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  1. Fulltext Synthesis and α-Glucosidase Inhibition Activity of 2-[3-(Benzoyl/4-bromobenzoyl)-4-hydroxy-1,1-dioxido-2H-benzo[e][1,2]thiazin-2-yl]-N-arylacetamides: An In Silico and Biochemical Approach
    Saddique FA, Aslam S, Ahmad M, Ashfaq UA, Muddassar M, Sultan S, et al.
    Molecules, 2021 May 20;26(10).
    PMID: 34065194 DOI: 10.3390/molecules26103043
    Diabetes mellitus (DM) is a chronic disorder and has affected a large number of people worldwide. Insufficient insulin production causes an increase in blood glucose level that results in DM. To lower the blood glucose level, various drugs are employed that block the activity of the α-glucosidase enzyme, which is considered responsible for the breakdown of polysaccharides into monosaccharides leading to an increase in the intestinal blood glucose level. We have synthesized novel 2-(3-(benzoyl/4-bromobenzoyl)-4-hydroxy-1,1-dioxido-2H-benzo[e][1,2]thiazin-2-yl)-N-arylacetamides and have screened them for their in silico and in vitro α-glucosidase inhibition activity. The derivatives 11c, 12a, 12d, 12e, and 12g emerged as potent inhibitors of the α-glucosidase enzyme. These compounds exhibited good docking scores and excellent binding interactions with the selected residues (Asp203, Asp542, Asp327, His600, Arg526) during in silico screening. Similarly, these compounds also showed good in vitro α-glucosidase inhibitions with IC50 values of 30.65, 18.25, 20.76, 35.14, and 24.24 μM, respectively, which were better than the standard drug, acarbose (IC50 = 58.8 μM). Furthermore, a good agreement was observed between in silico and in vitro modes of study.
    Matched MeSH terms: Hypoglycemic Agents/chemistry
  2. Fulltext Investigation of α-Glucosidase Inhibitory Metabolites from Tetracera scandens Leaves by GC-MS Metabolite Profiling and Docking Studies
    Nokhala A, Siddiqui MJ, Ahmed QU, Ahamad Bustamam MS, Zakaria AZA
    Biomolecules, 2020 02 12;10(2).
    PMID: 32059529 DOI: 10.3390/biom10020287
    Stone leaf (Tetracera scandens) is a Southeast Asian medicinal plant that has been traditionally used for the management of diabetes mellitus. The underlying mechanisms of the antidiabetic activity have not been fully explored yet. Hence, this study aimed to evaluate the α-glucosidase inhibitory potential of the hydromethanolic extracts of T. scandens leaves and to characterize the metabolites responsible for such activity through gas chromatography-mass spectrometry (GC-MS) metabolomics. Crude hydromethanolic extracts of different strengths were prepared and in vitro assayed for α-glucosidase inhibition. GC-MS analysis was further carried out and the mass spectral data were correlated to the corresponding α-glucosidase inhibitory IC50 values via an orthogonal partial least squares (OPLS) model. The 100%, 80%, 60% and 40% methanol extracts displayed potent α-glucosidase inhibitory potentials. Moreover, the established model identified 16 metabolites to be responsible for the α-glucosidase inhibitory activity of T. scandens. The putative α-glucosidase inhibitory metabolites showed moderate to high affinities (binding energies of -5.9 to -9.8 kcal/mol) upon docking into the active site of Saccharomyces cerevisiae isomaltase. To sum up, an OPLS model was developed as a rapid method to characterize the α-glucosidase inhibitory metabolites existing in the hydromethanolic extracts of T. scandens leaves based on GC-MS metabolite profiling.
    Matched MeSH terms: Hypoglycemic Agents/chemistry
  3. α-glucosidase inhibitors isolated from Mimosa pudica L
    Tasnuva ST, Qamar UA, Ghafoor K, Sahena F, Jahurul MHA, Rukshana AH, et al.
    Nat Prod Res, 2019 May;33(10):1495-1499.
