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Sung-In Choi, Mi Hwa Park, Ji-Sook Han
This study was designed to investigate the inhibitory effect of Gynura procumbens extract against carbohydrate digesting enzymes and its ability to ameliorate postprandial hyperglycemia in streptozotocin (STZ)-induced diabetic mice. G. procumbens extract showed prominent α-glucosidase and α-amylase inhibitory effects. The half-maximal inhibitory concentration (IC50) of G. procumbens extract against α-glucosidase and α-amylase was 0.092±0.018 and 0.084±0.027 mg/mL, respectively, suggesting that the α-amylase inhibition activity of the G...
September 2016: Preventive Nutrition and Food Science
A P van Beek, M Emous, M Laville, J Tack
BACKGROUND: Dumping syndrome, a common complication of esophageal, gastric or bariatric surgery, includes early and late dumping symptoms. Early dumping occurs within 1 h after eating, when rapid emptying of food into the small intestine triggers rapid fluid shifts into the intestinal lumen and release of gastrointestinal hormones, resulting in gastrointestinal and vasomotor symptoms. Late dumping occurs 1-3 h after carbohydrate ingestion, caused by an incretin-driven hyperinsulinemic response resulting in hypoglycemia...
October 17, 2016: Obesity Reviews: An Official Journal of the International Association for the Study of Obesity
Faten K Abd El-Hady, Walid Fayad, Carmine Iodice, Zeinab A El-Shahid, Mohamed S Abdel-Aziz, Egle Crudele, Giuseppina Tommonaro
Marine organisms have been considered as the richest sources of novel bioactive metabolites, which can be used for pharmaceutical purposes. In the last years, the interest for marine microorganisms has grown for their enormous biodiversity and for the evidence that many novel compounds isolated from marine invertebrates are really synthesized by their associated bacteria. Nevertheless, the discovery of a chemical communication Quorum sensing (QS) between bacterial cells and between bacteria and host has gained the researchers to expand the aim of their study toward the role of bacteria associated with marine invertebrates, such as marine sponge...
October 14, 2016: Current Microbiology
- Alamgeer, Muhammad Naveed Mushtaq, Sajid Bashir, Ikram Ullah, Sabeha Karim, Muhammad Rashid, Muhammad Nasir Hayat Malik, Haroonur Rashid
The aim of present study was to evaluate and compare the hypoglycemic activity of different solvents extracts of Thymus serpyllum in rabbits. Diabetes was induced with single intravenous injection of alloxan monohydrate (150mg/kg). Glibenclamide and acarbose were used as standard drugs. The crude powder of Thymus serpyllum (500 mg/kg b.w) significantly reduced blood glucose level in both normal and diabetic rabbits. Various extracts of Thymus serpyllum were compared for their hypoglycemic activity in diabetic rabbits...
September 2016: Pakistan Journal of Pharmaceutical Sciences
Na Wang, Jin-Ping Zhang, Xiao-Yan Xing, Zhao-Jun Yang, Bo Zhang, Xin Wang, Wen-Ying Yang
BACKGROUND: This post-hoc analysis investigated whether changes in endogenous glucagon-like peptide-1 (GLP-1) levels were associated with weight loss in newly diagnosed diabetes patients. METHODS: Seven hundred eighty-four subjects from the MARCH (Metformin and AcaRbose in Chinese as initial Hypoglycemic treatment) study were stratified by changes in GLP-1 levels (∆GLP-1). Changes in clinical and physiological parameters were evaluated across ∆GLP-1 subgroups to assess correlations between ∆GLP-1 and weight loss in acarbose vs...
September 22, 2016: Journal of Diabetes
Francesca Santilli, Rossella Liani, Patrizia Di Fulvio, Gloria Formoso, Paola Simeone, Romina Tripaldi, Thor Ueland, Pål Aukrust, Giovanni Davì
Resistin is an adipokine that promotes inflammation and insulin resistance by targeting several cells including platelets. We hypothesised that in type 2 diabetes (T2DM), resistin may foster in vivo oxidative stress, thromboxane-dependent platelet activation and platelet-derived inflammatory proteins release, key determinants of atherothrombosis. A cross-sectional comparison of circulating resistin, sCD40L, as a marker of platelet-mediated inflammation, asymmetric dimethylarginine (ADMA), endothelial dysfunction marker, Dickkopf (DKK)-1, reflecting the inflammatory interaction between platelets and endothelial cells, and urinary 8-iso-PGF2α and 11-dehydro-TxB2, reflecting in vivo lipid peroxidation and platelet activation, respectively, was performed between 79 T2DM patients and 30 healthy subjects...
