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Oral Anti-hyperglycemics

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https://www.readbyqxmd.com/read/28390958/discovery-of-liver-directed-glucokinase-activator-having-anti-hyperglycemic-effect-without-hypoglycemia
#1
Anil M Deshpande, Debnath Bhuniya, Siddhartha De, Bhavesh Dave, Vinod P Vyavahare, Santosh H Kurhade, Sachin R Kandalkar, Keshav P Naik, Balasaheb S Kobal, Rahul D Kaduskar, Sujay Basu, Vaibhav Jain, Pratima Patil, Sandhya Chaturvedi Joshi, Ganesh Bhat, Amol A Raje, Satyanarayana Reddy, Jayasagar Gundu, Vamsi Madgula, Suhas Tambe, Prasad Shitole, Dhananjay Umrani, Anita Chugh, Venkata P Palle, Kasim A Mookhtiar
Glucokinase activators (GKAs) are among the emerging drug candidates for the treatment of type 2 diabetes (T2D). Despite effective blood glucose lowering in clinical trials, many pan-GKAs "acting both in pancreas and liver" have been discontinued from clinical development mainly because of their potential to cause hypoglycemia. Pan-GKAs over sensitize pancreatic GK, resulting in insulin secretion even at sub-normoglycemic level which might be a possible explanation for hypoglycemia. An alternative approach to minimize the risk of hypoglycemia is to use liver-directed GKAs, which are reported to be advancing well in clinical development...
March 24, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28330423/geraniol-a-natural-monoterpene-ameliorates-hyperglycemia-by-attenuating-the-key-enzymes-of-carbohydrate-metabolism-in-streptozotocin-induced-diabetic-rats
#2
Sukumar Babukumar, Veerasamy Vinothkumar, Chandrasekaran Sankaranarayanan, Subramani Srinivasan
CONTEXT: Geraniol, an acyclic monoterpene alcohol is found in medicinal plants, is used traditionally for several medical purposes including diabetes. OBJECTIVES: The present study evaluates the antihyperglycemic potential of geraniol on key enzymes of carbohydrate metabolism in streptozotocin (STZ)-induced diabetic rats. MATERIALS AND METHODS: Diabetes was induced in experimental rats, by a single intraperitoneal (i.p) injection of STZ [40 mg/kg body weight (b...
December 2017: Pharmaceutical Biology
https://www.readbyqxmd.com/read/28306534/ameliorative-potential-of-blighia-sapida-k-d-koenig-bark-against-pancreatic-%C3%AE-cell-dysfunction-in-alloxan-induced-diabetic-rats
#3
Oluwafemi Adeleke Ojo, Basiru Olaitan Ajiboye, Adebola Busola Ojo, Babatunji Emmanuel Oyinloye, Oluwatosin Debbie Imiere, Oluwatosin Adeyonu
Background In West Africa, the fruit, seed, leaf and stem of Blighia sapida K.D. Koenig are commonly used as remedy against a variety of diseases, including diabetes mellitus. This study investigated the ameliorative potential of B. sapida K.D. Koenig stem bark ethanol extract against pancreatic β-cell dysfunction in diabetic rats. Methods Diabetes was induced by intraperitoneal injection of alloxan (65 mg/kg body weight) for 21 days, and orally administered with glibenclamide (5 mg/kg body weight), 50-150 mg/kg body weight of B...
March 17, 2017: Journal of Complementary & Integrative Medicine
https://www.readbyqxmd.com/read/28282223/analytical-methods-for-metformin-estimation
#4
Durgawati Patel, Puspendra Kumar, Swapnil Sharma, Jaya Dwivedi
Metformin is a widely prescribed oral anti-hyperglycemic agent used in the management of non-insulin dependent diabetes mellitus (NIDDM) or type II diabetes. This article accentuates various analytical methods viz. HPLC, HPTLC, spectrophotometric, electrochemical, capillary electrophoresis and LC-MS for the estimation of metformin in pharmaceutical formulations and in biological matrices.
