging activity experiments showed that the IC50 values of PSPs-1 were 19.2 and 4.3 μg/mL, respectively. Its molar ratio of monosaccharide composition is rhamnose: galactose: galacturonic acid: glucose: glucuronic acid: arabinose: mannose: xylose = 33.6:13.3:6.5:3:2.6:2:1.4:1. Therefore, this study can provide an experimental basis for the establishment of an industrialized production process of polysaccharides and the study of their biological activities.

Phytochemicals and health-promoting evaluations of Ophiorrhiza puffii, a chinese endemic plant

There has been no phytochemical or and pharmacological report of the Chinese endemic plant Ophiorrhiza puffii till now. At present, seven structurally diverse compounds were obtained, including six triterpenoids (1–6) and one anthraquinone (7). Interestingly, 1–6 furnished three distinct carbon skeletons. Additionally, these phytochemical constituents showed multiple health-promoting effects. Triterpene 3 displayed considerable tyrosinase inhibitory activity (IC50 = 5.42 μM). Components 4 and 5 demonstrated significant antioxidant activity (IC50 = 4.23 and 2.03 mM, respectively). Meanwhile, compounds 2 and 5 exhibited moderate α-glucosidase inhibitory activity (IC50 = 0.89 and 0.72 mM, respectively). Moreover, the binding mechanisms for bioactive compounds 2, 3 and 5 and the corresponding α-glucosidase and tyrosinase proteins were preliminarily inspected by molecular docking experiments. This study filled up the knowledge gap of the unexplored chemical and biological profiles of secondary metabolites from the plant O. puffii for the first time.

A New Benzofuran from the Roots of Eupatorium chinense L. and Its α-glucosidase and PTP1B Inhibitory Activities

A New Benzofuran from the Roots of Eupatorium chinense L. and Its α-glucosidase and PTP1B Inhibitory Activities

β-amyrin heptadecanoate, a new oleanane triterpenoid with α-glucosidase inhibitory and cytotoxic activities from the leaves of Averrhoa bilimbi L.

A previously unreported oleanane triterpenoid, β-amyrin heptadecanoate (1), was isolated from the leaves of Thai Averrhoa bilimbi (Oxalidaceae), along with five known compounds, β-amyrin (2), β-sitosterol (3), β-sitosterol-D-glucoside (4), β-sitosteryl oleate (5), and α-tocopherol (6). Their structures were elucidated through spectroscopic analysis, including extensive NMR and HRESIMS, and by comparison with the previous literature. All isolated compounds were evaluated for their α-glucosidase inhibitory and cytotoxic activities. Compound 6 exhibited the highest α-glucosidase inhibition (IC50 of 0.72 ± 1.02 µM), significantly outperforming the standard acarbose (IC50 of 82.00 ± 0.24 μM). Furthermore, compound 4 demonstrated the most potent cytotoxicity against HeLa cells (IC50 of 34.92 ± 0.45 μM), while compound 3 exhibited the strongest cytotoxicity towards A549 cells (IC50 of 9.17 ± 0.30 μM). Additionally, a molecular docking study was conducted on the active α-glucosidase inhibitors to estimate their binding affinities and to identify the ligand-binding sites within the enzyme.

Hydroxydiorygmone A, a New Guaiane-Sesquiterpene from the Cultured Lichen Mycobiont of Diorygma sp

Objective: Cultured mycobiont of the Vietnamese crustose-lichen Diorygma sp. has been chemically investigated. Biological activities including cytotoxicity against HepG2 cell line, α-glucosidase inhibition, and nitric oxide inhibitory activity were evaluated. Methods: Extensive spectroscopic methods (NMR and ECD) and HRESI mass data were employed for structural elucidation. These isolates were evaluated for their cytotoxicity against HepG2 cell line, α-glucosidase inhibition, and inhibitory activity toward nitric oxide production in LPS-stimulated RAW 264.7 cells. Results: Four compounds (1–4), including a new guaiane-sesquiterpene, hydroxydiorygmone A (1), along with three known analogues, diorygmones A and B (2 and 3) and pruinosone (4), were isolated and characterized. Compound 1 showed moderate α-glucosidase inhibition with an IC50 value of 160 ± 2.2 µM and significant inhibitory activity toward nitric oxide production in LPS-stimulated RAW 264.7 cells with an IC50 value of 8.11 ± 0.21 µM. Others were inactive in α-glucosidase inhibitory and nitric oxide inhibitory tests. Conclusion: A new guaiane-sesquiterpene, hydroxydiorygmone A (1) was isolated and showed moderate α-glucosidase inhibition with an IC50 value of 160 ± 2.2 µM and significant inhibitory activity toward nitric oxide production in LPS-stimulated RAW 264.7 cells with an IC50 value of 8.11 ± 0.21 µM.

