Α-amylase Enzyme Inhibition Research Articles

Chemical composition, structural features, surface morphology and bioactivities of chitosan derivatives from lobster (Thenus unimaculatus) shells

The chemical composition, structural features and bioactivities of chitosan derivatives were studied and reported here. Chitin and chitosan was extracted by chemical methods and yield was recorded 35% and 41%, moisture and ash has showed 7.4, 0.73, 1.2 and 0.79% and Ca was recorded high level (590 ppm). The IR spectrum has showed NH primary and secondary amines, OH group and several sugar stretching. N-acetyl glucosamine (GlcNAc), H-2 proton of glucosamine (GlcN), Anomeric protons, H-1 [GlcN (H-1D), GlcNAc (H-1A)] were noticed in 1H NMR and anomeric, methyl carbon atoms in 13C NMR. Rough surface, irregular block, crystalline with cluster and porosity structure was noticed by SEM observation. Antioxidant effect has showed good and concentration depended in four antioxidant assays. The α-amylase and β-glucosidase enzyme inhibition effect of chitosan has showed promising and dose depend also anticoagulant potential. Chitosan could be used in pharmaceutical industry and tissue engineering.

Ингибирование α-амилазы и α-глюкозидазы новыми производными β-аминопропиоамидоксимов

В связи с актуальностью проблемы диабета в мире ведется поиск новых противодиабетических средств. Известно о противодиабетической активности производных амидо-ксимов. Нами проведено in vitro тестирование производных β-аминопропиоамидоксимов – оснований и фармакологически приемлемых солей О-ароил-β-(морфолин-1-ил)пропиоамидоксимов и 5-замещенных фенил-3-β-(пиперидин-1-ил и морфолин-1-ил)этил- 1,2,4-оксадиазолов на противодиабетическую активность по ингибированию ферментов α-амилазы и α-глюкозидазы. Выявлены соединения, обладающие выраженными противодиабетическими свойствами; причем ряд 3,5-дизамещенных 1,2,4-оксадиазолов более активен, чем ряд О-ароил-β-аминопропиоамидоксимов. Полученные данные могут быть использованы в дальнейшей in vivo проверке противодиабетических свойств наиболее перспективных образцов с предварительной оценкой их среднетоксической дозы на животных.

Measurement of anticancer, antidiabetic and anticholinergic properties of sumac (Rhus coriaria): analysis of its phenolic compounds by LC–MS/MS

The present study aimed to investigate Sumac (Rhus coriaria) for anticancer, antidiabetic, anticholinergic activities and total phenolic and flavonoid contents. Two solvents, water and ethanol, were used for extraction. For anticancer activity, the extracts were tested against human cancer cell lines including HT-29 and MCF-7. The cell growth inhibition rate was measured via XTT assay. The antidiabetic activity of the sumac extracts was measured by the inhibition of α-glycosidase and α-amylase enzymes, whereas the anticholinergic activity was measured via the inhibition of acetylcholinesterase and butyrylcholinesterase enzymes. The total phenolic and flavonoid contents were determined using the Folin–Ciocalteau and the aluminum chloride colorimetric methods, respectively. Liquid chromatography–mass spectrometry/mass spectrometry (LC–MS/MS) method was used for the separation, identification and quantification of phenolic compounds in the samples. The ethanolic extract had higher phenolic and phenolic contents than aqueous extract. It exhibited substantial antiproliferative, antidiabetic and anticholinergic activities. The aqueous extract of sumac showed moderate therapeutic efficiency in all the preformed assays. LC–MS/MS study revealed fumaric acid as a main compound in both the ethanolic (452.78 mg/kg) and aqueous (180.72 mg/kg) extracts. These results suggest that sumac may have health-enhancing effects and act as inhibitors of certain enzymes or interfering with some cellular pathways.

Isolation, characterization, and structural elucidation of 4-methoxyacetanilide from marine actinobacteria Streptomyces sp. SCA29 and evaluation of its enzyme inhibitory, antibacterial, and cytotoxic potential.

