Α-amylase Enzyme Inhibition Research Articles

Functional properties and encapsulation of a proanthocyanidin-rich cinnamon extract (Cinnamomum zeylanicum) by complex coacervation using gelatin and different polysaccharides

The phenolic compounds present in the cinnamon extract are responsible for its beneficial effect on health. However, these compounds can undergo degradation reactions and have undesirable sensorial characteristics, which makes it difficult to apply and consume a large quantity of this extract. Thus, the present work evaluated cinnamon extract rich in proanthocyanidins in liquid, spray-dried and lyophilized forms for content of phenolic compounds, antioxidant and antimicrobial capacity, as well as inhibition of α-amylase and α-glycosidase enzymes. In addition, it was proposed to encapsulate the extract by complex coacervation using polymeric pairs formed between gelatin and five different polysaccharides (gum arabic, pectin, cashew gum, carboxymethylcellulose, and κ-carrageenan), as well as characterize the encapsulated extract particles. Drying of the extract caused losses in the initial content of the phenolic compounds. The dry extracts, especially the atomized sample, presented high antioxidant capacity and high potential to inhibit the digestive enzymes, but they lost the antimicrobial capacity in relation to the liquid extract. The microparticles of the encapsulated extract had high efficiency and yield for encapsulation, varied sizes, and irregular shapes. Infrared spectra demonstrated the interaction between protein and polysaccharides in the formation of encapsulated extract particles. The results indicate that the complex coacervation and the materials used have the potential to encapsulate the cinnamon extract, which can contribute to protect its bioactive compounds, their beneficial properties, and mask their undesirable sensorial characteristics.

In vitro and in vivo assessment of anti-hyperglycemic and antioxidant effects of Oak leaves (Quercus convallata and Quercus arizonica) infusions and fermented beverages

The aim of this study was to evaluate the anti-hyperglycemic and antioxidant effects of oak leaves infusions and fermented beverages from Quercus convallata and Q. arizonica in vitro and in vivo. Female C57BL/6 mice fed with high saturated fat and fructose diet-induced obesity were treated with oak leaves beverages (200 μL/per day equivalent to 15mg of lyophilized sample/Kg of body weight for infusions and 31mg of lyophilized sample/Kg of body weight for fermented beverages) for 3months and an oral glucose tolerance test (OGTT) was performed. Blood plasma was obtained for determination of glucose, lipid profile, and oxidative stress markers (ABTS, nitric oxide, and ORAC assays). Insulin resistance was estimated using the product of triglycerides and glucose (TyG). Oak leaves infusions and fermented beverages exhibited exerted inhibition of α-amylase (8–15% and 5–9%, respectively) and α-glucosidase (98% and 99%, respectively) enzymes. After OGTT, the groups treated with either oak leaves infusions or fermented beverages showed lower glucose levels compared with the obesity control group (18%) and a similar glucose tolerance to healthy control group. On long-term evaluation, intervention groups showed a significant reduction in fasting glucose concentrations (41–50% for oak leaves infusions and 52–66% for fermented beverages) and TyG index (4.2–4.6% for oak leaves infusions and 5.9–7.5% for fermented beverages) compared with the obese control group. Oak leaves infusions and fermented beverages had antioxidant potential in vitro and scavenging activity for radicals such as peroxyl and peroxynitrite anions. Our results suggest anti-hyperglycemic and antioxidant effects of beverages prepared with leaves of Quercus species in vitro and in vivo.

Molecular Weight Affected Antioxidant, Hypoglycemic and Hypotensive Activities of Cold Water Extract from Pleurotus citrinopileatus.

