Recent progress on the discovery of NLRP3 inhibitors and their therapeutic potential.
CONCLUSION: The findings of this review confirmed the importance of developing NLRP3 inflammasome inhibitors. Various NLRP3 inhibitors have been discovered as effective therapeutic treatments to multiples diseases such as type II diabetes, experimental autoimmune encephalomyelitis, stress-related mood disorders, etc. The development of a full range of NLRP3 inflammasome inhibitors is still at its foundational phase. We are looking forward to identification of inhibitory agents which provide the most potent therapeutic strategies and efficiently treat NLRP3 inflammasome-related inflammatory diseases. PMID: 31971103 ...
Source: Current Medicinal Chemistry - January 21, 2020 Category: Chemistry Authors: Su M, Wang W, Liu F, Li H Tags: Curr Med Chem Source Type: research
Brucella abortus Infection Elicited Hepatic Stellate Cell-Mediated Fibrosis Through Inflammasome-Dependent IL-1 β Production
In human brucellosis, the liver is frequently affected. Brucella abortus triggers a profibrotic response on hepatic stellate cells (HSCs) characterized by inhibition of MMP-9 with concomitant collagen deposition and TGF-β1 secretion through type 4 secretion system (T4SS). Taking into account that it has been reported that the inflammasome is necessary to induce a fibrotic phenotype in HSC, we hypothesized that Brucella infection might create a microenvironment that would promote inflammasome activation with concomitant profibrogenic phenotype in HSCs. B. abortus infection induces IL-1β secretion in HSCs in a T4SS-depende...
Source: Frontiers in Immunology - January 20, 2020 Category: Allergy & Immunology Source Type: research
317: Population-level fetal growth outcomes before and after gestational diabetes treatment guideline change
The objective of this population-level study is to assess the impact of an insulin-first prescribing strategy on the incidence of accelerated fetal growth. (Source: American Journal of Obstetrics and Gynecology)
Source: American Journal of Obstetrics and Gynecology - December 31, 2019 Category: OBGYN Authors: Esther Ellsworth Bowers, Shannon Santo, Bernadette O'Grady, Sue E. Sarsam, Suzanne Halt, Ronda Slickman, Avinash Patil Tags: Poster Session I Source Type: research
713: Oral hypoglycemic agents in the treatment of gestational diabetes mellitus: a cost-effectiveness analysis
Recent studies have shown statistically significant adverse neonatal outcomes associated with the use of oral hypoglycemic agents in pregnancy for the treatment of GDM. Due to robust patient preference for oral agents over subcutaneous insulin, we sought to explore the cost-effectiveness and outcomes associated with both glyburide and metformin. (Source: American Journal of Obstetrics and Gynecology)
Source: American Journal of Obstetrics and Gynecology - December 31, 2019 Category: OBGYN Authors: Caroline C. Davitt, Alyssa R. Hersh, Claire H. Packer, Allison Munn, Abigail Vinson, Aaron B. Caughey Tags: Poster Session III Source Type: research
651: Comparative impact of pharmacological treatments for gestational diabetes on neonatal anthropometry: systematic review and meta-analysis
Three commonly-used pharmacological options are available to treat gestational diabetes (GDM) that cannot be managed with lifestyle interventions alone: insulin, glyburide, and metformin. However, there is little international consensus on optimal management strategies. We aimed to compare the impacts of pharmacological treatments for GDM on birthweight, independent of maternal glycaemic control. (Source: American Journal of Obstetrics and Gynecology)
Source: American Journal of Obstetrics and Gynecology - December 31, 2019 Category: OBGYN Authors: Catherine Aiken, Jane Tarry-adkins, Susan Ozanne Tags: Poster Session III Source Type: research
759: Comparing insulin, metformin, and glyburide in treating diabetes in pregnancy and analyzing obstetric outcomes
