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Ganiyu Oboh, Sunday I Oyeleye, Omoyemi A Akintemi, Tosin A Olasehinde
There are strong correlations between diabetes mellitus and cognitive dysfunction. This study sought to investigate the modulatory effects of Moringa oleifera leaf (ML) and seed (MS) inclusive diets on biomolecules [acetylcholinesterase (AChE), butyrylcholinesterase (BChE)] angiotensin-I converting enzyme (ACE), arginase, catalase, glutathione transferase (GST) and glutathione peroxidase (GSH-Px) activities, glutathione (GSH) and nitric oxide (NO) levels] associated with cognitive function in the brain of streptozotocin (STZ)-induced diabetic rats treated with acarbose (ACA)...
February 12, 2018: Metabolic Brain Disease
Sajjad Lalegani, Hassan Ahmadi Gavlighi, Mohammad Hossein Azizi, Roghayeh Amini Sarteshnizi
Phenolic compounds as agro-industrial by-products have been associated with health benefits since they exhibit high antioxidant activity and anti-diabetic properties. In this study, polyphenol-rich extract from pistachio green hull (PGH) was evaluated for antioxidant activity and its ability to inhibit α-amylase and α-glucosidase activity in vitro. The effect of PGH extract powder on in vitro starch digestibility was also evaluated. The results showed that PGH had stronger antioxidant activity than Trolox...
March 2018: Food Research International
Meng-Hsun Yu, Ming-Cheng Lin, Chien-Ning Huang, Kuei-Chuan Chan, Chau-Jong Wang
Atherosclerosis involves the proliferation and migration of vascular smooth muscle cells (VSMCs). The migration of VSMCs from the media into the intima and their subsequent proliferation are important processes in neointima formation in atherosclerosis and restenosis after percutaneous coronary interventions. Acarbose, an alpha-glucosidase inhibitor, has been demonstrated to not affect serum levels of glucose and decrease the progression of intima-media thickening in rabbits fed with a high cholesterol diet (HCD)...
February 9, 2018: Vascular Pharmacology
Wenlong Sun, Bowei Zhang, Xiaoxia Yu, Chunlin Zhuang, Xia Li, Jin Sun, Yan Xing, Zhilong Xiu, Yuesheng Dong
BACKGROUND: Oroxylum indicum (L.) Kurz (Bignoniaceae) has been widely used for the treatment of respiratory infections and gastrointestinal disorders. Our previous study showed that an ethanol-water O. indicum seed extract (OISE), when combined with acarbose, reduced the risk of diabetes by 75% and effectively prevented the associated complications. Oroxin A, a major component of OISE, can activate PPARγ and inhibit α-glucosidase and it represents a promising candidate for diabetes intervention...
January 1, 2018: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
Adriano Mollica, Gokhan Zengin, Serdar Durdagi, Ramin Ekhteiari Salmas, Giorgia Macedonio, Azzurra Stefanucci, Marilisa Pia Dimmito, Ettore Novellino
Human α-glucosidase is an enzyme involved in the catalytic cleavage of the glucoside bond and involved in numerous functionalities of the organism, as well as in the insurgence of diabetes mellitus 2 and obesity. Thus, developing chemicals that inhibit this enzyme is a promising approach for the treatment of several pathologies. Small peptides such as di- and tri-peptides may be in natural organism as well as in the GI tract in high concentration, coming from the digestive process of meat, wheat and milk proteins...
February 8, 2018: Journal of Biomolecular Structure & Dynamics
Hamideh Nikookar, Maryam Mohammadi-Khanaposhtani, Somaye Imanparast, Mohammad Ali Faramarzi, Parviz Rashidi Ranjbar, Mohammad Mahdavi, Bagher Larijani
A novel series of dihydropyrano[3,2-c]quinoline derivatives 6a-q were synthesized and evaluated for their in vitro α-glucosidase inhibitory activities. All newly synthesized compounds displayed potent α-glucosidase inhibitory activity in the range of 10.3 ± 0.3 µM-172.5 ± 0.8 µM against the yeast α-glucosidase enzyme when compared to the standard drug acarbose (IC50 = 750.0 ± 1.5 µM). Among these compounds, compounds 6e and 6d displayed the most potent α-glucosidase inhibitory activity (IC50 = 10...
