Displaying publications 101 - 120 of 575 in total

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  1. Zhao YF, Chaw JK, Ang MC, Tew Y, Shi XY, Liu L, et al.
    PLoS One, 2025;20(1):e0317662.
    PMID: 39869550 DOI: 10.1371/journal.pone.0317662
    Patients with type 1 diabetes and their physicians have long desired a fully closed-loop artificial pancreas (AP) system that can alleviate the burden of blood glucose regulation. Although deep reinforcement learning (DRL) methods theoretically enable adaptive insulin dosing control, they face numerous challenges, including safety and training efficiency, which have hindered their clinical application. This paper proposes a safe and efficient adaptive insulin delivery controller based on DRL. It employed ten tricks to enhance the proximal policy optimization (PPO) algorithm, improving training efficiency. Additionally, a dual safety mechanism of 'proactive guidance + reactive correction' was introduced to reduce the risks of hyperglycemia and hypoglycemia and to prevent emergencies. Performance evaluations in the Simglucose simulator demonstrate that the proposed controller achieved an 87.45% time in range (TIR) median, superior to baseline methods, with a lower incidence of hypoglycemia, notably eliminating severe hypoglycemia and treatment failures. These encouraging results indicate that the DRL-based fully closed-loop AP controller has taken an essential step toward clinical implementation.
    Matched MeSH terms: Hypoglycemic Agents/administration & dosage; Hypoglycemic Agents/therapeutic use
  2. Fox CK, Barrientos-Pérez M, Bomberg EM, Dcruz J, Gies I, Harder-Lauridsen NM, et al.
    N Engl J Med, 2025 Feb 06;392(6):555-565.
    PMID: 39258838 DOI: 10.1056/NEJMoa2407379
    BACKGROUND: No medications are currently approved for the treatment of nonmonogenic, nonsyndromic obesity in children younger than 12 years of age. Although the use of liraglutide has been shown to induce weight loss in adults and adolescents with obesity, its safety and efficacy have not been established in children.

    METHODS: In this phase 3a trial, which consisted of a 56-week treatment period and a 26-week follow-up period, we randomly assigned children (6 to <12 years of age) with obesity, in a 2:1 ratio, to receive either once-daily subcutaneous liraglutide at a dose of 3.0 mg (or the maximum tolerated dose) or placebo, plus lifestyle interventions. The primary end point was the percentage change in the body-mass index (BMI; the weight in kilograms divided by the square of the height in meters). The confirmatory secondary end points were the percentage change in body weight and a reduction in BMI of at least 5%.

    RESULTS: A total of 82 participants underwent randomization; 56 were assigned to the liraglutide group and 26 to the placebo group. At week 56, the mean percentage change from baseline in BMI was -5.8% with liraglutide and 1.6% with placebo, representing an estimated difference of -7.4 percentage points (95% confidence interval [CI], -11.6 to -3.2; P<0.001). The mean percentage change in body weight was 1.6% with liraglutide and 10.0% with placebo, representing an estimated difference of -8.4 percentage points (95% CI, -13.4 to -3.3; P = 0.001), and a reduction in BMI of at least 5% occurred in 46% of participants in the liraglutide group and in 9% of participants in the placebo group (adjusted odds ratio, 6.3 [95% CI, 1.4 to 28.8]; P = 0.02). Adverse events occurred in 89% and 88% of participants in the liraglutide and placebo groups, respectively. Gastrointestinal adverse events were more common in the liraglutide group (80% vs. 54%); serious adverse events were reported in 12% and 8% of participants in the liraglutide and placebo groups, respectively.

    CONCLUSIONS: Among children (6 to <12 years of age) with obesity, treatment with liraglutide for 56 weeks plus lifestyle interventions resulted in a greater reduction in BMI than placebo plus lifestyle interventions. (Funded by Novo Nordisk; SCALE Kids ClinicalTrials.gov number, NCT04775082.).