Identification of new structure of indol-3-acetyl-arylsulfonohydrazide as potent α-glucosidase and α-amylase inhibitors and molecular docking

Herein this work, indole analogs (1-16) were synthesized by treating 2-(1H-indol-3-yl)acetohydrazide with various aryl sulfonyl chloride in pyridine as solvent and screened for α-amylase and α-glucosidase inhibitory activity under positive control of standard drug acarbose (IC50 = 12.80 ± 0.10 μM /12.90 ± 0.10 μM. All analogs of the series appeared with excellent to good inhibitory activity as compared to standard drug. The inhibitory activity range for α-amylase is 0.70 ± 0.01 μM to 19.40 ± 0.40 μM, while for α-glucosidase inhibitory activity is 1.20 ± 0.10 μM to 20.40 ± 0.40 μM respectively. Most of the analogs appeared with excellent inhibitory activity, and some analogs like 5, 6, 7, 8, 9, 10,13 and 14 for both enzymes displayed many folds better inhibitory activity than standard drug acarbose. The influences of substituents on inhibitory activity were superficially resonated via structure activity relationship. Docking studies were established to confirm the binding interaction between analogs and active sites of enzymes.

Extraction and Quantification of Flavonoids from Vietnamese Dicranopteris linearis Leaves Using Green Method and Determination of their α-Glucosidase Inhibitory Activity

Extraction and Quantification of Flavonoids from Vietnamese Dicranopteris linearis Leaves Using Green Method and Determination of their α-Glucosidase Inhibitory Activity

Effect of processing and simulated digestion on phenolics, antioxidant and hypoglycemic potential of winter jujube

The wellknown winter jujube (Zizyphus jujuba Mill. cv. Dongzao), has been proved to contain a series of bioactive compounds. To investigate the impact of processing and digestion on its phenolics, winter jujube was processed (steaming and freeze-drying) and digested. The treated winter jujubes' phenolic content, antioxidant capacity, and hypoglycemic potential were assessed. The results showed that processing reduced the number of total phenolics/flavonoids, antioxidant, and α-glucosidase inhibitory activity by 0.74 ∼ 25.26%. With the exception of α-glucosidase inhibitory activity, which increased by 16.67 ∼ 19.25% after digestion, these declines were more pronounced. After processing, the six discovered phenolics in winter jujube were mostly constant, but after digestion, their contents dropped by 6.72 ∼38.64 %. These results suggested that following processing and digestion, the phenolic content and activity of winter jujube remained high (61.36 ∼ 97.93%), indicating that freeze-drying and steaming are viable approaches to prepare and consume winter jujube.

Efficient synthesis and molecular docking of new organoselenium and organosulphur compounds as dual inhibitors for the therapy of Alzheimer's disease as well as Diabetes Mellitus

