Design, synthesis, α-amylase and glucose diffusion inhibition, and molecular docking studies of new indenopyrazolones bearing benzothiazole derivatives.

An eco-friendly facile synthesis of a series of twenty 1-(4/6-substitutedbenzo[d]thiazol-2-yl)-3-(phenyl/substitutedphenyl)indeno[1,2-c]pyrazol-4(1H)-ones 7a-t was achieved by the reaction of 2-(benzoyl/substitutedbenzoyl)-(1H)-indene-1,3(2H)-dione 3a-t and 2-hydrazinyl-4/6-substitutedbenzo[d]thiazole 6a-t in presence of freshly dried ethanol and glacial acetic acid under reflux conditions in good yields. The newly synthesized derivatives were well characterized using different physical and spectral techniques (FTIR, 1H NMR & 13C NMR, and HRMS). All the compounds were subjected to assess their in vitro α-amylase and glucose diffusion inhibitory activity. Amongst them, the compounds 7i and 7l showed better α-amylase inhibitory activity demonstrating IC50 values of 92.99±1.94 µg/mL and 95.41±3.92 µg/mL, respectively in comparison to the standard drug acarbose (IC50 value of 103.60±2.15 µg/mL). The derivatives 7d and 7k exhibited good glucose diffusion inhibition with values of 2.25±1.16 µg/mL and 2.63±1.45 µg/mL, respectively with standard reference acarbose (2.76±0.55 µg/mL). The observed α-amylase inhibitory activity findings were corroborated through molecular docking investigations, particularly for the highly active compounds 7i (binding energy -8.0 kcal/mol) and 7l (binding energy -8.2 kcal/mol) respectively, in comparison to acarbose with a value of binding energy -6.9 kcal/mol for α-amylase.

Hyperhydration of Cancers: A Characteristic Biophysical Trait Strongly Increasing O2, CO2, Glucose and Lactate Diffusivities, and Improving Thermophysical Properties of Solid Malignancies.

Cancers are complex, heterogeneous, dynamic and aggressive diseases exhibiting a series of characteristic biophysical traits which complement the original biological hallmarks of cancers favouring progressive growth, metastasis, and contributing to immune evasion and treatment resistance. One of the prevalent differences between most solid tumors and their corresponding, healthy tissues is a significantly higher water content (hyperhydration) in cancers. As a consequence, cancers have distinctly higher (Fick's) diffusion coefficients D [cm2 s-1] for the respiratory gases O2 and CO2, the key substrate glucose, and for the oncometabolite lactate. In addition, cancers have (a) clearly increased specific heat capacities cp [J g-1 K-1], thus representing high-capacity-tissues upon therapeutic heating induced by electromagnetic irradiation, and (b) higher thermal conductivities k [W m-1 K-1], i.e., increased abilities to conduct heat. Therefore, in diffusion analyses (e.g., when describing critical O2 and glucose supplies or CO2 removal, and the development of hypoxic subvolumes) and for modeling temperature distributions in hyperthermia treatment planning, these specific cancer-related data must be considered in order to reliably reflect oncologic thermo-radiotherapy settings.

Exploring antidiabetic potential of a polyherbal formulation Madhurakshak Activ: An in vitro and in silico study.