Marine actinobacteria are less explored than their terrestrial counterparts as potential source of natural products. The present study was aimed to elucidate the bioactive potential of metabolites produced by marine-derived actinobacterial strain Streptomyces sp.SCA29 isolated from Havelock Island, Andaman and Nicobar Islands, India. The potential isolate SCA29 was identified as Streptomyces sp. by phenotypic, genotypic (16S-rRNA) and phylogenetic analyses. The crude bioactive compound was extracted using organic solvents. The compounds were subjected to separation and purification by column chromatography which yielded six fractions. Each fraction was assayed for inhibition of α-glucosidase and α-amylase enzymes, antagonistic activity against bacterial pathogens, and cytotoxic activity against various cell lines. The fraction F3c was considered to be highly active owing to its significant inhibition potential against α-glucosidase and α-amylase enzymes with IC50 values as 44.26 and 53.19µg/mL, respectively. The active fraction showed antibacterial activity against test bacterial pathogens with the MIC value ranged from 3.90 to 31.25µg/mL. The compound also exhibited concentration-dependent cytotoxicity on various cell lines without significant effect against human normal cells. The bioassay-guided fractionation of extract led to the identification of 4-methoxyacetanilide, an acetamide derivative. The structure of the bioactive compound was confirmed by HR-MS, NMR (1H and 13C) and FT-IR spectra, and by comparison with literature data.

ANTI-DIABETIC POTENTIAL OF PEPTIDE FROM P. NIRURI REVEALS THROUGH CARBOHYDRATE HYDROLYZING ENZYME INHIBITION ASSAY

Herb Phyllanthus niruri (P. niruri) is known to have various pharmacological functions including anti-diabetic properties. In this research, protein extracts from different plant parts (leave, fruit and stem) of P. niruri were investigated for their anti-diabetic potential through α-amylase and α-glucosidase enzyme inhibition assays. For the enzyme inhibition assay, fruit was found to have the highest inhibition percentage (90.0%) against α-glucosidase followed by leave (62.6%) and stem (38.4%). The similar patterns were also recorded for the α-amylase enzyme inhibition assay, in which, fruit showed the highest inhibition percentage (64.1%) followed by leave (33.3%) and stem (18.2%). The findings of this research suggest that fruit of P. niruri is a potential plant part with regards to antidiabetic properties since it exhibits the highest inhibition activity against both α-amylase and α-glucosidase enzyme compared to leave and stem.

Antihyperglycemic Activity of Carthamus oxyacantha growing in Saudi Arabia; an in vitro and in vivo Study

The main objective of the current study was to investigate the in vitro and in vivo antidiabetic activity of methanol extracts Carthamus ‎oxyacantha leaves and corollas. In vitro antidiabetic assays such as inhibition of α-amylase enzyme, non-enzymatic glycosylation of hemoglobin and glucose uptake in yeast cells were carried out. The results of α-amylase inhibition assay revealed that the IC50 of methanol extracts of leaf and corolla were almost same (‎58.5 and ‎57.1 µg/ml, respectively) when compared with positive control acarbose (‎45.3‎ µg/ml). Glycosylation of hemoglobin was inhibited and the methanol extract of corolla showed an IC50 value of 61.7 µg/ml, while methanol extract of the leaf showed 93.9 µg/ml when compared to the positive control, α-tocopherol (‎35.4 µg/ml‎). On the other hand, the percent glucose uptake in yeast cells caused by methanol extracts of leaf and corolla was distinctly greater when compared to that of metformin. In vivo antidiabetic study revealed that the two methanol extracts at a dose of 200 mg/kg reduced the fasting plasma glucose level (‎94.6‎±‎4.4 and ‎102.1±5.5 mg/dl, respectively) when compared to that of glibenclamide (79.4±3.4‎ mg/dl, p<0.001). The results from this study indicated that Carthamus ‎oxyacantha leaf and corolla methanol extracts exhibited considerable in vitro and in vivo antidiabetic activities, which would make Carthamus ‎oxyacantha ‎a potential antidiabetic agent.