    PMID: 29281898 DOI: 10.1080/14786419.2017.1419224
    The aim of the study was to isolate digestive enzymes inhibitors from Mimosa pudica through a bioassay-guided fractionation approach. Repeated silica gel and sephadex LH 20 column chromatographies of bioactive fractions afforded stigmasterol, quercetin and avicularin as digestive enzymes inhibitors whose IC50 values as compared to acarbose (351.02 ± 1.46 μg mL-1) were found to be as 91.08 ± 1.54, 75.16 ± 0.92 and 481.7 ± 0.703 μg mL-1, respectively. In conclusion, M. pudica could be a good and safe source of digestive enzymes inhibitors for the management of diabetes in future.
    Matched MeSH terms: Hypoglycemic Agents/chemistry
  4. Fulltext Antidiabetic properties and mechanism of action of Gynura procumbens water extract in streptozotocin-induced diabetic rats
    Hassan Z, Yam MF, Ahmad M, Yusof AP
    Molecules, 2010;15(12):9008-23.
    PMID: 21150821 DOI: 10.3390/molecules15129008
    Gynura procumbens (Lour.) Merr (family Compositae) is cultivated in Southeast Asia, especially Indonesia, Malaysia and Thailand, for medicinal purposes. This study evaluated the in vivo hypoglycemic properties of the water extract of G. procumbens following 14 days of treatment and in vitro in RIN-5F cells. Glucose absorption from the intestines and its glucose uptake in abdominal skeletal muscle were assessed. The antidiabetic effect of water extract of G. procumbens leaves was investigated in streptozotocin-induced diabetic rats. The intraperitoneal glucose tolerance test (IPGTT) was performed in diabetic rats treated with G. procumbens water extract for 14 days. In the IPGTT, blood was collected for insulin and blood glucose measurement. After the IPGTT, the pancreases were collected for immunohistochemical study of β-cells of the islets of Langerhans. The possible antidiabetic mechanisms of G. procumbens were assessed through in vitro RIN-5F cell study, intestinal glucose absorption and glucose uptake by muscle. The results showed that G. procumbens significantly decreased blood glucose levels after 14 days of treatment and improved outcome of the IPGTT. However, G. procumbens did not show a significant effect on insulin level either in the in vivo test or the in vitro RIN-5F cell culture study. G. procumbens also showed minimal effects on β-cells of the islets of Langerhans in the pancreas. However, G. procumbens only significantly increased glucose uptake by muscle tissues. From the findings we can conclude that G. procumbens water extract exerted its hypoglycemic effect by promoting glucose uptake by muscles.
    Matched MeSH terms: Hypoglycemic Agents/chemistry*
  5. Fulltext Antihyperglycemic effect of orthosiphon stamineus benth leaves extract and its bioassay-guided fractions
    Mohamed EA, Mohamed AJ, Asmawi MZ, Sadikun A, Ebrika OS, Yam MF
    Molecules, 2011 May 04;16(5):3787-801.
    PMID: 21544041 DOI: 10.3390/molecules16053787
    Preliminary investigations were carried out to evaluate the antidiabetic effects of the leaves of O. stamineus extracted serially with solvents of increasing polarity (petroleum ether, chloroform, methanol and water); bioassay-guided purification of plant extracts using the subcutaneous glucose tolerance test (SbGTT) was also carried out. Only the chloroform extract, given at 1 g/kg body weight (b.w.), significantly reduced (P < 0.05) the blood glucose level of rats loaded subcutaneously with 150 mg/kg (b.w.) glucose. The active chloroform extract of O. stamineus was separated into five fractions using a dry flash column chromatography method. Out of the five fractions tested, only chloroform fraction 2 (Cƒ2), at the dose of 1 g/kg (b.w.) significantly inhibited (P < 0.05) blood glucose levels in SbGTT. Active Cƒ2 was split into two sub-fractions Cƒ2-A and Cƒ2-B, using a dry flash column chromatography method. The activities Cƒ2-A and Cƒ2-B were investigated using SbGTT, and the active sub-fraction was then further studied for anti-diabetic effects in a streptozotocin-induced diabetic rat model. The results clearly indicate that Cƒ2-B fraction exhibited a blood glucose lowering effect in fasted treated normal rats after glucose-loading of 150 mg/kg (b.w.). In the acute streptozotocin-induced diabetic rat model, Cƒ2-B did not exhibit a hypoglycemic effect on blood glucose levels up to 7 hours after treatment. Thus, it appears that Cƒ2-B functions similarly to metformin, which has no hypoglycemic effect but demonstrates an antihyperglycemic effect only in normogycemic models. The effect of Cƒ2-B may have no direct stimulatory effects on insulin secretion or on blood glucose levels in diabetic animal models. Verification of the active compound(s) within the active fraction (Cƒ2-B) indicated the presence of terpenoids and, flavonoids, including sinensitin.
