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Fulltext Hypoglycemic and anti-hyperglycemic study of Gynura procumbens leaf extracts

Algariri K, Meng KY, Atangwho IJ, Asmawi MZ, Sadikun A, Murugaiyah V, et al.

Asian Pac J Trop Biomed, 2013 May;3(5):358-66.
PMID: 23646298 DOI: 10.1016/S2221-1691(13)60077-5

To study the antidiabetic activity of Gynura procumbens (G. procumbens) used in the traditional management of diabetes in Southern Asia.

Matched MeSH terms: Hypoglycemic Agents/chemistry
Fulltext Antidiabetic and antioxidant properties of Ficus deltoidea fruit extracts and fractions

Misbah H, Aziz AA, Aminudin N

BMC Complement Altern Med, 2013;13:118.
PMID: 23718315 DOI: 10.1186/1472-6882-13-118

Diabetes is a serious metabolic disorder affecting the metabolism of carbohydrate, protein and fat. A number of studies have shown that diabetes mellitus is associated with oxidative stress, leading to an increased production of reactive oxygen species. Ficus deltoidea is traditionally used in Malaysia for regulating blood sugar, blood pressure and cholesterol levels. The use of F. deltoidea as an alternative medicinal herb is increasingly gaining popularity with the sale of F. deltoidea tea bags and capsules in the local market. The present study was undertaken to investigate the antidiabetic and antioxidant activities of the fruits from different varieties of F. deltoidea, employing in vitro methods.

Matched MeSH terms: Hypoglycemic Agents/chemistry*
Fulltext Urinary metabolomics study on the protective role of Orthosiphon stamineus in Streptozotocin induced diabetes mellitus in rats via (1)H NMR spectroscopy

Azam AA, Pariyani R, Ismail IS, Ismail A, Khatib A, Abas F, et al.

BMC Complement Altern Med, 2017 May 25;17(1):278.
PMID: 28545435 DOI: 10.1186/s12906-017-1777-1

BACKGROUND: Orthosiphon stamineus (OS) is a herb known in ethnomedicine for treating diabetes mellitus (DM). In this study, a (1)H NMR based urine metabolomics tool has been used for the first time to identify the metabolic protective mechanism of OS in DM using Streptozotocin (STZ) induced experimental model in rats.
METHODS: Four different solvent extracts of OS, namely aqueous, ethanolic, 50% aqueous ethanolic and methanolic, at a dose of 500 mg/kg body weight (bw) were orally administered for 14 days to diabetic rats induced via intraperitoneal injection of 60 mg/kg bw STZ. NMR metabolomics approach using pattern recognition combined with multivariate statistical analysis was applied in the rat urine to study the resulted metabolic perturbations.
RESULTS: OS aqueous extract (OSAE) caused a reversal of DM comparable to that of 10 mg/kg bw glibenclamide. A total of 15 urinary metabolites, which levels changed significantly upon treatment were identified as the biomarkers of OSAE in diabetes. A systematic metabolic pathways analysis identified that OSAE contributed to the antidiabetic activity mainly through regulating the tricarboxylic acid cycle, glycolysis/gluconeogenesis, lipid and amino acid metabolism.
CONCLUSIONS: The results of this study validated the ethnopharmacological use of OS in diabetes and unveiled the biochemical and metabolic mechanisms involved.

Matched MeSH terms: Hypoglycemic Agents/chemistry
Antidiabetic effects of Brucea javanica seeds in type 2 diabetic rats

Ablat A, Halabi MF, Mohamad J, Hasnan MH, Hazni H, Teh SH, et al.

BMC Complement Altern Med, 2017 Feb 06;17(1):94.
PMID: 28166749 DOI: 10.1186/s12906-017-1610-x

Brucea javanica (B. javanica) seeds, also known as "Melada pahit" in Indo-Malay region are traditionally used to treat diabetes. The objective of this study was to determine antidiabetic, antioxidant and anti-inflammatory effects of B. javanica seeds on nicotinamide (NA)-streptozotocin (STZ) induced type 2 diabetic (T2D) rats and to analyze its chemical composition that correlate with their pharmacological activities.