Anti-diabetic activities of Dactylorhiza hatagirea leaf extract in 3T3-L1 cell line model

Background: Diabetes is an endocrine disorder that results in altered carbohydrate, protein, and lipid metabolism. Several synthetic drugs used to treat diabetes have adverse effects on prolonged usage. This has given the impetus to the search for alternative medicines with no or less side effects. The plants of Orchidaceae family have displayed antimicrobial, anti-inflammatory, antioxidant, anticancer, and antidiabetic activity. However, their antidiabetic properties are yet to be explored. Materials and Methods: The in vitro antidiabetic properties of Dactylorhiza hatagirea leaf extract were studied by biochemical assays such as α-amylase and α-glucosidase inhibition assays and in vitro cellular assays such as glucose uptake assay and glucose transporter type 4 (GLUT4) expression studies in 3T3-L1 cell line. Results: The methanolic extract of D. hatagirea, at varying concentrations (25 μg-400 μg/mL), did not exhibit cytotoxicity against 3T3-L1 cell line after 24 h of incubation. Methanolic extract of D. hatagirea leaves showed significant inhibition of α-Amylase and α-Glucosidase enzymes. After 24 h of exposure of 3T3-L1 cells to 100 μg/mL of D. hatagirea leaf extract and 100 μM of metformin, the relative expression rates of GLUT4 receptor were elevated when compared with untreated cells. The results also revealed that the amount of 2-(N-(7-Nitrobenz-2-oxa-1,3-diazol-4-yl) Amino)-2-Deoxyglucose taken up by 3T3-L1 cells treated with D. hatagirea leaf extract and metformin is higher than that of untreated cells. Conclusion: Our results suggest that methanolic extract of D. hatagirea leaves has potential antidiabetic activity and could be a plausible resource for antidiabetic agents.

SUNCA standardized extract from Helianthus annus L exerts enhanced digestive enzyme activity and subsides obesity through inhibition of C/EBP-α and PPAR-γ expression both in in vitro and in vivo model

Background: Helianthus annuus L. (sunflower) is well known for its edible oil, sunflower seed has been used as folk remedy for several diseases including cancer. Materials and Methods: In this study, SUNCA, a standardized extract enriched with chlorogenic acid (CGA) from sunflower seed was investigated for in vitro antidiabetic activity using α-amylase and α-glucosidase enzyme inhibition assay. Further, for preventing obesity, we demonstrated anti-adipogenesis in 3T3-L1 cell culture system and on body weight gain and adiposity in rat fed high-fat diet (HFD). Results:SUNCA showed significant inhibitory activity toward digestive enzymes such as α-amylase and α-glucosidase. On the other hand, SUNCA significantly inhibits lipid accumulation during adipogenesis in a dose-dependent manner. The treatment with 100 μg/kg b.w of SUNCA apparently prevented the body weight gain and the increase of triglyceride and total cholesterol level in rat fed an HFD for 6 weeks. Further immunoblotting studies reveal that SUNCA significantly down-regulates the expression of transcription factors peroxisome proliferator-activated receptor gamma and CCAT/enhancer-binding protein alpha, both in adipocytes and adipose tissues. Conclusion: The findings reported here provide the therapeutic potential of SUNCA, a standardized extract from Helanthus annus L.

Screening of Musa balbisiana Colla. seeds for antidiabetic properties and isolation of apiforol, a potential lead, with antidiabetic activity.