March 10, 2017: Critical Reviews in Analytical Chemistry
https://www.readbyqxmd.com/read/28261096/antioxidant-activities-metabolic-profiling-proximate-analysis-mineral-nutrient-composition-of-salvadora-persica-fruit-unravel-a-potential-functional-food-and-a-natural-source-of-pharmaceuticals
#5
Asha Kumari, Asish K Parida, Jaykumar Rangani, Ashok Panda
Salvadora persica is a medicinally important plant mainly used in oral hygiene. However, little attention has been given towards the nutritional prominence of this plant. This study encloses the proximate and mineral nutrient contents, amino acid composition, metabolite profiling and antioxidant potential of S. persica fruit. The ripen fruit contained substantial amount of sugars, mineral nutrients, carotenoids, polyphenols and flavonoids. The metabolic profiling of the fruit extract by GC-MS revealed a total of 22 metabolites comprising of sugars, sugar alcohols, organic acids, organic base, and aromatic silica compound...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28258533/current-therapeutic-approaches-in-the-management-of-hyperglycemia-in-chronic-renal-disease
#6
REVIEW
Vishnu Garla, Licy Yanes-Cardozo, Lillian F Lien
Diabetes mellitus (DM) and chronic kidney disease (CKD) are intricately intertwined. DM is the most common cause of CKD. Adequate control of DM is necessary for prevention of progression of CKD, while careful management of the metabolic abnormalities in CKD will assist in achieving better control of DM. Two of the key organs involved in glucose production are the kidney and the liver. Furthermore, the kidney also plays a role in glucose filtration and reabsorption. In CKD, monitoring of glycemic control using traditional methods such as Hemoglobin A1c (Hba1c) must be done with caution secondary to associated hematological abnormalities in CKD...
March 3, 2017: Reviews in Endocrine & Metabolic Disorders
https://www.readbyqxmd.com/read/28250659/antidiabetic-effects-of-aqueous-and-dichloromethane-methanol-stem-bark-extracts-of-pterocarpus-soyauxii-taub-papilionaceae-on-streptozotocin-induced-diabetic-rats
#7
Marie Claire Tchamadeu, Paul Désiré Djomeni Dzeufiet, Nelly Blaes, Jean-Pierre Girolami, Pierre Kamtchouing, Théophile Dimo
AIM OF THE STUDY: The aim is to evaluate the hypoglycemic and antidiabetic effects of aqueous and CH2Cl2/CH3OH stem bark extracts of Pterocarpus soyauxii Taub in normal and diabetic rats. MATERIALS AND METHODS: Streptozotocin (STZ)-induced diabetic and normal adult Wistar rats were orally administered with aqueous and CH2Cl2/CH3OH plant extracts of P. soyauxii at various doses (38-300 mg/kg) in a single administration. In addition, STZ-induced diabetic rats received prolonged daily administration for 14 days...
January 2017: Pharmacognosy Research
https://www.readbyqxmd.com/read/28238911/anti-hyperglycemic-activity-of-polysaccharides-from-calyx-of-physalis-alkekengi-var-franchetii-makino-on-alloxan-induced-mice
#8
Yu Guo, Sujuan Li, Jianxin Li, Zhiyuan Ren, Feng Chen, Xiaowen Wang
The present study was undertaken to investigate the hypoglycemic effect of polysaccharides (PPSC) isolated from calyx of Physalis alkekengi var. franchetii Makino in alloxan-induced diabetic mice. Seven polysaccharide fractions were obtained through a DEAE-52 column and Sephadex G-100 gel column and they were the main composes of PPSC. The PPSC treatment could prevent the loss of body weight in diabetic mice and result in a decrease of fasting blood glucose (FBG) and glycated serum protein (GSP) and an increase of fasting serum insulin in a dose-dependent manner...
