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  1. 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/isolation & purification; Hypoglycemic Agents/pharmacology*; Hypoglycemic Agents/chemistry
  2. Hollow fiber liquid-phase microextraction for the determination of trace amounts of rosiglitazone (anti-diabetic drug) in biological fluids using capillary electrophoresis and high performance liquid chromatographic methods
    Al Azzam KM, Makahleah A, Saad B, Mansor SM
    J Chromatogr A, 2010 Jun 4;1217(23):3654-9.
    PMID: 20409552 DOI: 10.1016/j.chroma.2010.03.055
    A three-phase hollow fiber liquid-phase microextraction (HF-LPME) coupled either with capillary electrophoresis (CE) or high performance liquid chromatography (HPLC) with UV detection methods was successfully developed for the determination of trace levels of the anti-diabetic drug, rosiglitazone (ROSI) in biological fluids. The analyte was extracted into dihexyl ether that was immobilized in the wall pores of a porous hollow fiber from 10 mL of aqueous sample, pH 9.5 (donor phase), and was back extracted into the acceptor phase that contained 0.1M HCl located in the lumen of the hollow fiber. Parameters affecting the extraction process such as type of extraction solvent, HCl concentration, donor phase pH, extraction time, stirring speed, and salt addition were studied and optimized. Under the optimized conditions (extraction solvent, dihexyl ether; donor phase pH, 9.5; acceptor phase, 0.1M HCl; stirring speed, 600 rpm; extraction time, 30 min; without addition of salt), enrichment factor of 280 was obtained. Good linearity and correlation coefficients of the analyte was obtained over the concentration ranges of 1.0-500 and 5.0-500 ng mL(-1) for the HPLC (r(2)=0.9988) and CE (r(2)=0.9967) methods, respectively. The limits of detection (LOD) and limits of quantitation (LOQ) for the HPLC and CE methods were (0.18, 2.83) and (0.56, 5.00) ng mL(-1), respectively. The percent relative standard deviation (n=6) for the extraction and determination of three concentration levels (10, 250, 500 ng mL(-1)) of ROSI using the HPLC and CE methods were less than 10.9% and 13.2%, respectively. The developed methods are simple, rapid, sensitive and are suitable for the determination of trace amounts of ROSI in biological fluids.
    Matched MeSH terms: Hypoglycemic Agents/analysis*; Hypoglycemic Agents/blood; Hypoglycemic Agents/urine
  3. Chitosan and its use in design of insulin delivery system
    Wong TW
    Recent Pat Drug Deliv Formul, 2009 Jan;3(1):8-25.
    PMID: 19149726 DOI: 10.2174/187221109787158346
    The global burden of diabetes is estimated to escalate from about 171 million in 2000 to 366 million people in 2030. The routine of diabetes treatment by injection of insulin incurs pain and has been one major factor negating the quality of life of diabetic patients. The possibility of administering insulin via alternative routes such as oral and nasal pathways has been investigated over the years, but with insulin experiencing risks of enzymatic degradation and poor transmucosal absorption. This leads to the rising needs to develop new formulation strategies emphasizing on the assembly of insulin and excipients into a physical structure to maintain the stability and increase the bioavailability of insulin. Chitosan and its derivatives or salts have been widely investigated as functional excipients of delivering insulin via oral, nasal and transdermal routes. The overview of various recent patented strategies on non-injection insulin delivery denotes the significance of chitosan for its mucoadhesive and able to protect the insulin from enzymatic degradation, prolong the retention time of insulin, as well as, open the inter-epithelial tight junction to facilitate systemic insulin transport. The chitosan can be employed to strengthen the physicochemical stability of insulin and multi-particulate matrix. The introduction of chitosan coat or co-formulation of chitosan with cationic gelatin or electrolytes which provide solidified or partially crosslinked structures retain and/or enhance the positive charges of dosage form necessary to induce mucoadhesiveness. The chitosan is modifiable chemically to produce water-soluble low molecular weight polymer which renders insulin able to be processed under mild conditions, and sulphated chitosan which markedly opens the paracellular channels for insulin transport. Combination of chitosan and fatty acid as hydrophobic nanoparticles promotes the insulin absorption via lymphoid tissue. Attainment of optimized formulations with higher levels of pharmacological bioavailability is deemed possible in future through targeted delivery of insulin using chitosan with specific adhesiveness to the intended absorption mucosa.
