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https://www.readbyqxmd.com/read/29134977/metformin-effects-are-augmented-by-chronic-intermittent-cold-stress-in-high-fat-diet-fed-male-wistar-rats
#1
A O Ige, O I Iwaloye, E O Adewoye
This study investigated the effects of metformin on some glucose regulatory indices in high fat diet (HFD) fedmale Wistar rats exposed to room temperature and chronic intermittent cold stress (CICS). Thirty rats were randomly dividedinto 5 groups. Group 1(control) was maintained on standard rat chow while groups 2-5 were maintained on HFD for 8weeksrespectively prior to experimental procedures. Control, group 2(HFD untreated) and group 3(HFD+metformin (250mg/kg)were exposed to room temperature while groups 4(HFD untreated+CICS) and 5(HFD+CICS+metformin) were exposed toCICS for 21days...
June 30, 2017: Nigerian Journal of Physiological Sciences: Official Publication of the Physiological Society of Nigeria
https://www.readbyqxmd.com/read/29132091/effect-of-anti-diabetic-drugs-on-bone-metabolism-evidence-from-preclinical-and-clinical-studies
#2
REVIEW
Mohammad Adil, Rashid Ali Khan, Abul Kalam, Shiva Kumar Venkata, Amit Dattatraya Kandhare, Pinaki Ghosh, Manju Sharma
Diabetes mellitus is associated with abnormal bone health and an increased risk of fracture even though patients have normal or higher BMD. The mechanisms behind diabetes mellitus- induced various skeletal disorders remain unclear. Anti-diabetic drugs may have negative or positive impact on bone metabolism. For instance, thiazolidinediones increases the bone loss and risk of fracture possibly through PPARγ activation in bone marrow cells and hamper osteoblastogenesis via decreasing Runx2 transcription factor, IGF-1 and Wnt signalling pathways...
May 25, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/29128163/depsidone-and-xanthones-from-garcinia-xanthochymus-with-hypoglycemic-activity-and-the-mechanism-of-promoting-glucose-uptake-in-l6-myotubes
#3
Yunfang Li, Ping Zhao, Yu Chen, Yanze Fu, Kuan Shi, Liu Liu, Hui Liu, Mingrui Xiong, Qing-Hua Liu, Guangzhong Yang, Yuxiu Xiao
Garcinia xanthochymus is a widely used folk medicine in southwestern China. Previous studies indicated it possesses potential anti-diabetic activities both in vitro (Fu et al., 2014; Nguyen et al., 2017) and in vivo (Shivanand et al., 2017). To discover bioactive ingredients from it and unveil their mechanism of action against diabetes, the present study was designed to isolate constituents from extract of G. xanthochymus, determine their structures, screen their activities and investigate mechanism of action of the active substances...
November 8, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29126698/hybrid-drug-combination-combination-of-ferulic-acid-and-metformin-as-anti-diabetic-therapy
#4
REVIEW
Rakesh Nankar, P K Prabhakar, Mukesh Doble
BACKGROUND AND PURPOSE: Ferulic acid, an anti-oxidant phytochemical present in several dietary components, is known to produce wide range of pharmacological effects. It is approved for use in food industry as a preservative and in sports food. Previous reports from our lab have shown synergistic interaction of ferulic acid with metformin in cell lines and diabetic rats. The purpose of this review is to compile information about anti-diabetic activity of ferulic acid in in vitro and in vivo models with special emphasis on activity of ferulic acid when combined with metformin...
October 24, 2017: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
https://www.readbyqxmd.com/read/29123386/geroprotectors-as-a-therapeutic-strategy-for-copd-where-are-we-now
#5
REVIEW
Joanna Miłkowska-Dymanowska, Adam J Białas, Joanna Makowska, Aleksandra Wardzynska, Paweł Górski, Wojciech J Piotrowski
Although current therapies in chronic obstructive pulmonary disease (COPD) improve the quality of life, they do not satisfactorily reduce disease progression or mortality. There are still many gaps in knowledge about the cellular, molecular, and genetic mechanisms contributing to pathobiology of this disease. However, increasing evidence suggests that accelerated aging, chronic systemic inflammation, and oxidative stress play major roles in pathogenesis in COPD, thus opening new opportunities in therapy. Therefore, the aim of our review was to describe and discuss some of the most widely used therapeutics that affect the root cause of aging and oxidative stress (metformin, melatonin, sirolimus, statins, vitamin D, and testosterone) in context of COPD therapy...