Matched MeSH terms: Hypoglycemic Agents/chemistry
Fulltext Identification of Antidiabetic Metabolites from Paederia foetida L. Twigs by Gas Chromatography-Mass Spectrometry-Based Metabolomics and Molecular Docking Study

Tan DC, Kassim NK, Ismail IS, Hamid M, Ahamad Bustamam MS

Biomed Res Int, 2019;2019:7603125.
PMID: 31275982 DOI: 10.1155/2019/7603125

Paederia foetida L. (Rubiaceae) is a climber which is widely distributed in Asian countries including Malaysia. The plant is traditionally used to treat various diseases including diabetes. This study is to evaluate the enzymatic inhibition activity of Paederia foetida twigs extracts and to identify the metabolites responsible for the bioactivity by gas chromatography-mass spectrometry (GC-MS) metabolomics profiling. Three different twig extracts, namely, hexane (PFH), chloroform (PFC), and methanol (PFM), were submerged for their α-amylase and α-glucosidase inhibition potential in 5 replicates for each. Results obtained from the loading column scatter plot of orthogonal partial least square (OPLS) model revealed the presence of 12 bioactive compounds, namely, dl-α-tocopherol, n-hexadecanoic acid, 2-hexyl-1-decanol, stigmastanol, 2-nonadecanone, cholest-8(14)-en-3-ol, 4,4-dimethyl-, (3β,5α)-, stigmast-4-en-3-one, stigmasterol, 1-ethyl-1-tetradecyloxy-1-silacyclohexane, ɣ-sitosterol, stigmast-7-en-3-ol, (3β,5α,24S)-, and α-monostearin. In silico molecular docking was carried out using the crystal structure α-amylase (PDB ID: 4W93) and α-glucosidase (PDB ID: 3WY1). α-Amylase-n-hexadecanoic acid exhibited the lowest binding energy of -2.28 kcal/mol with two hydrogen bonds residue, namely, LYS178 and TYR174, along with hydrophobic interactions involving PRO140, TRP134, SER132, ASP135, and LYS172. The binding interactions of α-glucosidase-n-hexadecanoic acid complex ligand also showed the lowest binding energy among 5 major compounds with the energy value of -4.04 kcal/mol. The complex consists of one hydrogen bond interacting residue, ARG437, and hydrophobic interactions with ALA444, ASP141, GLN438, GLU432, GLY374, LEU373, LEU433, LYS352, PRO347, THR445, HIS348, and PRO351. The study provides informative data on the potential antidiabetic inhibitors identified in Paederia foetida twigs, indicating the plant has the therapeutic effect properties to manage diabetes.

Matched MeSH terms: Hypoglycemic Agents/chemistry
Fulltext Antioxidant and Antidiabetic Effects of Flavonoids: A Structure-Activity Relationship Based Study

Sarian MN, Ahmed QU, Mat So'ad SZ, Alhassan AM, Murugesu S, Perumal V, et al.

Biomed Res Int, 2017;2017:8386065.
PMID: 29318154 DOI: 10.1155/2017/8386065

The best described pharmacological property of flavonoids is their capacity to act as potent antioxidant that has been reported to play an important role in the alleviation of diabetes mellitus. Flavonoids biochemical properties are structure dependent; however, they are yet to be thoroughly understood. Hence, the main aim of this work was to investigate the antioxidant and antidiabetic properties of some structurally related flavonoids to identify key positions responsible, their correlation, and the effect of methylation and acetylation on the same properties. Antioxidant potential was evaluated through dot blot, 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging, ABTS+ radical scavenging, ferric reducing antioxidant power (FRAP), and xanthine oxidase inhibitory (XOI) assays. Antidiabetic effect was investigated through α-glucosidase and dipeptidyl peptidase-4 (DPP-4) assays. Results showed that the total number and the configuration of hydroxyl groups played an important role in regulating antioxidant and antidiabetic properties in scavenging DPPH radical, ABTS+ radical, and FRAP assays and improved both α-glucosidase and DPP-4 activities. Presence of C-2-C-3 double bond and C-4 ketonic group are two essential structural features in the bioactivity of flavonoids especially for antidiabetic property. Methylation and acetylation of hydroxyl groups were found to diminish the in vitro antioxidant and antidiabetic properties of the flavonoids.

Matched MeSH terms: Hypoglycemic Agents/chemistry*
Animal models and natural products to investigate in vivo and in vitro antidiabetic activity

Hasan MM, Ahmed QU, Mat Soad SZ, Tunna TS

Biomed Pharmacother, 2018 May;101:833-841.
PMID: 29635892 DOI: 10.1016/j.biopha.2018.02.137

Diabetes mellitus is a chronic disease which has high prevalence. The deficiency in insulin production or impaired insulin function is the underlying cause of this disease. Utilization of plant sources as a cure of diabetes has rich evidence in the history. Recently, the traditional medicinal plants have been investigated scientifically to understand the underlying mechanism behind antidiabetic potential. In this regard, a substantial number of in vivo and in vitro models have been introduced for investigating the bottom-line mechanism of the antidiabetic effect. A good number of methods have been reported to be used successfully to determine antidiabetic effects of plant extracts or isolated compounds. This review encompasses all the possible methods with a list of medicinal plants which may contribute to discovering a novel drug to treat diabetes more efficaciously with the minimum or no side effects.