There are several oxidative stress-related pathways interconnecting Alzheimer's disease and type II diabetes, two public health problems worldwide. Therefore, development of potential multifunctional agents for dual therapy of AD and T2D has received much attention. The present study was aimed to synthesize a new selenocarbonyl and thiocarbonyl compounds and evaluating multifunctional ability of them in the AD and T2D dual therapy. [(PhP(Se)(μ-Se)]2, the selenium counterpart of the well-known sulfur transfer Lawesson's reagent, is a useful reagent for the synthesis of selenocarbonyl compounds. For the conversion of various carbonyl compounds into thiocarbonyl derivatives was formulated by its reaction with LR, [(p-MeOC6H4)P(S)(μ-S)]2. The reactions are carried out under mild conditions and afforded the seleno and thio compounds in good yields. By measuring the newly created compounds' overall antioxidant capacity, iron-reducing ability, and scavenging activity against DPPH and ABTS radicals, they were investigated as antioxidant molecules. Additionally, all the compounds were subjected to further investigation by testing their acetylcholinesterase, α-amylase and α-glucosidase inhibiting activity. According to our findings, the amide derivatives exhibited more promising biological inhibitory actions in comparison to the other compounds. With a total antioxidant capacity (TAC) of 75.11 ± 0.04 mg gallic acid/gm, an iron-reducing power (IRP) of 69.86 ± 0.04 µg/mL, a DPPH radical-scavenging activity (%) of 55.89 ± 0.03 (IC50 = 6.19 ± 0.03 µg/ml), and an ABTS radical-scavenging activity (%) of 61.14 ± 0.03 (IC50 = 4.97 ± 0.06 µg/mL), benzoselenoamide derivative 11b in particular showed the highest antioxidant activities when compared to ascorbic acid. It also affected the activity of acetylcholinesterase through competitive inhibition, which was on par with Donepezil as indicated by in vitro percentage of inhibition 57.44 ± 0.07 % (IC50 = 5.13 ± 0.03 µg/mL). Additionally, it exhibited a comparable level of inhibition to Acarbose in the in vitro percentage of inhibition for α-amylase and α-glucosidase activity, 53.17 ± 0.03 (IC50 = 4.32 ± 0.02) and 42.92 ± 0.03 (IC50 = 2.99 ± 0.02) respectively. Furthermore, molecular docking calculations were made to explain the dual inhibitors for the therapy of Alzheimer's as well as Diabetes Mellitus for all synthesized compounds. In silco docking results revealed that compound 11b were the top docked bioactive compounds against the target proteins (AChE as a cholinergic enzyme and 11-Beta-Hydroxysteroid dehydrogenase-1(11β-HSD1)). After these calculations, ADMET analysis was performed to examine the drug properties of all novel compounds. Overall, the results demonstrated that the organoselenium-based compounds might serve as possible drugs for the therapy of Alzheimer's disease as well as Diabetes Mellitus.

Insights into the culturable fungal endophytes of Dioscorea bulbifera L. in terms of their diversity, antidiabetic and antioxidant activity

The research on endophytes is focused on understanding the complex microbiome compositions, their interactions with host plants and their bioactive potential. Our study provided an overview of the diversity, distribution and bioactivities of culturable endophytic fungi associated with fungal endophytes of Dioscorea bulbifera L. The phylogenetic analysis depicted the evolutionary relationship among taxa of endophytic fungal isolates. The isolated fungal endophytes belonged to twenty-five genera and thirty-eight species. Further, diversity indices demonstrated significant diversity of fungal endophytes in the different tissues: stem, leaf, tuber and bulbil. A higher consistency of endophytic fungal isolates in the bulbils was found using Shannon index. Furthermore, Simpson's index revealed that the leaf tissue harboured highly diverse fungal endophytes. Likewise, Margalef's index depicted high taxonomic richness in bulbils. The isolates such as Acrocalymma medicaginis, Curvularia lycoperscii, Talaromyces macrospora, Fusarium laceratum, Paecilomyces formosus and Microascus cirrosus isolated in this study have been reported as endophytes for the first time from any plant. In-vitro antioxidant and antidiabetic activities of the ethyl acetate extracts revealed that Nigrospora oryzae (Z2) effectively inhibited α-glucosidase activity with IC50 value of 0.6 µg/ml whereas IC50 value of the acarbose, the positive control was reported to be 0.040 µg/ml. The results of antioxidant activity demonstrated that H15A (Acrocalymma medicaginis) and BD5 (Phomopsis longicolla) could be used as potential sources of antioxidant agents. Moreover, H15A (Acrocalymma medicaginis) was reported to produce 687.1 ± 0.17 µg GAE/mg of TPC and 78.55 ± 0.29 µg QE/mg of TFC quantitatively. These findings suggest that the potential endophytes could be explored using systematic bio-guided investigations to further discover novel natural products. Our study provides an important resource for a deeper understanding of endophyte-plant interactions at molecular and genetic levels.

Investigation of Phytochemical Composition, Radical Scavenging Potential, Anti-Obesogenic Effects, and Anti-Diabetic Activities of Kaempferia parviflora Rhizomes.