    Matched MeSH terms: Hypoglycemic Agents/administration & dosage*; Hypoglycemic Agents/adverse effects; Hypoglycemic Agents/pharmacokinetics
  4. Method development and validation of repaglinide in human plasma by HPLC and its application in pharmacokinetic studies
    Ruzilawati AB, Wahab MS, Imran A, Ismail Z, Gan SH
    J Pharm Biomed Anal, 2007 Apr 11;43(5):1831-5.
    PMID: 17240100
    In this study, the development and validation of a high-performance liquid chromatography (HPLC) assay for determination of repaglinide concentration in human plasma for pharmacokinetic studies is described. Plasma samples containing repaglinide and an internal standard, indomethacin were extracted with ethylacetate at pH 7.4. The recovery of repaglinide was 92%+/-55.31. Chromatographic separations were performed on Purospher STAR C-18 analytical column (4.8 mm x 150 mm; 5 microm particle size). The mobile phase composed of acetonitrile-ammonium formate (pH 2.7; 0.01 M) (60:40, v/v). The flow rate was 1 ml/min. The retention time for repaglinide and indomethacin were approximately 6.2 and 5.3 min, respectively. Calibration curves of repaglinide were linear in the concentration range of 20-200 ng/ml in plasma. The limits of detection and quantification were 10 ng/ml and 20 ng/ml, respectively. The inter-day precision was from 5.21 to 11.84% and the intra-day precision ranged from 3.90 to 6.67%. The inter-day accuracy ranged 89.95 to 105.75% and intra-day accuracy ranged from 92.37 to 104.66%. This method was applied to determine repaglinide concentration in human plasma samples for a pharmacokinetic study.
    Matched MeSH terms: Hypoglycemic Agents/blood*; Hypoglycemic Agents/pharmacokinetics*; Hypoglycemic Agents/chemistry
  5. α-Glucosidase inhibitors: consistency of in silico docking data with in vitro inhibitory data and inhibitory effect prediction of quercetin derivatives
    Zhu J, Zhang B, Tan C, Huang Q
    Food Funct, 2019 Sep 13.
    PMID: 31517355 DOI: 10.1039/c9fo01333d
    The present study aims to investigate the relationship between in silico experimental data and in vitro inhibitory data of polyphenols against α-glucosidase. The CDOCKER protocol in Discovery Studio was used to dock various polyphenols to the Saccharomyces cerevisiae α-glucosidase crystal structure. -CDOCKER energy values and the energy gap between the highest occupied molecular orbital energy and the lowest unoccupied molecular orbital energy were used to study its consistency with in vitro inhibitory data. The results showed that the correlation trend was trustworthy regardless of the data deviation and low correlation coefficient. Despite slight disagreements with some specific polyphenols, the docking data generally explained the effect of the groups (-OH, glycosyl, galloyl, and caffeoyl). The docking results showed that compound 7, a quercetin derivative, can be recommended as a lead antidiabetic compound, with additional anti-obesity effects. Galloyl and caffeoyl moieties are favorable to develop novel αG inhibitors.
    Matched MeSH terms: Hypoglycemic Agents
  6. Exploring antidiabetic potential of adamantyl-thiosemicarbazones via aldose reductase (ALR2) inhibition
    Shehzad MT, Hameed A, Al-Rashida M, Imran A, Uroos M, Asari A, et al.
    Bioorg Chem, 2019 11;92:103244.
    PMID: 31541804 DOI: 10.1016/j.bioorg.2019.103244
    The role of aldose reductase (ALR2) in diabetes mellitus is well-established. Our interest in finding ALR2 inhibitors led us to explore the inhibitory potential of new thiosemicarbazones. In this study, we have synthesized adamantyl-thiosemicarbazones and screened them as aldehyde reductase (ALR1) and aldose reductase (ALR2) inhibitors. The compounds bearing phenyl 3a, 2-methylphenyl 3g and 2,6-dimethylphenyl 3m have been identified as most potent ALR2 inhibitors with IC50 values of 3.99 ± 0.38, 3.55 ± 0.26 and 1.37 ± 0.92 µM, respectively, compared with sorbinil (IC50 = 3.14 ± 0.02 μM). The compounds 3a, 3g, and 3m also inhibit ALR1 with IC50 value of 7.75 ± 0.28, 7.26 ± 0.39 and 7.04 ± 2.23 µM, respectively. Molecular docking was also performed for putative binding of potent inhibitors with target enzyme ALR2. The most potent 2,6-dimethylphenyl bearing thiosemicarbazone 3m (IC50 = 1.37 ± 0.92 µM for ALR2) and other two compound 3a and 3g could potentially lead for the development of new therapeutic agents.