'Phytonutrients' have been reported to exert an incredible impact on the healthcare system and offer medical benefits including the prevention or treatment of lifestyle-associated diseases. We chose one of the most common and important plant families, Musaceae, for our present study and explored its antidiabetic potential. Seeds of the edible fruits of Musa balbisiana Colla. were investigated for their antidiabetic potential. After estimating the proximate composition, the seeds were extracted with various solvents and evaluated for antidiabetic potential in terms of the inhibition of digestive enzymes, antiglycation activity and in vitro glucose uptake. The acetone extract demonstrated the highest inhibition of α-amylase and α-glucosidase enzymes with IC50 values of 36.67±0.367 and 100.61±0.707 µg mL-1 , respectively. The extract also exhibited significant glycation inhibition with an IC50 value of 86.48±0.751 µg mL-1 . Furthermore, a major phytochemical, apiforol, was isolated from the acetone extract for the first time, which demonstrated promising α-glucosidase inhibition (IC50 =48.25±0.255 µmol L-1 ), antiglycation property (IC50 =114.23±0.567 µmol L-1 ) and enhanced glucose uptake in L6 myoblasts. In molecular docking studies, apiforol efficiently bonded to the active sites of α-glucosidase enzyme 3A4A. As dietary intervention is one of the effective strategies for addressing diabetes, special attention is always given to natural food bio-actives or agro-products for better human health. The results of our study suggest that Musa balbisiana has significant potential as an ingredient in health food formulations by reducing postprandial hyperglycaemia. © 2018 Society of Chemical Industry.

Bioactive Peptides from Germinated Soybean with Anti-Diabetic Potential by Inhibition of Dipeptidyl Peptidase-IV, α-Amylase, and α-Glucosidase Enzymes

Functional foods containing peptides offer the possibility to modulate the absorption of sugars and insulin levels to prevent diabetes. This study investigates the potential of germinated soybean peptides to modulate postprandial glycaemic response through inhibition of dipeptidyl peptidase IV (DPP-IV), salivary α-amylase, and intestinal α-glucosidases. A protein isolate from soybean sprouts was digested by pepsin and pancreatin. Protein digest and peptide fractions obtained by ultrafiltration (<5, 5–10 and >10 kDa) and subsequent semipreparative reverse phase liquid chromatography (F1, F2, F3, and F4) were screened for in vitro inhibition of DPP-IV, α-amylase, maltase, and sucrase activities. Protein digest inhibited DPP-IV (IC50 = 1.49 mg/mL), α-amylase (IC50 = 1.70 mg/mL), maltase, and sucrase activities of α-glucosidases (IC50 = 3.73 and 2.90 mg/mL, respectively). Peptides of 5–10 and >10 kDa were more effective at inhibiting DPP-IV (IC50 = 0.91 and 1.18 mg/mL, respectively), while peptides of 5–10 and <5 kDa showed a higher potency to inhibit α-amylase and α-glucosidases. Peptides in F1, F2, and F3 were mainly fragments from β-conglycinin, glycinin, and P34 thiol protease. The analysis of structural features of peptides in F1–F3 allowed the tentative identification of potential antidiabetic peptides. Germinated soybean protein showed a promising potential to be used as a nutraceutical or functional ingredient for diabetes prevention.

Synthesis and α-Amylase Inhibition Studies of Some Coumarin Derivatives

A series of nine molecules of coumarin hydrazone derivatives have been synthesized. The purpose of this study was to investigate the anti-diabetic activity of synthesized coumarin derivatives by inhibition of α-amylase enzyme isolated from Aspergillus niger microbial strain. The experiment was conducted by taking 5, 10, 50, and 100 μg/mL of each compound and acarbose as a positive control. The tests showed that compounds 3f (IC50 = 49.70 μg/mL), 3g (IC50 = 79.20 μg/mL), and 3i (IC50 = 48.80 μg/mL) as well as reference drug (IC50 = 81.70 μg/mL) exhibited inhibition activity against the enzyme. The synthesized compounds may be helpful in controlling the glucose level as α-amylase is one of the causes of increased sugar level in human body.