February 2, 2018: Bioorganic Chemistry
Madiha Kazmi, Sumera Zaib, Aliya Ibrar, Sayyeda Tayyeba Amjad, Zainab Shafique, Saifullah Mehsud, Aamer Saeed, Jamshed Iqbal, Imtiaz Khan
Diabetes mellitus (DM), a chronic multifarious metabolic disorder resulting from impaired glucose homeostasis has become one of the most challenging diseases with severe life threat to public health. The inhibition of α-glucosidase, a key carbohydrate hydrolyzing enzyme, could serve as one of the effective methodology in both preventing and treating diabetes through controlling the postprandial glucose levels and suppressing postprandial hyperglycemia. In this context, three series of diamine-bridged bis-coumarinyl oxadiazole conjugates were designed and synthesized by one-pot multi-component methodology...
January 16, 2018: Bioorganic Chemistry
Daniel Rosas-Ramírez, Sonia Escandón-Rivera, Rogelio Pereda-Miranda
Twenty-seven individual resin glycosides from the morning glory family (Convolvulaceae) were evaluated for their α-glucosidase inhibitory potential. Four of these compounds displayed an inhibitory activity comparable to acarbose, which was used as a positive control. Molecular modeling studies performed by docking analysis were accomplished to predict that the active compounds and acarbose bind to the α-1,4-glucosidase enzyme catalytic site of MAL12 from the yeast Saccharomyces cerevisiae through stable hydrogen bonds primarily with the amino acid residues HIS279 and GLN322...
February 1, 2018: Phytochemistry
Xue-Qing Zhang, Xiao-Feng Mou, Ning Mao, Jie-Jie Hao, Ming Liu, Ji-Yong Zheng, Chang-Yun Wang, Yu-Cheng Gu, Chang-Lun Shao
Terphenyllin (1), a naturally abundant p-terphenyl metabolite, was isolated from the coral derived fungus Aspergillus candidus together with four natural analogues 2-5. To evaluate their potency and selectivity, a series of new derivatives of 1 were designed and semisynthesized. They were evaluated for their α-glucosidase inhibitory, cytotoxic, and antibacterial activities. Compounds 1, 3, 4, 7, 8, 10, 11, 14, 15, 21, 23, 24, 29, 39, and 40 showed significant α-glucosidase inhibitory activity with IC50 values of 4...
February 1, 2018: European Journal of Medicinal Chemistry
Timothy M E Davis, Hillary Mulder, Yuliya Lokhnygina, Pablo Aschner, Lee-Ming Chuang, Carlos A Raffo Grado, Eberhard Standl, Eric D Peterson, Rury R Holman
AIM: Pooled efficacy studies suggest that glycaemic responses to dipeptidyl-peptidase 4 inhibitors in type 2 diabetes are greatest in Asians, who may also respond better to alpha-glucosidase inhibitors. We assessed the glycaemic impact of sitagliptin by race in the Trial Evaluating Cardiovascular Outcomes with Sitagliptin (TECOS), and whether this was enhanced in Asians with concomitant acarbose therapy. MATERIALS AND METHODS: TECOS enrolled 14,671 patients with type 2 diabetes, cardiovascular disease and HbA1c of 48-64 mmol/mol (6...