June 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28216594/anti-hyperglycemic-activity-of-major-compounds-from-calea-ternifolia
#9
Sonia Escandón-Rivera, Araceli Pérez-Vásquez, Andrés Navarrete, Mariana Hernández, Edelmira Linares, Robert Bye, Rachel Mata
Demethylisoencecalin (1) and caleins A (4) and C (5) (3.16-31.6 mg/kg, p.o.), the major components from an infusion of Calea ternifolia controlled postprandial glucose levels during an oral sucrose tolerance test (OSTT, 3 g/kg) in normal and nicotinamide/streptozotocin (NA/STZ, 40/100 mg/kg) hyperglicemic mice. The effects were comparable to those of acarbose (5 mg/kg). During the isolation of 1, 4, and 5, four additional metabolites not previously reported for the plant, were obtained, namely 6-acetyl-5-hydroxy-2-methyl-2-hydroxymethyl-2H-chromene (3), herniarin (6), scoparone (7), and 4',7-dimethylapigenin (8)...
February 14, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28182659/metformin-exhibits-preventive-and-therapeutic-efficacy-against-experimental-cystic-echinococcosis
#10
Julia A Loos, Valeria A Dávila, Christian R Rodrígues, Romina Petrigh, Jorge A Zoppi, Fernando A Crocenzi, Andrea C Cumino
Metformin (Met) is an anti-hyperglycemic and potential anti-cancer agent which may exert its anti-proliferative effects via the induction of energetic stress. In this study we investigated the in vitro and in vivo efficacy of Met against the larval stage of Echinococcus granulosus. Metformin showed significant dose- and time-dependent killing effects on in vitro cultured protoscoleces and metacestodes. Notably, the combination of Met together with the minimum effective concentration of ABZSO had a synergistic effect after days 3 and 12 on metacestodes and protoscoleces, respectively...
February 2017: PLoS Neglected Tropical Diseases
https://www.readbyqxmd.com/read/28160554/pharmacogenetics-of-dipeptidyl-peptidase-4-inhibitors-in-a-taiwanese-population-with-type-2-diabetes
#11
Wen-Ling Liao, Wen-Jane Lee, Ching-Chu Chen, Chieh Hsiang Lu, Chien-Hsiun Chen, Yi-Chun Chou, I-Te Lee, Wayne H-H Sheu, Jer-Yuarn Wu, Chi-Fan Yang, Chung-Hsing Wang, Fuu-Jen Tsai
Dipeptidyl peptidase-4 (DPP-4) inhibitors are oral anti-hyperglycemic drugs enabling effective glycemic control in type 2 diabetes (T2D). Despite DPP-4 inhibitors' advantages, the patients' therapeutic response varies. In this retrospective cohort study, 171 Taiwanese patients with T2D were classified as sensitive or resistant to treatment based on the mean change in HbA1c levels. Using an assumption-free genome-wide association study, 45 single nucleotide polymorphisms (SNPs) involved in the therapeutic response to DPP-4 inhibitors (P < 1 × 10-4) were identified at or near PRKD1, CNTN3, ASK, and LOC10537792...
March 14, 2017: Oncotarget
https://www.readbyqxmd.com/read/28103701/metformin-prevents-the-progression-of-dysplastic-mucosa-of-the-head-and-neck-to-carcinoma-in-nondiabetic-patients
#12
Michael Zvi Lerner, Niv Mor, Hyung Paek, Andrew Blitzer, Marshall Strome
OBJECTIVE: Metformin is an oral anti-hyperglycemic agent used to treat type 2 diabetes mellitus (DM). In vitro and animal models have shown that metformin can prevent the progression of oral lesions to carcinoma; however, there is conflicting data in the clinical literature regarding risk reduction for malignancy in head and neck cancer (HNC). STUDY DESIGN: Case series. METHODS: We present 3 cases in which adjuvant metformin therapy was used to treat recurrent and multifocal dysplastic lesions in previously treated nondiabetic HNC patients...