    Matched MeSH terms: Hypoglycemic Agents/chemical synthesis*; Hypoglycemic Agents/pharmacology; Hypoglycemic Agents/chemistry
  7. Benzoxazinone-thiosemicarbazones as antidiabetic leads via aldose reductase inhibition: Synthesis, biological screening and molecular docking study
    Shehzad MT, Imran A, Njateng GSS, Hameed A, Islam M, Al-Rashida M, et al.
    Bioorg Chem, 2019 06;87:857-866.
    PMID: 30551808 DOI: 10.1016/j.bioorg.2018.12.006
    Aldose reductase is an important enzyme in the polyol pathway, where glucose is converted to fructose, and sorbitol is released. Aldose reductase activity increases in diabetes as the glucose levels increase, resulting in increased sorbitol production. Sorbitol, being less cell permeable tends to accumulate in tissues such as eye lenses, peripheral nerves and glomerulus that are not insulin sensitive. This excessive build-up of sorbitol is responsible for diabetes associated complications such as retinopathy and neuropathy. In continuation of our interest to design and discover potent inhibitors of aldo-keto reductases (AKRs; aldehyde reductase ALR1 or AKR1A, and aldose reductase ALR2 or AKR1B), herein we designed and investigated a series of new benzoxazinone-thiosemicarbazones (3a-r) as ALR2 and ALR1 inhibitors. Most compounds exhibited excellent inhibitory activities with IC50 values in lower micro-molar range. Compounds 3b and 3l were found to be most active ALR2 inhibitors with IC50 values of 0.52 ± 0.04 and 0.19 ± 0.03 μM, respectively, both compounds were more effective inhibitors as compared to the standard ALR2 inhibitor (sorbinil, with IC50 value of 3.14 ± 0.02 μM).
    Matched MeSH terms: Hypoglycemic Agents/chemical synthesis; Hypoglycemic Agents/pharmacology*; Hypoglycemic Agents/chemistry
  8. Fulltext Anti-diabetic activity and microbial quality of ready-to-serve Momordica charantia (MC) drink
    Chern, Pei Ern, Nor Ainy Mahyudin, Hazrina Ghazali, Norkhaizura Mahmud @ Ab Rashid
    The Pertanika Journal of Scholarly Research Reviews, 2017;3(3):102-106.
    MyJurnal
    Diabetes mellitus has a high prevalence in Malaysia and is expected to rise in the future due to lifestyle changes. Thus, consumers are turning to alternative methods in the prevention and cure of the disease. The Momordica charantia has been studied for its anti-diabetic activity both in vitro and in vivo and is shown to be effective in inhibiting glucose absorption. Therefore, the MC is used as a main ingredient in the development of health beverages to offer alternatives for patients or the health conscious. The microbial quality of the product is examined to ensure the safety of the product and to find methods to enhance its shelf life.
    Matched MeSH terms: Hypoglycemic Agents
  9. Fulltext Defining Disease Progression and Drug Durability in Type 2 Diabetes Mellitus
    Kalra S, Kamaruddin NA, Visvanathan J, Santani R
    Eur Endocrinol, 2019 Aug;15(2):67-69.
    PMID: 31616495 DOI: 10.17925/EE.2019.15.2.67
    This communication shares insights into the definition of disease progression and drug durability in type 2 diabetes. Disease progression may be defined as gradual worsening of beta-cell function, clinically observed as an increase in drug dosage, drug frequency or number of glucose lowering drugs needed to maintain HbA1c control; and/or a ≥0.5% rise in HbA1c, unexplained by acute, modifiable factors, while using the same drug regimen; and/or as the occurrence or worsening of cardiovascular or microvascular complications, in spite of standard care, over a pre-specified time period. Durability of a drug or a drug combination may be defined as its ability to postpone or delay progression of disease, in a safe and well tolerated manner. Thus, all drugs that are able to prevent disease progression (i.e., postpone loss of glycaemic control, need for intensification of therapy or onset or worsening of complications) may be termed 'durable'.
