MyMedR

Enriched zinc oxide nanoparticles by Nasturtium officinale leaf extract: Joint ultrasound-microwave-facilitated synthesis, characterization, and implementation for diabetes control and bacterial inhibition

Bayrami A, Ghorbani E, Rahim Pouran S, Habibi-Yangjeh A, Khataee A, Bayrami M

Ultrason Sonochem, 2019 Nov;58:104613.

PMID: 31450359 DOI: 10.1016/j.ultsonch.2019.104613

The leaf extract of a medicinally important plant, watercress (Nasturtium officinale), was obtained through an ultrasound-facilitated method and utilized for the preparation of ZnO nanoparticles via a joint ultrasound-microwave assisted procedure. The characteristics of the extract enriched nanoparticles (Ext/ZnO) were determined by SEM, TEM, XRD, EDX, BET, FTIR, TGA, and UV-Vis DRS analyses and compared to that of ZnO prepared in the absence of the extract (ZnO). The presence of carbon and carbonaceous bonds, changes in the morphology, size, band gap energy, and weight-decay percentage were a number of differences between ZnO and Ext/ZnO that confirmed the link of extract over nanoparticles. Ext/ZnO, watercress leaf extract, ZnO, and insulin therapies were administrated to treat alloxan-diabetic Wister rats and their healing effectiveness results were compared to one another. The serum levels of the main diabetic indices such as insulin, fasting blood glucose, and lipid profile (total triglyceride, total cholesterol, and high-density lipoprotein cholesterol) were estimated for healthy, diabetic, and the rats rehabilitated with the studied therapeutic agents. The watercress extract-enriched ZnO nanoparticles offered the best performance and suppressed the diabetic status of rats. Moreover, both ZnO samples satisfactory inhibited the activities of Staphylococcus aureus and Escherichia coli bacteria. Based on the results, the application of Nasturtium officinale leaf extract can strongly empower ZnO nanoparticles towards superior antidiabetic and enhanced antibacterial activities.

Matched MeSH terms: Hypoglycemic Agents/chemistry

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

Fulltext Evaluation of antidiabetic and antioxidant properties of Brucea javanica seed

Ablat A, Mohamad J, Awang K, Shilpi JA, Arya A

ScientificWorldJournal, 2014;2014:786130.

PMID: 24688431 DOI: 10.1155/2014/786130

The ethanol extract of B. javanica seed was fractionated with solvents of different polarities and tested for antioxidant activities by several assays including DPPH radical scavenging activity, ferric reducing antioxidant power (FRAP), ferrous ion chelating activity (FCA), and nitric oxide radical scavenging activity (NORSA) along with their polyphenolic contents. Antidiabetic activity was evaluated both in vitro and in vivo using a glycogen phosphorylase α (GPα) inhibition assay and oral glucose tolerance test (OGTT) in nondiabetic rats. The ethyl acetate fraction (EAF), rich in tannin, exhibited the strongest antioxidant activities to DPPH, FRAP, and NORSA, except for FCA. The EAF also exerted a dose-depended inhibition of GPα (IC50 = 0.75 mg/ml). Further evaluation of hypoglycemic effect on OGGT indicated that rats treated with EAF (125 mg/kg bw) showed a 39.91% decrease (P < 0.05) in blood glucose levels at 30 min, and continuous fall (P < 0.05) of 28.89% and 20.29% was observed in the following hours (60 and 90 min) compared to the normal control during OGTT. The EAF was applied to polyamide column chromatography, and the resulting tannin-free fraction was tested for both GPα inhibition and antioxidant (DPPH only) activity. The GP α inhibitory activity was retained, while antioxidant activity was lost (4.6-fold) after tannin removal. These results concluded that the GPα inhibitory activity initially detected was primarily due to the compounds other than tannins, whereas antioxidant activity was mainly due to the tannins.

Matched MeSH terms: Hypoglycemic Agents/chemistry*

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

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

A QSAR model for predicting antidiabetic activity of dipeptidyl peptidase-IV inhibitors by enhanced binary gravitational search algorithm

Al-Fakih AM, Algamal ZY, Lee MH, Aziz M, Ali HTM

SAR QSAR Environ Res, 2019 Jun;30(6):403-416.