2017: Clinical Interventions in Aging
https://www.readbyqxmd.com/read/29122714/diethanolamine-modified-pectin-based-core-shell-composites-as-dual-working-gastroretentive-drug-cargo
#6
Hriday Bera, Sanoj Kumar
The current study aimed at developing diethonolamine-modified high-methoxyl pectin (DMP)-alginate (ALG) based core-shell composites for controlled intragastric delivery of metformin HCl (MFM) by combined approach of floating and bioadhesion. DMP with degree of amidation of 48.72% was initially accomplished and characterized by FTIR, DSC and XRD analyses. MFM-loaded core matrices were then fabricated by ionotropic gelation technique employing zinc acetate as cross-linker. The core matrices were further coated by fenugreek gum (FG)-ALG gel membrane via diffusion-controlled interfacial complexation method...
November 6, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/29117997/metformin-an-anti-proliferative-agent-and-methylation-regulator-in-treating-prostatic-disease
#7
Zongwei Wang, Aria F Olumi
Existing drugs that have been used in clinical practice for other purposes can prove useful for reutilization, since much of the safety profile, pharmacokinetics have been completed. Therefore, the drugs can enter clinical practice for variety of causes with less regulatory burden. Metformin may prove to be such a drug where it may have a role in other diseases, beside management of diabetes. In this perspective, we provide our finding and understanding of metformin as an alternate way to treat urological abnormal proliferation...
November 8, 2017: American Journal of Physiology. Renal Physiology
https://www.readbyqxmd.com/read/29113111/the-mxl-3-sbp-1-axis-is-responsible-for-glucose-dependent-fat-accumulation-in-c-elegans
#8
Fanny Mejia-Martinez, Berenice Franco-Juarez, Elizabeth Moreno-Arriola, Alain Hernández-Vázquez, Marco Martinez-Avila, Saul Gómez-Manzo, Jaime Marcial-Quino, Karla Carvajal, Antonio Velazquez-Arellano, Daniel Ortega-Cuellar
Chronic exposure to elevated glucose levels leads to fatty acid accumulation, which promotes the development of metabolic diseases such as obesity and type 2 diabetes. MXL-3 is a conserved transcriptional factor that modulates the inhibition of lipolysis in Caenorhabditis elegans. However, the role of MXL-3 in lipid metabolism during nutrient excess remains unknown. We hypothesized that inhibition of MXL-3 prevents glucose-dependent fat accumulation. Nematodes from wild-type N2, MXL-3::GFP and sbp-1 or mxl-3 null strains were grown on standard, high glucose or high glucose plus metformin plates for 24 h...
November 6, 2017: Genes
https://www.readbyqxmd.com/read/29111280/akt-activation-a-potential-strategy-to-ameliorate-insulin-resistance
#9
REVIEW
Zhengyi Zhang, Huadong Liu, Jiankang Liu
Insulin resistance is a hallmark of type 2 diabetes and obesity while the mechanism remains unclear. Current therapy to treat type 2 diabetes is metformin, the 5'-monophosphate-activated protein kinase (AMPK) activator, owing to the ability to augment peripheral glucose uptake. However, metformin also displays limitations, as AMPK activation remains intact and regular in most type 2 diabetes and metformin does not seem to facilitate peripheral insulin resistance. Evidence has shown that PI3K-Akt/PKB pathway could be induced via insulin and act as an important effector...
October 27, 2017: Diabetes Research and Clinical Practice
https://www.readbyqxmd.com/read/29110587/momordica-charantia-extracts-ameliorate-insulin-resistance-by-regulating-the-expression-of-socs-3-and-jnk-in-type-2-diabetes-mellitus-rats
#10
Chunyu Ma, Hongyu Yu, Ying Xiao, Huijiao Wang
CONTEXT: Momordica charantia L. (Cucurbitaceae) has long been widely used as a traditional remedy for diabetes mellitus in some countries. However, detailed antidiabetic mechanisms are largely unknown. OBJECTIVES: This study clarified the ameliorating effects of M. charantia ethanol extracts (MCE) on the insulin resistance in type 2 diabetes mellitus (T2DM) rats. MATERIALS AND METHODS: T2DM rat model was established by high-fat diet and streptozotocin (STZ) injection...