Madhurakshak Activ (MA), a commercial polyherbal antidiabetic preparation is known to manage diabetes mellitus (DM) by reducing blood glucose levels. However, lacks systematic mechanistic evaluation for their molecular and cellular mode of actions. In the present study, hydro-alcoholic and aqueous extract of MA were evaluated for their effects on glucose adsorption, diffusion, amylolysis kinetics and transport across the yeast cells using in vitro techniques. Bioactive compounds identified from MA by LC-MS/MS were assessed for their binding potential against DPP-IV and PPARγ via an in silico approach. Our results revealed that the adsorption of glucose increased dose dependently (5 mM -100 mM). Both extracts exhibited linear glucose uptake into the yeast cells (5 mM - 25 mM), whereas glucose diffusion was directly proportional to time (30-180 min). Pharmacokinetic analysis revealed drug-like properties and low toxicity levels for all the selected compounds. Among the tested compounds, 6-hydroxyluteolin (-8.9 against DPP-IV and PPARγ) and glycyrrhetaldehyde (DPP-IV -9.7 and PPARγ -8.5) have exhibited higher binding affinity compared to the positive control. Therefore, the above compounds were further considered for molecular dynamics simulation which showed stability of the docked complexes. Hence, studied mode of actions might produce a concerted role of MA in increasing the rate of glucose absorption and uptake followed by the in silico studies which suggest that the compounds identified from MA may inhibit DPP-IV and PPARγ phosphorylation.

Inhibition of α-amylase and amyloglucosidase by cellulose nanofibrils with different surface charge and spectroscopic analysis of their interaction mechanism.

We investigated the inhibition effect of carboxymethylated cellulose nanofibrils with four different surface chargeon α-amylase and amyloglucosidase via enzyme activity inhibition assay, fluorescence spectra and secondary structure change analysis. These results revealed that cellulose nanofibril with lowest surface charge displayed the greatest inhibition effects against α-amylase (9.81 mg/mL) and amyloglucosidase (13.16 mg/mL). All cellulose nanofibrils in starch model significantly (p < 0.05) inhibited the starch digestion, where the inhibition effect was negatively correlated with the magnitude of particle surface charge. Cellulose nanofibrils could bind α-amylase or amyloglucosidase to form new complex in the manner of static quenching. The thermodynamic parameters demonstrated that the cellulose nanofibrils-starch hydrolase (α-amylase or amyloglucosidase) complexes were formed spontaneously via hydrophobic effects. Additionally, Fourier transform Infrared spectra exhibited the changes in the fraction of secondary structures of starch hydrolase after the interactions with carboxymethylated cellulose nanofibrils. These data provide a convenient and simple method tailor gastrointestinal digestion of starch by changing cellulose surface charge, to control postprandial serum glucose upsurge.

Acidic polysaccharides from black ear and silver ear mushrooms modulated the release and transport of glucose from gelatinised sorghum starch during digestion.

This study investigated the ability of acidic polysaccharides from Auricularia auricula-judae (AAP) and Tremella fuciformis (TFP) mushrooms to modulate starch digestion and absorption. Gelatinised sorghum starch was used as starch-rich material, and its digestion and glucose transport were determined through in vitro digestion/Caco-2 cells model. Results showed that fortification with 0.6% AAP/TFP increased the proportion of high molecular weight α-dextrin and delayed glucose diffusion from digested starch gels. Gelatinisation of sorghum starch with AAP and TFP reduced the amount of transported glucose by 34.2% and 38.7%, respectively. This reduction was related to the inhibition of AAP/TFP on α-glucosidase and the difficulty in the hydrolysis of high molecular weight maltooligosaccharides. The potential bonding of AAP/TFP to glucose transporter (SGLT1) also impeded glucose transport. The findings suggest that AAP/TFP could act as natural hypoglycaemic agents used in starch-based foods and provide a better understanding of the hypoglycaemic mechanism of mushroom polysaccharides.

Grain boundary enriched CuO nanobundle for efficient non-invasive glucose sensors/fuel cells.

Glucose oxidation reaction (GOR) plays a significant role in glucose fuel cells anode and glucose sensors. Therefore, optimizing the GOR catalyst nanostructure is auxiliary to their efficient operation. In this study, we present a cascade-assembled strategy to prepare CuO nanobundles (CuO-NB) with high-density and homogenous grainboundaries (GBs). The essence of activity in GOR that depended on GBs are thoroughly investigated. The increased glucose diffusion coefficient of CuO-NB means that GBs has a faster glucose mass transfer, which is attributed to the terraces in GBs dislocation surface. Furthermore, the accumulation of electrons on GBs makes the glucose adsorption increased and the free energy of dehydrogenation step decreased, leading to a lower glucose oxidation barrier. Therefore, CuO-NB is appropriate for non-invasive glucose detection and glucose fuel cells. This study sheds new light on the GBs effect in GOR and paves the way for developing high-efficiency electrocatalysts.