October 6, 2016: Thrombosis and Haemostasis
Feng-Fei Li, Li-Yuan Fu, Xiao-Hua Xu, Xiao-Fei Su, Jin-Dan Wu, Lei Ye, Jian-Hua Ma
The aim of the present study was to evaluate the add-on effect of acarbose therapy in oxidative stress, and the lipid and inflammatory profiles of patients with type 2 diabetes mellitus (T2DM) treated with insulin. This was an open and unblended study. Patients (n=134) with T2DM (haemoglobin A1c range, 9.0-12.0%) were recruited. After continuous subcutaneous insulin infusion for 7 days for initial rapid correction of hyperglycaemia, a premixed insulin titration period (duration, 4-6 days) subsequently followed...
October 2016: Biomedical Reports
Guangcheng Wang, Zhiyun Peng, Jing Wang, Xin Li, Juan Li
A novel series of triazine-triazole derivatives 7a-7m were synthesized, characterized by (1)H NMR and evaluated for their α-glucosidase inhibitory activity. All the synthesized compounds displayed potent α-glucosidase inhibitory activity with IC50 range of 11.63 ± 0.15 to 37.44 ± 0.35 μM, when compared to the standard drug acarbose (IC50 = 817.38 ± 6.27 μM). Among the series, compound 7i (IC50 = 11.63 ± 0.15 μM) bearing 2,5-dichloro substitution at phenyl ring, represented the most potent α-glucosidase inhibitory activity...
September 21, 2016: European Journal of Medicinal Chemistry
Zhong Chen, Xiaoying Fu, Jian Kuang, Ju Chen, Hongmei Chen, Jianhao Pei, Huazhang Yang
BACKGROUND: Acarbose slows down the intestinal absorption of carbohydrates, but its effects on the secretion of incretins are still poorly known. This study aimed to examine the effects of single-dose acarbose on the secretion of incretins in patients with newly diagnosed type 2 diabetes mellitus (T2DM). METHODS: In this pilot study, twenty-three patients diagnosed with T2DM were randomly assigned to the oral glucose tolerance test (OGTT) group (n = 11) and the mixed meal test (MMT) group (n = 12)...
September 29, 2016: BMC Endocrine Disorders
Mouna Chakroun, Bassem Khemakhem, Hazem Ben Mabrouk, Hanen El Abed, Mohamed Makni, Mohamed Bouaziz, Noureddine Drira, Naziha Marrakchi, Hafedh Mejdoub
Among various chronic disorders, cancer and diabetes mellitus are the most common disorders. This study was designed to evaluate the effectiveness of hydroalcoholic extract of Phoenix dactylifera L. leaves (HEPdL) in animal models of type II diabetes in vitro/in vivo and in a human melanoma-derived cell line (IGR-39). A liquid chromatography-tandem mass spectrometry (LC-MS/MS) analysis was also performed to determine the amount of phenolic and flavonoid compounds in this plant. The physicochemical results by LC-MS/MS analysis of HEPdL showed the presence of 10 phenolic compounds...
September 23, 2016: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
Kristina Bljajić, Nina Šoštarić, Roberta Petlevski, Lovorka Vujić, Andrea Brajković, Barbara Fumić, Isabel Saraiva de Carvalho, Marijana Zovko Končić
B. pendula leaf is a common ingredient in traditional herbal combinations for treatment of diabetes in southeastern Europe. Present study investigated B. pendula ethanolic and aqueous extract as inhibitors of carbohydrate hydrolyzing enzymes, as well as their ability to restore glutathione concentration in Hep G2 cells subjected to glucose-induced oxidative stress. Phytochemical analysis revealed presence of rutin and other quercetin derivatives, as well as chlorogenic acid. In general, ethanolic extract was richer in phenolic substances than the aqueous extract...
2016: Evidence-based Complementary and Alternative Medicine: ECAM
Violet Kasabri, Entisar K Al-Hallaq, Yasser K Bustanji, Khalid K Abdul-Razzak, Ismail F Abaza, Fatma U Afifi
CONTEXT: Adiantum capillus-veneris L. (Adiantaceae) hypocholesterolemic activity is therapeutically praised. OBJECTIVES: Pharmacological modulation of pancreatic triacylglycerol lipase (PL) and α-amylase/α-glucosidase by A. capillus-veneris are evaluated. MATERIALS AND METHODS: Using positive controls (acarbose, orlistat, guar gum, atorvastatin, glipizide and metformin) as appropriate, crude aqueous extracts (AEs) of A. capillus-veneris aerial parts were tested via a combination of in vitro enzymatic (0...
September 23, 2016: Pharmaceutical Biology
Pham Van Khang, Dao Mai Phuong, Lei Ma
Two new steroids were isolated from acid hydrolysis residue of the rhizomes of Anemarrhena asphodeloides. Their structures were identified on the basis of several spectroscopic analysis approaches including 1D, 2D-NMR techniques, and MS data, and by the comparison of spectral data of the known compounds. The biological activities of these two isolated compounds were explored on α-glucosidase. Compound 1 displayed 4.7 folds inhibitory activity against α-glucosidase compared with the positive control acarbose...
