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https://www.readbyqxmd.com/read/29223804/oxindole-based-oxadiazole-hybrid-analogs-novel-%C3%AE-glucosidase-inhibitors
#1
Muhammad Taha, Syahrul Imran, Fazal Rahim, Abdul Wadood, Khalid Mohammed Khan
Inhibition of α-glucosidase is an effective strategy for controlling post-prandial hyperglycemia in diabetic patients. Beside these α-glucosidase inhibitors has been also used as anti-obesity and anti-viral drugs. Keeping in view the greater importance of α-glucosidase inhibitors here in this study we are presenting oxindole based oxadiazoles hybrid analogs (1-20) synthesis, characterized by different spectroscopic techniques including 1H NMR and EI-MS and their α-glucosidase inhibitory activity. All compounds were found potent inhibitors for the enzyme with IC50 values ranging between 1...
December 2, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/29209017/new-hybrid-hydrazinyl-thiazole-substituted-chromones-as-potential-%C3%AE-amylase-inhibitors-and-radical-dpph-abts-scavengers
#2
Uzma Salar, Khalid Mohammed Khan, Sridevi Chigurupati, Muhammad Taha, Abdul Wadood, Shantini Vijayabalan, Mehreen Ghufran, Shahnaz Perveen
Current research is based on the identification of novel inhibitors of α-amylase enzyme. For that purpose, new hybrid molecules of hydrazinyl thiazole substituted chromones 5-27 were synthesized by multi-step reaction and fully characterized by various spectroscopic techniques such as EI-MS, HREI-MS, 1H-NMR and 13C-NMR. Stereochemistry of the iminic bond was confirmed by NOESY analysis of a representative molecule. All compounds 5-27 along with their intervening intermediates 1-4, were screened for in vitro α-amylase inhibitory, DPPH and ABTS radical scavenging activities...
December 5, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29208524/synthesis-in-vitro-%C3%AE-glucosidase-inhibitory-activity-and-docking-studies-of-novel-chromone-isatin-derivatives
#3
Guangcheng Wang, Ming Chen, Jie Qiu, Zhenzhen Xie, Anbai Cao
A novel series of chromone-isatin derivatives 6a-6p were designed, synthesized and characterized by 1H NMR, 13C NMR and HRMS. These novel synthetic compounds were evaluated for inhibitory activity against yeast α-glucosidase enzyme. The results of biological test have shown that all tested compounds exhibited excellent to potent inhibitory activity in the range of IC50 = 3.18 ± 0.12-16.59 ± 0.17 μM as compared to the standard drug acarbose (IC50 = 817.38 ± 6.27 μM). Compound 6j (IC50 = 3...
November 28, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29200718/%C3%AE-glucosidase-inhibitory-activity-from-ethyl-acetate-extract-of-antidesma-bunius-l-spreng-stem-bark-containing-triterpenoids
#4
Marista Gilang Mauldina, Rani Sauriasari, Berna Elya
Background: Buni (Antidesma bunius [L.] Spreng) has been used as a traditional antidiabetic agent in Asia. Objective: The mechanism of antidiabetic properties was studied in this study by determine its α-glucosidase inhibitory activity. Method: Inhibition of α-glucosidase was performed in all fraction of Buni stem bark with acarbose and miglitol as standards. The half maximal inhibitory concentration (IC50) value of acarbose and miglitol was 5...
October 2017: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/29200716/antioxidant-and-inhibitory-effects-of-saponin-extracts-from-dianthus-basuticus-burtt-davy-on-key-enzymes-implicated-in-type-2-diabetes-in-vitro
#5
Mikhail Olugbemiro Nafiu, Anofi Omotayo Tom Ashafa
Context: Dianthus basuticus is a plant of South African origin with various acclaimed pharmaceutical potentials. Aims: This study explored the antioxidant and antidiabetic activities of saponin extract from D. basuticus in vitro. Materials and Methods: Antioxidant activity of saponin was evaluated by 2,2-diphenyl-1-picrylhydrazyl (DPPH) and nitric oxide (*NO)-free radical scavenging activity while antidiabetic potentials were measured by the α-amylase and α-glucosidase inhibitory activities of the saponin extract...
