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Yang Li, Wei Zheng, Wuyun Qiqige, Shujuan Cao, Jishou Ruan, Yanping Zhang
Alzheimer's disease (AD) is a chronic and progressive neurodegenerative disorder and the pathogenesis of AD is poorly understood. G protein-coupled receptors (GPCRs) are involved in numerous key AD pathways and play a key role in the pathology of AD. To fully understand the pathogenesis of AD and design novel drug therapeutics, analyzing the connection between AD and GPCRs is of great importance. In this paper, we firstly build and analyze the AD-related pathway by consulting the KEGG pathway of AD and a mass of literature and collect 25 AD-related GPCRs for drug discovery...
2018: BioMed Research International
Fansheng Kong, Yaru Qin, Zhipeng Su, Zhengxiang Ning, Shujuan Yu
Grape seeds full with oil and also rich in hypoglycemic ingredients. This study is to improve the comprehensive utilization of grape seeds and the quality of grape seeds oil. Extract water soluble active substances before extracting oil from grape seeds, which show the grape seeds in water soluble extracts containing TP, TC, PC contents, respectively, are 171.1 ± 1.1, 658.8 ± 0.2, 482.3 ± 0.2 (mg GSAE/g). Also we found GSAE samples containing catechin and epicatechin were 44.12 ± 0.21 mg/mL, 111.23 ± 1...
April 18, 2018: Journal of Food Science
Can Xu, Ningbo Qin, Chunyan Yan, Shumei Wang
The root of Pueraria lobata is considered to be a medicinal and edible herb for the treatment of diabetes, and it has a long history of application in China. To explore the constituents responsible for the anti-hyperglycemic activities of P. lobata, a water-soluble polysaccharide (PL70-1-1) was isolated and purified by using a DEAE-Cellulose 52 anion exchange column and a Sephacryl S-100 gel filtration column. Its molecular weight (2584 Da) was determined by high performance gel permeation chromatography (HPGPC)...
April 18, 2018: Food & Function
He Li, Zhong-Bin Liao, Dan Tang, Wen-Bo Han, Qiang Zhang, Jin-Ming Gao
Four new secondary metabolites, chaetosemins G-J (1-4), along with 11 known ones (5-15) were isolated from the culture of C. seminudum C208 and Chaetomium sp. C521. Their structures were determined by extensive NMR spectroscopic analyses. These metabolites were evaluated in vitro for antifungal, antioxidant, toxicity, and α-glucosidase inhibitory activities. Chaetosemin J (4) and monaschromone (5) significantly inhibited the growth of four plant pathogenic fungi Botrytis cinerea, Alternaria solani, Magnaporthe oryzae, and Gibberella saubinettii with the minimum inhibitory concentrations (MIC) values ranging from 6...
April 16, 2018: Journal of Antibiotics
Anthony D Santilli, Elizabeth M Dawson, Kristi Whitehead, Daniel C Whitehead
A new approach for the non-microbicidal phenotypic manipulation of prominent gastrointestinal microbes is presented. Low micromolar concentrations of a chemical probe, acarbose, can selectively inhibit the Starch Utilization System and ablate the ability of Bacteroides thetaiotaomicron and B. fragilis strains to metabolize potato starch and pullulan. This strategy has potential therapeutic relevance for the selective modulation of the GI microbiota in a non-microbicidal manner.
April 16, 2018: ACS Chemical Biology
Hanae Naceiri Mrabti, Nidal Jaradat, Ismail Fichtali, Wessal Ouedrhiri, Shehdeh Jodeh, Samar Ayesh, Yahia Cherrah, My El Abbes Faouzi
Phytopharmaceuticals play an essential role in medicine, since the need to investigate highly effective and safe drugs for the treatment of diabetes mellitus disease remains a significant challenge for modern medicine. Arbutus unedo L. root has various therapeutic properties, and has been used widely in the traditional medicine as an antidiabetic agent. The current study aimed to isolate the pharmacologically active compound from A. unedo roots using accelerated solvent extraction technology, to determine its chemical structure using different instrumental analytical methods, and also to evaluate the α-glucosidase inhibitory activity...
April 12, 2018: Plants (Basel, Switzerland)
Muhammad Jihad Sandikapura, Shaik Nyamathulla, Mohamed Ibrahim Noordin
The study was aimed to perform aqueous extraction of two plants using different extraction methods, and evaluate their antioxidant and antidiabetic potential. Plant materials were extracted by maceration, soxhlet, sonication and fresh juice methods to produce aqueous extracts. In vitro antioxidant DPPH (1,1-diphenyl-2- picrylhydrazyl) and FRAP (Ferric reducing antioxidant power), antidiabetic α-amylase and α-glucosidase enzyme inhibitory assays were carried out on the extracts. Extracts of Syzygium polyanthum demonstrated better free radical scavenging and antidiabetic activity than Momordica charantia...