In Vitro Antioxidant Properties, Glucose-Diffusion Effects, α-Amylase Inhibitory Activity, and Antidiabetogenic Effects of C. Europaea Extracts in Experimental Animals.

Caralluma europaea (Guss.) N.E.Br. (C. europaea), is a medicinal plant used traditionally to treat diabetes mellitus (DM) in Morocco. This study aimed to investigate the in vitro antioxidant properties, glucose diffusion effects, α-amylase inhibitory activity, and pancreatic protective effects of C. europaea in experimental alloxan-induced diabetes in mice. Total phenolic contents were determined by Folin-Ciocalteu colorimetric method, total flavonoid contents were measured by aluminum chloride colorimetric assay, and tannins contents were determined by employing the vanillin method. C. europaea ethyl acetate fraction exhibited high antioxidant potential in terms of radical scavenging (DPPH) (IC50 = 0.22 ± 0.01 mg/mL), ß-carotene bleaching activity (IC50 = 1.153 ± 0.07 mg/mL), and Ferric-reducing antioxidant power. Glucose diffusion was significantly inhibited by the ethyl acetate fraction at 60,120and 180 min, while the aqueous extract did not have this inhibitory effect when compared with the control group. Potent α-amylase inhibitory activity was observed in the ethyl acetate fraction and the aqueous extract in vitro and in vivo using STZ-diabetic rats. On the other hand, the administration of the ethyl acetate fraction (60 mg/kg) significantly attenuated alloxan-induced death and hyperglycemia in treated mice. Furthermore, histopathological investigations revealed that the ethyl acetate fraction protected islets of Langerhans against alloxan-induced tissue alterations. These results suggest that C. europaea exhibited an important antihyperglycemic effect via the inhibition of glucose diffusion and pancreatic α-amylase activity. In addition, the antidiabetogenic effect of C. europaea might be attributed to their polyphenol and flavonoid compounds, which could be reacted alone, or in synergy, to scavenge the free radicals produced by the alloxan.

Phenomenological-based model of glucose transport from liver to abdominal subcutaneous adipose tissue.

BACKGROUND: A good treatment for type 1 diabetes mellitus (T1DM) requires accurate measurements of blood glucose levels. Continuous glucose monitors (CGM) measure the glucose concentration in the interstitial fluid of the abdominal subcutaneous adipose tissue. However, glucose measured in the abdominal interstitial fluid does not represent blood glucose concentrations accurately due to the complex blood transport through the body and glucose diffusion in interstitial fluid. METHODS: To gain insight into this problem, a phenomenological-based semiphysical model (PBSM) of glucose transport by volumetric flow and diffusion from the bloodstream to interstitial fluid was constructed. A published 10-step modeling procedure was used to obtain a model for glucose transport time through the blood vessels and from the blood capillaries to the interstitial fluid, glucose diffusion within the interstitial fluid, and glucose diffusion through the semipermeable coating of the sensor needle. For this model, a healthy person is considered at rest with average parameters. RESULTS: The simulations performed using the PBSM allow obtaining the glucose transport time from the liver to the sensor needle. In this way, it is possible to reconstruct an accurate dynamic measurement of blood glucose from the measurements in the interstitial fluid of the abdominal subcutaneous adipose tissue. CONCLUSIONS: PBSMs with parameters interpretability illustrate the connection of glucose concentrations in the interstitial fluid with that currently in the blood. Implementing this model in a CGM will result in more reliable measurements of blood glucose levels for T1DM treatment.

In vitro antidiabetic, antioxidant activities and GC-MS analysis of Rhynchostylis Retusa and Euphorbia Neriifolia leaf extracts.