Cold water extract of P. citrinopileatus (CWEPC) was fractioned into 4 fractions, PC-I (<1 kDa), PC-II (1-3.5 kDa), PC-III (3.5-10 kDa), and PC-IV (>10 kDa), by ultrafiltration. The antioxidant activities, the inhibition of pancreatic α-amylase, intestinal α-glucosidase, and hypertension-linked angiotensin converting enzyme (ACE), as well as the contents of polysaccharides, protein, and phenolic compounds of 4 fractions were determined. The results showed that lower MW fractions exerted a higher antioxidant activity, which was correlated to phenolic contents. The high molecular fraction (PC-IV) exhibited significantly higher inhibitory activity on α-amylase, α-glucosidase, and ACE compared to CWEPC and the other 3 lower MW fractions (<10 kDa), which was more related to protein contents. The inhibition capability of CWEPC and PC-IV on α-amylase activity was 1/13.4 to 1/2.7 relative to that of acarbose, respectively. Kinetic data revealed that PC-IV fraction followed a noncompetitive inhibition pattern on α-glucosidase activity. The study demonstrated that various MW fractions and types of components contribute to different biological functions of P. citrinopileatus and it is protein constituents but not peptides responsible for the hypoglycemic potential of CWEPC.

Aqueous extract of Psidium guajava leaves: phenolic compounds and inhibitory potential on digestive enzymes.

Leaves of Psidium guajava L. (guava) have been widely used in the popular way for prevention and treatment of various diseases. Thus, the objective of this study was to evaluate the inhibitory potential of leaves aqueous extract from three cultivars of P. guajava (Pedro Sato, Paluma and Século XXI) on α-amylase, α-glycosidase, lipase, and trypsin enzymes, in the presence or not of simulated gastric fluid and to determine the content of phenolic compounds by high performance liquid chromatography. All cultivars presented the same composition in phenolic compounds, but in different proportions. The compounds identified are gallic acid, epigallocatechin gallate, syringic acid, o-coumaric acid, resveratrol, quercetin, and catechin (which was the major compound in all the cultivars evaluated). In the absence of simulated gastric fluid, it was observed different inhibitions exercised by the leaves aqueous extracts from three cultivars of P. guajava on each enzyme. In presence of simulated gastric fluid, all cultivars showed increase in the inhibition of lipase and α-glycosidase, and decrease in inhibition of α-amylase and trypsin enzymes. These results indicate that P. guajava leaves aqueous extracts from all cultivars evaluated possess potential of use as an adjuvant in the treatment of obesity and other dyslipidemias.

Molecular docking analysis and antidiabetic activity of Rifabutin against STZ-NA induced diabetes in albino wistar rats

Computer Aided Drug Design (CADD) molecular docking program used in this study and as a result Rifabutin was retrieved as structurally similar drug molecule to Lixisenatide (A widely used GLP-1 agonist). To afford beneficial reason in vitro study conducted which too provides a favourable mark for prospective inhibition of α-glucosidase and α-amylase enzyme and thereby evaluated for its antidiabetic potential against Streptozotocin (STZ) and Nicotinamide (NA) induced diabetes in albino wistar rats. Rifabutin demonstrated significant efficacy towards restoring the blood glucose, insulin and distorted lipid profile in the animals treated with STZ-NA. Rifabutin also regulated the inflammatory (Nitric Oxide) and oxidative stress (TBARs, SOD, Catalase, GSH and protein carbonyl) markers in the pancreatic tissue of the STZ-NA treated animals. When scrutinized on the grounds electrocardiographic and heart rate variability (HRV) changes, Rifabutin decreased the heart rate, without much affecting the QRS, QT and QTc interval. Rifabutin was also evident to be less hepatotoxic in comparison to the standard metformin, providing an added advantage as an anti-diabetic agent. The study concluded that the low dose of rifabutin can favourably regulate of the blood glucose and other biochemical paradigms in comparison to high dose of rifabutin.

The effects of Ficus carica on the activity of enzymes related to metabolic syndrome