Oral medication was once a mainstay of treating diabetes in pregnancy. Recently, statements from national organizations recommend using only insulin in diabetes management in pregnancy. With few studies comparing the three commonly used agents (insulin, metformin, and glyburide), this study examines current patterns of antidiabetic medication use during pregnancy and describes maternal outcomes. (Source: American Journal of Obstetrics and Gynecology)
Source: American Journal of Obstetrics and Gynecology - December 31, 2019 Category: OBGYN Authors: Meryl Sperling, Jason Bentley, Anna Girsen, Stephanie A. Leonard, Elizabeth B. Sherwin, Danielle M. Panelli, Sanaa Suharwardy, Yasser El Sayed, Tiffany Herrero Tags: Poster Session III Source Type: research
1124: Glyburide is the least effective gestational diabetes therapy to improve neonatal outcomes. A network Meta-analysis
Metformin and glyburide therapy of gestational diabetes mellitus (GDM) continues to increase. Our objective was to compare pre-selected neonatal outcomes in women with GDM treated with insulin, metformin, glyburide or any combination of these. (Source: American Journal of Obstetrics and Gynecology)
Source: American Journal of Obstetrics and Gynecology - December 31, 2019 Category: OBGYN Authors: Julio Mateus, Luis Sanchez Ramos, Kathryn Gonzalez, Melanie Mitta, Jared Roeckner Tags: Poster Session V Source Type: research
The Use of Non-insulin Agents in Gestational Diabetes: Clinical Considerations in Tailoring Therapy
AbstractPurpose of ReviewTo assess evidence to date for use of non-insulin agents in treatment of gestational diabetes mellitus.Recent FindingsThere has been increasing interest in the use of non-insulin agents, primarily metformin and glyburide (which both cross the placenta). Metformin has been associated with less maternal weight gain; however, recent studies have shown a trend toward increased weight in offspring exposed to metformin in utero. Glyburide has been associated with increased neonatal hypoglycemia.SummaryGlycemic control during pregnancy is essential to optimize both maternal and fetal outcomes. There are a...
Source: Current Diabetes Reports - December 5, 2019 Category: Endocrinology Source Type: research
GLP-1 Relaxes Rat Coronary Arteries by Enhancing ATP-Sensitive Potassium Channel Currents.
Abstract GLP-1 is a new type of antidiabetic agent that possesses many beneficial effects. Although its cardiovascular actions have been widely examined, little is known about GLP-1's effects on the rat coronary artery (RCA) or about the mechanisms underpinning these effects. Here, we report that GLP-1 inhibits depolarization- or thromboxane receptor agonist (U46619)-induced RCA contraction in a dosage-dependent manner. Vasorelaxation was attenuated by denuding the endothelium, L-NAME (nitric oxide synthase inhibitor), and glyburide (KATP channel blocker) but was not affected by indomethacin (cyclooxygenas...
Source: Cardiology Research and Practice - November 29, 2019 Category: Cardiology Authors: Xiong QF, Fan SH, Li XW, Niu Y, Wang J, Zhang X, Chen YF, Shi YW, Zhang LH Tags: Cardiol Res Pract Source Type: research
Effect of Berberine on In Vitro Metabolism of Sulfonylureas: A herb-drug interactions study.
CONCLUSIONS: The metabolism of sulfonylureas and berberine was affected when these compounds were co-incubated with each other. This may be attributable to competitive binding of the herb and drug to the catalytic sites of same isozymes. PMID: 31721320 [PubMed - as supplied by publisher] (Source: Rapid Communications in Mass Spectrometry : RCM)
Source: Rapid Communications in Mass Spectrometry : RCM - November 11, 2019 Category: Chemistry Authors: Singh A, Zhao K, Bell C, Shah AJ Tags: Rapid Commun Mass Spectrom Source Type: research
The second-generation anti-diabetic sulfonylureas inhibit Candida albicans and Candidalysin mediated activation of the NLRP3 inflammasome.
