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Amir Ziaee, Neda Esmailzadehha, Maryam Honardoost
OBJECTIVE: All the aforementioned data have stimulated interest in studying other potential therapies for T1DM including noninsulin pharmacological therapies. The present study attempts to investigate the effect of adjunctive therapy with metformin and acarbose in patients with Type-1 diabetes mellitus. METHOD: In a single-center, placebo-controlled study (IRCT201102165844N1) we compared the results of two clinical trials conducted in two different time periods on 40 patients with Type-1 diabetes mellitus...
May 2017: Pakistan Journal of Medical Sciences Quarterly
En Gao, Fei-Fei Ren, Jian Zou, Yang Yu, Hong-Xia Fan, Zheng-Qun Zhou, Guo-Dong Chen, Rong-Rong He, Xin-Sheng Yao, Hao Gao
A new asarone-derived racemate (1) was isolated from the rhizome of Acorus tatarinowii. The structure of 1 was established by comprehensive spectroscopic analyses, and it was successfully resolved by chiral HPLC, demonstrating that it is racemic. The absolute configurations of 1a [(-)-acortatarone A] and 1b [(+)-acortatarone A] were determined using quantum chemical calculations. Compounds 1a and 1b were the first cases of asarone derivatives with the 5,7-dialkyl-6-aryl-8-oxabicyclo[3.2.1]oct-3-en-2-one core...
August 12, 2017: Fitoterapia
Songsong Zhang, Dandan Wu, Huan Li, Jinhua Zhu, Weiping Hu, Minghua Lu, Xiuhua Liu
Dioscorea opposita Thunb, commonly known as "yam" that has a long dietary therapy history for diabetes, is widely consumed as a botanical dietary supplement and widely cultivated in China. In this work, a method for rapid screening of α-glucosidase inhibitors from Dioscorea opposita Thunb peel extract was developed using α-glucosidase functionalized magnetic nanoparticles (αG-MNPs) as a solid phase extraction absorbent in combination with high performance liquid chromatography-mass spectrometry (HPLC-MS)...
August 15, 2017: Food & Function
E Chinedum, S Sanni, N Theressa, A Ebere
The effect of processing on starch digestibility, predicted glycemic indices (pGI), polyphenol contents and alpha amylase inhibitory properties of beans (Phaseolis vulgaris) and breadfruit (Treculia africana) was studied. Total starch ranged from 4.3 to 68.3g/100g, digestible starch ranged from 4.3 to 59.2 to 65.7g/100g for the raw and processed legumes; Resistance starch was not detected in most of the legumes except in fried breadfruit and the starches in both the raw and processed breadfruit were more rapidly digested than those from raw and cooked beans...
August 9, 2017: International Journal of Biological Macromolecules
Fan Xie, Shaoyun Wang, Li Zhang, Jinhong Wu, Zhengwu Wang
BACKGROUND: We synthesized a novel sericin peptide (SP-GI) with α-D-glucosidase inhibitory activity, which has a sequence of SEDSSEVDIDLGN. The kinetics of its peptide-induced inhibition on α-D-glucosidase activity and its interaction mechanism merging with molecular docking were both investigated. RESULTS: SP-GI exhibited significant inhibitory activity with an IC50 of 2.9 ± 0.1 μM and this inhibition was reversible and non-competitive with a Ki value of 1...
August 11, 2017: Journal of the Science of Food and Agriculture
Pervaiz Ali Channar, Aamer Saeed, Fayaz Ali Larik, Sajid Rashid, Qaiser Iqbal, Maryam Rozi, Saima Younis, Jamaluddin Mahar
Ten fused heterocyclic derivatives bearing the 2,6-di(subsituted phenyl)thiazolo[3,2-b]-1,2,4-triazoles as central rings were synthesized and structures of the compounds were established by analytical and spectral data using FTIR, EI-MS, (1)H NMR and (13)C NMR techniques. In vitro inhibitory activities of synthesized compounds on α-amylase, α-glucosidase and α-burylcholinesterase (α-BuChE) were evaluated using a purified enzyme assays. Compound 5c demonstrated strong and selective α-amylase inhibitory activity (IC50=1...
August 3, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
Madiha Kazmi, Sumera Zaib, Sayyeda Tayyeba Amjad, Imtiaz Khan, Aliya Ibrar, Aamer Saeed, Jamshed Iqbal
A series of iminothiazolines (4a-j) featuring 2,4,5-trichlorophenyl moiety and aroyl/heteroaroyl substituents has been prepared from readily accessible thioureas. In-vitro screening against glucosidase enzymes showed highly specific inhibition of α-glucosidase with a marked dependence of the potency upon the nature of the aroyl/heteroaroyl substituents. The most potent representatives, bearing ortho-tolyl and bulky naphthyl groups displayed the highest inhibitory potential with IC50 value of 0.15±0.01µM compared to standard drug acarbose (IC50=38...