    Matched MeSH terms: Hypoglycemic Agents/adverse effects; Hypoglycemic Agents/therapeutic use
  3. Ruzilawati AB, Gan SH
    Pharmacology, 2010;85(6):357-64.
    PMID: 20523106 DOI: 10.1159/000302731
    AIM: To investigate the effects of CYP3A4 and CYP2C8 enzymes on repaglinide's pharmacokinetics in healthy Malaysian subjects.

    METHODS: Subjects (n = 121) received oral repaglinide (4 mg). Blood samples were taken at 0, 30, 60, 120, 180 and 240 min and serum concentrations of repaglinide were determined using high-performance liquid chromatography. Subjects were also genotyped by polymerase chain reaction-restriction fragment length polymorphism (PCR-RFLP) for CYP3A4*4, *5 and*18 and by an allele-specific multiplex PCR for CYP2C8*2, *3, *4 and *5 alleles.

    RESULTS: The allele frequencies of CYP2C8*1, *2, *3, *4 and *5 were 95.04, 0.40, 0.40, 0 and 4.13%, respectively. The frequencies of the CYP3A4*1, *4, *5 and *18 alleles were 97.93, 0, 0 and 2.07%, respectively. CYP2C8 and CYP3A4 genotypes were not significantly associated with repaglinide's blood glucose-lowering effect. However, the CYP3A4 genotype significantly influenced some of repaglinide's pharmacokinetics, where the mean elimination rate constant was 44.0% lower (p = 0.04) and the mean half-life was 33.8% higher (p = 0.04) in subjects with the CYP3A4*1/*18 genotype as compared to those with the normal CYP3A4*1/*1 genotype. This result confirms that CYP3A4 plays a large role in metabolizing repaglinide.

    CONCLUSION: Genetic polymorphisms of CYP3A4, specifically CYP3A4*18, play a major role in contributing to the interindividual variability in repaglinide's pharmacokinetics.