    Matched MeSH terms: Hypoglycemic Agents/chemistry*
  6. Animal models and natural products to investigate in vivo and in vitro antidiabetic activity
    Hasan MM, Ahmed QU, Mat Soad SZ, Tunna TS
    Biomed Pharmacother, 2018 May;101:833-841.
    PMID: 29635892 DOI: 10.1016/j.biopha.2018.02.137
    Diabetes mellitus is a chronic disease which has high prevalence. The deficiency in insulin production or impaired insulin function is the underlying cause of this disease. Utilization of plant sources as a cure of diabetes has rich evidence in the history. Recently, the traditional medicinal plants have been investigated scientifically to understand the underlying mechanism behind antidiabetic potential. In this regard, a substantial number of in vivo and in vitro models have been introduced for investigating the bottom-line mechanism of the antidiabetic effect. A good number of methods have been reported to be used successfully to determine antidiabetic effects of plant extracts or isolated compounds. This review encompasses all the possible methods with a list of medicinal plants which may contribute to discovering a novel drug to treat diabetes more efficaciously with the minimum or no side effects.
    Matched MeSH terms: Hypoglycemic Agents/chemistry
  7. Fulltext Phytofabrication of Selenium Nanoparticles with Moringa oleifera (MO-SeNPs) and Exploring Its Antioxidant and Antidiabetic Potential
    Ahamad Tarmizi AA, Nik Ramli NN, Adam SH, Abdul Mutalib M, Mokhtar MH, Tang SGH
    Molecules, 2023 Jul 10;28(14).
    PMID: 37513196 DOI: 10.3390/molecules28145322
    The advancement in nanotechnology is the trigger for exploring the synthesis of selenium nanoparticles and their use in biomedicine. Therefore, this study aims to synthesize selenium nanoparticles using M. oleifera as a reducing agent and evaluate their antioxidant and antidiabetic potential. Our result demonstrated a change in the color of the mixture from yellow to red, and UV-Vis spectrometry of the suspension solution confirmed the formation of MO-SeNPs with a single absorbance peak in the range of 240-560 nm wavelength. FTIR analysis revealed several bioactive compounds, such as phenols and amines, that could possibly be responsible for the reduction and stabilization of the MO-SeNPs. FESEM + EDX analysis revealed that the amorphous MO-SeNPs are of high purity, have a spherical shape, and have a size of 20-250 nm in diameter, as determined by HRTEM. MO-SeNPs also exhibit the highest DPPH scavenging activity of 84% at 1000 μg/mL with an IC50 of 454.1 μg/mL and noteworthy reducing ability by reducing power assay. Furthermore, MO-SeNPs showed promising antidiabetic properties with dose-dependent inhibition of α-amylase (26.7% to 44.53%) and α-glucosidase enzyme (4.73% to 19.26%). Hence, these results demonstrated that M. oleifera plant extract possesses the potential to reduce selenium ions to SeNPs under optimized conditions with notable antioxidant and antidiabetic activities.
    Matched MeSH terms: Hypoglycemic Agents/chemistry
  8. Chemical constituents and medical benefits of Plantago major
    Adom MB, Taher M, Mutalabisin MF, Amri MS, Abdul Kudos MB, Wan Sulaiman MWA, et al.
    Biomed Pharmacother, 2017 Dec;96:348-360.