This study aimed to assess the antidiabetic, and antioxidant potential of Rhynchostylis retusa and Euphorbia neriifolia, well known for traditional ethnomedicinal uses in North-east India. Leaf extracts prepared in water, methanol and petroleum ether were evaluated for in vitro antidiabetic and antioxidant assay using α-amylase inhibition, glucose diffusion method and DPPH radical scavenging activity. The α-amylase inhibition with E. neriifolia methanolic extract at 400 µg/ml (66.67%) and R. retusa aqueous extract at 300 µg/ml (58.15%) were stronger than in equivalent concentrations of acarbose, i.e., 62.17, and 51.52%, respectively. Aqueous extract R. retusa showed a maximum 67.65% inhibition of glucose diffusion at 180 min in comparison to control without leaf extract. The DPPH radical scavenging activity of E. neriifolia extract in methanol was significantly better than equivalent aqueous or ether extract. However, the solvent choice had little impact on antioxidant activity in R. retusa. GC-MS analysis revealed the presence of a large number of phytochemicals in methanol fraction of E. neriifolia aqueous extracts in comparison to R. retusa. Though the in vitro α-amylase inhibition or glucose diffusion retardation implied potential medicinal use of endangered orchid R. retusa and E. neriifolia, further investigation may be warranted for identification of relevant bio-active compounds and in vivo validation of their pharmacological properties.

Disposable electrochemical glucose sensor based on water-soluble quinone-based mediators with flavin adenine dinucleotide-dependent glucose dehydrogenase.

Glucose level measurement is essential for the point-of-care diagnosis, primarily for persons with diabetes. A disposable electrochemical glucose sensor is constructed using flavin adenine dinucleotide-dependent glucose dehydrogenase (FAD-GDH) and redox mediator for electron transfer from the enzyme to the electrode surface. Ideally, a suitable mediator should have high water solubility, high kinetic constant, high stability, and redox potential between -0.2 and 0.1 V vs. Ag|AgCl|sat. KCl. We designed and synthesized two new quinone-based water-soluble mediators: quinoline-5,8-dione (QD) and isoquinoline-5,8-dione (IQD). The formal potentials for both QD and IQD at pH 7.0 were -0.07 V vs. Ag|AgCl|sat. KCl. The logarithms of the electron exchange rate constants (k2/(M-1 s-1)) between QD/IQD and FAD-GDH were 7.7 ± 0.1 and 7.4 ± 0.1 for QD and IQD, respectively, which are the highest value among the water-soluble mediators for FAD-GDH reported to date. Disposable amperometric glucose sensors were fabricated by dropping FAD-GDH and QD or IQD onto a test strip. The sensor achieved a linear response up to glucose concentrations of 55.5 mM. The linear response was obtained even when the mediator loading was low (0.5 nmol/strip); loading was only 0.2 mol% of glucose. The results proved that the response current was primarily controlled by glucose diffusion. In addition, the sensor using QD exhibited high stability over 3 months at room temperature.

Structure characterization and in vitro hypoglycemic effect of partially degraded alginate.

Alginate is a low-cost polysaccharide found abundantly in seaweeds which consists of mannuronate and guluronate, and it is considered a sustainable gum source for dietary fiber. To solve the high viscosity-related problems while retaining its physiological properties, four partially degraded alginate products (PDA1-4) with molecular weight of 1.05-0.40 × 105 g mol-1 and intrinsic viscosity of 170.9-38.9 mL g-1 were enzymatically prepared and characterized. 1H Nuclear magnetic resonance analysis showed the used alginate lyase had a preference to degrade guluronate-blocks. PDA1 and PDA2 presented random coil conformation, whereas PDA3 and PDA4 displayed compact spherical-coil conformation over random coil conformation in solution. In vitro assays suggested a glucose-adsorption capacity order of PDA1 < PDA2 < alginate < PDA3 < PDA4 and a glucose-diffusion retardation capacity order of PDA3 < PDA1 ≤ alginate < PDA2 < PDA4, indicating that partially degraded alginate reinforced the hypoglycemic effect, especially mannuronate-rich PDA4. Overall, the study may have important implications for development of PDA as dietary fiber with potential hypoglycemic activity.