    Matched MeSH terms: Hypoglycemic Agents/administration & dosage; Hypoglycemic Agents/blood; Hypoglycemic Agents/pharmacokinetics; Hypoglycemic Agents/pharmacology
  4. 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/chemical synthesis*; Hypoglycemic Agents/pharmacology*; Hypoglycemic Agents/therapeutic use; Hypoglycemic Agents/chemistry
  5. Kadir A, Mokhtar MT, Wong TW
    J Pharm Sci, 2013 Dec;102(12):4353-63.
    PMID: 24258282 DOI: 10.1002/jps.23742
    The relationship of high and low molecular weight mannuronic acid (M)- and guluronic acid (G)-rich alginate nanoparticles as oral insulin carrier was elucidated. Nanoparticles were prepared through ionotropic gelation using Ca(2+) , and then in vitro physicochemical attributes and in vivo antidiabetic characteristics were examined. The alginate nanoparticles had insulin release retarded when the matrices had high alginate-to-insulin ratio or strong alginate-insulin interaction via OH moiety. High molecular weight M-rich alginate nanoparticles were characterized by assemblies of long polymer chains that enabled insulin encapsulation with weaker polymer-drug interaction than nanoparticles prepared from other alginate grades. They were able to encapsulate and yet release and have insulin absorbed into systemic circulation, thereby lowering rat blood glucose. High molecular weight G- and low molecular weight M-rich alginate nanoparticles showed remarkable polymer-insulin interaction. This retarded the drug release and negated its absorption. Blood glucose lowering was, however, demonstrated in vivo with insulin-free matrices of these nanoparticles because of the strong alginate-glucose binding that led to intestinal glucose retention. Alginate nanoparticles can be used as oral insulin carrier or glucose binder in the treatment of diabetes as a function of its chemical composition. High molecular weight M-rich alginate nanoparticles are a suitable vehicle for future development into oral insulin carrier.
    Matched MeSH terms: Hypoglycemic Agents/administration & dosage*; Hypoglycemic Agents/pharmacology
  6. Mohamed EA, Siddiqui MJ, Ang LF, Sadikun A, Chan SH, Tan SC, et al.
    PMID: 23039079 DOI: 10.1186/1472-6882-12-176
    In the present study, we tested a 50% ethanolic extract of Orthosiphon stamineus plants and its isolated bioactive compound with respect to their α-glucosidase and α-amylase inhibitory activities.
    Matched MeSH terms: Hypoglycemic Agents/isolation & purification; Hypoglycemic Agents/pharmacology*
  7. Sarmadi B, Aminuddin F, Hamid M, Saari N, Abdul-Hamid A, Ismail A
    Food Chem, 2012 Sep 15;134(2):905-11.
    PMID: 23107706 DOI: 10.1016/j.foodchem.2012.02.202
    Fat, alkaloid and polyphenol contents of two clones of cocoa (UIT1 and PBC 140) were removed and the remaining powder was autolyzed at pH 3.5 and 5.2. Based on the results, autolysates of UIT produced at pH 3.5 exhibited the highest ability to inhibit α-amylase activity. However, no α-glucosidase inhibition activity was observed under the conditions specified. Autolysates produced under pH 3.5 caused the highest amount of insulin secretion. In streptozotocin-diabetic rats, all cocoa autolysates significantly decreased blood glucose at 4h. To assure that the results from the assays were not due to the polyphenols of cocoa autolysates qualitative and quantitative tests were applied. According to their results cocoa autolysates were found to be free from polyphenols. Analysis of amino acid composition revealed that cocoa autolysates were abundant in hydrophobic amino acids. It can be suggested that besides other compounds of cocoa, its peptides and amino acids could contribute to its health benefits.
    Matched MeSH terms: Hypoglycemic Agents/administration & dosage*; Hypoglycemic Agents/analysis
  8. 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/pharmacology*; Hypoglycemic Agents/chemistry*
  9. Umar A, Ahmed QU, Muhammad BY, Dogarai BB, Soad SZ
    J Ethnopharmacol, 2010 Aug 19;131(1):140-5.
    PMID: 20600771 DOI: 10.1016/j.jep.2010.06.016
    The present study was aimed to investigate the anti-diabetic potential of the leaves of Tetracera scandens Linn. Merr. (Dilleniaceae) in vivo with regard to prove its efficacy by local herbalists in the treatment of diabetes frailties.
    Matched MeSH terms: Hypoglycemic Agents/isolation & purification; Hypoglycemic Agents/therapeutic use*
  10. Ilyanie Y, Wong TW, Choo CY
    PMID: 22754938 DOI: 10.2202/1553-3840.1469
    Ficus deltoidea Jack (Moraceae) leaf extract is used as an antidiabetic in traditional medicine. Its widespread usage is reflected by the available preparations in the present commercial market. The efficacy of other Ficus species has not been entirely satisfactory and many antidiabetic herbs have demonstrated poor safety profiles. This study examined hypoglycemic and toxicity profiles of F. deltoidea leaf extract in rodent models. Extracts of dried powdered leaves were obtained using methanol solution, n-hexane, chloroform, and n-butanol. These extracts were orally administered to rodents. Their blood glucose and insulin levels, acute and subchronic toxicity, biochemical and histological profiles of liver and kidney were determined. Methanol extract exhibited blood glucose lowering activity in mildly insulin resistant diabetic rats as well as in normoglycemic mice unlike hydrophilic butanol subextract which only expressed its activity in normoglycemic mice. Methanol extract could contain both insulin receptor sensitization and secretagogue constituents. Different from toxic chloroform and hexane subextracts, hydrophilic methanol extract gave zero percent mortality up to 6400 mg/kg in 14 days. It did not induce liver and kidney toxicity upon four-week consumption at 200 mg/kg. The methanol extract possessed mixed antidiabetic actions and exhibited a low level of oral toxicity.
    Matched MeSH terms: Hypoglycemic Agents/pharmacology*; Hypoglycemic Agents/toxicity
  11. Ahmad B, Khalid BA, Zaini A, Hussain NA, Quek KF
    Diabetes Res Clin Pract, 2011 Jul;93(1):e12-4.
    PMID: 21397969 DOI: 10.1016/j.diabres.2011.02.020
    The objective of this study was to elucidate influencing factors of HbA1C in various health care settings. The glycaemic control was suboptimal in all settings. Multivariate analysis confirmed three factors were significant in HbA1C outcome; insulin (p=0.000), medication (p=0.043) and ethnicity (p=0.000).
    Matched MeSH terms: Hypoglycemic Agents/administration & dosage; Hypoglycemic Agents/therapeutic use
  12. Bebakar WM, Chow CC, Kadir KA, Suwanwalaikorn S, Vaz JA, Bech OM, et al.
    Diabetes Obes Metab, 2007 Sep;9(5):724-32.
    PMID: 17593237 DOI: 10.1111/j.1463-1326.2007.00743.x
    Aim: To evaluate the efficacy and safety of adding biphasic insulin aspart 30 (BIAsp30; NovoMix 30) to existing oral antidiabetic agents (OADs) vs. optimizing OADs in a subgroup of Western Pacific patients with type 2 diabetes inadequately controlled on oral monotherapy or oral combination therapy.