February 6, 2018: Diabetes, Obesity & Metabolism
Myoung-Uoon Jang, Hye-Jeong Kang, Chang-Ku Jeong, Yewon Kang, Ji-Eun Park, Tae-Jip Kim
Cyclomaltodextrinases (CDases) belong to Glycoside Hydrolases (GH) family 13, which show versatile hydrolyzing and/or transglycosylation activity against cyclodextrin (CD), starch, and pullulan. Especially, some CDases have been reported to hydrolyze acarbose, a potent α-glucosidase inhibitor, and transfer the resulting acarviosine-glucose to various acceptors. In this study, a novel CDase (LPCD) gene was cloned from Lactobacillus plantarum WCFS1, which encodes 574 amino acids (64.6 kDa) and shares less than 44% of identities with the known CDase-family enzymes...
February 2018: Journal of Microbiology / the Microbiological Society of Korea
Zaahira Aumeeruddy-Elalfi, Namrita Lall, Bianca Fibrich, Analike Blom van Staden, Muzzammil Hosenally, Mohamad Fawzi Mahomoodally
Essential oils (EOs) extracted from six medicinal herbs and food plants [Cinnamomum zeylanicum (CZ), Psiadia arguta (PA), Psiadia terebinthina (PT), Citrus grandis (CGp), Citrus hystrix (CH), and Citrus reticulata (CR)] were studied for any inhibitory potential against key physiological enzymes involved in diabetes (α-glucosidase), skin aging (collagenase and elastase), and neurodegenerative disorders (acetylcholinesterase). Kinetic studies of the active EOs on the aforementioned enzymes were determined using Lineweaver-Burk plots...
January 2018: Journal of Food and Drug Analysis
Lu Wang, Yufeng Liu, You Luo, Kuiying Huang, Zhenqiang Wu
Guava leaves tea (GLT) has a potential anti-hyperglycemic effect. Nevertheless, it is unclear which compound plays a key role in reducing blood sugar. In this study, GLT extract (IC50 = 19.37 ± 0.21 μg/mL) exhibited a stronger inhibitory potency against α-glucosidase than did acarbose (positive control) at IC50 = 178.52 ± 1.37 μg/mL. To rapidly identify the specific α-glucosidase inhibitor components from GLT, an approach based on bio-affinity ultrafiltration combined with high performance liquid chromatography coupled to electrospray ionization-time of flight-mass spectrometry (BAUF-HPLC-ESI-TOF/MS) was developed...
January 30, 2018: Journal of Agricultural and Food Chemistry
Hui Zhang, Yuan-Yuan Wu, Chen-Ye Huang, Xiao-Jing Zhang, Ji-Zhong Yan
This paper describes a study exploring the interaction between gomizine D and α-glucosidase. The inhibitory activity of α-glucosidase by gomizine D was determined using PNPG as substrates Gomizine D gave the IC₅₀ value of 0.59 mmol•L⁻¹, which was higher than that of acarbose (1.95 mmol•L⁻¹). Gomizine D was a reversible and non-competitiveα-glucosidase inhibitor with an inhibition constant Ki=4.026 g•L⁻¹. The binding mode between gomizine D and α-glucosidase was analyzed by AutoDock Vina molecular docking software...
December 2017: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
Gagandeep Singh, Amanjot Singh, Raman K Verma, Rajiv Mall, Uzma Azeem
A novel series of N-substituted-benzimidazolyl linked para substituted benzylidene based molecules containing three pharmacologically potent hydrogen bonding parts namely; 2,4-thiazolidinedione (TZD: a 2,4-dicarbonyl), diethyl malonate (DEM: a 1,3-diester and an isooxazolidinedione analog) and methyl acetoacetate (MAA: a β-ketoester) (6a-11b) were synthesized and evaluated for in vitro α-glucosidase inhibition. The structure of the novel synthesized compounds was confirmed through the spectral studies (LC-MS, 1H NMR, 13C NMR, FT-IR)...
