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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
Bo-Wei Zhang, Yuan-Bin Sang, Wen-Long Sun, He-Shui Yu, Bai-Ping Ma, Zhi-Long Xiu, Yue-Sheng Dong
The combined effect of Oroxylum indicum seed extracts (OISE) or major flavonoids from OISE and acarbose on reducing postprandial blood glucose (PBG) levels was investigated in vitro and in vivo. In vitro, the IC50 values of OISE and baicalein against α-glucosidase were 43.4±0.731μgmL(-1) and 25.9±0.412μgmL(-1) respectively. A combination of acarbose with OISE or baicalein synergistically inhibited rat intestinal α-glucosidase. The combination index (CI) values for acarbose with OISE ranged from 0.33 to 0...
May 12, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
Guangcheng Wang, Ming Chen, Jing Wang, Yaping Peng, Luyao Li, ZhenZhen Xie, Bing Deng, Shan Chen, Wenbiao Li
A series of chromone hydrazone derivatives 4a-4p have been synthesized, characterized by (1)H NMR and (13)C NMR and evaluated for theirinvitro α-glucosidase inhibitory activity. Out of these tested compounds, six (4a, 4b, 4d, 4j, 4o and 4p) displayed potent α-glucosidase inhibitory activity with IC50 values in the range of 20.1±0.19μM to 45.7±0.23μM, as compared to the standard drug acarbose (IC50=817.38±6.27μM). Among this series, compound 4d (IC50=20.1±0.19μM) with 4-sulfonamide substitution at phenyl part of hydrazide was found to be the most active compound...
May 5, 2017: Bioorganic & Medicinal Chemistry Letters
Weiheng Kong, Di Wu, Lian Xia, Xuefeng Chen, Guoliang Li, Nannan Qiu, Guang Chen, Zhiwei Sun, Jinmao You, Yongning Wu
Recently, α-glucosidase inhibitor has been widely used in clinic for diabetic therapy. In the present study, a facile and sensitive fluorescent assay based on enzyme activated inner filter effect (IFE) on nitrogen-doped carbon dots (CDs) was first developed for the detection of α-glucosidase. The N-doped CDs with green emission were prepared by a one-step hydrothermal synthesis and gave the fluorescence quantum yield of 30%, which were used as the signal output. Through α-glucosidase catalysis, 4-nitrophenol was released from 4-nitrophenyl-α-d-glucopyranoside (NGP)...
June 22, 2017: Analytica Chimica Acta
Luana Pulvirenti, Vera Muccilli, Nunzio Cardullo, Carmela Spatafora, Corrado Tringali
A chemoenzymatic synthesis of a small library of dimeric neolignans inspired by magnolol (1) is reported. The 2-iodoxybenzoic acid (IBX)-mediated regioselective ortho-hydroxylation of magnolol is described, affording the bisphenols 6 and 7. Further magnolol analogues (12, 13, 15-17, 19-23) were obtained from eugenol (3), tyrosol (4), and homovanillic alcohol (5), through horseradish peroxidase (HRP)-mediated oxidative coupling and regioselective ortho-hydroxylation or ortho-demethylation in the presence of IBX, followed by reductive treatment with Na2S2O4...
May 12, 2017: Journal of Natural Products
Guilin Chen, Mingquan Guo
Gymnema sylvestre R. Br. (Asclepiadaceae) has been known to posses potential anti-diabetic activity, and the gymnemic acids were reported as the main bioactive components in this plant species. However, the specific components responsible for the hypoglycemic effect still remain unknown. In the present study, the in vitro study revealed that the extract of G. sylvestre exhibited significant inhibitory activity against α-glucosidase with IC50 at 68.70 ± 1.22 μg/mL compared to acarbose (positive control) at 59...
2017: Frontiers in Pharmacology
Sivaprasad Kasturi, Sujatha Surarapu, Srinivas Uppalanchi, Jaya Shree Anireddy, Shubham Dwivedi, Hasitha Shilpa Anantaraju, Yogeeswari Perumal, Dilep Kumar Sigalapalli, Bathini Nagendra Babu, Krishna S Ethiraj
A new series of Deacetylsarmentamide A and B derivatives, amides and sulfonamides of 3,4-dihydroxypyrrolidines as α-glucosidase inhibitors were designed and synthesized. The biological screening test against α-glucosidase showed that some of these compounds have the positive inhibitory activity against α-glucosidase. Saturated aliphatic amides were more potent than the olefinic amides. Among all the compounds, 5o/6o having polar -NH2 group, 10f/11f having polar -OH group on phenyl ring displayed 3-4-fold more potent than the standard drugs...