September 23, 2016: Journal of Asian Natural Products Research
Seung Hwan Hwang, Zhiqiang Wang, Ha Na Yoon, Soon Sung Lim
Phytochemical investigation of the natural products from Xanthium strumarium led to the isolation of fourteen compounds including seven caffeoylquinic acid (CQA) derivatives. The individual compounds were screened for inhibition of α-glucosidase, protein tyrosine phosphatase 1β (PTP1β), advanced glycation end products (AGEs), and ABTS⁺ radical scavenging activity using in vitro assays. Among the isolated compounds, methyl-3,5-di-caffeoyquinic acid exhibited significant inhibitory activity against α-glucosidase (18...
2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Chao He, Jing Li, Wei Li, Yi Xue, Zeming Fang, Wei Fang, Xuecheng Zhang, Xiaotang Wang, Yazhong Xiao
Here we report the first crystal structure of a secretory α-glucoside hydrolase isolated from Pseudoalteromonas sp. K8, PspAG97A, which belongs to glycoside hydrolase family 97 and exhibits halophilic property. PspAG97A lacks an acidic surface, that is considered essential for protein stability at high salinity. Interestingly, PspAG97A unusually contains a chloride ion coordinated by the guanidinium group of Arg171 and the main chain amide groups of Tyr172 and Glu173 at the active site. The structures of PspAG97A complexed with acarbose and panose demonstrate that residues Glu173, Arg171 and Asn170 for subsite +1 decide the substrate specificity of the enzyme for the α-1,6-glucosidic linkage...
September 16, 2016: Journal of Structural Biology
Jing Wei, Ling-Li Liu, Shuai Dong, Hui Li, Dan Tang, Qiang Zhang, Quan-Hong Xue, Jin-Ming Gao
Two new polyoxygenated cyclohexenone 'ketocarbasugars', named gabosines P and Q (1 and 2), were isolated from the culture of the actinomycete Streptomycetes strain no. 8, along with two known cyclic dipeptides. The structures and absolute configurations of the new metabolites were determined by spectroscopic data (1D- and 2D-NMR, HR-ESI-MS, and IR), chemical transformation, and electronic circular dichroism (ECD). These compounds were evaluated for α-glucosidase inhibitory activity in vitro. Only compound 1 exhibited IC50 values of 9...
October 15, 2016: Bioorganic & Medicinal Chemistry Letters
Rimke C Vos, Mariëlle Jp van Avendonk, Hanneke Jansen, Alexander N Goudswaard, Maureen van den Donk, Kees Gorter, Anneloes Kerssen, Guy Ehm Rutten
BACKGROUND: It is unclear whether people with type 2 diabetes mellitus on insulin monotherapy who do not achieve adequate glycaemic control should continue insulin as monotherapy or can benefit from adding oral glucose-lowering agents to the insulin therapy. OBJECTIVES: To assess the effects of insulin monotherapy compared with the addition of oral glucose-lowering agents to insulin monotherapy for people with type 2 diabetes already on insulin therapy and inadequate glycaemic control...
September 18, 2016: Cochrane Database of Systematic Reviews
Guangcheng Wang, Jing Wang, Dianxiong He, Xin Li, Juan Li, Zhiyun Peng
This study synthesized a series of novel coumarin-isatin derivatives and evaluated them for α-glucosidase inhibitory activity. The majority of the screened compounds exhibited excellent inhibition activities with IC50 values of 2.56 ± 0.08-268.79 ± 3.04 μm, when compared to acarbose. Among the newly derivatives, compound 5p was found to be the most active compound in the library of coumarin-isatin derivatives. Furthermore, enzyme kinetic studies showed that compound 5p is a non-competitive inhibitor with a Ki of 2...
September 12, 2016: Chemical Biology & Drug Design
Guangcheng Wang, Zhiyun Peng, Jing Wang, Juan Li, Xin Li
A novel series of N-arylbenzo[d]oxazol-2-amines (4a-4m) were synthesized and evaluated for their α-glucosidase inhibitory activity. Compounds 4f-4i, 4k and 4m displayed potent inhibitory activity against α-glucosidase with IC50 values in the range of 32.49±0.17-120.24±0.51μM as compared to the standard drug acarbose. Among all tested compounds, compound 4g having 4-phenoxy substitution at the phenyl ring was found to be the most active inhibitor of α-glucosidase with an IC50 value of 32.49±0.17μM. Analysis of the kinetics of enzyme inhibition indicated that compound 4g is a noncompetitive inhibitor of α-glucosidase with a Ki value of 31...
November 1, 2016: Bioorganic & Medicinal Chemistry
Aytaç Güdr
The majority of the antioxidant and antidiabetic activities of fruits are anthocyanins; a group of polyphenolics that are responsible for the color of many fruits, vegetables and flowers. The harvesting time, storage conditions, maturity, extraction steps etc. are very important for the biological activities based on the alteration of chemical composition. The free radical scavenging and antidiabetic activities of total anthocyanins from bitter melon (Momordica charantia Linn) fruit (TAMC) were evaluated by considering four harvesting times...
2016: Iranian Journal of Pharmaceutical Research: IJPR
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