Characterization of women with gestational diabetes who failed to achieve glycemic control by lifestyle modifications
ConclusionsMaternal baseline characteristics and diabetes diagnostic parameters may predict which women will fail to achieve good glycemic control solely by lifestyle modifications. (Source: Archives of Gynecology and Obstetrics)
Source: Archives of Gynecology and Obstetrics - March 1, 2021 Category: OBGYN Source Type: research

Hypoglycemia and glycemic control with glyburide in women with gestational diabetes and genetic variants of cytochrome P450 2C9 and/or OATP1B3.
In conclusion, the no function variants CYP2C9*3 and OATP1B3*4 are associated with a higher risk of hypoglycemia and a lower dose of glyburide in women with gestational diabetes treated with glyburide, which is consistent with the pharmacokinetic roles of both CYP2C9 and OATP1B3. PMID: 33341937 [PubMed - as supplied by publisher] (Source: Clinical Pharmacology and Therapeutics)
Source: Clinical Pharmacology and Therapeutics - December 20, 2020 Category: Drugs & Pharmacology Authors: Bouchghoul H, Bouyer J, Senat MV, Mandelbrot L, Letourneau A, Bourcigaux N, Becquemont L, Verstuyft C Tags: Clin Pharmacol Ther Source Type: research

Glyburide inhibits non-enzymatic glycation of HSA: An approach for the management of AGEs associated diabetic complications.
In this study, the antiglycation activity of glyburide was investigated using HSA as model protein both against glucose and methylglyoxal mediated glycation. The possible mechanism of action was also deciphered using biophysical and computational tools. Approximately 70% inhibition of both early and advanced glycation end products were recorded in the presence of glyburide. Free lysine modification was reduced by glyburide treatment and improvement in biochemical markers such as free thiol groups and carbonyl content was observed. Interaction studies revealed that glyburide showed moderate to strong binding affinity toward...
Source: International Journal of Biological Macromolecules - December 15, 2020 Category: Biochemistry Authors: Qais FA, Sarwar T, Ahmad I, Khan RA, Shahzad SA, Husain FM Tags: Int J Biol Macromol Source Type: research

Glyburide therapy for gestational diabetes: Glycaemic control, maternal hypoglycaemia, and treatment failure.
CONCLUSIONS: Glyburide is an effective treatment for reaching glycaemic goals during pregnancy in women with GDM. The risk of maternal hypoglycaemia may be minimized by clinical practice experience. These findings could be taken into account in the management of GDM. PMID: 33249198 [PubMed - as supplied by publisher] (Source: Diabetes and Metabolism)
Source: Diabetes and Metabolism - November 26, 2020 Category: Endocrinology Authors: Affres H, Senat MV, Letourneau A, Deruelle P, Coustols-Valat M, Bouchghoul H, Bouyer J Tags: Diabetes Metab Source Type: research

MCCS: a novel recognition pattern-based method for fast track discovery of anti-SARS-CoV-2 drugs.
Abstract Given the scale and rapid spread of the coronavirus disease 2019 (COVID-19) caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2, or 2019-nCoV), there is an urgent need to identify therapeutics that are effective against COVID-19 before vaccines are available. Since the current rate of SARS-CoV-2 knowledge acquisition via traditional research methods is not sufficient to match the rapid spread of the virus, novel strategies of drug discovery for SARS-CoV-2 infection are required. Structure-based virtual screening for example relies primarily on docking scores and does not take the...
Source: Briefings in Bioinformatics - October 20, 2020 Category: Bioinformatics Authors: Feng Z, Chen M, Xue Y, Liang T, Chen H, Zhou Y, Nolin TD, Smith RB, Xie XQ Tags: Brief Bioinform Source Type: research

The antidiabetic drug glibenclamide exerts direct retinal neuroprotection.
Abstract Sulfonylureas, widely used as hypoglycaemic agents in adults with type 2 diabetes, have neuroprotective effects in preclinical models of central nervous system injury, and in children with neuropsychomotor impairments linked to neonatal diabetes secondary to ATP-sensitive potassium channel mutations. In the human and rodent retina, we show that the glibenclamide activated channel SUR1 is expressed in the retina and enriched in the macula; we also show that it co-localizes with the potassium channel Kir6.2, and with the cation channel transporter TRPM4. Glibenclamide (glyburide), administered at do...
Source: Translational Research : the journal of laboratory and clinical medicine - October 17, 2020 Category: Laboratory Medicine Authors: Berdugo M, Delaunay K, Naud MC, Guegan J, Moulin A, Savoldelli M, Picard E, Radet L, Jonet L, Djerada Z, Gozalo C, Daruich A, Beltrand J, Jeanny JC, Kermorvant-Duchemin E, Crisanti P, Polak M, Behar-Cohen F Tags: Transl Res Source Type: research

New drugs on the horizon for cerebral edema: what's in the clinical development pipeline?
Authors: Robert SM, Reeves BC, Alper SL, Zhang J, Kahle KT Abstract INTRODUCTION: Research has advanced our understanding of the molecular and cellular mechanisms of cerebral edema and has propelled the development of novel anti-edema therapeutics. Current evidence supports aberrant neuro-glial ion transport as a central mechanism that underlies pathological fluid accumulation after central nervous system injury. AREAS COVERED: Novel agents in clinical development show potential in altering the natural history and treatment of cerebral edema. Using the PubMed and Google Scholar databases, we review...
Source: Expert Opinion on Investigational Drugs - August 22, 2020 Category: Drugs & Pharmacology Tags: Expert Opin Investig Drugs Source Type: research

Cadmium exposure induces pyroptosis of lymphocytes in carp pronephros and spleens by activating NLRP3.
In this study, lymphocytes were extracted from the pronephros and spleens in carps, respectively. After treating cells with low concentration of Cd, the mRNA and protein expression levels of pyroptosis-related genes, NLRP3, Caspase-1, and pro-inflammatory cytokines, increased obviously. And the content of reactive oxygen species (ROS) and mitochondria reactive oxygen species (mtROS) increased significantly, we also found the activities of CAT, GSH-px and T-SOD reduce significantly, and the content of MDA have a clear upward trend. We then added NLRP3 inhibitor, Glyburide, to the Cd-treated group, further confirming that NL...
Source: Ecotoxicology and Environmental Safety - August 18, 2020 Category: Environmental Health Authors: Zhang Y, Liu Q, Yin H, Li S Tags: Ecotoxicol Environ Saf Source Type: research