Antidiabetic and antiparasitic potentials: Inhibition effects of some natural antioxidant compounds on α-glycosidase, α-amylase and human glutathione S-transferase enzymes

The glutathione S-transferase (GST) was purified from fresh blood erythrocytes using affinity column chromatography. Also, α-amylase from porcine pancreas and α-glycosidase from Saccharomyces cerevisiae were used as target enzymes. In this study, these compounds were tested on α-amylase, α-glycosidase, and GST enzymes and demonstrated effective inhibitor compounds with Ki values in the range of 8.34–40.78 μM against GST, and 120.53–892.36 nM against α-glycosidase. Additionally, the phenolic molecules were tested for the inhibition of α-amylase enzyme which determined effective inhibition profile with IC50 values in the range of 175.01–626.58 nM. Indeed, these molecules can be elective inhibitors of GST, α-glycosidase and α-amylase enzymes as antidiabetic and antiparasitic agents.

Evaluation of Antimicrobial, Enzyme Inhibitory, Antioxidant and Cytotoxic Activities of Partially Purified Volatile Metabolites of Marine Streptomyces sp.S2A.

In the present study, marine actinobacteria Streptomyces sp.S2A was isolated from the Gulf of Mannar, India. Identification was carried out by 16S rRNA analysis. Bioactive metabolites were extracted by solvent extraction method. The metabolites were assayed for antagonistic activity against bacterial and fungal pathogens, inhibition of α-glucosidase and α-amylase enzymes, antioxidant activity and cytotoxic activity against various cell lines. The actinobacterial extract showed significant antagonistic activity against four gram-positive and two gram-negative pathogens. Excellent reduction in the growth of fungal pathogens was also observed. The minimum inhibitory concentration of the partially purified extract (PPE) was determined as 31.25 μg/mL against Klebsiella pneumoniae, 15.62 μg/mL against Staphylococcus epidermidis, Staphylococcus aureus and Bacillus cereus. The lowest MIC was observed against Micrococcus luteus as 7.8 μg/mL. MIC against fungal pathogens was determined as 62.5 μg/mL against Bipolaris maydis and 15.62 μg/mL against Fusarium moniliforme. The α-glucosidase and α-amylase inhibitory potential of the fractions were carried out by microtiter plate method. IC50 value of active fraction for α-glucosidase and α-amylase inhibition was found to be 21.17 μg/mL and 20.46 μg/mL respectively. The antioxidant activity of partially purified extract (PPE) (DPPH, ABTS, FRAP and Metal chelating activity) were observed and were also found to have significant cytotoxic activity against HT-29, MDA and U-87MG cell lines. The compound analysis was performed using gas chromatography-mass spectrometry (GC-MS) and resulted in three constituents; pyrrolo[1–a]pyrazine-1,4-dione,hexahydro-3-(2-methylpropyl)-, being the main component (80%). Overall, the strain possesses a wide spectrum of antimicrobial, enzyme inhibitory, antioxidant and cytotoxic activities which affords the production of significant bioactive metabolites as potential pharmacological agents.

Insulinomimetic Effect of Citrullus Colocynthis Roots in STZ Challenged Rat Model