    PMID: 29028587 DOI: 10.1016/j.biopha.2017.09.152
    The medicinal benefits of Plantago major have been acknowledged around the world for hundreds of years. This plant contains a number of effective chemical constituents including flavonoids, alkaloids, terpenoids, phenolic acid derivatives, iridoid glycosides, fatty acids, polysaccharides and vitamins which contribute to its exerting specific therapeutic effects. Correspondingly, studies have found that Plantago major is effective as a wound healer, as well as an antiulcerative, antidiabetic, antidiarrhoeal, anti-inflammatory, antinociceptive, antibacterial, and antiviral agent. It also combats fatigue and cancer, is an antioxidant and a free radical scavenger. This paper provides a review of the medicinal benefits and chemical constituents of Plantago major published in journals from year 1937 to 2015 which are available from PubMed, ScienceDirect and Google Scholar.
    Matched MeSH terms: Hypoglycemic Agents/chemistry
  9. Synthesis, molecular docking and anti-diabetic studies of novel benzimidazole-pyrazoline hybrid molecules
    Ibraheem F, Ahmad M, Ashfaq UA, Aslam S, Khan ZA, Sultan S
    Pak J Pharm Sci, 2020 Mar;33(2(Supplementary)):847-854.
    PMID: 32863261
    Pyrazoline and benzimidazoles derivatives have been widely studied due to their potential applications in the medicinal field. In this research project, we have hybridized these two heterocyclic systems in the same molecule. A new series of compounds, 2-((3,5-diaryl-4,5-dihydro-1H-pyrazol-1-yl)methyl)-1H-benzo[d]imidazole (5a-i) were synthesized through a multistep reaction. In the first step, chalcones 3a-i were prepared by coupling of various acetophenones and benzaldehydes under alkaline conditions. These chalcones were cyclized with hydrazine hydrate to form a series of pyrazolines which were finally coupled with 2-chloromethyl-1H-benzimidazole to get a new series of titled hybrid molecules. The structures of these compounds were elucidated by spectral (1H NMR and 13C NMR) analysis. The anti-diabetic potential of these compounds was studied by screening them for their α-glucosidase inhibition activity. The SAR was established through molecular docking analysis. Compound 5d appeared as effective inhibitor with IC50 = 50.06μM as compared to reference drug (acarbose) having IC50 = 58.8μM.
    Matched MeSH terms: Hypoglycemic Agents/chemistry*
  10. alpha-Amylase inhibitory activity of some Malaysian plants used to treat diabetes; with particular reference to Phyllanthus amarus
    Ali H, Houghton PJ, Soumyanath A
    J Ethnopharmacol, 2006 Oct 11;107(3):449-55.
    PMID: 16678367
    Extracts of six selected Malaysian plants with a reputation of usefulness in treating diabetes were examined for alpha-amylase inhibition using an in vitro model. Inhibitory activity studied by two different protocols (with and without pre-incubation) showed that Phyllanthus amarus hexane extract had alpha-amylase inhibitory properties. Hexane and dichloromethane extracts of Anacardium occidentale, Lagerstroemia speciosa, Averrhoa bilimbiPithecellobium jiringa and Parkia speciosa were not active when tested without pre-incubation. Extraction and fractionation of Phyllanthus amarus hexane extract led to the isolation of dotriacontanyl docosanoate, triacontanol and a mixture of oleanolic acid and ursolic acid. Dotriacontanyl docosanoate and the mixture of oleanolic acid and ursolic acid are reported from this plant species for the first time. All compounds were tested in the alpha-amylase inhibition assay and the results revealed that the oleanolic acid and ursolic acid (2:1) mixture was a potent alpha-amylase inhibitor with IC(50)=2.01 microg/ml (4.41 microM) and that it contributes significantly to the alpha-amylase inhibition activity of the extract. Three pure pentacyclic triterpenoids, oleanolic acid, ursolic acid and lupeol were shown to inhibit alpha-amylase.
    Matched MeSH terms: Hypoglycemic Agents/chemistry
  11. Fulltext Anti-Diabetic Activity and Metabolic Changes Induced by Andrographis paniculata Plant Extract in Obese Diabetic Rats
    Akhtar MT, Bin Mohd Sarib MS, Ismail IS, Abas F, Ismail A, Lajis NH, et al.
    Molecules, 2016 Aug 09;21(8).