October 2017: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/29194730/novel-pyridine-2-4-6-tricarbohydrazide-thiourea-compounds-as-small-key-organic-molecules-for-the-potential-treatment-of-type-2-diabetes-mellitus-in-vitro-studies-against-yeast-%C3%AE-and-%C3%AE-glucosidase-and-in-silico-molecular-modeling
#6
Tanzeel Ur Rehman, Sadaf Riaz, Islam Ullah Khan, Muhammad Ashraf, Marek Bajda, Alicja Gawalska, Muhammad Yar
A range of novel pyridine-2,4,6-tricarbohydrazide thiourea compounds (4a-i) were synthesized in good to excellent yields (63-92%). The enzyme inhibitory potentials of these compounds were investigated against α- and β-glucosidases because these enzymes play a crucial role in treating type-2 diabetes mellitus (T2DM). As compared to the reference compound acarbose (IC50 38.22 ± 0.12 μM), compounds 4i (IC50 25.49 ± 0.67 μM), 4f (IC50 28.91 ± 0.43 μM), 4h (IC50 30.66 ± 0.52 μM), and 4e (IC50 35...
December 1, 2017: Archiv der Pharmazie
https://www.readbyqxmd.com/read/29183150/effect-of-agave-americana-l-on-the-human-and-aspergillus-oryzae-s2-%C3%AE-amylase-inhibitions
#7
Mouna Sahnoun, Samir Bejar, Lobna Daoud, Leila Ayadi, Faiçal Brini, Walid Saibi
Among phenolic compounds, Agave americana L. extract contained puerarin (38.4%) and p-coumaric acid (12.29%) (pCa). From the Lineweaver-Burk plots, pCa and puerarin demonstrated a competitive and a non competitive inhibitions towards human α-amylase activity, respectively. PCa exhibited a higher human inhibitory activity with an IC50 of 98.8 μM which was about 2.3 times than acarbose. Puerarin (IC50 = 3.87 μM) and pCa (IC50 = 10.16 μM) also showed an excellent inhibition for Aspergillus oryzae S2 α-amylase activity...
November 28, 2017: Natural Product Research
https://www.readbyqxmd.com/read/29180050/potential-of-potentilla-inclinata-and-its-polyphenolic-compounds-in-%C3%AE-glucosidase-inhibition-kinetics-and-interaction-mechanism-merged-with-docking-simulations
#8
Didem Şöhretoğlu, Suat Sari, Michal Šoral, Burak Barut, Arzu Özel, Tibor Liptaj
In the present study we aimed to identify the α-glucosidase enzyme inhibitory potential of Potentilla inclinata Vill. MeOH and n-BuOH extracts which possessed remarkable α-glucosidase enzyme inhibitory effects with IC50 values of 1.06±0.02 and 0.93±0.01μg/ml respectively, compared to that of acarbose (IC50 31.92±0.17). Thus, BuOH extract was chosen for further phytochemical investigations. A phenolic acid, six flavonol glycosides, and two hydrolysable tannins were isolated from the most active n-BuOH extract of the title plant...
November 24, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/29176714/analyses-of-gut-microbiota-and-plasma-bile-acids-enable-stratification-of-patients-for-antidiabetic-treatment
#9
Yanyun Gu, Xiaokai Wang, Junhua Li, Yifei Zhang, Huanzi Zhong, Ruixin Liu, Dongya Zhang, Qiang Feng, Xiaoyan Xie, Jie Hong, Huahui Ren, Wei Liu, Jing Ma, Qing Su, Hongmei Zhang, Jialin Yang, Xiaoling Wang, Xinjie Zhao, Weiqiong Gu, Yufang Bi, Yongde Peng, Xiaoqiang Xu, Huihua Xia, Fang Li, Xun Xu, Huanming Yang, Guowang Xu, Lise Madsen, Karsten Kristiansen, Guang Ning, Weiqing Wang
Antidiabetic medication may modulate the gut microbiota and thereby alter plasma and faecal bile acid (BA) composition, which may improve metabolic health. Here we show that treatment with Acarbose, but not Glipizide, increases the ratio between primary BAs and secondary BAs and plasma levels of unconjugated BAs in treatment-naive type 2 diabetes (T2D) patients, which may beneficially affect metabolism. Acarbose increases the relative abundances of Lactobacillus and Bifidobacterium in the gut microbiota and depletes Bacteroides, thereby changing the relative abundance of microbial genes involved in BA metabolism...
November 27, 2017: Nature Communications
https://www.readbyqxmd.com/read/29142405/antihyperglycemic-activity-of-caralluma-fimbriata-an-in-vitro-approach
#10
Shenai Ashwini, Roy Anitha
Background: An increase in prevalence of diabetes mellitus necessitates the need to develop new drugs for its effective management. Plants and their bioactive compounds are found to be an alternative therapeutic approach. Caralluma fimbriata, used in this study, is well known for its various biological effects. Objective: The present study was designed to investigate the antihyperglycemic effect of the ethanolic leaf extract of C. fimbriata. Materials and Methods: Different concentrations (1-1000 mg/mL) of the ethanolic leaf extract of C...