    Methods: This 26-week, multi-centre, open-labelled, randomized, two-arm parallel trial consisted of a 2-week screening period, followed by 24 weeks of treatment. Subjects randomized to BIAsp30 treatment (n = 129) received BIAsp30 once daily (o.d.) at dinnertime between Week 2 and Week 14, and those not reaching treatment targets were switched to twice daily (b.i.d.) BIAsp30 at Week 14 (n = 50). Subjects randomized to the OAD-only arm (n = 63) continued with their previous OAD treatment and, in an attempt to reach treatment goals, the dose was optimized (but OAD unchanged) in accordance to local treatment practice and labelling.

    Results: Significantly greater reductions in HbA(1c) over Weeks 0-13 with BIAsp30 (o.d.) vs. OAD-only treatment (1.16 vs. 0.58%; p < 0.001), and over Weeks 0-26, with BIAsp30 (o.d.) and BIAsp30 (b.i.d.) treatments vs. OAD-only treatment (1.24 vs. 1.34 vs. 0.67%; p < 0.01). Hypoglycaemic episodes were reported in 54% of the patients in BIAsp30 (o.d. and b.i.d. pooled) and 30% of the patients in OAD-only group. All episodes were minor or symptomatic, except for one in each treatment group, which was major.

    Conclusions: Initiating BIAsp30 treatment is a safe and more effective way to improve glycaemic control in Western Pacific patients with type 2 diabetes inadequately controlled with oral monotherapy or oral combination therapy compared with optimizing oral combination therapy alone. In patients not reaching treatment target on BIAsp30 (o.d.), treatment with BIAsp30 (b.i.d.) should be considered.
    Matched MeSH terms: Hypoglycemic Agents/administration & dosage*; Hypoglycemic Agents/adverse effects
  13. 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/pharmacology*; Hypoglycemic Agents/chemistry
  14. Imran S, Taha M, Ismail NH
    Curr Med Chem, 2015;22(38):4412-33.
    PMID: 26438249
    Bisindolylmethane and its derivatives are pharmacologically active and applicable in the field of pharmaceutical chemistry. Bisindolylmethanes have a variety of biological activities such as antihyperglycemic, antiinflammatory, antibacterial, anticancer, and antileishmanial activities, including enzyme inhibition activity. They play a crucial role in many diseases especially anticancer activity. Modifying their structure had proven to be useful in the search of new therapeutic agents. Extensive research carried out on bisindolylmethane and its derivatives shows that they are pharmacologically significant. The present review focuses on the pharmacological profile of bisindolylmethane derivatives. This review includes the current literature with an update of research findings as well as the perspectives that they hold for future research.
    Matched MeSH terms: Hypoglycemic Agents/pharmacology; Hypoglycemic Agents/chemistry*
  15. Cheng SH, Ismail A, Anthony J, Ng OC, Hamid AA, Yusof BN
    BMC Complement Altern Med, 2016 Feb 27;16:84.
    PMID: 26920910 DOI: 10.1186/s12906-016-1047-7
    BACKGROUND: Type 2 diabetes mellitus is a major health threat worldwide. Cosmos caudatus is one of the medicinal plants used to treat type 2 diabetes. Therefore, this study aims to determine the effectiveness and safety of C. caudatus in patients with type 2 diabetes. Metabolomic approach will be carried out to compare the metabolite profiles between C. Caudatus treated diabetic patients and diabetic controls.