Abstract Diabetes mellitus is a metabolic disease characterized by hyperglycemia resulting from either defect in insulin secretion, insulin action, or both. Postprandial hyperglycemia is a prime characteristic of diabetes mellitus and has been a focus in the therapy for diabetes. One of the therapeutic approaches which involve decreasing hyperglycemia aims at lowering blood glucose by decreasing insulin resistance, raising insulin sensitivity at the tissues and inhibiting the carbohydrate absorbance in the intestine. Plants contain different chemical constituents with potential for insulin mimetic action, decrease in insulin resistance and of α-amylase inhibitory activity may be used as therapeutic agents in the treatment of diabetes mellitus. The present study investigates the hypoglycemic activity and insulinomimetic action of aqueous and ethanolic extracts of Citrullus colocynthis by invitro α-amylase enzyme inhibition and by histopathological studies in streptozotocin (STZ) induced diabetic rats. Male Wistar rats weighing about 180- 250g were taken and divided into fifteen groups. Diabetes was induced by giving streptozotocin (STZ) (30-50mg/kg) intraperitoneally. Rats that showed blood glucose levels > 250mg/dl were selected for the study. Metformin (45mg/kg) was given as standard oral hypoglycemic agent. The aqueous and ethanolic extracts of Citrullus colocynthis (AECC and EECC) at 100mg/kg, 200mg/kg and 300mg/kg were administered to the normal and diabetic rats. The invitro α – amylase inhibitory activity was done by spectrophotometric method. Blood glucose levels were measured by glucose oxidase method. Estimation of glycogen in the lever was carried out with anthrone method. Liver and pancreas were isolated and subjected to histopathological studies. Serum insulin was monitored through chemiluminescence assay. Oral administration of both extracts showed significant inhibition of α-amylase enzyme in-vitro and decrease in blood glucose also. Glycogen and Insulin levels too were found to increase in extract treated groups which attributed for its insulinomimetic activity. The findings revealed that Citrullus colocynthis possess a very strong anti-hyperglycemic potential justifying the use of the drug for the treatment of diabetes mellitus.

Bioaccessibility and inhibitory effects on digestive enzymes of carnosic acid in sage and rosemary

In this study, the aim was to determine the bioaccessibilities of carnosic acid in sage and rosemary and in vitro inhibitory effects of these samples on lipid and starch digestive enzymes by evaluating the lipase, α-amylase and α-glucosidase enzyme inhibition activities. The content of carnosic acid in rosemary (18.72 ± 0.33 mg/g) was found to be higher than that content of that in sage (3.76 ± 0.13 mg/g) (p < 0.05). The carnosic acid bioaccessibilities were found as 45.10 ± 1.88% and 38.32 ± 0.21% in sage and rosemary, respectively. The tested sage and rosemary showed inhibitory activity against α-glucosidase (Concentration of inhibitor required to produce a 50% inhibition of the initial rate of reaction - IC50 88.49 ± 2.35, 76.80 ± 1.68 μg/mL, respectively), α-amylase (IC50 107.65 ± 12.64, 95.65 ± 2.73 μg/mL, respectively) and lipase (IC50 6.20 ± 0.63, 4.31 ± 0.62 μg/mL, respectively). Furthermore, to the best of our knowledge, this is the first work that carnosic acid standard equivalent inhibition capacities (CAEIC50) for these food samples were determined and these values were in agreement with the IC50 values. These results show that sage and rosemary are potent inhibitors of lipase, α-amylase and α-glucosidase digestive enzymes.

Identification of Bioactive Peptides with α-Amylase Inhibitory Potential from Enzymatic Protein Hydrolysates of Red Seaweed (Porphyra spp).

Inhibition of α-amylase enzyme is one therapeutic approach in lowering glucose level in the blood to manage diabetes mellitus. In this study α-amylase inhibitory peptides were identified from proteolytic enzymes hydrolysates of red seaweed laver ( Porphyra species) using consecutive chromatographic techniques. In the resultant fractions from RP-HPLC (D1-10), D2 inhibited α-amylase activity (88.67 ± 1.05%) significantly ( p ≤ 0.5) at 1 mg/mL protein concentration. A mass spectrometry (ESI-Q-TOF- MS) analysis was used to identify peptides from this fraction. Two novel peptides were identified as Gly-Gly-Ser-Lys and Glu-Leu-Ser. To validate their α-amylase inhibitory activity, these peptides were synthesized chemically. The peptides were demonstrated inhibitory activity at IC50 value: 2.58 ± 0.08 mM (Gly-Gly-Ser-Lys) and 2.62 ± 0.05 mM (Glu-Leu-Ser). The inhibitory kinetics revealed that these peptides exhibited noncompetitive binding mode. Thus, laver can be a potential source of novel ingredients in food and pharmaceuticals in diabetes mellitus management.