PMID: 31122062 DOI: 10.1080/1062936X.2019.1607899

Time-varying binary gravitational search algorithm (TVBGSA) is proposed for predicting antidiabetic activity of 134 dipeptidyl peptidase-IV (DPP-IV) inhibitors. To improve the performance of the binary gravitational search algorithm (BGSA) method, we propose a dynamic time-varying transfer function. A new control parameter,
μ
, is added in the original transfer function as a time-varying variable. The TVBGSA-based model was internally and externally validated based on

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, Y-randomization test, and applicability domain evaluation. The validation results indicate that the proposed TVBGSA model is robust and not due to chance correlation. The descriptor selection and prediction performance of TVBGSA outperform BGSA method. TVBGSA shows higher

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compared to obtained results by BGSA, indicating the best prediction performance of the proposed TVBGSA model. The results clearly reveal that the proposed TVBGSA method is useful for constructing reliable and robust QSARs for predicting antidiabetic activity of DPP-IV inhibitors prior to designing and experimental synthesizing of new DPP-IV inhibitors.

Matched MeSH terms: Hypoglycemic Agents/chemistry*

Effect of Ipomoea aquatica ethanolic extract in streptozotocin (STZ) induced diabetic rats via1H NMR-based metabolomics approach

Abu Bakar Sajak A, Mediani A, Maulidiani, Mohd Dom NS, Machap C, Hamid M, et al.

Phytomedicine, 2017 Dec 01;36:201-209.

PMID: 29157816 DOI: 10.1016/j.phymed.2017.10.011

BACKGROUND: Ipomoea aquatica (locally known as "kangkung") has previously been reported to have hypoglycemic activities on glucose level in diabetes patients. However, the effect of I. aquatica ethanolic extract on the metabolites in the body has remained unknown.

PURPOSE: This study provides new insights on the changes of endogenous metabolites caused by I. aquatica ethanolic extract and improves the understanding on the therapeutic efficacy and mechanism of I. aquatica ethanolic extract.

METHODS: By using a combination of 1H nuclear magnetic resonance (NMR) with multivariate analysis (MVDA), the changes of metabolites due to I. aquatica ethanolic extract administration in obese diabetic-induced Sprague Dawley rats (OB+STZ+IA) were identified.

RESULTS: The results suggested 19 potential biomarkers with variable importance projections (VIP) above 0.5, which include creatine/creatinine, glucose, creatinine, citrate, carnitine, 2-oxoglutarate, succinate, hippurate, leucine, 1-methylnicotinamice (MNA), taurine, 3-hydroxybutyrate (3-HB), tryptophan, lysine, trigonelline, allantoin, formiate, acetoacetate (AcAc) and dimethylamine. From the changes in the metabolites, the affected pathways and aspects of metabolism were identified.

CONCLUSION: I. aquatica ethanolic extract increases metabolite levels such as creatinine/creatine, carnitine, MNA, trigonelline, leucine, lysine, 3-HB and decreases metabolite levels, including glucose and tricarboxylic acid (TCA) intermediates. This implies capabilities of I. aquatica ethanolic extract promoting glycolysis, gut microbiota and nicotinate/nicotinamide metabolism, improving the glomerular filtration rate (GFR) and reducing the β-oxidation rate. However, the administration of I. aquatica ethanolic extract has several drawbacks, such as unimproved changes in amino acid metabolism, especially in reducing branched chain amino acid (BCAA) synthesis pathways and lipid metabolism.

Matched MeSH terms: Hypoglycemic Agents/chemistry

A potent alpha-glucosidase inhibitor from Myristica cinnamomea King

Sivasothy Y, Loo KY, Leong KH, Litaudon M, Awang K

Phytochemistry, 2016 Feb;122:265-269.

PMID: 26712615 DOI: 10.1016/j.phytochem.2015.12.007

A dimeric acylphenol and a potent α-glucosidase inhibitor, giganteone D (IC50 5.05μM), was isolated and characterized from the bark of Myristica cinnamomea King. The bark also yielded an acylphenol with an unprecedented skeleton for which the name cinnamomeone A (IC50 358.80μM) was proposed. Their structures were established by means of NMR and MS spectrometric analyses. The Lineweaver-Burk plot of giganteone D indicated that it was a mixed-type inhibitor. This is the first report on the α-glucosidase inhibiting potential of acylphenols.

Matched MeSH terms: Hypoglycemic Agents/chemistry

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*

Fulltext Comparative study of the antidiabetic potential of Paederia foetida twig extracts and compounds from two different locations in Malaysia

Tan DC, Idris KI, Kassim NK, Lim PC, Safinar Ismail I, Hamid M, et al.

Pharm Biol, 2019 Dec;57(1):345-354.