March 2018: Pakistan Journal of Pharmaceutical Sciences
John I Glendinning, Gabrielle S Lubitz, Sarah Shelling
We reported previously that when C57BL/6 (B6) mice ingest glucose, plasma insulin levels rise above baseline before blood glucose levels do so. This observation led us to speculate that the taste of glucose elicits cephalic-phase insulin release (CPIR) in mice. Here, we examined the specific contributions of taste and glucose to CPIR. In Experiment 1, we bypassed the mouth and delivered glucose directly to the stomach. We found that plasma insulin levels did not rise above baseline until after blood glucose levels did so...
April 2, 2018: Physiology & Behavior
Shazia Shah, Arshia, Kulsoom Javaid, Humaira Zafar, Khalid Mohammed Khan, Ruqaiya Khalil, Zaheer Ul-Haq, Shahnaz Perveen, M Iqbal Choudhary
Twenty-five derivatives of 5-chloro-2-aryl benzo[d]thiazole (1-25) were synthesized and evaluated for their α-glucosidase (S. cerevisiae EC inhibitory activity in vitro. Among them eight compounds showed potent activity with IC50 values between 22.1 ± 0.9 and 136.2 ± 5.7 μM, when compared with standard acarbose (IC50 = 840 ± 1.73 μM). The most potent compounds 4, 9, and 10 showed IC50 values in the range of 22.1 ± 0.9 to 25.6 ± 1.5 μM. Compounds 2, 5, 11, and 19 showed IC50 values within the range of 40...
February 12, 2018: Bioorganic Chemistry
Muhammad Tariq Javid, Fazal Rahim, Muhammad Taha, Haseeb Ur Rehman, Mohsan Nawaz, Abdul Wadood, Syahrul Imran, Imad Uddin, Ashik Mosaddik, Khalid Mohammed Khan
α-Glucosidase is a catabolic enzyme that regulates the body's plasma glucose levels by providing energy sources to maintain healthy functioning. 2-Amino-thiadiazole (1-13) and 2-amino-thiadiazole based Schiff bases (14-22) were synthesized, characterized by1 H NMR and HREI-MS and screened for α-glucosidase inhibitory activity. All twenty-two (22) analogs exhibit varied degree of α-glucosidase inhibitory potential with IC50 values ranging between 2.30 ± 0.1 to 38.30 ± 0.7 μM, when compare with standard drug acarbose having IC50 value of 39...
March 20, 2018: Bioorganic Chemistry
Guangcheng Wang, Zhiyun Peng, Zipeng Gong, Yongjun Li
A novel 5,6-diaryl-1,2,4-triazine thiazole derivatives (7a-7q) were synthesized and characterized by1 H NMR and13 C NMR and evaluated for their α-glucosidase inhibitory activity. All tested compounds displayed good α-glucosidase inhibitory activity with IC50 values ranging between 2.85 ± 0.13 and 14.19 ± 0.23 μM when compared to the standard drug acarbose (IC50  = 817.38 ± 6.27 μM). Compound 7i (IC50  = 2.85 ± 0.13 μM) exhibited the highest activity among this series of compounds...
March 21, 2018: Bioorganic Chemistry
Rabeb Ben Slama-Ben Salem, Naourez Ktari, Intidhar Bkhairia, Rim Nasri, Leticia Mora, Rim Kallel, Safa Hamdi, Kamel Jamoussi, Tahia Boudaouara, Abdelfettah El-Feki, Fidel Toldrá, Moncef Nasri
This study aims to examine the effects of non-hydrolyzed octopus (Octopus vulgaris) muscle proteins (NHOPs) and their hydrolysates (OPHs) on alloxan induced diabetes in Wistar rats (AIDR). Animals were allocated into seven groups of six rats each: control group (C), diabetic group (D) and diabetic rats treated with acarbose (D + Acar), non-hydrolyzed octopus proteins (D + NHOPs) and octopus proteins hydrolysates (D + OPHs) groups. The diabetic rats presented a significant increase in glycemic status such as α-amylase activity (in plasma, pancreas and intestine), hepatic glycogen, blood glucose and glycated hemoglobin (HbA1c) levels, as well as a significant decrease in the levels of plasma insulin and total hemoglobin compared to control group...
April 2018: Food Research International
Gurkamaljit Kaur, Bharati Pandey, Arbind Kumar, Naina Garewal, Abhinav Grover, Jagdeep Kaur
The lipolytic protein LipU was conserved in mycobacterium sp. including M. tuberculosis (MTB LipU) and M. leprae (MLP LipU). The MTB LipU was identified in extracellular fraction and was reported to be essential for the survival of mycobacterium. Therefore to address the problem of drug resistance in pathogen, LipU was selected as a drug target and the viability of finding out some FDA approved drugs as LipU inhibitors in both the cases was explored. Three dimensional (3D) model structures of MTB LipU and MLP LipU were generated and stabilized through molecular dynamics (MD)...