Effects of Scaffold Pore Morphologies on Glucose Transport Limitations in Hollow Fibre Membrane Bioreactor for Bone Tissue Engineering: Experiments and Numerical Modelling.

In the current research, three electrospun polycaprolactone (PCL) scaffolds with different pore morphology induced by changing the electrospinning parameters, spinning time and rate, have been prepared in order to provide a fundamental understanding on the effects pore morphology have on nutrient transport behaviour in hollow fibre membrane bioreactor (HFMB). After determining the porosity of the scaffolds, they were investigated for glucose diffusivity using cell culture media (CCM) and distilled water in a diffusion cell at 37 °C. The scanning electron microscope (SEM) images of the microstructure of the scaffolds were analysed further using ImageJ software to determine the porosity and glucose diffusivity. A Krogh cylinder model was used to determine the glucose transport profile with dimensionless variables within the HFMB. The paper discusses the roles of various dimensionless numbers (e.g., Péclet and Damköhler numbers) and non-dimensional groups of variables (e.g., non-dimensional fibre radius) on determining glucose concentration profiles, especially in the scaffold region. A negative linear relationship between glucose diffusivities across PCL scaffolds and the minimum glucose concentrations (i.e., concentration on the outer fibre edge on the outlet side (at z = 1 and r = 3.2) was also found. It was shown that the efficiency of glucose consumption improves with scaffolds of higher diffusivities. The results of this study are expected to help in optimizing designs of HFMB as well as carry out more accurate up scaling analyses for the bioreactor.

Finite Element Analysis of Glucose Diffusivity in Cellulose Nanofibril Peripheral Nerve Conduits.

Peripheral neuropathy arising from physical trauma is estimated to afflict 20 million people in the United States alone. In one common surgical intervention, neural conduits are placed over the nerve stumps to bridge the gap and create a microenvironment conducive to regeneration. It has been proposed that a biocompatible material such as cellulose nanofiber may serve as a viable conduit material, providing a non-inflammatory and mechanically stable system. Preliminary studies have shown that cellulose nanofiber conduits successfully aid neural regeneration and further, that the dimensions of the conduit relative to the nerve gap have an impact on efficacy in murine models. It has been hypothesized that the reliance of regeneration upon the physical dimensions of the conduit may be related to modified modes of diffusion and/or distances of key cellular nutrients and waste metabolites to/from the injury site. The present work investigates the concentration profile of glucose within the conduit via finite element analysis as a function of the physical dimensions of the conduit. It was determined that the magnitude of glucose diffusion was greater through the conduit walls than through the luminal space between the nerve and the inner wall of the conduit, and that as such radial diffusion is dominant over axial diffusion.

In-Vitro Antioxidant, Hypoglycemic Activity, and Identification of Bioactive Compounds in Phenol-Rich Extract from the Marine Red Algae Gracilaria edulis (Gmelin) Silva.

Obesity and diabetes are major metabolic disorders which are prevalent worldwide. Algae has played an important role in managing these disorders. In this study, Gracilaria edulis, a marine red algae, was investigated for antioxidant and hypoglycemic potential using in vitro models. De-polysaccharide methanol extract of G. edulis was sequentially partitioned with hexane, chloroform, ethyl acetate, and antioxidants, and hypoglycemic potentials were evaluated using multiple methods. High antioxidant potential was observed in the ethyl acetate fraction in terms of ferric reducing antioxidant power, iron chelating, and DPPH and ABTS radical scavenging activities, while the crude methanol extract exhibited potent oxygen radical-absorbance capacity. Potent α-amylase inhibitory activity was observed in the ethyl acetate fraction, while the ethyl acetate fraction was effective against α-glucosidase inhibition. Glucose diffusion was inhibited by the ethyl acetate fraction at 180 min, and the highest antiglycation activity was observed in both chloroform and ethyl acetate fractions. Additionally, gas chromatography-mass spectrometry analysis of the ethyl acetate fraction revealed the presence of several potent anti-diabetic compounds. In conclusion, G. edulis exhibited promising antidiabetic potential via multiple mechanisms. The ethyl acetate fraction exhibited the strongest hypoglycemic and antiglycation potential among the four fractions, and hence the isolation of active compounds is required to develop leads for new drugs to treat diabetes.