PMID: 31185767 DOI: 10.1080/13880209.2019.1610462

Context:Paederia foetida L. (Rubiaceae) is an edible plant distributed in Asian countries including Malaysia. Fresh leaves have been traditionally used as a remedy for indigestion and diarrhea. Several phytochemical studies of the leaves have been documented, but there are few reports on twigs. Objective: This study investigates the enzyme inhibition of P. foetida twig extracts and compound isolated from them. In addition, in silico molecular docking of scopoletin was investigated. Materials and methods: Plants were obtained from two locations in Malaysia, Johor (PFJ) and Pahang (PFP). Hexane, chloroform and methanol extracts along with isolated compound (scopoletin) were evaluated for their enzyme inhibition activities (10,000-0.000016 µg/mL). The separation and identification of bio-active compounds were carried out using column chromatography and spectroscopic techniques, respectively. In silico molecular docking of scopoletin with receptors (α-amylase and α-glucosidase) was carried out using AutoDock 4.2. Results: The IC50 values of α-amylase and α-glucosidase inhibition activity of PFJ chloroform extract were 9.60 and 245.6 µg/mL, respectively. PFP chloroform extract exhibited α-amylase and α-glucosidase inhibition activity (IC50 = 14.83 and 257.2 µg/mL, respectively). The α-amylase and α-glucosidase inhibitory activity of scopoletin from both locations had IC50 values of 0.052 and 0.057 µM, respectively. Discussion and conclusions: Separation of PFJ chloroform extract afforded scopoletin (1), stigmasterol (2) and γ-sitosterol (3) and the PFP chloroform extract yielded (1), (2), (3) and ergost-5-en-3-ol (4). Scopoletin was isolated from this species for the first time. In silico calculations gave a binding energy between scopoletin and α-amylase of -6.03 kcal/mol.

Matched MeSH terms: Hypoglycemic Agents/chemistry

Fulltext α-Amylase and dipeptidyl peptidase-4 (DPP-4) inhibitory effects of Melicope latifolia bark extracts and identification of bioactive constituents using in vitro and in silico approaches

Quek A, Kassim NK, Lim PC, Tan DC, Mohammad Latif MA, Ismail A, et al.

Pharm Biol, 2021 Dec;59(1):964-973.

PMID: 34347568 DOI: 10.1080/13880209.2021.1948065

CONTEXT: Melicope latifolia (DC.) T. G. Hartley (Rutaceae) was reported to contain various phytochemicals including coumarins, flavonoids, and acetophenones.

OBJECTIVE: This study investigates the antidiabetic and antioxidant effects of M. latifolia bark extracts, fractions, and isolated constituents.

MATERIALS AND METHODS: Melicope latifolia extracts (hexane, chloroform, and methanol), fractions, and isolated constituents with varying concentrations (0.078-10 mg/mL) were subjected to in vitro α-amylase and dipeptidyl peptidase-4 (DPP-4) inhibitory assay. Molecular docking was performed to study the binding mechanism of active compounds towards α-amylase and DPP-4 enzymes. The antioxidant activity of M. latifolia fractions and compounds were determined by 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging and β-carotene bleaching assays.

RESULTS: Melicope latifolia chloroform extract showed the highest antidiabetic activity (α-amylase IC50: 1464.32 μg/mL; DPP-4 IC50: 221.58 μg/mL). Fractionation of chloroform extract yielded four major fractions (CF1-CF4) whereby CF3 showed the highest antidiabetic activity (α-amylase IC50: 397.68 μg/mL; DPP-4 IC50: 37.16 μg/mL) and resulted in β-sitosterol (1), halfordin (2), methyl p-coumarate (3), and protocatechuic acid (4). Isolation of compounds 2-4 from the species and their DPP-4 inhibitory were reported for the first time. Compound 2 showed the highest α-amylase (IC50: 197.53 μM) and β-carotene (88.48%) inhibition, and formed the highest number of molecular interactions with critical amino acid residues of α-amylase. The highest DPP-4 inhibition was exhibited by compound 3 (IC50: 911.44 μM).

DISCUSSION AND CONCLUSIONS: The in vitro and in silico analyses indicated the potential of M. latifolia as an alternative source of α-amylase and DPP-4 inhibitors. Further pharmacological studies on the compounds are recommended.

Matched MeSH terms: Hypoglycemic Agents/chemistry

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*

Evaluation of in vitro antidiabetic and antioxidant characterizations of Elettaria cardamomum (L.) Maton (Zingiberaceae), Piper cubeba L. f. (Piperaceae), and Plumeria rubra L. (Apocynaceae)

Ahmed AS, Ahmed Q, Saxena AK, Jamal P

Pak J Pharm Sci, 2017 Jan;30(1):113-126.