Matched MeSH terms: Hypoglycemic Agents/chemistry
Chemical constituents and medical benefits of Plantago major

Adom MB, Taher M, Mutalabisin MF, Amri MS, Abdul Kudos MB, Wan Sulaiman MWA, et al.

Biomed Pharmacother, 2017 Dec;96:348-360.
PMID: 29028587 DOI: 10.1016/j.biopha.2017.09.152

The medicinal benefits of Plantago major have been acknowledged around the world for hundreds of years. This plant contains a number of effective chemical constituents including flavonoids, alkaloids, terpenoids, phenolic acid derivatives, iridoid glycosides, fatty acids, polysaccharides and vitamins which contribute to its exerting specific therapeutic effects. Correspondingly, studies have found that Plantago major is effective as a wound healer, as well as an antiulcerative, antidiabetic, antidiarrhoeal, anti-inflammatory, antinociceptive, antibacterial, and antiviral agent. It also combats fatigue and cancer, is an antioxidant and a free radical scavenger. This paper provides a review of the medicinal benefits and chemical constituents of Plantago major published in journals from year 1937 to 2015 which are available from PubMed, ScienceDirect and Google Scholar.

Matched MeSH terms: Hypoglycemic Agents/chemistry
Fulltext Investigation of α-Glucosidase Inhibitory Metabolites from Tetracera scandens Leaves by GC-MS Metabolite Profiling and Docking Studies

Nokhala A, Siddiqui MJ, Ahmed QU, Ahamad Bustamam MS, Zakaria AZA

Biomolecules, 2020 02 12;10(2).
PMID: 32059529 DOI: 10.3390/biom10020287

Stone leaf (Tetracera scandens) is a Southeast Asian medicinal plant that has been traditionally used for the management of diabetes mellitus. The underlying mechanisms of the antidiabetic activity have not been fully explored yet. Hence, this study aimed to evaluate the α-glucosidase inhibitory potential of the hydromethanolic extracts of T. scandens leaves and to characterize the metabolites responsible for such activity through gas chromatography-mass spectrometry (GC-MS) metabolomics. Crude hydromethanolic extracts of different strengths were prepared and in vitro assayed for α-glucosidase inhibition. GC-MS analysis was further carried out and the mass spectral data were correlated to the corresponding α-glucosidase inhibitory IC50 values via an orthogonal partial least squares (OPLS) model. The 100%, 80%, 60% and 40% methanol extracts displayed potent α-glucosidase inhibitory potentials. Moreover, the established model identified 16 metabolites to be responsible for the α-glucosidase inhibitory activity of T. scandens. The putative α-glucosidase inhibitory metabolites showed moderate to high affinities (binding energies of -5.9 to -9.8 kcal/mol) upon docking into the active site of Saccharomyces cerevisiae isomaltase. To sum up, an OPLS model was developed as a rapid method to characterize the α-glucosidase inhibitory metabolites existing in the hydromethanolic extracts of T. scandens leaves based on GC-MS metabolite profiling.

Matched MeSH terms: Hypoglycemic Agents/chemistry
Fulltext Synthesis, In Vitro Evaluation and Molecular Docking of the 5-Acetyl-2-aryl-6-hydroxybenzo[b]furans against Multiple Targets Linked to Type 2 Diabetes

Mphahlele MJ, Choong YS, Maluleka MM, Gildenhuys S

Biomolecules, 2020 03 07;10(3).
PMID: 32156083 DOI: 10.3390/biom10030418

The 5-acetyl-2-aryl-6-hydroxybenzo[b]furans 2a-h have been evaluated through in vitro enzymatic assay against targets which are linked to type 2 diabetes (T2D), namely, α-glucosidase, protein tyrosine phosphatase 1B (PTP1B) and β-secretase. These compounds have also been evaluated for antioxidant activity using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) free-radical scavenging method. The most active compounds against α-glucosidase and/or PTP1B, namely, 4-fluorophenyl 2c, 4-methoxyphenyl 2g and 3,5-dimethoxyphenyl substituted 2h derivatives were also evaluated for potential anti-inflammatory properties against cyclooxygenase-2 activity. The Lineweaver-Burk and Dixon plots were used to determine the type of inhibition on compounds 2c and 2h against α-glucosidase and PTP1B receptors. The interactions were investigated in modelled complexes against α-glucosidase and PTP1B via molecular docking.