May 2, 2017: Bioorganic & Medicinal Chemistry Letters
Jing Li, Bing Niu, Xiaoling Wang, Huaiqiang Hu, Bingzhen Cao
RATIONALE: Hereditary neuropathy with liability to pressure palsy (HNPP) is an episodic, multifocal neuropathy, with a typical clinical presentation of recurrent transient pressure palsies, which is induced by a PMP22 deletion. Another neuropathy caused by a PMP22 duplication is Charcot-Marie-Tooth disease type 1A (CMT1A). PMP22 is a gene coding a protein called peripheral myelin protein 22 (PMP22), which plays an essential role in the formation and maintenance of compact myelin. Coexistence of type 2 diabetes mellitus (T2DM) and CMT1A has been reported in many work, however HNPP patients with T2DM are rare, and comorbidity of HNPP and psoriasis has not been reported previously...
May 2017: Medicine (Baltimore)
Qiang Zhang, Hao-Yu Tang, Min Chen, Jie Yu, Hui Li, Jin-Ming Gao
(-)-β-Caryophyllene was decorated with a privileged β-lactam motif and subsequently converted into highly diverse scaffolds via remodeling of the ring system. The structures were defined by spectroscopic data, X-ray diffraction analysis, and experimental and calculated ECD data. Compound 19 displayed the most potent activity against the rice blast fungus, while 6 had a more potent α-glucosidase inhibition than the drug acarbose. These findings demonstrate a concise protocol to exploit natural product-driven diversity...
May 23, 2017: Organic & Biomolecular Chemistry
Tayyaba Noreen, Muhammad Taha, Syahrul Imran, Sridevi Chigurupati, Fazal Rahim, Manikandan Selvaraj, Nor Hadiani Ismail, Jahidul Islam Mohammad, Hayat Ullah, Muhammad Tariq Javid, Faisal Nawaz, Maryam Irshad, Muhammad Ali
Twenty five derivatives of indole carbohydrazide (1-25) had been synthesized. These compounds were characterized using (1)H NMR and EI-MS, and further evaluated for their α-amylase inhibitory potential. The analogs (1-25) showed varying degree of α-amylase inhibitory potential. ranging between 9.28 and 599.0µM when compared with standard acarbose having IC50 value 8.78±0.16µM. Six analogs, 25 (IC50=9.28±0.153µM), 22 (IC50=9.79±0.43µM), 4 (IC50=11.08±0.357µM), 1 (IC50=12.65±0.169µM), 8 (IC50=21...
April 21, 2017: Bioorganic Chemistry
Guangcheng Wang, Jing Wang, Zhenzhen Xie, Ming Chen, Luyao Li, Yaping Peng, Shan Chen, Wenbiao Li, Bin Deng
3,3-Di(indolyl)indolin-2-ones 4a-4n were synthesized and evaluated for their in vitro α-glucosidase inhibitory activity. These newly synthesized compounds showed moderate to potent α-glucosidase inhibitory activity with IC50 range from 5.98±0.11 to 145.95±0.46μM, when compared to the standard drug acarbose. Among this series of 3,3-di(indolyl)indolin-2-ones, compound 4j(5.98±0.11μM) having a 2-fluorobenzyl group on the indole ring was found to be the most active compound. Molecular docking studies showed that compound 4j have high binding affinities with the active site of α-glucosidase enzyme through hydrogen bonds, arene-cation, π-π stacking and hydrophobic interactions...
May 3, 2017: Bioorganic Chemistry
Anjali Verma, Anil Kumar, Dalip Kumar Upreti, Veena Pande, Mahesh Pal
BACKGROUND: Leucas cephalotes has been used by many tribes to treat variety of diseases and known to have many essential secondary metabolites. To the best of our knowledge, it is the first comparative analysis of total fatty acid (FA) composition and α-amylase inhibition activity of L. cephalotes. OBJECTIVE: The present study is carried out to explore the antihyperglycemic activity and FA contents of all parts of L. cephalotes. MATERIAL AND METHOD: Fruits, leaves, stems, and roots part of L...
January 2017: Pharmacognosy Magazine
Giuseppe Derosa, Pamela Maffioli, Angela D'Angelo, Elena Fogari, Lucio Bianchi, Arrigo F G Cicero
This article has been retracted: please see Elsevier Policy on Article Withdrawal (
May 3, 2017: Journal of Diabetes and its Complications
Firdoz Shaik, Anil Kumar
The authors report a controlled synthesis of biocompatible ZnO and acarbose-capped nanohybrids, and examined the inhibition activities of these nanosystems with human salivary α-amylase (HSA) activity. XRD measurements reveal ZnO present in wurtzite phase with hexagonal structure. The average size of ZnO particles for the two studied nanosystems was estimated to lie between 10 to 12 nm using Scherrer equation. These particles depict the onset of absorption at about 320 nm and the band-gap emission at about 370 nm, which are fairly blue shifted as compared with the bulk ZnO and have been understood due to the size quantisation effect...