The present study aimed to investigate the effects of the various parts of Ficus carica L. (figs) on antioxidant, antidiabetic, and antiobesogenic effects in vitro. Fruit, leaves, and stembark of the F. carica plant were sequentially extracted using organic and inorganic solvents and their total polyphenol and flavonoid contents were estimated. The effects of the extracts on antioxidative, antidiabetic (inhibition of α-amylase and α-glucosidase enzymes), and antiobesogenic (antilipase) activities were measured using several experimental models. The fruit ethanolic extract contained a high quantity of polyphenols and flavonoids (104.67±5.51 μg/mL and 81.67±4.00 μg/mL) compared with all other extracts. The activity of the ethanolic extract of F. carica fruit was significantly (p<0.05) higher than all other extracts and parts of the plant in terms of antioxidative, antidiabetic, and antiobesogenic effects. The IC50 values of the fruit ethanolic extract in terms of antioxidative (134.44±18.43 μg/mL), and inhibition of α-glucosidase (255.57±36.46 μg/mL), α-amylase (315.89±3.83 μg/mL), and pancreatic lipase (230.475±9.65 μg/mL) activity indicate that the activity of fruit ethanolic extract is better than all other extracts of the plant. The gas chromatography–mass spectroscopy analysis of the fruit ethanolic extract showed the presence of a number of bioactive compounds such as butyl butyrate, 5-hydroxymethyl furfural, 1-butoxy-1-isobutoxy butane, malic acid, tetradecanoic acid, phytol acetate, trans phytol, n-hexadecanoic acid, 9Z,12Z-octadecadienoic acid, stearic acid, sitosterol, 3,5-dihydroxy-6-methyl-2,3-dihydro-4H-pyran-4-one, and 2,4,5-trimethyl-2,4-dihydro-3H-pyrazol-3-one. The results of this study suggest that the ethanolic extract of the fruit of F. carica may have potential antidiabetic and antiobesogenic agents.

Antibacterial and Hypoglycemic Diterpenoids from Salvia chamaedryoides.

A surface extract of the aerial parts of Salvia chamaedryoides afforded 13 diterpenes (1-13), with seven compounds (1, 3, 4, 7-9, 12) described for the first time. The structures of the new compounds were established using 1D and 2D NMR spectroscopic methods, HRESIMS, and ECD data. The potential hypoglycemic effects of the crude extract, fractions, and pure compounds from S.chamaedryoides were investigated by inhibition of α-glucosidase and α-amylase enzymes. The extract and its fractions showed a moderate dose-dependent inhibition; the pure compounds exhibited differential inhibitory activity against these two enzymes. Molecular modeling studies were also performed to suggest the interaction mode of compound 3 in the α-glucosidase enzyme active site. The antimicrobial activity of the purified compounds was investigated against 26 clinical pathogens. No activity was detected for the Gram-negative species tested nor on Candida albicans and C.glabrata, while variable susceptibilities were observed using Gram-positive staphylococcal and enterococcal species.

Extraction, HPTLC Estimation, In silico and In vitro Evaluation of α- Amylase Inhibition Potential of Stem Bark of Terminalia arjuna

Background: The problem of diabetes and associated treatments had mentioned herbal plants in several studies. The cardioactive Terminalia arjuna has also been reported for antidiabetic principles yet no scientific evidence is available. Hence, an attempt has been made by the authors to find the probable mechanism and biomarker involved for α-amylase enzyme inhibition Keywords: α-Amylase, arjunic acid; arjunolic acid; HPTLC; room temperature extraction (RTE); Soxhlet extraction (SE).

Biofabrication of size controllable silver nanoparticles – A green approach

A facile biosynthetic approach for the size controllable production of silver nanoparticles (AgNPs) using the leaf extract of Cinnamomum tsoi as reducing and capping agent is developed. The polyphenolic functionalities present in the extract are essentially responsible for the synthesis and stabilization of AgNPs. The size and morphology of the AgNPs were effectively tuned by changing the volume of the extract. The availability of oxidized polyphenols play key role in tuning the size and morphology of the prepared NPs. The as prepared AgNPs were characterized by X-ray diffraction (XRD), Ultraviolet–visible spectroscopy (UV–visible), Transmission electron microscopy (TEM), Selected area electron diffraction (SAED), Dynamic light scattering (DLS) and Fourier transform infrared (FTIR) techniques. FTIR and Zeta potential measurements have confirmed the decoration of oxidized polyphenols on the surface of synthesized AgNPs. TEM and DLS measurements revealed the size variation of AgNPs with change in the volume of plant extract. The prepared AgNPs showed the significant inhibition of α-amylase and α-glucosidase enzymes and exhibited a dose dependent activity. The enhanced in-vitro antidiabetic activity of the AgNPs may be due to the oxidized polyphenols present on the AgNPs surface which was confirmed by FTIR analysis. In addition, the present method is substitute to the chemical approaches of size controlled AgNPs synthesis that are being used nowadays.