PMID: 28603121

Inhibition of intestinal α-amylase and α-glucosidase is an important strategy to regulate diabetes mellitus (DM). Antioxidants from plants are widely regarded in the prevention of diabetes. Fruits of Elettaria cardamomum (L.) Maton (Zingiberaceae) and Piper cubeba L. f. (Piperaceae) and flowers of Plumeria rubra L. (Apocynaceae) are traditionally used to cure DM in different countries. However, the role of these plants has been grossly under reported and is yet to receive proper scientific evaluation with respect to understand their traditional role in the management of diabetes especially as digestive enzymes inhibitors. Hence, methanol and aqueous extracts of the aforementioned plants were evaluated for their in vitro α-glucosidase and α-amylase inhibition at 1 mg/mL and quantification of their antioxidant properties (DPPH, FRAP tests, total phenolic and total flavonoids contents). In vitro optimization studies for the extracts were also performed to enhance in vitro biological activities. The % inhibition of α-glucosidase by the aqueous extracts of the fruits of E. cardamomum, P. cubeba and flowers of P. rubra were 10.41 (0.03), 95.19 (0.01), and -2.92 (0.03), while the methanol extracts exhibited % inhibition 13.73 (0.02), 92.77 (0.01), and -0.98 (0.01), respectively. The % inhibition of α-amylase by the aqueous extracts were 82.99 (0.01), 64.35 (0.01), and 20.28 (0.02), while the methanol extracts displayed % inhibition 39.93 (0.01), 31.06 (0.02), and 39.40 (0.01), respectively. Aqueous extracts displayed good in vitro antidiabetic and antioxidant activities. Moreover, in vitro optimization experiments helped to increase the α-glucosidase inhibitory activity of E. cardamomum. Our findings further justify the traditional claims of these plants as folk medicines to manage diabetes, however, through digestive enzymes inhibition effect.

Matched MeSH terms: Hypoglycemic Agents/chemistry

Antidiabetic and antidyslipidemic potential of Echinops echinatus in rat models of type I and type II diabetes

Chaudhry SRY, Akram A, Aslam N, Wajid M, Iqbal Z, Nazir I, et al.

Pak J Pharm Sci, 2019 Mar;32(2):505-514.

PMID: 31081759

Echinops echinatus is traditionally an important plant that finds its extensive use as a diuretic, anti-inflammatory, anti-pyretic, nerve tonic, abortifacient, aphrodisiac, antiasthmatic, and antidiabetic agent. The current study investigates protection against the hyperglycemia and dyslipidemia in alloxan-induced (type I diabetes) and fructose-fed insulin resistance (type II diabetes) models of diabetes treated with aqueous methanolic root extract of E. echinatus (Ee.Cr). Albino rats were treated orally with Ee.Cr at doses 100, 300 and 500mg/kg. The fasting blood glucose was measured by glucometer, while standard kits were used to determine the levels of serum total cholesterol, triglycerides and HDL. The administration of Ee.Cr significantly (P<0.001) reduced the FBG concentration in a dose-dependent pattern in alloxan-induced and fructose-fed diabetic rats. The Ee.Cr also corrected the dyslipidemia associated with fructose and alloxan-induced diabetes by significantly (P<0.001) decreasing the concentration of serum total cholesterol, triglycerides, and LDL and by increasing HDL concentration. Ee.Cr also significantly (P<0.001) improved the glucose tolerance in fructose-fed rats. We conclude that Ee.Cr has antidiabetic and antidyslipidemic effects in both insulin-dependent alloxan-induced diabetes and fructose-induced insulin resistance diabetes rat models.

Matched MeSH terms: Hypoglycemic Agents/chemistry

Antihyperglycaemic effects of ethanol extracts of Carica papaya and Pandanus amaryfollius leaf in streptozotocin-induced diabetic mice

Sasidharan S, Sumathi V, Jegathambigai NR, Latha LY

Nat Prod Res, 2011 Dec;25(20):1982-7.

PMID: 21707251 DOI: 10.1080/14786419.2010.523703

Diabetes mellitus is a global disease that is increasing in an alarming rate. The present study was undertaken to study the antidiabetic effect of the ethanol extracts of Carica papaya and Pandanus amaryfollius on streptozotocin-induced diabetic mice. The results of the present study indicated that there was no significant difference in the body weight of the treated groups when compared to diabetic control. Whereas, there was significant (P

Matched MeSH terms: Hypoglycemic Agents/chemistry

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

Fulltext Computer aided screening of secreted frizzled-related protein 4 (SFRP4): a potential control for diabetes mellitus

Bukhari SA, Shamshari WA, Ur-Rahman M, Zia-Ul-Haq M, Jaafar HZ

Molecules, 2014 Jul 11;19(7):10129-36.