October 2017: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/29142401/phytochemical-compositions-and-in-vitro-assessments-of-antioxidant-and-antidiabetic-potentials-of-fractions-from-ehretia-cymosa-thonn
#11
Akintayo Ogundajo, Anofi Tom Ashafa
Background: Ehretia cymosa Thonn. is a popular medicinal plant used in different parts of West Africa for the treatment of various ailments including diabetes mellitus. Objective: The current study investigates bioactive constituents and in vitro antioxidant and antidiabetic potentials of fractions from extract of E. cymosa. Materials and Methods: Phytochemical investigation and antioxidant assays were carried out using standard procedures...
October 2017: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/29138876/lower-risk-of-dementia-with-pioglitazone-compared-with-other-second-line-treatments-in-metformin-based-dual-therapy-a-population-based-longitudinal-study
#12
Chieh-Hsiang Lu, Chen-Yi Yang, Chung-Yi Li, Cheng-Yang Hsieh, Huang-Tz Ou
AIMS/HYPOTHESIS: The effect of pioglitazone was compared with that of other second-line glucose-lowering drugs on the risk of dementia among individuals with type 2 diabetes receiving metformin-based dual therapy. METHODS: A total of 204,323 individuals with type 2 diabetes aged ≥18 years who were stable metformin users and dementia-free before the initiation of second-line glucose-lowering medication were identified in the period 2000-2011 from Taiwan's National Health Insurance Research Database and followed to the end of 2013...
November 14, 2017: Diabetologia
https://www.readbyqxmd.com/read/29124880/costus-spiralis-jacq-roscoe-a-novel-source-of-flavones-with-%C3%AE-glycosidase-inhibitory-activity
#13
Ana P de Oliveira, Juliana S Coppede, Bianca W Bertoni, Antônio E M Crotti, Suzelei C França, Ana Maria S Pereira, Silvia H Taleb-Contini
Costus spiralis, a plant used in traditional Brazilian medicine for the treatment of complications in diabetes, was investigated. Assay of hexane, ethyl acetate, methanol and aqueous fractions obtained by partition of a crude methanol extract of dried leaves of C. spiralis revealed that AGI activity was confined to the ethyl acetate fraction. Purification of this fraction yielded schaftoside and isoschaftoside. The AGI activities of the two flavones were lower than, but comparable with, that of the anti-diabetic drug acarbose...
November 10, 2017: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/29116780/bioactive-asarone-derived-phenylpropanoids-from-the-rhizome-of-acorus-tatarinowii-schott
#14
En Gao, Zheng-Qun Zhou, Jian Zou, Yang Yu, Xiao-Lin Feng, Guo-Dong Chen, Rong-Rong He, Xin-Sheng Yao, Hao Gao
Eight new (1a/1b, 2a, 3a, 4a/4b, and 5a/5b) and seven known (2b, 3b, and 6-10) asarone-derived phenylpropanoids, a known asarone-derived lignan (12), and four known lignan analogues (11 and 13-15) were isolated from the rhizome of Acorus tatarinowii Schott. The structures were elucidated via comprehensive spectroscopic analyses, modified Mosher's method, and quantum chemical calculations. Compounds 1-8 were present as enantiomers, and 1-5 were successfully resolved via chiral-phase HPLC. Compounds 1a/1b were the first cases of asarone-derived phenylpropanoids with an isopropyl C-3 side-chain tethered to a benzene core from nature...
November 8, 2017: Journal of Natural Products
https://www.readbyqxmd.com/read/29112160/reclamation-of-marine-chitinous-materials-for-the-production-of-%C3%AE-glucosidase-inhibitors-via-microbial-conversion
#15
Van Bon Nguyen, San-Lang Wang
Six kinds of chitinous materials have been used as sole carbon/nitrogen (C/N) sources for producing α-glucosidase inhibitors (aGI) by Paenibacillus sp. TKU042. The aGI productivity was found to be highest in the culture supernatants using demineralized crab shell powder (deCSP) and demineralized shrimp shell powder (deSSP) as the C/N source. The half maximal inhibitory concentration (IC50) and maximum aGI activity of fermented deCSP (38 µg/mL, 98%), deSSP (108 µg/mL, 89%), squid pen powder (SPP) (422 µg/mL, 98%), and shrimp head powder (SHP) (455 µg/mL, 92%) were compared with those of fermented nutrient broth (FNB) (81 µg/mL, 93%) and acarbose (1095 µg/mL, 74%), a commercial antidiabetic drug...