Matched MeSH terms: Hypoglycemic Agents/chemistry*
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/chemistry
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/chemistry
Coumarin-chalcone hybrids targeting insulin receptor: Design, synthesis, anti-diabetic activity, and molecular docking

Konidala SK, Kotra V, Danduga RCSR, Kola PK

Bioorg Chem, 2020 11;104:104207.
PMID: 32947135 DOI: 10.1016/j.bioorg.2020.104207

Four series of thirteen new coumarin-chalcone hybrids (DPCU 1-13, DPCT 1-13, DCCU 1-13 and DCCT 1-13) were designed and synthesized using Biginelli synthesis, Pechmann condensation, Acetylation, and Claisen-Schmidt reactions. Synthesized compounds were tested for insulin receptor in silico docking studies (PDB ID: 1IR3); DCCU 13 and DCCT 13 derivatives received the lowest docking score; Streptozocin (STZ) and Nicotinamide (NA) induced type II diabetes was tested for their anti-diabetic activity in rats. In vivo tests suggested that fasting blood glucose levels of animals treated with DCCU 13 (30 mg/kg body weight) and DCCT 13 (30 mg/kg body weight) were significantly and moderately suppressed, respectively, relative to fasting blood glucose levels of diabetic control animals. Similarly, therapy with DCCU 13 and DCCT 13 attenuated oxidative stress parameters such as lipid peroxidation (MDA), superoxide dismutase (SOD) and increased the glutathione (GSH) in the liver and pancreas in a dose-dependent manner. In comparison, therapy with DCCU 13 (30 mg/kg body weight) mitigated alterations in the histological architecture of the liver and pancreatic tissue. These results indicated that the hybrids DUUC 13 and DCCT 13 at 30 mg/kg had an anti-hyperglycemic and antioxidant impact on STZ + NA mediated type II diabetes in rats. Further detailed work could be required to determine the precise mode of action of the anti-diabetic behavior of hybrids.

Matched MeSH terms: Hypoglycemic Agents/chemistry
Synthesis, α-glucosidase inhibitory activity and in silico study of tris-indole hybrid scaffold with oxadiazole ring: As potential leads for the management of type-II diabetes mellitus

Taha M, Rahim F, Imran S, Ismail NH, Ullah H, Selvaraj M, et al.

Bioorg Chem, 2017 10;74:30-40.
PMID: 28750203 DOI: 10.1016/j.bioorg.2017.07.009

Discovery of α-glucosidase inhibitors has been actively pursued with the aim to develop therapeutics for the treatment of type-II diabetes mellitus and the other carbohydrate mediated disease. In continuation of our drug discovery research on potential antidiabetic agents, we synthesized novel tris-indole-oxadiazole hybrid analogs (1-21), structurally characterized by various spectroscopic techniques such as 1H NMR, EI-MS, and 13C NMR. Elemental analysis was found in agreement with the calculated values. All compounds were evaluated for α-glucosidase inhibiting potential and showed potent inhibitory activity in the range of IC50=2.00±0.01-292.40±3.16μM as compared to standard acarbose (IC50=895.09±2.04µM). The pharmacokinetic predictions of tris-indole series using descriptor properties showed that almost all compounds in this series indicate the drug aptness. Detailed binding mode analyses with docking simulation was also carried out which showed that the inhibitors can be stabilized by the formation of hydrogen bonds with catalytic residues and the establishment of hydrophobic contacts at the opposite side of the active site.

Matched MeSH terms: Hypoglycemic Agents/chemistry
Evaluation and docking of indole sulfonamide as a potent inhibitor of α-glucosidase enzyme in streptozotocin -induced diabetic albino wistar rats

Taha M, Imran S, Salahuddin M, Iqbal N, Rahim F, Uddin N, et al.

Bioorg Chem, 2021 05;110:104808.
PMID: 33756236 DOI: 10.1016/j.bioorg.2021.104808

We have synthesized new hybrid class of indole bearing sulfonamide scaffolds (1-17) as α-glucosidase inhibitors. All scaffolds were found to be active except scaffold 17 and exhibited IC50 values ranging from 1.60 to 51.20 µM in comparison with standard acarbose (IC50 = 42.45 µM). Among the synthesized hybrid class scaffolds 16 was the most potent analogue with IC50 value 1.60 μM, showing many folds better potency as compared to standard acarbose. Whereas, synthesized scaffolds 1-15 showed good α-glucosidase inhibitory potential. Based on α-glucosidase inhibitory effect, Scaffold 16 was chosen due to highest activity in vitro for further evaluation of antidiabetic activity in Streptozotocin induced diabetic rats. The Scaffold 16 exhibited significant antidiabetic activity. All analogues were characterized through 1H, 13CNMR and HR MS. Structure-activity relationship of synthesized analogues was established and confirmed through molecular docking study.