INHIBITORY EFFECT OF A STANDARDIZED HYDROETHANOLIC EXTRACT OF TERMINALIA ARJUNA BARK ON ALPHA-AMYLASE ENZYMEINHIBITORY EFFECT OF A STANDARDIZED HYDROETHANOLIC EXTRACT OF TERMINALIA ARJUNA BARK ON ALPHA-AMYLASE ENZYME

Objective: The present study was initiated to screen the hydroethanolic bark extract for α-amylase inhibitory activity and standardization of the Terminalia arjuna for polyphenolic phytochemicals using high-performance liquid chromatography-photo diode array (HPLC-PDA) method.Methods: The T. arjuna bark sample was extracted with ethanol: water (70:30 v/v) using Soxhlet extraction. A Dionex P680 HPLC system was used to acquire chromatograms. The screening of extract of T. arjuna bark has performed for in vitro α-amylase inhibitory assay. Each experiment was repeated 3 times. All values were expressed mean ± standard deviation.Results: The content of arjunetin, arjungenin, gallic acid, ellagic acid, and quercetin was 0.47, 8.22, 2.443, 7.901, and 3.20 mg/g, respectively, in a hydroethanolic extract of T. arjuna. The hydroethanolic extract of T. arjuna bark and acarbose has shown an inhibitory activity with an IC50 value 145.90 and 62.35 μg/mL, respectively.Conclusion: The hydroethanolic extract T. arjuna bark demonstrates α-amylase inhibitory activity due to a synergistic effect of the phytochemical constituents present in it. This study suggests that one of the mechanisms of this plant for antidiabetic activity is through the inhibition of α-amylase enzyme.

ANTIDIABETIC AND ANTIOXIDANT ACTIVITIES OF ETHANOLIC EXTRACT OF PIPER BETLE L. LEAVES IN CATFISH, CLARIAS GARIEPINUS

Objective: The present study was undertaken to assess the α-amylase inhibitory activity and antidiabetic experimental catfish model and antioxidant properties of Piper betle L. ethanolic (PBE) extract.Methods: The phytochemical analysis of PBE extract was performed. The PBE extract was tested for their inhibitory effect on the α-amylase assay, which compared to the control, acarbose. The absorbance was read at 540 nm using a spectrophotometer, and IC50 values were calculated. In this present investigation, diabetes mellitus was induced in catfish, Clarias gariepinus by epaxial musculature injection to glucose and standard drug, Metformin hydrochloride. After 24-h incubation, the treated fishes were dissected, and the blood, liver, tissue samples, and epaxial musculature regions were collected. In addition, the antioxidant properties of PBE were determined by 2,2-diphenyl-l-picrylhydrazyl (DPPH) radical scavenging and 2,2’-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) radical scavenging (ABTS) assays.Results: The phytochemical screening of PBE revealed the presence of alkaloid, flavonoids, tannins, phenol, glycosides, sterols, saponins, and quinines. Furthermore, the values of (μg/ml) 3.038 and 7.672 α-amylase enzyme inhibition were excellent activity when compared to the acarbose. Moreover, elevated the glucose level (mg/dl) was estimated in blood 1.9±0.35, liver 0.5±0.25, tissue 0.2±0.25, and epaxial musculature 0.8±0.2 after 24-h incubation. The antioxidant effect of maximum activity was found in PBE; IC50 values (μg/ml) of DPPH and ABTS were 9.362 and 6.606, respectively.Conclusions: These studies might be responsible for the P. betle L. that was used as the new source of antidiabetic and antioxidant agents.