Kaempferia parviflora or commonly known as "Kunyit hitam" by locals, is an edible plant, native to tropical regions, has been extensively utilized for culinary and medicinal applications. The present study aimed to investigate the phytochemical composition and biological activities of the rhizomes of K. parviflora. The ethanol crude and fractionated extracts (hexane and chloroform) of the rhizomes were evaluated for their total phenolic content, total steroidal content, as well as antioxidant, anti-obesogenic, and anti-diabetic activities. The chloroform extract demonstrated the highest concentration of plant sterols (432±0.23 mg BSE/g extract) and a substantial amount of phenolic compounds (1.19×103±0.41 mg GAE/g extract). Gas chromatography-mass spectrometry (GC/MS) analysis revealed that the chloroform extract of the rhizomes is predominantly composed of bioactive flavonoids including tectochrysin (1), 5,7-dimethoxyflavone (2), 3,5,7-trimethoxyflavone (3), 3,4',5,7-tetramethoxyflavone (4), and 4',5,7-trimethoxyflavone (5). Furthermore, the chloroform extract exhibited the highest overall radical scavenging and α-glucosidase inhibitory activities, which can be attributed to the presence of compounds 1-5 in the extract. Collectively, these findings suggest that the chloroform extract of the rhizomes of K. parviflora is a potentially valuable source of bioactive compounds with antioxidant, anti-obesogenic, and anti-diabetic properties, with potential application in therapeutics and functional foods.

'Bhim Kol (Musa Balbisiana)' Wine: Chemical Profiling and Antidiabetic Properties with MD Simulation Insights.

Musa balbisiana (Bhim Kol), an exotic fruit that offers numerous benefits can be fermented to obtain a unique indigenous wine. This study explores the fermentation of Musa balbisiana (Bhim Kol) fruit to produce a unique indigenous wine using strain of Saccharomyces cerevisiae and sugar over a 21-day period. Chemical profiling via GC-MS analysis revealed the presence of major volatile compounds such as butan-1-ol, propanoic acid, 2-phenylethanol, oxolane-2,5-dione etc. The wine exhibited in vitro α-glucosidase inhibition activity with an IC50 value of 8.56±0.14 μg/mL and antioxidant properties (DPPH⋅ scavenging activity (AAR) of 1.29±0.18 mM TRE). Molecular docking and simulation studies indicated potential binding of volatile compounds like 4-Hydroxy-3-methoxybenzoic acid, 2-phenylethanol, butan-1-ol and butane-2,3-diol with α-glucosidase enzyme. The study suggests the medicinal potential of the wine and its suitability for commercial production in the winery industry. Further studies are warranted to explore its full medicinal benefits.

Novel coumarin-thiazolidine-2,4‑dione hybrids as potential α-glucosidase inhibitors: Synthesis and bioactivity evaluation

To discover novel α-glucosidase inhibitors, a series of coumarin- thiazolidine-2,4‑dione hybrids (BJX1∼20) were synthesized and assessed their inhibitory activities against α-glucosidase. Compared to acarbose (IC50 = 655.01 ± 52.54 μM), coumarin-thiazolidinedione hybrids (BJX1∼20) displayed stronger α-glucosidase inhibitory activity, with IC50 values ranging from 5.12 ± 0.48 to 24.07 ± 1.96 μM. BJX3, BJX9, and BJX15 exhibited strongest inhibitory activities against α-glucosidase and acted as non-competitive inhibitors. The fluorescence quenching experiment revealed that the interaction between BJX3, BJX9, BJX15, and α-glucosidase followed a static binding process. CD spectra and 3D fluorescence spectra analysis revealed that the binding of BJX3, BJX9, and BJX15 to α-glucosidase induced a conformation change of α-glucosidase, thereby inhibiting its activity. Molecular docking simulation revealed the binding mechanism of BJX3, BJX9, and BJX15 with α-glucosidase. In vitro cytotoxicity assay indicated BJX15 (0∼64 μM) showed no obvious cytotoxicity against HEK 293 cells. In vivo experiments in mice demonstrated the ameliorative effect of orally administered BJX15 (50 mg kg-1) on postprandial hyperglycemia.