Interaction between barley ß-glucan and corn starch and its effects on the in vitro digestion of starch.

A ß-glucan was extracted from hull-less barley (HBBG) and its effects on the solution properties and in vitro digestion of corn starch (CS) were studied. Rheological results showed that HBBG diminished the gelling ability and increased the apparent viscosity of CS solution. The critical concentration was lowered from 1.10% (CS) to 0.48% (CS/HBBG mixture), and the slow relaxation component T22 decreased from 1417.47 to 464.16 ms after the incorporation of HBBG to CS solution. In vitro digestion study indicated that HBBG significantly increased the apparent viscosity of digesta and inhibited the starch hydrolysis and glucose diffusion. The entanglement and overlap formed by HBBG and CS interaction and aggregates of HBBG itself were considered to enhance the viscosity, thus limiting the water mobility of the system, reducing the contact of digestive enzyme with starch and diffusion of glucose to the small intestinal microvilli. This study suggests that HBBG can be recognized as an important ingredient in starch food to reduce postprandial glycemic responses.

In vitro hypoglycemic, cholesterol-lowering and fermentation capacities of fiber-rich orange pomace as affected by extrusion.

Our previous study suggested that extrusion can enhance the soluble dietary fiber (SDF) and improve the physicochemical properties of fiber-rich orange pomace (OP). The aim of this study was to determine the predictive indices for the hypoglycemic, hypocholesterolemic, and fermentation capacities of extruded orange pomace (EOP) with several in vitro assays. The results revealed that EOP could effectively retard glucose diffusion and inhibit α-amylase activity relative to OP. Moreover, EOP had the binding capacities of cholesterol micelles and bile acids. During the in vitro fermentation of EOP, a high content of short chain fatty acid was produced. Scanning electron microscope images showed a more porous and irregular shaped structure of the EOP, which may influence physiological activities, relative to OP. The morphological alterations in the EOP were caused by mechanical shear. Thus, EOP has potential to become a functional food additive for glycemic control and the attenuation of blood cholesterol.

Influence of nano-fibrillated cellulose (NFC) on starch digestion and glucose absorption.

Nano-fibrillated cellulose (NFC) is of interest in several fields due to its unique physical properties derived from its nanoscale dimensions. NFC has potential use in food systems as a dietary fiber that increases viscosity and limit diffusion of glucose. This study focused on the effects of added NFC on solution viscosity, starch digestion and glucose absorption. NFC did not affect α-amylase and α-glucosidase activity, but significantly retarded glucose diffusion, delayed amylolysis and reduced the amount of glucose released during in vitro digestion of starch. Specifically, 1% NFC retarded ∼26.6% of glucose released during the amylolysis process. The greatly increased viscosity of NFC at concentrations >0.5% was thought to be the main mechanism for its potential hypoglycemic effects. NFC suspensions also had higher glucose adsorption capacity than those containing cellulose. In addition, NFC bound 35.6% of the glucose when the initial glucose level was within the range of 5-200 mM. These results suggest that NFC may be useful for building viscosity in food products and serving to inhibit glucose absorption in vivo in starch-containing products.

Studies on in-vitro hypoglycemic effects of root bark of Caesalpinia bonducella.