December 2017: Pharmaceutical Biology
https://www.readbyqxmd.com/read/29110119/metformin-synergistically-enhances-antitumor-activity-of-cisplatin-in-gallbladder-cancer-via-the-pi3k-akt-erk-pathway
#11
Tingting Bi, Ao Zhu, Xufeng Yang, Huiying Qiao, Jinmei Tang, Yan Liu, Rong Lv
Metformin (Met) is a widely used antidiabetic drug and has demonstrated interesting anticancer effects in various cancer models, alone or in combination with chemotherapeutic drugs. The aim of the present study is to investigate the synergistic effect of Met with cisplatin (Cis) on the tumor growth inhibition of gallbladder cancer cells (GBC-SD and SGC-996) and explore the underlying mechanism. Cells were treated with Met and/or Cis and subjected to cell viability, colony formation, apoptosis, cell cycle, western blotting, xenograft tumorigenicity assay and immunohistochemistry...
November 6, 2017: Cytotechnology
https://www.readbyqxmd.com/read/29106946/orodispersible-tablets-containing-taste-masked-solid-lipid-pellets-with-metformin-hydrochloride-influence-of-process-parameters-on-tablet-properties
#12
Gustavo Freire Petrovick, Peter Kleinebudde, Jörg Breitkreutz
Compaction of multiparticulates into tablets, particularly into orodispersible tablets (ODTs), is challenging. The compression of pellets, made by solid lipid extrusion/spheronization processes, presents peculiar difficulties since solid lipids usually soften or melt at relatively low temperature ranges and due to applied mechanical forces. Until now, there are no reports in literature about the development of ODTs based on solid lipid pellets. To investigate the feasibility of producing such tablets, a design of experiment (DoE) approach was performed to elucidate the influence of compression force and amount of two co-processed excipients (Ludiflash(®) and Parteck(®) ODT) on properties of the tablets (friability, tensile strength, and disintegration time)...
October 26, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/29100387/metabolic-modulation-of-ewing-sarcoma-cells-inhibits-tumor-growth-and-stem-cell-properties
#13
Atreyi Dasgupta, Matteo Trucco, Nino Rainusso, Ronald J Bernardi, Ryan Shuck, Lyazat Kurenbekova, David M Loeb, Jason T Yustein
Ewing sarcoma (EWS) is a highly aggressive and metabolically active malignant tumor. Metabolic activity can broadly be characterized by features of glycolytic activity and oxidative phosphorylation. We have further characterized metabolic features of EWS cells to identify potential therapeutic targets. EWS cells had significantly more glycolytic activity compared to their non-malignant counterparts. Thus, metabolic inhibitors of glycolysis such as 2-deoxy-D-glucose (2DG) and of the mitochondrial respiratory pathway, such as metformin, were evaluated as potential therapeutic agents against a panel of EWS cell lines in vitro...
September 29, 2017: Oncotarget
https://www.readbyqxmd.com/read/29099085/eburicoic-acid-a-triterpenoid-compound-from-antrodia-camphorata-displays-antidiabetic-and-antihyperlipidemic-effects-in-palmitate-treated-c2c12-myotubes-and-in-high-fat-diet-fed-mice
#14
Cheng-Hsiu Lin, Yueh-Hsiung Kuo, Chun-Ching Shih
This study was designed to investigate the antidiabetic and antihyperlipidemic effects and mechanisms of eburicoic acid (TRR); one component of Antrodia camphorata in vitro and in an animal model for 14 weeks. Expression levels of membrane glucose transporter type 4 (GLUT4); phospho-5'-adenosine monophosphate-activated protein kinase (AMPK)/total AMPK; and phospho-Akt/total-Akt in insulin-resistant C2C12 myotube cells were significantly decreased by palmitate; and such decrease was prevented and restored by TRR at different concentrations...
November 2, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29096431/combination-therapy-of-oral-hypoglycemic-agents-in-patients-with-type-2-diabetes-mellitus
#15
REVIEW
Min Kyong Moon, Kyu Yeon Hur, Seung-Hyun Ko, Seok-O Park, Byung-Wan Lee, Jin Hwa Kim, Sang Youl Rhee, Hyun Jin Kim, Kyung Mook Choi, Nan-Hee Kim
The Korean Diabetes Association (KDA) recently updated the Clinical Practice Guidelines on antihyperglycemic agent therapy for adult patients with type 2 diabetes mellitus (T2DM). In combination therapy of oral hypoglycemic agents (OHAs), general recommendations were not changed from those of the 2015 KDA guidelines. The Committee on Clinical Practice Guidelines of the KDA has extensively reviewed and discussed the results of meta-analyses and systematic reviews of effectiveness and safety of OHAs and many clinical trials on Korean patients with T2DM for the update of guidelines...