April 2017: Annals of Otology, Rhinology, and Laryngology
https://www.readbyqxmd.com/read/28017669/depression-can-be-prevented-by-astaxanthin-through-inhibition-of-hippocampal-inflammation-in-diabetic-mice
#13
Xiao-Yan Zhou, Fang Zhang, Xiao-Tong Hu, Jing Chen, Ren-Xian Tang, Kui-Yang Zheng, Yuan-Jian Song
The critical factor considered in a depression induced by diabetes is the inflammation eliciting hippocampal, amygdala and thalamic neuronal injury. Therefore, inhibiting inflammatory reactions in the brain and reducing neuronal injury can alleviate depression in rodents suffering from diabetes mellitus. The oral administration of astaxanthin has been employed in emotional disorders and diabetic complications due to its anti-depressant, anti-inflammatory and anti-apoptotic functions. However, it has not been reported whether astaxanthin can improve diabetes-related depression-like behavior, and its potential mechanisms have not been elucidated...
December 22, 2016: Brain Research
https://www.readbyqxmd.com/read/28006991/efficacy-of-autologous-bone-marrow-derived-mesenchymal-stem-cell-and-mononuclear-cell-transplantation-in-type-2-diabetes-mellitus-a-randomized-placebo-controlled-comparative-study
#14
Shobhit Bhansali, Pinaki Dutta, Vinod Kumar, Mukesh Kumar Yadav, Ashish Jain, Sunder Mudaliar, Shipra Bhansali, Ratti Ram Sharma, Vivekanand Jha, Neelam Marwaha, Niranjan Khandelwal, Anand Srinivasan, Naresh Sachdeva, Meredith Hawkins, Anil Bhansali
Drugs targeting β-cells have provided new options in the management of T2DM; however, their role in β-cell regeneration remains elusive. The recent emergence of cell-based therapies such as autologous bone marrow-derived mesenchymal stem cells (ABM-MSCs) and mononuclear cells (ABM-MNCs) seems to offer a pragmatic approach to augment β-cell function/mass. This study aims to examine the efficacy and safety of ABM-MSC and ABM-MNC transplantation in T2DM and explores alterations in glucose-insulin homeostasis by metabolic studies...
April 1, 2017: Stem Cells and Development
https://www.readbyqxmd.com/read/28002030/anti-hyperglycemic-activity-of-aegle-marmelos-l-corr-is-partly-mediated-by-increased-insulin-secretion-%C3%AE-amylase-inhibition-and-retardation-of-glucose-absorption
#15
Prawej Ansari, Nadia Afroz, Shahnaz Jalil, Sohel Bin Azad, Md Gazi Mustakim, Sabbir Anwar, S M Nazmul Haque, Saad Mosharraf Hossain, Ramisha Rifat Tony, J M A Hannan
BACKGROUND: Aegle marmelos (commonly known as Bael, golden apple) was formerly described to have anti-hyperglycemic activity. The present study aimed to explore the possible effects, in depth, of A. marmelos extracts on carbohydrate absorption, glucose utilization, and α-amylase inhibition and insulin content in pancreases of type 2 diabetic rats. METHODS: This research begins with fasting blood glucose and oral glucose tolerance test (OGTT) to evaluate the primary anti-hyperglycemic effect in chemically induced type 2 diabetic rats...
January 1, 2017: Journal of Pediatric Endocrinology & Metabolism: JPEM
https://www.readbyqxmd.com/read/27847209/in-vivo-study-for-anti-hyperglycemic-potential-of-aqueous-extract-of-basil-seeds-ocimum-basilicum-linn-and-its-influence-on-biochemical-parameters-serum-electrolytes-and-haematological-indices
#16
Sachin Chaudhary, Amit Semwal, Hitesh Kumar, Harish Chandra Verma, Amit Kumar
The study introduced anti-hyperglycemic influence of aqueous extract of Ocimum basilicum seeds (AEOBS) in Streptozotocin (STZ) induced diabetic rats and estimating its potential to ameliorate altered level of biochemical parameters, serum electrolytes level and haematological indices along with its effect on body weight of treated rats. The albino rats were selected to observe oral glucose tolerance test by oral intake of aq. glucose solution (4g/kg, body weight) in normal rats and estimation of blood glucose level after administration of AEOBS at 250mg/kg, 500mg/kg and standard drug glibenclamide at 0...