    METHODS AND DESIGN: This is a single-center, randomized, controlled, two-arm parallel design clinical trial that will be carried out in a tertiary hospital in Malaysia. In this study, 100 patients diagnosed with type 2 diabetes will be enrolled. Diabetic patients who meet the eligibility criteria will be randomly allocated to two groups, which are diabetic C. caudatus treated(U) group and diabetic control (C) group. Primary and secondary outcomes will be measured at baseline, 4, 8, and 12 weeks. The serum and urine metabolome of both groups will be examined using proton NMR spectroscopy.

    DISCUSSION: The study will be the first randomized controlled trial to assess whether C. caudatus can confer beneficial effect in patients with type 2 diabetes. The results of this trial will provide clinical evidence on the effectiveness and safety of C. caudatus in patients with type 2 diabetes.

    TRIAL REGISTRATION: ClinicalTrials.gov identifier: NCT02322268.

    Matched MeSH terms: Hypoglycemic Agents/pharmacology; Hypoglycemic Agents/therapeutic use*
  16. Razavi M, Karimian H, Yeong CH, Chung LY, Nyamathulla S, Noordin MI
    Drug Des Devel Ther, 2015;9:4373-86.
    PMID: 26273196 DOI: 10.2147/DDDT.S86263
    The present research was aimed at formulating a metformin HCl sustained-release formulation from a combination of polymers, using the wet granulation technique. A total of 16 formulations (F1-F16) were produced using different combinations of the gel-forming polymers: tamarind kernel powder, salep (palmate tubers of Orchis morio), and xanthan. Post-compression studies showed that there were no interactions between the active drug and the polymers. Results of in vitro drug-release studies indicated that the F10 formulation which contained 5 mg of tamarind kernel powder, 33.33 mg of xanthan, and 61.67 mg of salep could sustain a 95% release in 12 hours. The results also showed that F2 had a 55% similarity factor with the commercial formulation (C-ER), and the release kinetics were explained with zero order and Higuchi models. The in vivo study was performed in New Zealand White rabbits by gamma scintigraphy; the F10 formulation was radiolabeled using samarium (III) oxide ((153)Sm2O3) to trace transit of the tablets in the gastrointestinal tract. The in vivo data supported the retention of F10 formulation in the gastric region for 12 hours. In conclusion, the use of a combination of polymers in this study helped to develop an optimal gastroretentive drug-delivery system with improved bioavailability, swelling, and floating characteristics.
    Matched MeSH terms: Hypoglycemic Agents/administration & dosage; Hypoglycemic Agents/pharmacokinetics
  17. Thent ZC, Das S, Zaidun NH
    Curr Drug Deliv, 2018;15(4):453-460.
    PMID: 28545355 DOI: 10.2174/1567201814666170525122224
    BACKGROUND: The incidence of diabetes mellitus has increased drastically over the past few decades. This oxidant-antioxidant imbalance resulting in complication of diabetes mellitus includes macro- and microvascular complications. Resistance to conventional treatment and patient compliance has paved the way to the usage of effective natural products and supplements. Momordica charantia (bitter gourd) is widely consumed in many parts of Malaysia as a vegetable. Momordica charantia (MC) is mainly used in the management of diabetes mellitus.