In vitro evaluation of antidiabetic activity of aqueous and ethanolic leaves extracts of Chloroxylon swietenia

Background: Chloroxylon swietenia belongs to family Rutaceae. Common name - satin wood, Telugu name - billedu, bildu chettu, billu, Tamil name - vaaimaram or porasu. C. swietenia has been reported to have anti-inflammatory activity, antimicrobial activity, anthelmintic activity, analgesic activity, antioxidant activity, and mosquitocidal activity. Aims and Objective: To evaluate in vitro antidiabetic activity of aqueous and ethanolic leaves extracts of C. swietenia by α-amylase and α-glucosidase enzyme inhibitory assay. Materials and Methods: About 100, 200, 300, 400, 500 μg concentrations of acarbose, aqueous, and ethanolic leaves extracts of C. swietenia were used for the study. The absorbance values were taken in spectrophotometer at 540 nm and 546 nm for α-amylase and α-glucosidase enzyme, respectively. Results: The extracts exhibited significant inhibition of α-amylase and α-glucosidase enzyme in dose-dependent manner. Ethanolic extract exhibited more inhibitory activity when compared with aqueous extract. Conclusion: Results shows considerable α-amylase inhibitory activity as well as α-glucosidase inhibitory activity. The present findings indicate that aqueous and ethanolic leaves extracts of C. swietenia have in vitro antidiabetic activity.

Functional Properties of Partially Characterized Polysaccharide from the Medicinal Mushroom Ganoderma neo-japonicum (Agaricomycetes).

This study was conducted to evaluate the mycochemical composition and antiglycemic and antioxidant activities of Ganoderma neo-japonicum hot aqueous extracts, prepared at different boiling durations, and polysaccharides isolated from them. Ground basidiocarps of G. neo-japonicum were double-boiled at 100°C for 0.5, 3, or 4 hours, and the antiglycemic activity was assessed by α-amylase and α-glucosidase enzyme inhibition assays. The antioxidant capacity of the crude hot aqueous extracts (AE-1, AE-2, AE-3) was assessed by DPPH and ABTS radical scavenging and ferric-reducing antioxidant power assays. The total phenolics, protein, and sugar in the crude extracts were also determined. The hot aqueous extract (AE-3) containing a significant amount of total sugar and having enhanced antiglycemic and antioxidant activities was selected for polysaccharide isolation. The isolated crude polysaccharide was separated and purified using diethylaminoethyl-cellulose-52 and Sepharose 6B column chromatography. Fourier transform infrared spectroscopy studies of the purified polysaccharide fraction (PF) showed the presence of typical bands corresponding to polysaccharides. The estimated β-glucan concentration in the PF was 39.26%. In general, the PF exhibited significantly lower antioxidant activity than AE-3. Nevertheless, its potency in inhibiting carbohydratehydrolyzing enzymes may have potential in the management of diabetes mellitus.

Postprandial anti-hyperglycemic activity of marine Streptomyces coelicoflavus SRBVIT13 mediated gold nanoparticles in streptozotocin induced diabetic male albino Wister rats.

The present study focuses on the biosynthesis of gold nanoparticles (AuNPs) using Streptomyces coelicoflavus (S. coelicoflavus) SRBVIT13 isolated from marine salt pan soils collected from Ongole, Andhra Pradesh, India. The biosynthesised AuNPs are characterised by UV-visible spectroscopy, X-ray diffraction, Fourier transform infrared spectroscopy, high-resolution transmission electron microscopy and energy-dispersive X-ray analysis. Transmission electron microscopy study suggests that the biosynthesised AuNPs are spherical in shape within a size range of 12-20 nm (mean diameter as 14 nm). The anti-type II diabetes activity of AuNPs is carried out by testing it in vitro α-glucosidase and α-amylase enzyme inhibition activity and in vivo postprandial anti-hyperglycemic activity in sucrose and glucose-loaded streptozotocin induced diabetic albino Wister rats. AuNPs has shown a significant inhibitory activity of 84.70 and 87.82% with IC50 values of 67.65 and 65.59 μg/mL to α-glucosidase and α-amylase enzymes, while the diabetic rats have shown significant reduction in the post postprandial blood glucose level by 57.80 and 88.09%, respectively compared with control group after AuNPs treatment at the concentration of 300 and 600 mg/kg body weight. Hence, this biosynthesised AuNPs might be useful in combating type II diabetes mellitus for the betterment of human life.