July 25, 2017: Bioorganic Chemistry
Shazia Iqbal, Maria Aqeel Khan, Kulsoom Javaid, Rabia Sadiq, Saba Fazal-Ur-Rehman, M Iqbal Choudhary, Fatima Z Basha
In the present study, a series of new carbazole linked 1H-1,2,3-triazoles (2-27) were synthesized via click reaction of N-propargyl-9H-carbazole (1) and azides of appropriate acetophenones and heterocycles. Synthesized carbazole triazoles including 7, 9, 10, 19, 20, and 23-26 (IC50=0.8±0.01-100.8±3.6μM), exhibited several folds more potent α-glucosidase inhibitory in vitro activity as compared to standard drug, acarbose. Compounds 2-5, 7-13, and 17-27 did not show any cytotoxicity against 3T3 cell lines, except triazoles 6, and 14-16...
July 16, 2017: Bioorganic Chemistry
Didem Şöhretoğlu, Suat Sari, Arzu Özel, Burak Barut
α-Glucosidase enzyme inhibitors are clinically used for the treatment of Type 2 diabetes mellitus. We tested α-glucosidase inhibitory effects of Potentilla astracanica Jacq. extracts (1, 2), two compounds isolated from these extracts, prunetin 5-O-β-glucopyranoside (3) and genistein 5-O-β-glucopyranoside (4), and their aglycon forms (5 and 6). All the tested materials possessed remarkable α-glucosidase inhibitor activity compared to the positive control, acarbose. Genistein (6) showed the highest activity with an IC50 value of 1...
July 27, 2017: International Journal of Biological Macromolecules
Muhammad Taha, Fazal Rahim, Syahrul Imran, Nor Hadiani Ismail, Hayat Ullah, Manikandan Selvaraj, Muhammad Tariq Javid, Uzma Salar, Muhammad Ali, Khalid Mohammed Khan
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 (1)H NMR, EI-MS, and (13)C NMR. Elemental analysis was found in agreement with the calculated values...
July 18, 2017: Bioorganic Chemistry
Jie Ren, Shuang-Shuang Ding, Ao Zhu, Fei Cao, Hua-Jie Zhu
Six new azaphilone derivatives, talaraculones A-F (1-6), together with five known analogues (7-11), were obtained from the saline soil-derived fungus Talaromyces aculeatus. The absolute configurations of 1 and 6 were assigned by quantum chemical calculations of the electronic circular dichroism (ECD) spectra. Compounds 1 and 5 represent the first reported azaphilone derivatives with a C4 aliphatic side chain and a methylal group at C-3, respectively. Talaraculones A and B (1 and 2) exhibited stronger inhibitory activity against α-glucosidase than the positive control acarbose (IC50 = 101...
July 27, 2017: Journal of Natural Products
Maria A Khan, Kulsoom Javaid, Abdul Wadood, Alam Jamal, Farhana Batool, Saba Fazal-Ur-Rehman, Fatima Z Basha, M Iqbal Choudhary
BACKGROUND: α-Glucosidase inhibitors (AGIs) have been reported for their clinical potential against postprandial hyperglycemia, which is responsible for risks associated with diabetes mellitus 2 and cardiovascular diseases (CVDs). Besides, a number of compounds have been reported as potent AGIs, several side effects are associated with them. METHODS: The aim of present work is to explore new and potent molecules as AGIs. Therefore, a library of dibenzoazepine linked triazoles (1-15) was studied for their in vitro α-glucosidase inhibitory activity...
July 26, 2017: Medicinal Chemistry
Timo Wolf, Julian Droste, Tetiana Gren, Vera Ortseifen, Susanne Schneiker-Bekel, Till Zemke, Alfred Pühler, Jörn Kalinowski
BACKGROUND: Acarbose is used in the treatment of diabetes mellitus type II and is produced by Actinoplanes sp. SE50/110. Although the biosynthesis of acarbose has been intensively studied, profound knowledge about transcription factors involved in acarbose biosynthesis and their binding sites has been missing until now. In contrast to acarbose biosynthetic gene clusters in Streptomyces spp., the corresponding gene cluster of Actinoplanes sp. SE50/110 lacks genes for transcriptional regulators...