PMID: 25019556 DOI: 10.3390/molecules190710129

Diabetes mellitus is a life threatening disease and scientists are doing their best to find a cost effective and permanent treatment of this malady. The recent trend is to control the disease by target base inhibiting of enzymes or proteins. Secreted frizzled-related protein 4 (SFRP4) is found to cause five times more risk of diabetes when expressed above average levels. This study was therefore designed to analyze the SFRP4 and to find its potential inhibitors. SFRP4 was analyzed by bio-informatics tools of sequence tool and structure tool. A total of three potential inhibitors of SFRP4 were found, namely cyclothiazide, clopamide and perindopril. These inhibitors showed significant interactions with SFRP4 as compared to other inhibitors as well as control (acetohexamide). The findings suggest the possible treatment of diabetes mellitus type 2 by inhibiting the SFRP4 using the inhibitors cyclothiazide, clopamide and perindopril.

Matched MeSH terms: Hypoglycemic Agents/chemistry*

Fulltext Biological activities and phytochemicals of Swietenia macrophylla King

Moghadamtousi SZ, Goh BH, Chan CK, Shabab T, Kadir HA

Molecules, 2013 Aug 30;18(9):10465-83.

PMID: 23999722 DOI: 10.3390/molecules180910465

Swietenia macrophylla King (Meliaceae) is an endangered and medicinally important plant indigenous to tropical and subtropical regions of the World. S. macrophylla has been widely used in folk medicine to treat various diseases. The review reveals that limonoids and its derivatives are the major constituents of S. macrophylla. There are several data in the literature indicating a great variety of pharmacological activities of S. macrophylla, which exhibits antimicrobial, anti-inflammatory, antioxidant effects, antimutagenic, anticancer, antitumor and antidiabetic activities. Various other activities like anti-nociceptive, hypolipidemic, antidiarrhoeal, anti-infective, antiviral, antimalarial, acaricidal, antifeedant and heavy metal phytoremediation activity have also been reported. In view of the immense medicinal importance of S. macrophylla, this review aimed at compiling all currently available information on its ethnomedicinal uses, phytochemistry and biological activities of S. macrophylla, showing its importance.

Matched MeSH terms: Hypoglycemic Agents/chemistry

Fulltext Tropical plant extracts as potential antihyperglycemic agents

Manaharan T, Palanisamy UD, Ming CH

Molecules, 2012;17(5):5915-23.

PMID: 22609782 DOI: 10.3390/molecules17055915

Preliminary investigations on 14 plant extracts (obtained by ethanolic and aqueous extraction) identified those having high antioxidant and a significant total phenolic content. Antihyperglycemic, α-amylase and α-glucosidase inhibition activities were also observed. A correlation between the antihyperglycemic activity, total phenolic content and antioxidant (DPPH scavenging) activity was established. To further substantiate these findings, the possibility of tannins binding non-specifically to enzymes and thus contributing to the antihyperglycemic activity was also investigated. Our study clearly indicated that the antihyperglycemic activity observed in the plant extracts was indeed not due to non-specific tannin absorption.

Matched MeSH terms: Hypoglycemic Agents/chemistry

Fulltext In vitro anti-diabetic activities and chemical analysis of polypeptide-k and oil isolated from seeds of Momordica charantia (bitter gourd)

Ahmad Z, Zamhuri KF, Yaacob A, Siong CH, Selvarajah M, Ismail A, et al.

Molecules, 2012 Aug 10;17(8):9631-40.

PMID: 22885359 DOI: 10.3390/molecules17089631

The amino acid and fatty acid composition of polypeptide k and oil isolated from the seeds of Momordica charantia was analysed. The analysis revealed polypeptide k contained 9 out of 11 essential amino acids, among a total of 18 types of amino acids. Glutamic acid, aspartic acid, arginine and glycine were the most abundant (17.08%, 9.71%, 9.50% and 8.90% of total amino acids, respectively). Fatty acid analysis showed unusually high amounts of C18-0 (stearic acid, 62.31% of total fatty acid). C18-1 (oleic acid) and C18-2 (linoleic acid) were the other major fatty acid detected (12.53% and 10.40%, respectively). The oil was devoid of the short fatty acids (C4-0 to C8-0). Polypeptide k and oil were also subjected to in vitro α-glucosidase and α-amylase inhibition assays. Both polypeptide k and seed oil showed potent inhibition of α-glucosidase enzyme (79.18% and 53.55% inhibition, respectively). α-Amylase was inhibited by 35.58% and 38.02%, respectively. Collectively, the in vitro assay strongly suggests that both polypeptide k and seed oil from Momordica charantia are potent potential hypoglycemic agents.

Matched MeSH terms: Hypoglycemic Agents/chemistry

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