Abstract Repurposing of currently approved medications is an attractive option for development of novel treatment strategies against physiological and infectious diseases. The anti-diabetic sulfonylurea glyburide has demonstrated off-target capacity to inhibit activation of the NLRP3 inflammasome in a variety of disease models, including vaginal candidiasis caused primarily by the fungal pathogen Candida albicans Therefore, we sought to determine which of the currently approved sulfonylurea drugs prevent release of IL-1β, a major inflammasome effector, during C. albicans challenge of the human macrophage-...
Source: Antimicrobial Agents and Chemotherapy - November 10, 2019 Category: Microbiology Authors: Lowes DJ, Hevener KE, Peters BM Tags: Antimicrob Agents Chemother Source Type: research
Metformin promotes Mycobacterium tuberculosis killing and increases the production of human β-defensins in lung epithelial cells and macrophages
Publication date: Available online 2 November 2019Source: Microbes and InfectionAuthor(s): Adrian Rodriguez-Carlos, Claudia Valdez-Miramontes, Paulina Marin-Luevano, Irma González-Curiel, Jose A. Enciso-Moreno, Bruno Rivas-SantiagoAbstractDiabetes has been associated with an increased risk of developing tuberculosis. The reasons related to the increased susceptibility to develop TB in type 2 diabetes mellitus (T2DM) individuals, has not been completely elucidated. However, this susceptibility has been attributed to several factors including failures and misfunctioning of the immune system. In the present study, we aimed t...
Source: Microbes and Infection - November 2, 2019 Category: Infectious Diseases Source Type: research
Effect of Olive leaves extract on the antidiabetic effect of glyburide for possible herb-drug interaction
Publication date: Available online 11 October 2019Source: Saudi Pharmaceutical JournalAuthor(s): Maged S. Abdel-Kader, Gamal A. Soliman, Rehab F. Abdel-Rahman, Abdulaziz S. Saeedan, Reham M. Abd-Elsalam, Hanan A. OgalyAbstractThe concomitant use of olive leaves (OL) and glyburide (GLB) is a possible therapy for diabetic patients. However, there is no report about the effect of OL on the antidiabetic effect of GLB till now. In the current study, the possible interaction of olive leaves extract (OLE) with GLB was assessed to determine if there was any pharmacological benefit over GLB alone. Seven groups of male Sprague Dawle...
Source: Saudi Pharmaceutical Journal - October 12, 2019 Category: Drugs & Pharmacology Source Type: research
Mechanisms underlying the effect of an oral antihyperglycemic agent glyburide on calcium ion (Ca2+ ) movement and its related cytotoxicity in prostate cancer cells.
This study examined whether glyburide altered Ca2+ signaling and viability in PC3 human prostate cancer cells and investigated those underlying mechanisms. Intracellular Ca2+ concentrations ([Ca2+ ]i ) in suspended cells were measured by using the fluorescent Ca2+ -sensitive dye fura-2. Cell viability was examined by WST-1 assay. Glyburide at concentrations of 100-1000 μM induced [Ca2+ ]i rises. Ca2+ removal reduced the signal by approximately 60%. In Ca2+ -containing medium, glyburide-induced Ca2+ entry was inhibited by 60% by protein kinase C (PKC) activator (phorbol 12-myristate 13 acetate, PMA) and inhibitor (GF109203...
Source: Clinical and Experimental Pharmacology and Physiology - September 16, 2019 Category: Drugs & Pharmacology Authors: Sun GC, Liang WZ, Jan CR Tags: Clin Exp Pharmacol Physiol Source Type: research
Magnetic Resonance Imaging Pilot Study of Intravenous Glyburide in Traumatic Brain Injury
Journal of Neurotrauma, Ahead of Print. (Source: Journal of Neurotrauma)
Source: Journal of Neurotrauma - August 26, 2019 Category: Neurology Authors: Howard M. Eisenberg Martha E. Shenton Ofer Pasternak J. Marc Simard David O. Okonkwo Christina Aldrich Feng He Sonia Jain Erik G. Hayman Source Type: research