Antidiabetic and anti-obesity activity of Ficus carica: In vitro experimental studies

Aim The present study was aimed to investigate the role of Ficus carica L. (fig) aerial parts on antioxidant, antidiabetic and anti-obesogenic effects in vitro. Methods Fruit, leaves and stembark of Ficus carica plant were sequentially extracted by using organic and inorganic solvents and their total polyphenolics and flavonoids contents were estimated. The effects of the extracts on antioxidative, antidiabetic (inhibition of α-amylase and α-glucosidase enzymes) and anti-obesogenic (anti-lipase) activities were measured by using several experimental models. Results The fruit ethanolic extract contained a high amount of polyphenols and flavonoids (104.67±5.51μg·mL −1 and 81.67±4.00μg·mL −1 ). The ethanolic extract of Ficus carica fruit was significantly ( P −1 ), α-glucosidase (255.57±36.46μg·mL −1 ) α-amylase (315.89±3.83μg·mL −1 ) and pancreatic lipase (230.475±9.65μg·mL −1 ) assays indicate that fruit extracts were more active than other parts of the plant. The GC-MS analysis of the fruit extract shown the presence of sugars and polyphenolic compounds such as butyl butyrate, 5-hydroxy-methyl furfural, 1-butoxy-1-isobutoxy butane, malic acid, tetradecanoic acid, phytol acetate, trans phytol, n-hexadecanoic acid, 9Z,12Z-octadecadienoic acid, stearic acid, sitosterol, 3,5-dihydroxy-6-methyl-2,3-dihydro-4H-pyran-4-one, 2,4,5-trimethyl-2,4-dihydro-3H-pyrazol-3-one. Conclusion The results of this study suggest that the ethanolic extract of the fruit of Ficus carica may have potential antidiabetic and anti-obesogenic agents.

Poncirus trifoliata (L.) Raf.: Chemical composition, antioxidant properties and hypoglycaemic activity via the inhibition of α-amylase and α-glucosidase enzymes

The aim of this study was to investigate the phytochemical content of Poncirus trifoliata (L.) Raf. (Rutaceae) and to assess its hypoglycaemic and antioxidant effects. Hesperidin, naringin and chlorogenic acid were the most abundant compounds of the juice. Peel essential oil showed that limonene, myrcene, p-cimene and β-pinene were its main components. The antioxidant activity was studied through different in vitro tests. The hypoglycaemic effects were analysed via inhibition of carbohydrate-hydrolysing enzymes. IC50 values in the range 30.38–39.25 µg/mL were found respectively for juice and peel oil in the DPPH test. Juice inhibited α-amylase and α-glucosidase with IC50 values respectively of 138.14 and 81.27 µg/mL. Polyphenolic compounds identified in the juice were investigated. While neoeriocitrin displayed the strongest antioxidant activity and inhibited α-amylase (IC50 of 4.69 vs 77.45 µM for acarbose), didymin was found to be the most bioactive flavonoid against alpha-glucosidase (IC50 of 4.20 vs 54.99 µM for acarbose).