OBJECTIVE: The present investigation was undertaken to assess the hypoglycemic potential of ethanolic (ECB) and aqueous extracts (ACB) of root bark of Caesalpinia bonducella using various in vitro techniques. METHOD: The ethanolic and aqueous extracts of root bark of C. bonducella were studied for their effects on glucose adsorption capacity, in vitro glucose diffusion, in-vitro amylolysis kinetics and glucose transport across membrane of yeast cells. RESULT: It was observed that the extracts under study adsorbed glucose and the adsorption of glucose increased remarkably with an increase in glucose concentration. The results of amylolysis kinetic experimental model revealed that the rate of glucose diffusion was found to be increased with time from 30 to 180min and both the extracts demonstrated significant inhibitory effects on movement of glucose into external solution across dialysis membrane as compared to control. Also, the extracts under study promoted glucose uptake by the yeast cells. It was observed that the enhancement of glucose uptake was dependent on both the sample and glucose concentration. Ethanolic extract of C. bonducella extract exhibited significantly higher (P≤0.05) activity than the aqueous extract at all concentrations. CONCLUSION: The results of the study verified the hypoglycemic activity of the extracts of root bark of C. bonducella. However, the observed effects need to be confirmed by using different in vivo models and clinical trials for its effective utilization as a therapeutic agent in effective management of diabetes mellitus.

In vitro hypoglycemic effects of unripe and ripe fruits of Musa sapientum

ABSTRACT The present study was undertaken to verify the hypoglycemic potential of unripe and ripe fruit extracts of Musa sapientum by using various in-vitro techniques, namely glucose adsorption capacity, glucose diffusion, amylolysis kinetics and glucose transport across the yeast cells. The results revealed that the unripe and ripe fruit extracts of Musa sapientum adsorbed glucose and the adsorption of glucose increased remarkably with an increase in glucose concentration. There were no significant (p≤0.05) differences between their adsorption capacities. In the amylolysis kinetic experimental model the rate of glucose diffusion was found to be increased with time from 30 to 180 min and both extracts exhibited significant inhibitory effects on the movement of glucose into external solution across the dialysis membrane as compared to control. The plant extracts also promoted glucose uptake by the yeast cells and enhancement of glucose uptake was dependent on both the sample and glucose concentration. The hypoglycemic effect exhibited by the extracts was observed to be mediated by inhibiting α-amylase, inhibiting glucose diffusion by adsorbing glucose and by increasing glucose transport across the cell membranes as revealed by an in-vitro model of yeast cells.

Effects of Hibiscus sabdariffa Linn. fruit extracts on α-glucosidase enzyme, glucose diffusion and wound healing activities

Objective To provide in vitro evidence for antidiabetic activity through potential inhibition of α-glucosidase enzyme, glucose diffusion and enhancement in the wound healing using methanolic extract and fractions from Hibiscus sabdariffa Linn. fruit. Methods The inhibitory action of methanolic extract and fractions of such fruit on α-glucosidase enzyme and glucose movement through in vitro assay assessment was reported. Their activities on wound healing were tested using the scratch assay. Results Ethyl acetate fraction at 50 mg/mL concentration exhibited significant α-glucosidase inhibition (95.79 mg/mL) with P < 0.05. At the same concentration, the methanolic extract as well as other fractions revealed lower α-glucosidase inhibition and higher glucose diffusion retardation across the dialysis tube than the control. Ethyl acetate and butanol fractions displayed notably higher glucose diffusion inhibitory activity of 5.21 mmol/L and 5.2 mmol/L, respectively as compared to methanolic extract and n-hexane fraction of 6.58 mmol/L and 6.49 mmol/L, respectively. Conversely, compared to other fractions the methanolic extract and ethyl acetate fraction manifested proliferative effect at the incubation time of 6 h during the wound healing study. Conclusions It is established that methanolic extract and fractions from H. sabdariffa Linn. fruit can inhibit the α-glucosidase enzyme and glucose movement as well as influence the wound healing activity positively.