    PMID: 27517894 DOI: 10.3390/molecules21081026
    Andrographis paniculata is an annual herb and widely cultivated in Southeast Asian countries for its medicinal use. In recent investigations, A. paniculata was found to be effective against Type 1 diabetes mellitus (Type 1 DM). Here, we used a non-genetic out-bred Sprague-Dawley rat model to test the antidiabetic activity of A. paniculata against Type 2 diabetes mellitus (Type 2 DM). Proton Nuclear Magnetic Resonance (¹H-NMR) spectroscopy in combination with multivariate data analyses was used to evaluate the A. paniculata and metformin induced metabolic effects on the obese and obese-diabetic (obdb) rat models. Compared to the normal rats, high levels of creatinine, lactate, and allantoin were found in the urine of obese rats, whereas, obese-diabetic rats were marked by high glucose, choline and taurine levels, and low lactate, formate, creatinine, citrate, 2-oxoglutarate, succinate, dimethylamine, acetoacetate, acetate, allantoin and hippurate levels. Treatment of A. paniculata leaf water extract was found to be quite effective in restoring the disturbed metabolic profile of obdb rats back towards normal conditions. Thisstudy shows the anti-diabetic potential of A. paniculata plant extract and strengthens the idea of using this plant against the diabetes. Further classical genetic methods and state of the art molecular techniques could provide insights into the molecular mechanisms involved in the pathogenesis of diabetes mellitus and anti-diabetic effects of A. paniculata water extract.
    Matched MeSH terms: Hypoglycemic Agents/chemistry
  12. Fulltext Urinary metabolomics study on the protective role of Orthosiphon stamineus in Streptozotocin induced diabetes mellitus in rats via (1)H NMR spectroscopy
    Azam AA, Pariyani R, Ismail IS, Ismail A, Khatib A, Abas F, et al.
    BMC Complement Altern Med, 2017 May 25;17(1):278.
    PMID: 28545435 DOI: 10.1186/s12906-017-1777-1
    BACKGROUND: Orthosiphon stamineus (OS) is a herb known in ethnomedicine for treating diabetes mellitus (DM). In this study, a (1)H NMR based urine metabolomics tool has been used for the first time to identify the metabolic protective mechanism of OS in DM using Streptozotocin (STZ) induced experimental model in rats.

    METHODS: Four different solvent extracts of OS, namely aqueous, ethanolic, 50% aqueous ethanolic and methanolic, at a dose of 500 mg/kg body weight (bw) were orally administered for 14 days to diabetic rats induced via intraperitoneal injection of 60 mg/kg bw STZ. NMR metabolomics approach using pattern recognition combined with multivariate statistical analysis was applied in the rat urine to study the resulted metabolic perturbations.

    RESULTS: OS aqueous extract (OSAE) caused a reversal of DM comparable to that of 10 mg/kg bw glibenclamide. A total of 15 urinary metabolites, which levels changed significantly upon treatment were identified as the biomarkers of OSAE in diabetes. A systematic metabolic pathways analysis identified that OSAE contributed to the antidiabetic activity mainly through regulating the tricarboxylic acid cycle, glycolysis/gluconeogenesis, lipid and amino acid metabolism.

    CONCLUSIONS: The results of this study validated the ethnopharmacological use of OS in diabetes and unveiled the biochemical and metabolic mechanisms involved.

    Matched MeSH terms: Hypoglycemic Agents/chemistry
  13. 2-Furoic piperazide derivatives as promising drug candidates of type 2 diabetes and Alzheimer's diseases: In vitro and in silico studies
    Abbasi MA, Hassan M, Ur-Rehman A, Siddiqui SZ, Hussain G, Shah SAA, et al.
    Comput Biol Chem, 2018 Dec;77:72-86.