Lupane Analogue from Bark of Pithecellobium dulce and in vitro α-Glucosidase and α-Amylase Enzyme Inhibition Assay of Extract for Potential Antidiabetic Activity

Lupane Analogue from Bark of Pithecellobium dulce and in vitro α-Glucosidase and α-Amylase Enzyme Inhibition Assay of Extract for Potential Antidiabetic Activity

Assessment Of In-Vitro Antidiabetic - Antioxidant Effects Of Helianthus Tuberosus, Cydonia Oblonga And Allium Porrum

In-vivo antidiabetic activity of Cydonia oblonga Mill. (quince) leaves, Helianthus tuberosus L. (Jerusalem artichoke) tubers, and Allium porrum L. (leek) bulb and leaves was determined in our previous studies. These plants are traditionally used to lower blood glucose levels in Turkey. Therefore, inhibitory activities of quince leaves, Jerusalem artichoke tubers, leek bulbs and leaves on carbohydrate digestive enzymes (α-glucosidase and α-amylase) were investigated to enlighten the mechanism of action. On the other hand, their antioxidant activities, total phenol and flavonoid contents were investigated. The highest ABTS radical scavenging, total antioxidant activity and reducing power were found in C. oblonga leaf ethanol extract. Nevertheless, tested plant extracts did not inhibit α-amylase and α-glucosidase significantly. Total phenol and flavonoid contents of the extracts were found in the range of 7.91-163.33 mg gallic acid equivalent/g and 27.26-29.60 mg quercetin/g, respectively. Consequently, it is clearly seen that the mechanism of action of these three plants was not determined to be related to the inhibition of αamylase and α-glucosidase enzymes.

Effect of Drying Techniques on Antioxidant Capacity of Guava Fruit

Frequent consumption of fruits and vegetables has been associated with low risk of chronic diseases. Guava (Psidium guajava Linn.) is a tropical, seasonal fruit rich in antioxidants, vitamin C and polyphenol compounds. Drying is one of the common methods to preserve and extend the shelf life of guava. The objective of this study was to determine the effect of drying techniques on the antioxidant activity of guava fruit. Guava was air dried in air dryer (45°C), freeze dryer and by osmatic drying techniques. Fresh guava extracts (FGE), freeze dried guava extracts (FDGE), oven dried guava extracts (ODGE) and osmotic-dehydrated guava extracts (OSGE) guava extracts were prepared and analyzed for total polyphenols (TP), flavonoids, antioxidant potential by 2,2-diphenyl-1-picrylhydrazyl (DPPH), ferric reducing antioxidant power (FRAP), oxygen radical absorbance capacity (ORAC), trolox equivalent antioxidant capacity (TEAC), total antioxidant capacity (TAC) and nitric oxide radical scavenging activity (NORS). Inhibitory potential of guava extracts on enzymes α-glucosidase, α-amylase and lipase was also determined. TP in FG, FD, OD, and OS were 415.69 ± 56.95, 295.30 ± 4.11, 303.57 ± 1.41, and 182.93 ± 6.48 mg gallic acid equivalent (GAE)/100g, respectively. Flavonoids in Fresh, FD, OD, and OS were 202.01 ± 0.16, 96.93 ± 1.73, 105.07 ± 0.58, and 76.13 ± 2.74 mg catechin equivalent (CE)/100 g, respectively. FD extracts were the most effective in scavenging DPPH radical. Whereas FRAP, TEAC and TAC activities were found to be higher in FG followed by OD and FD. However, NORS activity of FD was significantly (p ≤ 0.05) lower compared to other treatments. Inhibition of α-glycosidase, α-amylase and lipase enzymes was (19% - 90%) observed at 0.4, 0.8, and 0.8 mg/ml, respectively. In conclusion, considering this in-vitro study, drying could be effectively utilized to preserve guava fruit with minimum effect on health benefits.

Scavenging activity, anti-inflammatory and diabetes related enzyme inhibition properties of ethanol leaves extract of &lt;i&gt;Phoenyx dactylifera&lt;/i&gt;

In this study we investigate the antioxidant, anti-inflammatory, and antidiabetic activities of ethanolic leaf extracts of three selected varieties of Phoenyx dactylifera L. namely: “Ghars”, “Deglet Nour” and “Hamraya”. The assessment of the antioxidant potential of crude leaf extracts, using superoxide anions inhibition, radical scavenging activity and total antioxidant activity essays, was carried out. Furthermore, the anti-inflammatory properties of the extracts were determined by measuring the inhibition of nitric oxide (NO) production. Moreover, the antidiabetic effect was evaluated by inhibition of α-amylase and α-glucosidase enzymes. The total phenolic content measured by Folin-ciocalteu method. The raw leaf extracts of the selected varieties were found to contain a high content of total phenolic content (342.45 mg GAE/ gDW for GE) and therefore exhibited a higher antioxidant activity and inhibitory effect of radicals scavenging activity against DPPH and superoxide anion (IC 50 =7.44 μg / mL and 39.11 μg / mL respectively). Keywords: Phoenyx dactyliferaL; antioxidant; anti-inflammatory; antidiabetic activities.