December 2016: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/27808120/ethanol-extract-of-lophatheri-herba-exhibits-anti-cancer-activity-in-human-cancer-cells-by-suppression-of-metastatic-and-angiogenic-potential
#17
Aeyung Kim, Minju Im, Min Jung Gu, Jin Yeul Ma
Lophatheri Herba (LH), dried leaf of Lophatherum gracile Brongn, has long been used to reduce thirst and treat fever and inflammation in Chinese medicine. Recent studies have shown that LH has anti-viral, anti-bacterial, anti-cancer, anti-oxidant, diuretic, and hyperglycemic properties. However, the effects of an ethanol extract of L. herba (ELH), at non-cytotoxic doses, on the metastatic and angiogenic abilities of malignant tumor cells have not been reported. We found that ELH significantly suppressed p38, JNK, and NF-κB activation and proteolytic activities under phorbol 12-myristate 13-acetate (PMA) stimulation, thus leading to a decrease in metastatic potential, including migration and invasion...
November 3, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27771987/dammarane-type-triterpene-extracts-of-panax-notoginseng-root-ameliorates-hyperglycemia-and-insulin-sensitivity-by-enhancing-glucose-uptake-in-skeletal-muscle
#18
Kumiko Kitamura, Yusuke Takamura, Taku Iwamoto, Mitsuru Nomura, Hideaki Iwasaki, Motoyasu Ohdera, Michiaki Murakoshi, Keikichi Sugiyama, Kazuki Matsuyama, Yasuko Manabe, Nobuharu L Fujii, Tohru Fushiki
Skeletal muscle is an important organ for controlling the development of type 2 diabetes. We discovered Panax notoginseng roots as a candidate to improve hyperglycemia through in vitro muscle cells screening test. Saponins are considered as the active ingredients of ginseng. However, in the body, saponins are converted to dammarane-type triterpenes, which may account for the anti-hyperglycemic activity. We developed a method for producing a dammarane-type triterpene extract (DTE) from Panax notoginseng roots and investigated the extract's potential anti-hyperglycemic activity...
February 2017: Bioscience, Biotechnology, and Biochemistry
https://www.readbyqxmd.com/read/27771924/lupeol-and-its-role-in-chronic-diseases
#19
Fan-Shiu Tsai, Li-Wei Lin, Chi-Rei Wu
Lupeol belongs to pentacyclic lupane-type triterpenes and exhibits in edible vegetables, fruits and many plants. Many researches indicated that lupeol possesses many beneficial pharmacological activities including antioxidant, anti-inflammatory, anti-hyperglycemic, anti-dyslipidemic and anti-mutagenic effects. From various disease-targeted animal models, these reports indicated that lupeol has anti-diabetic, anti-asthma, anti-arthritic, cardioprotective, hepatoprotective, nephroprotective, neuroprotective and anticancer efficiency under various routes of administration such as topical, oral, subcutaneous, intraperitoneal and intravenous...
2016: Advances in Experimental Medicine and Biology
https://www.readbyqxmd.com/read/27731814/ameliorative-potential-of-solanum-trilobatum-leaf-extract-and-fractions-on-lipid-profile-and-oxidative-stress-in-experimental-diabetes
#20
KhaderSyed Zameer Ahmed, Syed Zameer Ahmed Sidhra, Ponnusamy Ponmurugan, Balasubramanian Senthil Kumar
Solanum trilobatum Linn is a medicinal plants used in India from many centuries to cure various diseases. The purpose of the study is to evaluate the ameliorative potential of the ethanolic leaf extract and fractions of Solanum trilobatum (St) against alloxan induced diabetic rats. Solanum trilobatum leaf extract and fractions were administered orally at two different concentration (100-200mg/kg body weight) to alloxan induced diabetic rats. The antidiabetic efficacy was validated through various biochemical parameters, enzyme assays, renal markers and antioxidant properties were also determined...
September 2016: Pakistan Journal of Pharmaceutical Sciences
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