    PMID: 30245349 DOI: 10.1016/j.compbiolchem.2018.09.007
    The heterocyclic compounds have been extensively reported for their bioactivity potential. The current research work reports the synthesis of some new multi-functional derivatives of 2-furoic piperazide (1; 1-(2-furoyl)piperazine). The synthesis was initiated by reacting the starting compound 1 with 3,5-dichloro-2-hydroxybenzenesulfonyl chloride (2) in a basic, polar and protic medium to obtain the parent sulfonamide 3 which was then treated with different electrophiles, 4a-g, in a polar and aprotic medium to acquire the designed molecules, 5a-g. These convergent derivatives were evaluated for their inhibitory potential against α-glucosidase, acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes. Acarbose was used as a reference standard for α-glucosidase inhibition while eserine for AChE and BChE inhibition. Some of the synthesized compounds were identified as promising inhibitors of these three enzymes and their bioactivity potentials were also supported by molecular docking study. The most active compounds among the synthetic analogues might be helpful in drug discovery and development for the treatment of type 2 diabetes and Alzhiemer's diseases.
    Matched MeSH terms: Hypoglycemic Agents/chemistry
  14. Fulltext Chlorophytum borivilianum root extract maintains near normal blood glucose, insulin and lipid profile levels and prevents oxidative stress in the pancreas of streptozotocin-induced adult male diabetic rats
    Giribabu N, Kumar KE, Rekha SS, Muniandy S, Salleh N
    Int J Med Sci, 2014;11(11):1172-84.
    PMID: 25249786 DOI: 10.7150/ijms.9056
    The effect of C. borivilianum root on blood glucose, glycated hemoglobin (HbAIc), insulin and lipid profile levels in diabetes mellitus are not fully understood. This study therefore investigated the effect of C. borivilianum root on the above parameters and oxidative stress of the pancreas in diabetes.
    METHODS: C. borivilianum root aqueous extract (250 and 500 mg/kg/day) was administered to streptozotocin (STZ)-induced male diabetic rats for 28 days. Body weight, blood glucose, HbA1c, insulin, lipid profile levels and glucose homeostasis indices were determined. Histopathological changes and oxidative stress parameters i.e. lipid peroxidation (LPO) and antioxidant enzymes activity levels of the pancreas were investigated.
    RESULTS: C. borivilianum root extract treatment to diabetic rats maintained near normal body weight, blood glucose, HbA1c, lipid profile and insulin levels with higher HOMA-β cell functioning index, number of Islets/pancreas, number of β-cells/Islets however with lower HOMA-insulin resistance (IR) index as compared to non-treated diabetic rats. Negative correlations between serum insulin and blood glucose, HbA1c, triglyceride (TG) and total cholesterol (TC) levels were observed. C. borivilianum root extract administration prevented the increase in lipid peroxidation and the decrease in activity levels of superoxide dismutase (SOD), catalase (CAT) and glutathione peroxidase (GPx) with mild histopathological changes in the pancreas of diabetic rats.
    CONCLUSIONS: C. borivilianum root maintains near normal levels of these metabolites and prevented oxidative stress-induced damage to the pancreas in diabetes.
    KEYWORDS: Chlorophytum borivilianum; diabetes; glucose; lipid profile; oxidative stress.; pancreas
    Matched MeSH terms: Hypoglycemic Agents/chemistry
  15. Ion-pair vortex assisted liquid-liquid microextraction with back extraction coupled with high performance liquid chromatography-UV for the determination of metformin in plasma
    Alshishani A, Makahleh A, Yap HF, Gubartallah EA, Salhimi SM, Saad B
    Talanta, 2016 Dec 01;161:398-404.
    PMID: 27769423 DOI: 10.1016/j.talanta.2016.08.067
    A new sample preparation method, ion-pair vortex assisted liquid-liquid microextraction (VALLME-BE), for the determination of a highly polar anti-diabetic drug (metformin) in plasma sample was developed. The VALLME-BE was performed by diluting the plasma in borate buffer and extracted to 150µL 1-octanol containing 0.2M di-(2-ethylhexyl)phosphoric acid as intermediate phase. The drug was next back-extracted into 20µL of 0.075M HCl solution. The effects of pH, ion-pair concentration, type of organic solvent, volume of extraction phases, ionic strength, vortexing and centrifugation times on the extraction efficiency were investigated. The optimum conditions were at pH 9.3, 60s vortexing and 2min centrifugation. The microextract, contained metformin and buformin (internal standard), was directly injected into a HPLC unit using C1 column (250mm×4.6mm×10µm) and detected at 235nm. The method was validated and calibration curve was linear with r2>0.99 over the range of 20-2000µgL-1. The limits of detection and quantitation were 1.4 and 4.1µgL-1, respectively. The accuracy was within 94.8-108% of the nominal concentration. The relative standard deviation for inter- and intra-day precision was less than 10.8%. The method was conveniently applied for the determination of metformin in plasma samples.