    Matched MeSH terms: Hypoglycemic Agents
  10. Metabolic Control of Type 2 Diabetes by Targeting the GLUT4 Glucose Transporter: Intervention Approaches
    Alam F, Islam MA, Khalil MI, Gan SH
    Curr Pharm Des, 2016;22(20):3034-49.
    PMID: 26951104 DOI: 10.2174/1381612822666160307145801
    Type 2 diabetes mellitus (T2DM), the most common form of diabetes, is characterized by insulin resistance in the hepatic and peripheral tissues. Glucose transporter 4 (GLUT4) plays a major role in the pathophysiology of T2DM. Its defective expression or translocation to the peripheral cell plasma membrane in T2DM patients hinders the entrance of glucose into the cell for energy production. In addition to suitable drugs, an appropriate diet and/or exercise can be implemented to target the increase in GLUT4 expression, GLUT4 concentrations and GLUT4 translocation to the cell surface when managing the glucose metabolism of T2DM patients. In this review, we discussed successful intervention strategies that were individually administered or coupled with diet and/or exercise and affected the expression and translocation of GLUT4 in T2DM while reducing the excess glucose load from the blood. Additionally, some potentially good synthetic and natural compounds, which can activate the insulin-independent GLUT4 signaling pathways for the efficient management of T2DM, are highlighted as possible targets or emerging alternative sources for future anti-diabetic drug development.
    Matched MeSH terms: Hypoglycemic Agents/pharmacology; Hypoglycemic Agents/therapeutic use*; Hypoglycemic Agents/chemistry
  11. Antidiabetic effect of Ardisia elliptica extract and its mechanisms of action in STZ-NA-induced diabetic rat model via 1H-NMR-based metabolomics
    Wong PL, Zolkeflee NKZ, Ramli NS, Tan CP, Azlan A, Tham CL, et al.
    J Ethnopharmacol, 2024 Jan 10;318(Pt B):117015.
    PMID: 37572932 DOI: 10.1016/j.jep.2023.117015
    ETHNOPHARMACOLOGICAL RELEVANCE: Ardisia elliptica Thunb. (AE) (Primulaceae) is a medicinal plant found in the Malay Peninsula and has been traditionally used to treat diabetes. However, limited studies to date in providing scientific evidence to support the antidiabetic efficacy of this plant by in-vitro and in-vivo models.

    AIM OF THE STUDY: To investigate the anti-hyperglycemic potential of AE through in-vitro enzymatic activities and streptozotocin-nicotinamide (STZ-NA) induced diabetic rat models using proton-nuclear magnetic resonance (1H-NMR)-based metabolomics approach.

    MATERIALS AND METHODS: Anti-α-amylase and anti-α-glucosidase activities of the hydroethanolic extracts of AE were evaluated. The absolute quantification of bioactive constituents, using ultra-high performance liquid chromatography (UHPLC) was performed for the most active extract. Three different dosage levels of the AE extract were orally administered for 4 weeks consecutively in STZ-NA induced diabetic rats. Physical assessments, biochemical analysis, and an untargeted 1H-NMR-based metabolomics analysis of the urine and serum were carried out on the animal model.

    RESULTS: Type 2 diabetes mellitus (T2DM) rat model was successfully developed based on the clear separation observed between the STZ-NA induced diabetic and normal non-diabetic groups. Discriminating biomarkers included glucose, citrate, succinate, allantoin, hippurate, 2-oxoglutarate, and 3-hydroxybutyrate, as determined through an orthogonal partial least squares-discriminant analysis (OPLS-DA) model. A treatment dosage of 250 mg/kg body weight (BW) of standardized 70% ethanolic AE extract mitigated increase in serum glucose, creatinine, and urea levels, providing treatment levels comparable to that obtained using metformin, with flavonoids primarily contribute to the anti-hyperglycemic activities. Urinary metabolomics disclosed that the following disturbed metabolism pathways: the citrate cycle (TCA cycle), butanoate metabolism, glycolysis and gluconeogenesis, pyruvate metabolism, and synthesis and degradation of ketone bodies, were ameliorated after treatment with the standardized AE extract.

    CONCLUSIONS: This study demonstrated the first attempt at revealing the therapeutic effect of oral treatment with 250 mg/kg BW of standardized AE extract on chemically induced T2DM rats. The present study provides scientific evidence supporting the ethnomedicinal use of Ardisia elliptica and further advances the understanding of the fundamental molecular mechanisms affected by this herbal antidote.