November 2017: Korean Journal of Internal Medicine
https://www.readbyqxmd.com/read/29094287/targeting-ampk-mtor-and-%C3%AE-catenin-by-combined-metformin-and-aspirin-therapy-in-hcc-an-appraisal-in-egyptian-hcc-patients
#16
Doaa Ali Abdelmonsif, Ahmed S Sultan, Wessam F El-Hadidy, Dina Mohamed Abdallah
BACKGROUND: Hepatocellular carcinoma (HCC) is an expanding health problem with a great impact on morbidity and mortality, both in Egypt and worldwide. Recently, metformin and aspirin showed a potential anticancer effect on HCC, although the mechanism of this effect is not fully elucidated. OBJECTIVE: The current work aimed to investigate the possibility of targeting AMP-activated protein kinase (AMPK), mammalian target of rapamycin (mTOR), and β-catenin proteins through combined metformin/aspirin treatment in the HepG2 cell line, and to explore such molecular targets in Egyptian HCC patients...
November 1, 2017: Molecular Diagnosis & Therapy
https://www.readbyqxmd.com/read/29093681/quantitative-and-systems-pharmacology-3-network-based-identification-of-new-targets-for-natural-products-enables-potential-uses-in-aging-associated-disorders
#17
Jiansong Fang, Li Gao, Huili Ma, Qihui Wu, Tian Wu, Jun Wu, Qi Wang, Feixiong Cheng
Aging that refers the accumulation of genetic and physiology changes in cells and tissues over a lifetime has been shown a high risk of developing various complex diseases, such as neurodegenerative disease, cardiovascular disease and cancer. Over the past several decades, natural products have been demonstrated as anti-aging interveners via extending lifespan and preventing aging-associated disorders. In this study, we developed an integrated systems pharmacology infrastructure to uncover new indications for aging-associated disorders by natural products...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29089306/organic-cation-transporter-1-is-responsible-for-hepatocellular-uptake-of-the-tyrosine-kinase-inhibitor-pazopanib
#18
Waleed Elsayed Ahmed Ellawatty, Yusuke Masuo, Ken-Ichi Fujita, Erina Yamazaki, Hiroo Ishida, Hiroshi Arakawa, Noritaka Nakamichi, Ramadan Abdelwahed, Yasutsuna Sasaki, Yukio Kato
Pazopanib is an orally active tyrosine kinase inhibitor that exhibits hepatotoxicity in some patients. Despite the clinical importance of its hepatic distribution, the transporter(s) responsible for hepatic uptake of pazopanib in humans remain undetermined. In order to characterize its hepatic uptake mechanism, we screened the effects of several transporter inhibitors, including tetrapentylammonium (TPeA) for organic cation transporters (OCTs) and cyclosporin A (CsA) for organic anion-transporting polypeptides (OATPs), on both plasma disappearance and hepatic distribution of pazopanib in mice after its intravenous administration...
October 31, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/29080400/aging-and-stem-cell-therapy-ampk-as-an-applicable-pharmacological-target-for-rejuvenation-of-aged-stem-cells-and-achieving-higher-efficacy-in-stem-cell-therapy
#19
REVIEW
Mohammadhossein Khorraminejad-Shirazi, Mohammad Farahmandnia, Bahareh Kardeh, Alireza Estedlal, Sina Kardeh, Ahmad Monabati
In recent years, tissue regeneration has become a promising field for developing stem cell-based transplantation therapies for human patients. Adult stem cells are affected by the same aging mechanisms that involve somatic cells. One of the mechanisms involved in cellular aging is hyperactivation of mechanistic target of rapamycin complex 1 (mTORC1) and disruption of 5' adenosine monophosphate-activated protein kinase (AMPK). Aging of stem cells results in their impaired regenerative capacity and depletion of stem cell pools in adult tissue, which results in lower efficacy of stem cell therapy...
October 19, 2017: Hematology/oncology and Stem Cell Therapy
https://www.readbyqxmd.com/read/29080044/metformin-effect-on-tsh-in-subclinical-hypothyroidism-randomized-double-blind-placebo-controlled-clinical-trial
#20
Mateus Dornelles Severo, Thais Stürmer Andrade, Vicente Correa Junior, Alexandre Antonio Naujorks, Miguel Gus, Beatriz D Schaan
INTRODUCTION: Non-randomized trials suggest that metformin may reduce TSH levels through unknown mechanisms. OBJECTIVE: To evaluate whether metformin can reduce TSH levels in subjects with subclinical hypothyroidism. PATIENTS AND METHODS: This is a randomized, double-blind, placebo controlled clinical trial with 3 months duration that enrolled 48 individuals, between 18 and 65 years, with subclinical hypothyroidism. The patients were randomized to the use of metformin 850 mg or placebo twice a day for 3 months...
October 27, 2017: Endocrine
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