Alpha-amylase, antioxidant, and anti-inflammatory activities of Eucheuma denticulatum (N.L. Burman) F.S. Collins and Hervey

Eucheuma denticulatum is a red edible seaweed that grows in the East Malaysia coastal region. The objective of this study was to investigate the α-amylase, antioxidant and anti-inflammatory activities of E. denticulatum ethanol extract and its three fractions (n-hexane, ethyl acetate and acetone). α-Amylase activity was assessed by dinitrosalicylic acid (DNS) assay, while the antioxidant property was determined by oxygen radical absorbance capacity (ORAC) analysis. The anti-inflammatory effects of the seaweed samples were evaluated by nitric oxide (NO), interleukin-6 (IL-6), interleukin-1 (IL-1), tumor necrosis factor-alpha (TNF-α), and monocyte chemoattractant protein-1 (MCP-1) activities on the interferon-gamma/lipopolysaccharide (IFN-γ/LPS)-stimulated murine macrophage cell line (RAW 264.7) using Griess reaction and immunoassays, respectively. At 10 mg mL−1, E. denticulatum ethanol extract and three fractions inhibited α-amylase activities at variable levels. The highest (67 %) inhibition of α-amylase enzyme was by the ethanol crude extract. The three fractions showed inhibition with a mean of 42 %. Crude ethanol extracts also exhibited higher antioxidant capacity (36,400 ± 23.5 mol Trolox equivalent (TE) (100 g)−1) when compared to the fractions. Crude extract and fractions (1–100 μg mL−1), also exhibited anti-inflammatory activity without showing any cytotoxic effect to RAW 264.7 cells. The present study suggests that E. denticulatum has the potential to be a promising source of effective functional metabolite. An extensive research on the edible varieties would contribute to a better understanding of their importance as functional food.

In Vivo Anti-Hyperglycemic Potential of Brahmi Gritham and Docking Studies of Its Active Components Against Protein Kinase C and CD38

The anti-hyperglycemic and antioxidant effects of the Indian herbal formulation Brahmi gritham were studied in streptozotocin-induced diabetic female Wistar albino rats. Diabetes was induced by a single dose of streptozotocin (55 mg/kg body weight [b.w.], i.p.). Estimation of blood glucose levels, liver glycogen content and antioxidant levels were carried out in experimental rats. The tested parameters were compared with those of the glibenclamide (600 μg/kg b.w.) treated group. Molecular docking studies were carried out to analyze the interaction patterns of protein kinase C (PKC) and CD38 of chosen proteins of signal transduction pathways that are significant in the pathogenesis of diabetes against active components of Brahmi gritham. Immunohistochemistry of pancreas revealed that Brahmi gritham was able to restore β-cell mass and function near to that of the normal control. In silico studies showed that apigenin and quercetin showed significant interactions with PKC, while clitorin, bacopaside I and II showed significant interactions with CD38. Quercetin showed highest percentage inhibition of α-amylase enzyme. Practical Applications Brahmi gritham is a traditional polyherbal formulation used in Ayurveda to treat memory disorders. The individual components of this formulation are known to possess significant antioxidant properties and contain several biologically active compounds found to be effective in treating various disorders, including diabetes and obesity. The efficacy of Brahmi gritham in diabetes management has not yet been studied, and therefore, the present study provides insights into the anti-hyperglycemic potential of this formulation in rat model. In addition, the results of in silico analysis would pave way for better utilization of the flavonoids quercetin and apigenin in diabetes management and in particular microvascular diabetic complications.