April 2017: IET Nanobiotechnology
Cecilia Chi, Jennifer Snaith, Jenny E Gunton
INTRODUCTION: Patients with type 2 diabetes have an increased risk of developing adverse cardiovascular (CV) outcomes. The evidence relating to the effects of glucose-lowering medications on CV outcomes is of variable quality and there are numerous trials ongoing. RESULTS: In this review, we summarise the available literature on CV outcomes of the following diabetes treatments: metformin, the sulfonylureas, acarbose, glucagon-like peptide 1 (GLP1) receptor agonists, dipeptidyl peptidase-4 inhibitors (DPP4i), sodium-glucose co-transporter 2 inhibitors (SGLT2i), thiazolidinediones (TZDs) and insulin...
April 10, 2017: Heart, Lung & Circulation
Hyun Ah Jung, Pradeep Paudel, Su Hui Seong, Byung-Sun Min, Jae Sue Choi
Naturally occurring flavonoids co-exist as glycoside conjugates, which dominate aglycones in their content. To unveil the structure-activity relationship of a naturally occurring flavonoid, we investigated the effects of the glycosylation of naringenin on the inhibition of enzyme systems related to diabetes (protein tyrosine phosphatase 1B (PTP1B) and α-glycosidase) and on glucose uptake in the insulin-resistant state. Among the tested naringenin derivatives, prunin, a single-glucose-containing flavanone glycoside, potently inhibited PTP1B with an IC50 value of 17...
April 18, 2017: Bioorganic & Medicinal Chemistry Letters
Kristina Bljajić, Roberta Petlevski, Lovorka Vujić, Ana Čačić, Nina Šoštarić, Jasna Jablan, Isabel Saraiva de Carvalho, Marijana Zovko Končić
Vaccinium myrtillus (bilberry) leaf is traditionally used in southeastern Europe for the treatment of diabetes. In the present study, the ability of bilberry leaf extracts to inhibit carbohydrate-hydrolyzing enzymes and restore glutathione concentration in Hep G2 cells subjected to glucose-induced oxidative stress was investigated. A comprehensive analysis of the antioxidant activity of two bilberry leaf extracts was performed. The aqueous extract showed excellent total antioxidant and chelating activity. Its antioxidant activity in the β-carotene-linoleic acid assay was very good, reaching the activity of the antioxidant standard BHA (93...
April 28, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Timo Wolf, Susanne Schneiker-Bekel, Armin Neshat, Vera Ortseifen, Daniel Wibberg, Till Zemke, Alfred Pühler, Jörn Kalinowski
Actinoplanes sp. SE50/110 is the natural producer of acarbose, which is used in the treatment of diabetes mellitus type II. However, until now the transcriptional organization and regulation of the acarbose biosynthesis are only understood rudimentarily. The genome sequence of Actinoplanes sp. SE50/110 was known before, but was resequenced in this study to remove assembly artifacts and incorrect base callings. The annotation of the genome was refined in a multi-step approach, including modern bioinformatic pipelines, transcriptome and proteome data...
April 17, 2017: Journal of Biotechnology
Zhenzhen Xie, Guangcheng Wang, Jing Wang, Ming Chen, Yaping Peng, Luyao Li, Bing Deng, Shan Chen, Wenbiao Li
A series of novel isatin-thiazole derivatives were synthesized and screened for their in vitro α-glucosidase inhibitory activity. These compounds displayed a varying degree of α-glucosidase inhibitory activity with IC50 ranging from 5.36 ± 0.13 to 35.76 ± 0.31 μm as compared to the standard drug acarbose (IC50 = 817.38 ± 6.27 μm). Among the series, compound 6p bearing a hydroxyl group at the 4-position of the right phenyl and 2-fluorobenzyl substituent at the N1-positions of the 5-methylisatin displayed the highest inhibitory activity with an IC50 value of 5...
April 20, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Michal Shani, Alex Lustman, Shlomo Vinker
AIM: To assess the persistence of diabetic patients to oral medications. METHODS: The study included all type 2 diabetic patients over 40 years, members of one District of Clalit Health Services Israel, who were diagnosed with diabetes mellitus before 2008 and who filled at least one prescription per year during 2008-2010, for the following medications: metformin, glibenclamide, acarbose, statins, angiotensin converting enzyme inhibitors (ACEI) and angiotensin II receptor antagonists (ARBs)...
April 15, 2017: Primary Care Diabetes
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