    Matched MeSH terms: Hypoglycemic Agents/pharmacology; Hypoglycemic Agents/therapeutic use; Hypoglycemic Agents/chemistry
  12. In Silico Exploration of Isoxazole Derivatives of Usnic Acid: Novel Therapeutic Prospects Against α-Amylase for Diabetes Treatment
    Roney M, Issahaku AR, Huq AKMM, Sapari S, Abdul Razak FI, Wilhelm A, et al.
    Cell Biochem Biophys, 2024 Dec;82(4):3351-3366.
    PMID: 39020086 DOI: 10.1007/s12013-024-01419-1
    Diabetes mellitus (DM) a metabolic disorder characterized by high blood sugar levels causing damage to various organs over time. Current anti-diabetic drugs have limitations and side effects, prompting a search for new inhibitors targeting the α-amylase enzyme. This study aims to discover such inhibitors from thirty isoxazole derivatives of usnic acid using in silico approaches. The potential inhibitory effects of compounds were investigated using ADMET, molecular docking, molecular dynamic simulation, principal component analysis and density functional theory studies. ADMET analysis exhibited a wide range of physicochemical, pharmacokinetic, and drug-like qualities with no significant side effects which were then investigated using molecular docking experiment to determine the lead compound with the best binding affinity for the α-amylase enzyme. All compounds showed good binding affinity against α-amylase enzyme (-7.9 to -9.2 kcal/mol) where compound-13 showed the best binding affinity of -9.2 kcal/mol forming hydrogen bonds with Leu162, Tyr62, Glu233 and Asp300 amino acids. Furthermore, the binding posture and the stability of the compound-13-α-amylase enzyme complex was confirmed by molecular dynamic simulation experiment. Moreover, compound-13 showed binding energy value of -27.92 ± 5.61 kcal/mol, which indicated it could be an α-amylase inhibitor. Additionally, the reactivity of compound-13 was further confirmed by density functional theory analysis. The above findings suggest compound-13 to be a potential α-amylase inhibitor in DM. And setting the stage for further in vitro and in vivo experimental validation.
    Matched MeSH terms: Hypoglycemic Agents/pharmacology; Hypoglycemic Agents/therapeutic use; Hypoglycemic Agents/chemistry
  13. Unveiling the Biological Activities, Pharmacological Potential, and Health Benefits of Sorbifolin: A Comprehensive Review
    Belmehdi O, Mssillou I, Khalid A, Abdalla AN, Almalki M, Alqurashi RS, et al.
    Chem Biodivers, 2025 Feb;22(2):e202401463.
    PMID: 39402872 DOI: 10.1002/cbdv.202401463
    Bioactive phytochemicals act as important factors with preventive and therapeutic potential in the pathogenesis of several disorders, often related to oxidative stress. Many dietary plant secondary metabolites could lower these conditions. Sorbifolin is one of these metabolites. This work is the first review of sorbifolin, a flavone detected in various plant matrices as a major compound. The present study discussed the natural sources, extraction, purification, quantification, and assessment of the biological activities of sorbifolin. Several databases including Google Scholar, Web of Sciences, and Science-Direct were consulted for relevant English articles related to sorbifolin, the phytochemical profiles of several medicinal plants containing this compound, and its biological activities, such as antioxidant, anticancer, antimicrobial, anti-inflammatory, and antidiabetic. The positive in vitro and in silico outcomes reported in the literature should be followed by additional in vivo and clinical investigations to further research the mechanisms of action, pharmacokinetic/pharmacodynamic activities, toxicological effects, pharmacological properties, and therapeutic potential of sorbifolin.
    Matched MeSH terms: Hypoglycemic Agents/isolation & purification; Hypoglycemic Agents/pharmacology; Hypoglycemic Agents/chemistry
  14. Sequential hollow-fiber liquid phase microextraction for the determination of rosiglitazone and metformin hydrochloride (anti-diabetic drugs) in biological fluids
    Ben-Hander GM, Makahleh A, Saad B, Saleh MI, Cheng KW
    Talanta, 2015 Jan;131:590-6.