July 25, 2017: BMC Genomics
Eisuke Kato, Natsuka Kushibiki, Yosuke Inagaki, Mihoko Kurokawa, Jun Kawabata
Type 2 diabetes mellitus (T2DM) is a common global health problem. Prevention of this disease is an important task, and functional food supplements are considered an effective method. We found potent pancreatic α-amylase inhibition in Astilbe thunbergii root extract (AT) and confirmed that AT treatment in a T2DM rat model reduces post-starch administration blood glucose levels. Activity-guided isolation revealed procyanidin (AT-P) as the α-amylase inhibitory component with IC50 = 1.7 μg/mL against porcine pancreatic α-amylase...
September 2017: Bioscience, Biotechnology, and Biochemistry
Yen-Hsiu Liao, Yi-Ping Lo, Yu-Kai Liao, Chien-Hung Lin
No abstract text is available yet for this article.
July 2017: American Journal of Gastroenterology
Muhammad Taha, Syahrul Imran, Nor Hadiani Ismail, Manikandan Selvaraj, Fazal Rahim, Sridevi Chigurupati, Hayat Ullah, Fahad Khan, Uzma Salar, Muhammad Tariq Javid, Shantini Vijayabalan, Khalid Zaman, Khalid Mohammed Khan
A new library of 2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethyl aryl ether derivatives (1-23) were synthesized and characterized by EI-MS and (1)H NMR, and screened for their α-amylase inhibitory activity. Out of twenty-three derivatives, two molecules 19 (IC50=0.38±0.82µM) and 23 (IC50=1.66±0.14µM), showed excellent activity whereas the remaining compounds, except 10 and 17, showed good to moderate inhibition in the range of IC50=1.77-2.98µM when compared with the standard acarbose (IC50=1.66±0.1µM). A plausible structure-activity relationship has also been presented...
July 11, 2017: Bioorganic Chemistry
Zui Fujimoto, Nobuhiro Suzuki, Naomi Kishine, Hitomi Ichinose, Mitsuru Momma, Atsuo Kimura, Kazumi Funane
Paenibacillus sp. 598K α-1,6-glucosyltransferase (Ps6TG31A), a member of glycoside hydrolase family 31, catalyzes exo-α-glucohydrolysis and transglucosylation and produces α-1,6-glucosyl-α-glucosaccharides from α-glucan via its disproportionation activity. The crystal structure of Ps6TG31A was determined by an anomalous dispersion method using a terbium derivative. The monomeric Ps6TG31A consisted of one catalytic (β/α)8-barrel domain and six small domains, one on the N-terminal and five on the C-terminal side...
August 7, 2017: Biochemical Journal
Rade Vukovic, Tatjana Milenkovic, Maja Djordjevic, Katarina Mitrovic, Sladjana Todorovic, Adrijan Sarajlija, Khalid Hussain
BACKGROUND: Postprandial hyperinsulinemic hypoglycemia (PHH) is an increasingly recognized complication of gastric bypass surgery in obese adults, distinct from the "dumping syndrome". CASE PRESENTATION: Upon birth, primary repair of esophageal atresia was performed, and at the age of 14 months definite esophageal reconstruction was performed. At the age of 3 years, recurrent brief episodes of symptomatic hypoglycemia started. At the age of 5.7 years the girl was admitted to our clinic and investigations indicated hyperinsulinemic hypoglycemia...
June 24, 2017: Journal of Pediatric Endocrinology & Metabolism: JPEM
Chatchaporn Uraipong, Jian Zhao
BACKGROUND: The bioactivities of peptides released from the digestion of rice bran protein under in vitro simulated human digestive conditions were investigated. Four protein fractions extracted from rice bran were digested and the hydrolysates were fractionated by ultrafiltration and anion exchange chromatography. α-Glucosidase and angiotensin converting enzyme (ACE) inhibitory activities of the crude hydrolysates and their fractions were determined. RESULTS: Peptides with MW < 3 kDa gave markedly higher α-glucosidase inhibitory activities than the crude digests while the ACE-inhibitory activities of the MW <3 kDa fractions were similar to those of crude extracts...
July 5, 2017: Journal of the Science of Food and Agriculture
Rade Vukovic, Tatjana Milenkovic, Maja Djordjevic, Katarina Mitrovic, Sladjana Todorovic, Adrijan Sarajlija, Khalid Hussain
BACKGROUND: Postprandial hyperinsulinemic hypoglycemia (PHH) is an increasingly recognized complication of gastric bypass surgery in obese adults, distinct from the "dumping syndrome". CASE PRESENTATION: Upon birth, primary repair of esophageal atresia was performed, and at the age of 14 months definite esophageal reconstruction was performed. At the age of 3 years, recurrent brief episodes of symptomatic hypoglycemia started. At the age of 5.7 years the girl was admitted to our clinic and investigations indicated hyperinsulinemic hypoglycemia...
July 26, 2017: Journal of Pediatric Endocrinology & Metabolism: JPEM
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