    Matched MeSH terms: Hypoglycemic Agents/chemistry
  16. Reduction of postprandial blood glucose in healthy subjects by buns and flatbreads incorporated with fenugreek seed powder
    Robert SD, Ismail AA, Rosli WI
    Eur J Nutr, 2016 Oct;55(7):2275-80.
    PMID: 26358163 DOI: 10.1007/s00394-015-1037-4
    PURPOSE: This study aimed to determine whether fenugreek seed powder could reduce the glycemic response and glycemic index (GI) when added to buns and flatbreads.

    METHODS: In a randomised, controlled crossover trial, ten healthy human subjects (five men, five women) were given 50 g glucose (reference food, twice); buns (0 and 10 % fenugreek seed powder); and flatbreads (0 and 10 % fenugreek seed powder) on six different occasions. Finger prick capillary blood samples were collected at 0, 15, 30, 45, 60, 90 and 120 min after the start of the meal. The palatability of the test meals was scored using Likert scales.

    RESULTS: The incremental areas under the glucose curve value of buns and flatbreads with 10 % fenugreek (138 ± 17 mmol × min/L; 121 ± 16 mmol × min/L) were significantly lower than those of 0 % fenugreek bun and flatbreads (227 ± 15 mmol × min/L; 174 ± 14 mmol × min/L, P = <0.01). Adding 10 % fenugreek seed powder reduced the GI of buns from 82 ± 5 to 51 ± 7 (P 

    Matched MeSH terms: Hypoglycemic Agents/chemistry
  17. A facile ultrasonic-aided biosynthesis of ZnO nanoparticles using Vaccinium arctostaphylos L. leaf extract and its antidiabetic, antibacterial, and oxidative activity evaluation
    Bayrami A, Alioghli S, Rahim Pouran S, Habibi-Yangjeh A, Khataee A, Ramesh S
    Ultrason Sonochem, 2019 Jul;55:57-66.
    PMID: 31084791 DOI: 10.1016/j.ultsonch.2019.03.010
    The synthesis of nanoparticles often result in the generation of harmful chemical pollutants. As such, many researchers have focused on developing green processes, which include the biosynthesis. In this research, ZnO nanoparticles were prepared using the leaf extract of whortleberry (Vaccinium arctostaphylos L.) via a simple ultrasonic-assisted method. The morphology, crystal size and structure, surface, thermal, and optical properties of the bio-mediated ZnO sample (ZnOext) were analyzed and compared with that produced without incorporating the extract (ZnOchem). The ZnO samples were evaluated for their antidiabetic, antibacterial, as well as their sono- and photo-catalytic performances. Initially, the samples were intraperitoneal injected to alloxan-diabetic rats to examine their treatment efficiency in terms of effects on fasting blood glucose, insulin, cholesterol, high-density lipoprotein, and total triglyceride levels. The ZnOext showed significantly higher efficiency for improving the health status of alloxan-diabetic rats in contrast with other tested treatments, vis. ZnOchem, insulin, and only leaf extract. In addition, both the ZnO samples were assessed against gram-negative and gram-positive bacteria and through sono- and photo-catalytic processes for removing rhodamine B, respectively. The results of this study indicated that not only the ZnOext sample was pollution free, it also exhibited higher potentials for treating diabetic rats, bacterial decontamination, and also oxidative removal of organic compounds under the influences of ultrasound and UV irradiations when compared with ZnOchem sample.
    Matched MeSH terms: Hypoglycemic Agents/chemistry
  18. A comprehensive study on antidiabetic and antibacterial activities of ZnO nanoparticles biosynthesized using Silybum marianum L seed extract
    Mohammadi Arvanag F, Bayrami A, Habibi-Yangjeh A, Rahim Pouran S
    Mater Sci Eng C Mater Biol Appl, 2019 Apr;97:397-405.