March 20, 2018: Journal of Biomolecular Structure & Dynamics
Qinqin Zhao, Huixin Xie, Yao Peng, Xinran Wang, Linquan Bai
The α-glucosidase inhibitor acarbose is commercially produced by Actinoplanes sp. and used as a potent drug in the treatment of type-2 diabetes. In order to improve the yield of acarbose, an efficient genetic manipulation system for Actinoplanes sp. was established. The conjugation system between E. coli carrying ØC31-derived integrative plasmids and the mycelia of Actinoplanes sp. SE50/110 was optimized by adjusting the parameters of incubation time of mixed culture (mycelia and E. coli ), quantity of recipient cells, donor-to-recipient ratio and the concentration of MgCl2 , which resulted in a high conjugation efficiency of 29...
December 2017: Synthetic and Systems Biotechnology
Akande Akinsola Adegboye, Khalid Mohammed Khan, Uzma Salar, Sherifat Adeyinka Aboaba, Kanwal, Sridevi Chigurupati, Itrat Fatima, Mohammad Taha, Abdul Wadood, Jahidul Isalm Mohammad, Huma Khan, Shahnaz Perveen
Despite of many diverse biological activities exhibited by benzimidazole scaffold, it is rarely explored for the α-amylase inhibitory activity. For that purpose, 2-aryl benzimidazole derivatives 1-45 were synthesized and screened for in vitro α-amylase inhibitory activity. Structures of all synthetic compounds were deduced by various spectroscopic techniques. All compounds revealed inhibition potential with IC50 values of 1.48 ± 0.38-2.99 ± 0.14 μM, when compared to the standard acarbose (IC50  = 1...
March 6, 2018: European Journal of Medicinal Chemistry
Janelle Guirguis-Blake, Gina A Keppel, John Holmes, Rex W Force, William Kriegsman, Laura-Mae Baldwin
Background: Patients with chronic kidney disease (CKD) are at high risk for adverse drug events related to medication dosing errors and prescriptions for relatively contraindicated medications, such as non-steroidal anti-inflammatory drugs (NSAIDs). Objectives: To examine the scope of and variation in prescribing relatively contraindicated medications and medications above the recommended dose levels among patients with stage III/IV CKD in primary care practice...
February 26, 2018: Family Practice
Akintayo Lanre Ogundajo, Lateef Apollo Adeniran, Anofi Omotayo Ashafa
OBJECTIVE: This study evaluates the phytochemical constituents, antioxidant and anti-inflammatory activity, cytotoxicity, and inhibitory activity against carbohydrate metabolism of extracts from Ocotea bullata stem bark. METHODS: Hexane, ethyl acetate, methanol and water were used to extract the air-dried sample. The phytochemical investigation and antioxidant assays were carried out on the extracts using standard procedures. The antidiabetic and anti-inflammatory potentials were evaluated using α-amylase, α-glucosidase and 5-lipoxygenase enzymes respectively...
March 2018: Journal of Integrative Medicine
Yan Duan, Jia Liu, Yuan Xu, Ning Yang, Wenying Yang, Guang Wang
INTRODUCTION: The Metformin and Acarbose in Chinese as the initial Hypoglycemic treatment (MARCH) trial has demonstrated a similar efficacy in HbA1c reduction between acarbose and metformin treatments in newly diagnosed type 2 diabetes mellitus (T2DM) patients. The current sub-analysis of the MARCH trail aims to evaluate the baseline characteristics that may influence the improvement of pancreatic β-cell function and insulin resistance after acarbose therapy in Chinese patients with newly diagnosed T2DM...
March 9, 2018: Diabetes Therapy: Research, Treatment and Education of Diabetes and related Disorders
Siva Prasad Kasturi, Sujatha Surarapu, Srinivas Uppalanchi, Shubham Dwivedi, Perumal Yogeeswari, Dilep Kumar Sigalapalli, Nagendra Babu Bathini, Krishna S Ethiraj, Jaya Shree Anireddy
Biological evaluation of 3,4-dihydroxy piperidines as α-glucosidase inhibitors is being reported for the first time. Forty-five derivatives (amides, di-amides and sulfonamides) were made using cis and trans 3,4-dihydroxy piperidines to evaluate their α-glucosidase inhibition activity. Polar groups (-OH, -NH2 ) on phenyl ring having derivatives 5i, 5l, 7g, 7i &12j showed excellent activity compared to standard references. Acarbose, Voglibose and Miglitol were used as standard references. Molecular docking simulations were done for compounds to identify important binding modes responsible for inhibition activity of α-glucosidase...
February 26, 2018: European Journal of Medicinal Chemistry
Sheng Wu, Li Tian
A new flavone glucoside tricetin 4'-O-β-glucopyranoside (1) and four known ellagitannins and flavones tricetin (2), luteolin (3), ellagic acid (4), and granatin B (5) were isolated from the flowers of Punica granatum L. (Lythraceae). Their structures were established by 1D and 2D NMR as well as mass spectrometry analyses. Among all tested compounds, tricetin (2) exhibited the strongest α-glucosidase inhibitory activity that was comparable to the anti-diabetic drug acarbose. Comparative structure-function analysis of tri-, tetra-, and pentahydroxy flavones [apigenin, luteolin (3), and tricetin (2), respectively] suggested that a greater number of hydroxyl groups on the flavone molecule enhanced its suppression of α-glucosidase, α-amylase, and lipase activities...
March 3, 2018: Natural Product Research
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