    OBJECTIVE: The present review discusses the literature concerning the antidiabetic and antioxidant properties of MC focusing on the complication of diabetes mellitus along with its mode of delivery. We found that among the whole part of MC, its fruit extract has been widely studied, therapeutically. The evidence based analysis of the beneficiary effects of MC on the different organs involved in diabetes complication is also highlighted. This review elucidated an essential understanding of MC based drug delivery system in both clinical and experimental studies and appraised the great potential of the protein based MC extract against diabetes mellitus.

    CONCLUSION: The review paper is believed to assist the researchers and medical personnel in treating diabetic associated complications.

    Matched MeSH terms: Hypoglycemic Agents/administration & dosage; Hypoglycemic Agents/therapeutic use*
  18. Pang KL, Chin KY
    Molecules, 2019 Mar 06;24(5).
    PMID: 30845769 DOI: 10.3390/molecules24050923
    Obesity is a major risk factor for diabetes, and these two metabolic conditions cause significant healthcare burden worldwide. Chronic inflammation and increased oxidative stress due to exposure of cells to excess nutrients in obesity may trigger insulin resistance and pancreatic β-cell dysfunction. Tocotrienol, as a functional food component with anti-inflammatory, antioxidant, and cell signaling-mediating effects, may be a potential agent to complement the current management of obesity and diabetes. The review aimed to summarize the current evidence on the anti-obesity and antidiabetic effects of tocotrienol. Previous studies showed that tocotrienol could suppress adipogenesis and, subsequently, reduce body weight and fat mass in animals. This was achieved by regulating pathways of lipid metabolism and fatty acid biosynthesis. It could also reduce the expression of transcription factors regulating adipogenesis and increase apoptosis of adipocytes. In diabetic models, tocotrienol was shown to improve glucose homeostasis. Activation of peroxisome proliferator-activated receptors was suggested to be responsible for these effects. Tocotrienol also prevented multiple systemic complications due to obesity and diabetes in animal models through suppression of inflammation and oxidative stress. Several clinical trials have been conducted to validate the antidiabetic of tocotrienol, but the results were heterogeneous. There is no evidence showing the anti-obesity effects of tocotrienol in humans. Considering the limitations of the current studies, tocotrienol has the potential to be a functional food component to aid in the management of patients with obesity and diabetes.
    Matched MeSH terms: Hypoglycemic Agents/pharmacology; Hypoglycemic Agents/chemistry*
  19. Anwar A, Siddiqui R, Raza Shah M, Khan NA
    J Microbiol Biotechnol, 2019 May 28;29(5):713-720.
    PMID: 31030451 DOI: 10.4014/jmb/1903.03009
    Acanthamoeba castellanii belonging to the T4 genotype may cause a fatal brain infection known as granulomatous amoebic encephalitis, and the vision-threatening eye infection Acanthamoeba keratitis. The aim of this study was to evaluate the antiamoebic effects of three clinically available antidiabetic drugs, Glimepiride, Vildagliptin and Repaglinide, against A. castellanii belonging to the T4 genotype. Furthermore, we attempted to conjugate these drugs with silver nanoparticles (AgNPs) to enhance their antiamoebic effects. Amoebicidal, encystation, excystation, and host cell cytotoxicity assays were performed to unravel any antiacanthamoebic effects. Vildagliptin conjugated silver nanoparticles (Vgt-AgNPs) characterized by spectroscopic techniques and atomic force microscopy were synthesized. All three drugs showed antiamoebic effects against A. castellanii and significantly blocked the encystation. These drugs also showed significant cysticidal effects and reduced host cell cytotoxicity caused by A. castellanii. Moreover, Vildagliptin-coated silver nanoparticles were successfully synthesized and are shown to enhance its antiacanthamoebic potency at significantly reduced concentration. The repurposed application of the tested antidiabetic drugs and their nanoparticles against free-living amoeba such as Acanthamoeba castellanii described here is a novel outcome that holds tremendous potential for future applications against devastating infection.
    Matched MeSH terms: Hypoglycemic Agents/pharmacology*; Hypoglycemic Agents/chemistry
  20. 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/pharmacology*; Hypoglycemic Agents/chemistry*
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