    PMID: 30678925 DOI: 10.1016/j.msec.2018.12.058
    Green synthesis of ZnO nanoparticles (NPs) using the plants' extract and their potential application have driven a tremendous interest in recent years. This study reports a green microwave-assisted method for synthesis of ZnO NPs using Silybum marianum L. seed extract. Characteristics of the as-prepared sample was explored in terms of crystalline phase, morphology, composition, surface area, optical, and thermal properties. The particles of the biosynthesized sample (ZnO/extract) had smaller sizes than the chemically produced one (ZnO). The existence of biomolecules from Silybum marianum L seed extract linked to the ZnO/extract sample was approved by various analyses. The ZnO/extract sample was used for treating alloxan-induced diabetic rats and its efficiency was compared with ZnO, extract, and insulin treatments. For this purpose, the levels of blood glucose, insulin, total cholesterol, total triglyceride, and high-density lipoprotein were measured before and after treating with the studied treatment agents and compared with each other. Moreover, the antibacterial activities of both ZnO samples were investigated against E. coli to assess their potential antibacterial application. From the results, ZnO/extract NPs represented an outstanding performance in overcoming the diabetic disorders and good antibacterial activity against the studied bacteria.
    Matched MeSH terms: Hypoglycemic Agents/chemistry
  19. Fulltext Fabrication of Second Generation Smarter PLGA Based Nanocrystal Carriers for Improvement of Drug Delivery and Therapeutic Efficacy of Gliclazide in Type-2 Diabetes Rat Model
    Panda BP, Krishnamoorthy R, Bhattamisra SK, Shivashekaregowda NKH, Seng LB, Patnaik S
    Sci Rep, 2019 11 22;9(1):17331.
    PMID: 31758056 DOI: 10.1038/s41598-019-53996-4
    Drug delivery and therapeutic challenges of gliclazide, a BCS class II drug used in type 2 diabetes mellitus (T2DM) can be overcome by exploring smarter carriers of second-generation nanocrystals (SGNCs). A combined method of emulsion diffusion, high-pressure homogenization and solvent evaporation method were employed in the preparation of gliclazide loaded poly (D, L-lactide-co-glycolide) (PLGA) SGNCs. Taguchi experimental design was adopted in fabrication of Gliclazide SGNc using Gliclazide -PLGA ratio at 1:0.5, 1:0.75, 1:1 with stabilizer (Poloxamer-188, PEG 4000, HPMC E15 at 0.5, 0.75, 1% w/v). The formulated gliclazide of SGNCs were investigated for physicochemical properties, in vitro drug release, and in vivo performance studies using type-2 diabetes rat model. The formulation (SGNCF1) with Drug: PLGA 1: 0.5 ratio with 0.5% w/v Poloxamer-188 produced optimized gliclazide SGNCs. SGNCF1 showed spherical shape, small particle size (106.3 ± 2.69 nm), good zeta potential (-18.2 ± 1.30 mV), small PDI (0.222 ± 0.104) and high entrapment efficiency (86.27 ± 0.222%). The solubility, dissolution rate and bioavailability of gliclazide SGNCs were significantly improved compared to pure gliclazide. The findings emphasize gliclazide SGNCs produce faster release initially, followed by delayed release with improved bioavailability, facilitate efficient delivery of gliclazide in T2DM with better therapeutic effect.
    Matched MeSH terms: Hypoglycemic Agents/chemistry
  20. The physicochemical properties of geraniin, a potential antihyperglycemic agent
    Elendran S, Wang LW, Prankerd R, Palanisamy UD
    Pharm Biol, 2015;53(12):1719-26.
    PMID: 25853977 DOI: 10.3109/13880209.2014.1003356
    Natural products play a vital role in the discovery of leads for novel pharmacologically active drugs. Geraniin (GE) was identified as the major compound in the rind of Nephelium lappaceum L. (Sapindaceae), while ellagic and gallic acids have been shown to be its main metabolites. GE and its metabolites possess a range of bioactive properties including being an anti-infective, anticarcinogenic, antihyperglycemic, and antihypertensive.
    Matched MeSH terms: Hypoglycemic Agents/chemistry*
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