November 7, 2017: Marine Drugs
https://www.readbyqxmd.com/read/29102178/synthesis-of-piperazine-sulfonamide-analogs-as-diabetic-ii-inhibitors-and-their-molecular-docking-study
#16
Muhammad Taha, Maryam Irshad, Syahrul Imran, Sridevi Chigurupati, Manikandan Selvaraj, Fazal Rahim, Nor Hadiani Ismail, Faisal Nawaz, Khalid Mohammed Khan
Piperazine Sulfonamide analogs (1-19) have been synthesized, characterized by different spectroscopic techniques and evaluated for α-amylase Inhibition. Analogs 1-19 exhibited a varying degree of α-amylase inhibitory activity with IC50 values ranging in between 1.571 ± 0.05 to 3.98 ± 0.397 μM when compared with the standard acarbose (IC50 = 1.353 ± 0.232 μM). Compound 1, 2, 3 and 7 showed significant inhibitory effects with IC50 value 2.348 ± 0.444, 2.064 ± 0.04, 1.571 ± 0.05 and 2...
December 1, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29084182/synthesis-biological-evaluation-and-molecular-docking-study-of-2-substituted-4-6-diarylpyrimidines-as-%C3%AE-glucosidase-inhibitors
#17
Zipeng Gong, Zhenzhen Xie, Jie Qiu, Guangcheng Wang
A novel series of 2-substituted-4,6-diarylpyrimidines 6a-6t has been synthesized, characterized by ¹H-NMR, (13)C-NMR and HRMS, and screened for in vitro α-glucosidase inhibitory activity. The majority of the screened compounds possessed significant α-glucosidase inhibitory activity with IC50 values ranging from 19.6 ± 0.21 to 38.9 ± 0.35 μM, which is more potent than the positive control α-glucosidase inhibitor acarbose (IC50 = 817.38 ± 6.27 μM). Among them, 6j was found to be the most active compound against α-glucosidase with an IC50 of 19...
October 30, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29084164/new-biflavonoids-with-%C3%AE-glucosidase-and-pancreatic-lipase-inhibitory-activities-from-boesenbergia-rotunda
#18
Nutputsorn Chatsumpun, Boonchoo Sritularak, Kittisak Likhitwitayawuid
Roots of Boesenbergia rotunda (L.) Mansf. are prominent ingredients in the cuisine of several Asian countries, including Thailand, Malaysia, Indonesia, India, and China. An extract prepared from the roots of this plant showed strong inhibitory activity against enzymes α-glucosidase and pancreatic lipase and was subjected to chromatographic separation to identify the active components. Three new biflavonoids of the flavanone-chalcone type (9, 12, and 13) were isolated, along with 12 known compounds. Among the 15 isolates, the three new compounds showed stronger inhibitory activity against α-glucosidase than the drug acarbose but displayed lower pancreatic lipase inhibitory effect than the drug orlistat...
October 30, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29082253/evaluation-of-antioxidant-potentials-and-%C3%AE-amylase-inhibition-of-different-fractions-of-labiatae-plants-extracts-as-a-model-of-antidiabetic-compounds-properties
#19
Soheila Moein, Elham Pimoradloo, Mahmoodreza Moein, Mahmood Vessal
In an attempt to identify herbal drugs which may become useful in the prevention of diabetes, antioxidant potentials and α-amylase inhibition by the ethanol extracts of two plants belonging to Lamiaceae family, Otostegia persica and Zataria multiflora, and their different fractions were studied. Also, inhibition of α-amylase by Salvia mirzayanii and its fractions was evaluated. All of the samples exhibited antioxidant activities, among which ethyl acetate fraction of Zataria multiflora (17.21 ± 0.17 mg GAE/g) was found to contain the highest amounts of phenols and the ethyl acetate fraction of Zataria multiflora (218 ± 2...
2017: BioMed Research International
https://www.readbyqxmd.com/read/29069819/comparison-of-twelve-single-drug-regimens-for-the-treatment-of-type-2-diabetes-mellitus
#20
Shao-Lian Wang, Wen-Bin Dong, Xiao-Lin Dong, Wen-Min Zhu, Fang-Fang Wang, Fang Han, Xin Yan
We performed a network meta-analysis to compare the efficacy of 12 single-drug regimens (Glibenclamide, Glimepiride, Pioglitazone, Rosiglitazone, Repaglinide, Metformin, Sitaglitin, Exenatide, Liraglutide, Acarbose, Benfluorex, and Glipizide) in the treatment of type 2 diabetes mellitus (T2DM). Fifteen relevant randomized controlled trials (RCTs) were included; direct and indirect evidence from these studies was combined, and weighted mean difference (WMD) and surface under the cumulative ranking curves (SUCRAs) were examined to evaluate the monotherapies...
September 22, 2017: Oncotarget
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