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Victoria K Gibbs, Rachel A Brewer, Nathan D Miyasaki, Amit Patki, Daniel L Smith
Acarbose, an alpha-glucosidase inhibitor used in treating type 2 diabetes, impairs complex carbohydrate digestion and absorption and extends lifespan in mice (without a requisite reduction in food intake). To assess sex-differential effects coincident with calorie restriction versus a non-restricted longevity enhancing intervention, we evaluated the metabolite profiles (by LC/MS) from livers and cecal contents of C57BL/6J mice (n=4/sex/group,) which were maintained for 10 months under one of three diet treatments: ad libitum control diet (CON), ad libitum control diet containing 0...
June 23, 2017: Journals of Gerontology. Series A, Biological Sciences and Medical Sciences
Syahrul Imran, Muhammad Taha, Manikandan Selvaraj, Nor Hadiani Ismail, Sridevi Chigurupati, Jahidul Islam Mohammad
A series of twenty indole hydrazone analogs (1-21) were synthesized, characterized by different spectroscopic techniques such as (1)H NMR and EI-MS, and screened for α-amylase inhibitory activity. All analogs showed a variable degree of α-amylase inhibition with IC50 values ranging between 1.66 and 2.65μM. Nine compounds that are 1 (2.23±0.01μM), 8 (2.44±0.12μM), 10 (1.92±0.12μM), 12 (2.49±0.17μM), 13 (1.66±0.09μM), 17 (2.25±0.1μM), 18 (1.87±0.25μM), 20 (1.83±0.63μM), and 19 (1.97±0.02μM) showed potent α-amylase inhibition when compared with the standard acarbose (1...
June 19, 2017: Bioorganic Chemistry
Uzma Hameed, Ian Price, Ikram-Ul-Haq, Ailong Ke, David B Wilson, Osman Mirza
Thermostable α-amylases have many industrial applications and are therefore continuously explored from novel sources. We present the characterization of a novel putative α-amylase gene product (Tp-AmyS) cloned from Thermotoga petrophila. The purified recombinant enzyme is highly thermostable and able to hydrolyze starch into dextrin between 90 and 100°C, with optimum activity at 98°C and pH8.5. The activity increased in the presence of Rb(1+), K(1+) and Ca(2+) ions, whereas other ions inhibited activity...
June 22, 2017: Biochimica et Biophysica Acta
Marcelo D Catarino, Artur M S Silva, Susana M Cardoso
Fucaceae is the most dominant algae family along the intertidal areas of the Northern Hemisphere shorelines, being part of human customs for centuries with applications as a food source either for humans or animals, in agriculture and as remedies in folk medicine. These macroalgae are endowed with several phytochemicals of great industrial interest from which phlorotannins, a class of marine-exclusive polyphenols, have gathered much attention during the last few years due to their numerous possible therapeutic properties...
June 21, 2017: International Journal of Molecular Sciences
Maryem Ben Salem, Rihab Ben Abdallah Kolsi, Raouia Dhouibi, Kamilia Ksouda, Slim Charfi, Mahdi Yaich, Serria Hammami, Zouheir Sahnoun, Khaled Mounir Zeghal, Kamel Jamoussi, Hanen Affes
BACKGROUND: Diabetes mellitus (DM) is associated with hyperglycemia, inflammatory disorders and abnormal lipid profiles, currently the extracts from leaves of cynara scolymus has been discovered to treat metabolic disorders and has been stated by multitudinous scientists according to a good source of polyphenols compounds. The present study aimed to evaluate the protective effect of the ethanol leaves extract of C. scolymus in alloxan induced stress oxidant, hepatic-kidney dysfunction and histological changes in liver, kidney and pancreas of different experimental groups of rats...
June 19, 2017: BMC Complementary and Alternative Medicine
Chi N Nguyen, Binh T D Trinh, Toan B Tran, Le-Thu T Nguyen, Anna K Jäger, Lien-Hoa D Nguyen
An ethyl acetate extract the bark of Garcinia xanthochymus exhibited strong inhibition towards α-glucosidase and PTP1B with IC50 values of 0.3±0.1μg/mL and 2.3±0.4μg/mL, respectively. Chemical constituents of the extract were therefore examined, and two new compounds, xanthochymusxanthones A (1) and B (2), along with ten known xanthones (3-12), were isolated. Their structures were determined using spectroscopic methods, mainly 1D and 2D NMR. Inhibitory activity of the isolated compounds was then tested, and subelliptenone F (12) showed significant effect towards α-glucosidase with IC50 value of 4...