Matched MeSH terms: Hypoglycemic Agents/chemistry
Recent advances and structure-activity relationship studies of DPP-4 inhibitors as anti-diabetic agents

Singhal S, Manikrao Patil V, Verma S, Masand N

Bioorg Chem, 2024 May;146:107277.
PMID: 38493634 DOI: 10.1016/j.bioorg.2024.107277

Diabetes mellitus (DM) is one of the largest public health problems worldwide and in the last decades various therapeutic targets have been investigated. For the treatment of type-2 DM (T2DM), dipeptidyl peptidase-4 (DPP-4) is one of the well reported target and has established safety in terms of cardiovascular complexicity. Preclinical and clinical studies using DPP-4 inhibitors have demonstrated its safety and effectiveness and have lesser risk of associated hypoglycaemic effect making it suitable for elderly patients. FDA has approved a number of structurally diverse DPP-4 inhibitors for clinical use. The present manuscript aims to focus on the well reported hybrid and non-hybrid analogues and their structural activity relationship (SAR) studies. It aims to provide structural insights for this class of compounds pertaining to favourable applicability of selective DPP-4 inhibitors in the treatment of T2DM.

Matched MeSH terms: Hypoglycemic Agents/chemistry
Biogenic integrated ZnO/Ag nanocomposite: Surface analysis and in vivo practices for the management of type 1 diabetes complications

Rahim Pouran S, Bayrami A, Mohammadi Arvanag F, Habibi-Yangjeh A, Darvishi Cheshmeh Soltani R, Singh R, et al.

Colloids Surf B Biointerfaces, 2020 May;189:110878.
PMID: 32087528 DOI: 10.1016/j.colsurfb.2020.110878

In this research, a milk thistle seed extract (MTSE)-rich medium was used as a capping and reducing agent for the one-pot biosynthesis of ZnO/Ag (5 wt%) nanostructure. The sample was systematically characterized through various techniques and its strong biomolecule‒metal interface structure was supported by the results. The efficacy of the derived nanostructure (MTSE/ZnO/Ag) was evaluated in vivo on the basis of its therapeutic effects on the main complications of Type 1 diabetes (hyperglycemia, hyperlipidemia, and insulin deficiency). For this purpose, the changes in the plasma values of fasting blood glucose, total cholesterol, total triglyceride, high-density lipoprotein cholesterol, and insulin in alloxan-diabetic Wistar male rats were compared with those in healthy and untreated diabetic controls after a treatment period of 16 days. The antidiabetic results of MTSE/ZnO/Ag were compared with those obtained from pristine ZnO, MTSE, and insulin therapies. The health conditions of the rats with Type 1 diabetes were significantly enhanced after treatment with MTSE/ZnO/Ag (p 

Matched MeSH terms: Hypoglycemic Agents/chemistry
2-Furoic piperazide derivatives as promising drug candidates of type 2 diabetes and Alzheimer's diseases: In vitro and in silico studies

Abbasi MA, Hassan M, Ur-Rehman A, Siddiqui SZ, Hussain G, Shah SAA, et al.

Comput Biol Chem, 2018 Dec;77:72-86.
PMID: 30245349 DOI: 10.1016/j.compbiolchem.2018.09.007

The heterocyclic compounds have been extensively reported for their bioactivity potential. The current research work reports the synthesis of some new multi-functional derivatives of 2-furoic piperazide (1; 1-(2-furoyl)piperazine). The synthesis was initiated by reacting the starting compound 1 with 3,5-dichloro-2-hydroxybenzenesulfonyl chloride (2) in a basic, polar and protic medium to obtain the parent sulfonamide 3 which was then treated with different electrophiles, 4a-g, in a polar and aprotic medium to acquire the designed molecules, 5a-g. These convergent derivatives were evaluated for their inhibitory potential against α-glucosidase, acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes. Acarbose was used as a reference standard for α-glucosidase inhibition while eserine for AChE and BChE inhibition. Some of the synthesized compounds were identified as promising inhibitors of these three enzymes and their bioactivity potentials were also supported by molecular docking study. The most active compounds among the synthetic analogues might be helpful in drug discovery and development for the treatment of type 2 diabetes and Alzhiemer's diseases.

Matched MeSH terms: Hypoglycemic Agents/chemistry
A Review of Bisindolylmethane as an Important Scaffold for Drug Discovery

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/chemistry*
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/chemistry

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