    PMID: 25281145 DOI: 10.1016/j.talanta.2014.08.037
    A new analytical method for the simultaneous determination of the antidiabetic drugs rosiglitazone (ROS) and metformin hydrochloride (MH) with marked differences in their affinity towards organic solvents (log P of 2.4 and -1.43, respectively) was developed. Prior to the HPLC separation, the drugs were subjected to a sequential hollow fiber liquid phase microextraction (HF-LPME) procedure. Two sequential HF-LPME approaches were considered, the preferred one involves the use of two vials containing solution mixtures for the extraction of ROS (vial 1) and MH (vial 2), respectively, but using the same fiber and acceptor phase. Important parameters that affect the extraction efficiency such as extracting solvent, donor phase conditions, HCl concentration, agitation, extraction time, addition of salt, etc. were studied. Under the optimum conditions, good enrichment factors (EF, 471 and 86.6 for ROS and MH, respectively) were achieved. Calibration curves were linear over the range 1-500 (r(2)=0.998) and 5-2500 ng mL(-1) (r(2)=0.999) for ROS and MH, respectively. The relative standard deviation values (RSD%) for six replicates were below 8.4%. Detection and quantitation limits based on S/N ratio of 3 and 10 were 0.12, 1.0 and 0.36, 3.0 ng mL(-1) for ROS and MH, respectively. The proposed method is simple, sensitive and opens up new opportunities for the microextraction of analytes with contrasting properties.
    Matched MeSH terms: Hypoglycemic Agents/blood; Hypoglycemic Agents/urine
  15. Chemical compositions and antioxidative and antidiabetic properties of underutilized vegetable palm hearts from Plectocomiopsis geminiflora and Eugeissona insignis
    Ahmad Aufa Z, Hassan FA, Ismail A, Mohd Yusof BN, Hamid M
    J Agric Food Chem, 2014 Mar 5;62(9):2077-84.
    PMID: 24499380 DOI: 10.1021/jf403481p
    Underutilized vegetables are currently studied not only for their nutrient values but also for their health-promoting components for protection against chronic diseases. The present study was performed to evaluate chemical compositions and antioxidant properties of underutilized vegetable palm hearts, namely, lalis (Plectocomiopsis geminiflora) and pantu (Eugeissona insignis). Additionally, the vegetable extracts were evaluated for their activities in the inhibition of digestive enzymes and effects on insulin secretion using BRIN BD11 pancreatic cell lines. Both vegetables contain valuable sources of dietary fiber, potassium, and zinc. For the first time, the phenolic compounds of the vegetables were identified and quantified using HPLC-DAD and LC-ESI-MS. Appreciable amounts of chlorogenic acid were found in the studied vegetables. The sample extracts exhibited potential antioxidant capacities through chemical and biological in vitro assays. High inhibition of α-amylase activity (>50%) was found from the extracts. Thus, it was suggested the vegetable consumption could fulfill the nutrient requirements among local communities.
    Matched MeSH terms: Hypoglycemic Agents/pharmacology; Hypoglycemic Agents/chemistry*
  16. 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/pharmacology*; Hypoglycemic Agents/chemistry
  17. 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/therapeutic use*; Hypoglycemic Agents/chemistry*
  18. Population pharmacokinetic modelling of repaglinide in healthy volunteers by using Non-Parametric Adaptive Grid Algorithm
    Ruzilawati AB, Mohd Suhaimi AW, Gan SH
    J Clin Pharm Ther, 2010 Feb;35(1):105-12.
    PMID: 20175819 DOI: 10.1111/j.1365-2710.2009.01042.x
    To estimate population pharmacokinetic parameters of repaglinide in 121 healthy Malaysian volunteers.
    Matched MeSH terms: Hypoglycemic Agents/blood; Hypoglycemic Agents/pharmacokinetics*
  19. 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/isolation & purification; Hypoglycemic Agents/chemistry*
  20. Bioequivalence of a generic metformin tablet preparation
    Yuen KH, Wong JW, Billa N, Julianto T, Toh WT
    Int J Clin Pharmacol Ther, 1999 Jul;37(7):319-22.
    PMID: 10442505
    The bioavailability of a generic preparation of metformin (Diabetmin from Hovid Sdn Bhd) was evaluated in comparison with a proprietary product (Glucophage from Lipha Pharma Ltd., UK).
    Matched MeSH terms: Hypoglycemic Agents/blood; Hypoglycemic Agents/pharmacokinetics*
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