June 8, 2017: Bioorganic & Medicinal Chemistry Letters
Afifa Mushtaq, Saqib Ali, Muhammad Tahir, Hammad Ismail, Bushra Mirza, Muhammad Saadiq, Muhammad Haleem, Muhammad Iqbal
Two new binuclear O-bridged copper(II) carboxylates with chemical formulas [Cu2(3-ClC6H4CH2COO)4(phen)2] (1) and [Cu2(3-ClC6H4CH2COO)4(bipy)2] (2) where phen = 1,10-phenanthroline and bipy = 2,2'-bipyridine have been synthesized and characterized by FT-IR, UV-Visible spectroscopy, CHN analysis and single crystal XRD. The results revealed distorted square pyramidal geometry around each copper atom of 1 and 2. The DNA interaction studies showed strong binding with Kb = 5.07 × 103 and 4.62 × 103 M-1 for 1 and 2, respectively...
June 2017: Acta Chimica Slovenica
Zhongjie Liu, Xiaodong Zhao, Weiwei Sun, Yaoxian Wang, Shangjian Liu, Lei Kang
The present meta-analysis aimed to evaluate metformin combined with acarbose compared with monotherapy with either of the two drugs for type 2 diabetes (T2DM). Relevant trials were retrieved through searching PubMed, Embase, Cochrane library, China National Knowledge Infrastructure, Wanfang and Chongqing VIP information network databases. Heterogeneous and homogeneous data were statistically combined using a random- and fixed-effects model, respectively. For dichotomous and continuous data, the merged effect size was presented as the risk ratio (RR) and weighted mean differences (WMD), respectively, with 95% confidence interval (CI)...
June 2017: Experimental and Therapeutic Medicine
Alexander A Spasov, Denis A Babkov, Tatyana Yu Prokhorova, Ekaterina A Sturova, Diana R Muleeva, Maxim R Demidov, Dmitry V Osipov, Vitaly A Osyanin, Yuri N Klimochkin
A series of benzofuran derivatives was synthesized as analogues of known natural α-glucosidase inhibitors. Their activity was evaluated in enzymatic assay and in rat model of diabetes mellitus. Newly identified inhibitors demonstrate significant potency with IC50 values ranging from 6.50 to 722.2 μM, as well as hypoglycemic activity exceeding the reference drug acarbose. Docking simulations provided insight to structure-activity relationships to direct further development of these novel hypoglycemic agents...
June 6, 2017: Chemical Biology & Drug Design
Dae Jung Kim, Yun Hwan Kang, Kyoung Kon Kim, Tae Woo Kim, Jae Bong Park, Myeon Choe
BACKGROUND/OBJECTIVES: Recent living condition improvements, changes in dietary habits, and reductions in physical activity are contributing to an increase in metabolic syndrome symptoms including diabetes and obesity. Through such societal developments, humankind is continuously exposed to metabolic diseases such as diabetes, and the number of the victims is increasing. This study investigated Cordyceps militaris water extract (CMW)-induced glucose uptake in HepG2 cells and the effect of CMW treatment on glucose metabolism...
June 2017: Nutrition Research and Practice
Xia Liu, Fang Luo, Pao Li, Yin She, Wanru Gao
Flavonoids, a class of natural drugs with broad biological activity, exhibit inhibitory effect on α-amylase. Citrus peel is a good source of flavonoids. The real-time interactions between three Citrus flavonoids (naringin, neohesperidin, hesperidin) and α-amylase were investigated by surface plasmon resonance biosensor, and were compared with the α-amylase inhibitors, acarbose. These results showed the binding affinities of naringin, neohesperidin and hesperidin with α-amylase reach the highest at pH6 with KD values of 2...
July 2017: Food Research International
Gaku Fukuhara, Mayuko Sasaki, Munenori Numata, Tadashi Mori, Yoshihisa Inoue
Saccharide sensing in aqueous media is an intriguing but challenging goal in current chemistry. Herein we report the oligosaccharide-sensing behavior of newly synthesized porphyrin-curdlan conjugates, which are random coils in DMSO but become globules in aqueous solutions to induce circular dichroism (ICD) in the biologically accessible spectral region due to the conformational fixation of porphyrin reporters. The magnitude of ICD was significantly varied specifically in the presence of acarbose, a drug for type-2 diabetes, enabling us to detect the amino-saccharide at concentrations down to 200 μM...
June 2, 2017: Chemistry: a European Journal
Albert J Zhang, Agnes M Rimando, Cassia S Mizuno, Suresh T Mathews
Dietary polyphenols have been shown to inhibit α-glucosidase, an enzyme target of some antidiabetic drugs. Resveratrol, a polyphenol found in grapes and wine, has been reported to inhibit the activity of yeast α-glucosidase. This triggered our interest to synthesize analogs and determine their effect on mammalian α-glucosidase activity. Using either sucrose or maltose as substrate resveratrol, piceatannol and 3'-hydroxypterostilbene showed strong inhibition of mammalian α-glucosidase activity; pinostilbene, cis-desoxyrhapontigenin and trans-desoxyrhapontigenin had moderate inhibition...