Pharmacological potential of sulfated polygalactopyranosyl-fucopyranan from the brown seaweed Sargassum wightii

A sulfated polygalactopyranosyl-fucopyranan characterized as ∙∙∙∙ → 1)-α-Fucp-(2SO3−)-(3 → 1)-α-Fucp-(2SO3−)-(4 → 1)-β-Galp-(4 → 1)-β-Galp-(4 → ∙∙∙∙ was isolated from the brown seaweed Sargassum wightii and evaluated for pharmacological properties with reference to antioxidant, anti-inflammatory, antidiabetic, and antihypertensive activities using different in vitro models. The sulfated polygalactopyranosyl-fucopyranan displayed potential di(phenyl)-(2,4,6-trinitrophenyl) iminoazanium (DPPH), 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid (ABTS+) radical scavenging, and Fe2+ ion chelating activities (IC90 ~ 1 mg mL−1). The studied polysaccharide displayed higher anti-inflammatory selectivity towards inducive pro-inflammatory enzyme cyclooxygenase-2 (COX-2, IC90 1.13 mg mL−1) than constitutive cyclooxygenase-1 (COX-1, IC90 > 1.20 mg mL−1) resulting in greater selectivity index (IC90 COX-2/COX-1, 0.93) than synthetic non-steroidal anti-inflammatory drug aspirin (0.88) and also showed potent lipoxygenase-5 inhibition (LOX-5, IC90 1.02 mg mL−1). The studied polysaccharide displayed significantly higher (P < 0.05) antidiabetic properties compared to the antidiabetic agents acarbose and diprotein-A in terms of α-amylase (IC90 0.93 mg mL−1), α-glucosidase (IC90 1.48 mg mL−1), and dipeptidyl peptidase-4 (IC90 0.11 mg mL−1) enzyme inhibition potentials. The sulfated polygalactopyranosyl-fucopyranan also displayed potential antihypertensive activity with reference to angiotensin-converting enzyme-I inhibitory activity (IC90 0.2 mg mL−1). Extensive spectroscopic experiments in conjugation with monosaccharide compositional analysis attributed (1 → 3)-linked α-fucopyranose units in the polygalactofucan chain with C-2 sulfation and C-4 substituents as O-acetyl/O-methyl/(1 → 4)-linked β-galactopyranose. The previously undescribed sulfated polygalactopyranosyl-fucopyranan could function as a potential pharmacophore lead against inflammation, type 2 diabetics, hypertension and utilization as natural antioxidant.

Antidiabetic and nephroprotective potential of polyherbal self-fermented Ariṣṭa formulation: Evidence-based research

Background: Ayurvedic Ariṣṭa preparations hold an age-old heritage in the prevention and cure of metabolic disorders and associated complications. Aim: The aim of the study was to study the antidiabetic activity of a self-fermented Ariṣṭa preparation (DB-07) and its potential in preventing or curing diabetes-induced nephropathy in experimental models. Materials and Methods: Rats with Streptozotocin-induced diabetes were used for studying the various dose effects of DB-07 (2.5, 3, and 3.5 ml/kg/day) in preventive and therapeutic treatment schedules. Metformin (500 mg/kg) was used as a standard drug. Fasting blood glucose and biochemical parameters such as blood protein, urea, uric acid, and creatinine were accessed by various biochemical tests. In vitro α-amylase and α-glucosidase inhibition assay and 2-deoxy glucose uptake assay using rat L6 myotubes were studied for determining the antidiabetic mechanism of action. Results: A dose-dependent and statistically significant effect on lowering the fasting blood glucose level was observed in both preventive and therapeutic scheduled treatments. Treatment with DB-07 significantly reversed the altered biochemical parameters and the effects were comparable to metformin-treated rats. DB-07 exhibited concentration-dependent inhibition of both α-amylase and α-glucosidase enzymes with an IC50 values of 10.93 μg/ml and 8.73 μg/ml, respectively. DB-07 also showed glucose uptake potential (ca. 70% activity at 125 μg/ml) in differentiated L6 myotubes. Conclusions: These observations have revealed the antidiabetic and nephroprotective potential of DB-07. DB-07 can be a potential herbal alternative to maintain a healthy blood glucose level and will prove useful in diabetes-associated renal complications.