December 30, 2017: Computational Biology and Chemistry
Rong Huang, Bo-Guang Jiang, Xiao-Nian Li, Ya-Ting Wang, Si-Si Liu, Kai-Xuan Zheng, Jian He, Shao-Hua Wu
Seven new polyoxygenated cyclohexenoids, namely, phomopoxides A-G (1-7), were isolated from the fermentation broth extract of an endophytic fungal strain Phomopsis sp. YE3250 from the medicinal plant Paeonia delavayi Franch. The structures of these compounds were established by spectroscopic interpretation. The absolute configurations of compounds 1 and 4 were confirmed by X-ray crystallographic analysis and chemical derivative approach. All isolated compounds showed weak cytotoxic activities towards three human tumor cell lines (Hela, MCF-7, and NCI-H460), and weak antifungal activities against five pathogenic fungi (Candida albicans, Aspergillus niger, Pyricularia oryzae, Fusarium avenaceum, and Hormodendrum compactum)...
January 15, 2018: Journal of Agricultural and Food Chemistry
Mahesh Kumar, Jeyabalan Govindrajan, Narendra Kumar Nyola
Background: Indian traditional system of medicine uses Pithecellobium dulce for the treatment of diabetes mellitus. Objectives: This study aims to develop an extract rich in saponins derived from seeds of the plant and to evaluate its antihyperglycemic potential in vitro and in vivo. Materials and Methods: Defatted seeds were extracted with methanol and processed to afford saponin-enriched fraction (Pithecellobium dulce saponin-enriched fraction [PDSEF])...
December 2017: Pharmacognosy Research
Han-Kui Wu, Ting Sun, Feng Zhao, Li-Ping Zhang, Gang Li, Jie Zhang
Three new labdane diterpenoids, leojaponicone A (1), isoleojaponicone A (2) and methylisoleojaponicone A (3), were isolated from the herb of Leonurus japonicus. The chemical structures of these secondary metabolites were elucidated on the basis of 1D and 2D NMR, including HMQC, and HMBC spectroscopic techniques. All the new compounds were tested in vitro for their acetylcholinesterase and α-glucosidase inhibitory activity. Compounds 1-3 exhibited low inhibitory effects on α-glucosidase with respect to acarbose and exhibited high inhibitory effects on acetylcholinesterase with respect to huperzine A...
November 2017: Chinese Journal of Natural Medicines
Jia Xiong, Mary H Grace, Debora Esposito, Slavko Komarnytsky, Fei Wang, Mary Ann Lila
The present study was designed to characterize the polyphenols isolated from Acacia mearnsii bark crude extract (B) and fractions (B1-B7) obtained by high-speed counter-current chromatography (HSCCC) and evaluate their anti-inflammatory and carbolytic enzymes (α-glucosidase and α-amylase) inhibitory activities. Fractions B4, B5, B6, B7 (total phenolics 850.3, 983.0, 843.9, and 572.5 mg·g-1, respectively; proanthocyanidins 75.7, 90.5, 95.0, and 44.8 mg·g-1, respectively) showed significant activities against reactive oxygen species (ROS), nitric oxide (NO) production, and expression of pro-inflammatory genes interleukin-1β (IL-1β) and inducible nitric oxide synthase (iNOS) in a lipopolysaccharide (LPS)-stimulated mouse macrophage cell line RAW 264...
November 2017: Chinese Journal of Natural Medicines
Yating Sun, Jingtang Liu, Lei Li, Chi Gong, Shuping Wang, Fan Yang, Huiming Hua, Houwen Lin
Two new butenolide derivatives (±)-asperteretal D ((±)-1) and asperteretal E (2) containing rare 2-benzyl-3-phenyl substituted lactone core, together with nine known analogues (3-11) were obtained from a fungus Aspergillus terreus derived from the marine sponge Phakellia fusca. All the structures were elucidated on the basis of extensive NMR spectroscopic data. The chiral chromatography analyses allowed the separation of the (±)-asperteretal D, of which the absolute configurations were determined by comparing the experimental to calculated electronic circular dichroic (ECD) spectra...
December 22, 2017: Bioorganic & Medicinal Chemistry Letters
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