May 25, 2017: Journal of Nutritional Biochemistry
Nantiya Joycharat, Papawarin Issarachote, Chonlatid Sontimuang, Supayang Piyawan Voravuthikunchai
Albizia myriophylla Benth. is a medicinal herb which is used as a traditional remedy for various ailments including diabetes in Thailand. In our continued investigation of the biological activity of A. myriophylla, the ethanol extract, fractions and the isolated compounds from the wood of this plant were evaluated for in vitro α-glucosidase inhibition using spectrophotometric method. The plant ethanol extract and its different fractions possessed α-glucosidase inhibitory activity in a concentration-dependent manner...
May 31, 2017: Natural Product Research
Hamida Jdir, Rihab Ben Abdallah Kolsi, Sami Zouari, Khaled Hamden, Nacim Zouari, Nahed Fakhfakh
BACKGROUND: Type 2 diabetes mellitus is a prevalent systemic disease affecting an important proportion of the population worldwide. It has been suggested that excessive reactive oxygen species generation and therefore development of an oxidative stress status is a key factor leading to diabetic complications. Accordingly, it seems that medicinal plants can offer a wide range of new antidiabetic drugs. Diplotaxis simplex (Viv.) Spreng. (Brassicaceae) is an edible plant largely distributed in the Mediterranean region...
May 30, 2017: Lipids in Health and Disease
Hua Zhou, Hai-Mei Li, Yang-Min Du, Ri-An Yan, Shi-Yi Ou, Tian-Feng Chen, Yong Wang, Li-Xin Zhou, Liang Fu
YingDe black tea is produced from crude tea prepared from leaves of Camellia sinensis var. assamica. In this work, we isolated and identified five novel flavanones, namely, amelliaone A-E (1-5), along with seven known compounds 6-12 from the ethanol extract of YingDe black tea. The structures of these five novel phenolic compounds were determined using extensive 1D and 2D nuclear magnetic resonance spectroscopy experiments. The compounds were further evaluated for antioxidant, α-glucosidase inhibitory, and cytotoxic activities...
November 15, 2017: Food Chemistry
Qamar Abbas, Mubashir Hassan, Hussain Raza, Song Ja Kim, Ki-Wha Chung, Gwang-Hoon Kim, Sung-Yum Seo
OBJECTIVE: To evaluate the anti-hyperglycemic potential of sinigrin using in vitro, in silico and in vivo streptozotocin (STZ) induced hyperglycemic zebrafish model. METHODS: The in vitro enzyme inhibition assay was carried out to determine the IC50 value against α-glucosidase and α-amylase, in silico molecular docking was performed against both enzymes with PyRx tool and simulations were performed using GROMACS tool. Hyperglycemia was induced in zebrafishes using three intraperitoneal injections on alternating days for 1 week at 350 mg/kg of STZ...
April 2017: Asian Pacific Journal of Tropical Medicine
Lu Zhang, Zong-Cai Tu, Xing Xie, Hui Wang, Hao Wang, Zhen-Xing Wang, Xiao-Mei Sha, Yu Lu
Jackfruit (Artocarpus heterophyllus Lam.) peel is an underutilized by-product in both, the production and processing of jackfruit. This research compared the antioxidant and hypoglycemic potential of jackfruit peel with jackfruit pulp, flake and seed for the first time. The phytochemical profile of peel extract was characterized with HPLC-QTOF-MS/MS. Results revealed that peel extract exhibited the highest total phenolic and total flavonoid content, and the phenolics was 4.65, 4.12 and 4.95 times higher than that of pulp, flake and seed extract, respectively...
November 1, 2017: Food Chemistry
Marianna Sadagurski, Gillian Cady, Richard A Miller
Aging leads to hypothalamic inflammation, but does so more slowly in mice whose lifespan has been extended by mutations that affect GH/IGF-1 signals. Early-life exposure to GH by injection, or to nutrient restriction in the first 3 weeks of life, also modulate both lifespan and the pace of hypothalamic inflammation. Three drugs extend lifespan of UM-HET3 mice in a sex-specific way: acarbose (ACA), 17-α-estradiol (17αE2), and nordihydroguaiaretic acid (NDGA), with more dramatic longevity increases in males in each case...
May 20, 2017: Aging Cell
Faryal Chaudhry, Shahnaz Choudhry, Rahila Huma, Muhammad Ashraf, Mariya Al-Rashida, Rubina Munir, Ramsha Sohail, Bakhat Jahan, Munawar Ali Munawar, Misbahul Ain Khan
In search of better α-glucosidase inhibitors, a series of novel hetarylcoumarins (3a-3j) were designed and synthesized through a facile multicomponent route where p-toluenesulfonic acid (PTSA) was explored as an efficient catalyst. These new scaffolds were further evaluated for their α-glucosidase inhibition potentials. All the derivatives exhibited good to excellent results which were comparable or even better than of standard drug acarbose. Of these compounds, a dihalogenated compound 3f was found to be the most effective one with IC50: 2...
May 10, 2017: Bioorganic Chemistry
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