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Hypoxia Activated Nitric Oxide Donor Compounds for the Prevention and Treatment of Myocardial Hypoxia-Induced Injury.
J Med Chem
January 2025
Pharmaceutical Research Center and School of Chemistry and Chemical Engineering, Southeast University, Nanjing 211189, China.
A series of hypoxia-targeted nitric oxide donor compounds were designed and synthesized by using an ether linker to connect -methyl--nitroso--phenol and nitrobenzyl alcohols, respectively. Among them, , with acceptable pharmacokinetic parameters in mice, exhibited a high selective NO release in H9c2 cells under hypoxia and in the dissected heart tissue of the tested mice as desired. Mechanistic investigations revealed that could regulate vascular dilation and modulate proteins associated with myocardial injury both and .
View Article and Find Full Text PDFOrganic vs. inorganic nitrates: Metabolic and vascular outcomes in STZ-induced diabetes in mice.
Life Sci
December 2024
Biotechnology Center, Federal University of Paraíba, João Pessoa, Brazil. Electronic address:
Background: Diabetic animals often display dysregulated nitric oxide (NO) metabolism, contributing to vascular dysfunction. This study evaluates the metabolic and vascular effects of organic nitrate isosorbide mononitrate (ISMN) versus inorganic sodium nitrate (NaNO3) in mice with type 1 diabetes mellitus (T1DM) induced by streptozotocin (STZ).
Experimental Approach: T1DM was induced in male C57Bl6 mice with STZ ip and confirmed by fasting glucose.
Combination treatment with cilostazol and isosorbide mononitrate attenuates microemboli-mediated vascular cognitive impairment and improves imaging and plasma biomarkers in diabetic rats.
Exp Neurol
January 2025
Ralph H. Johnson VA Medical Center, Charleston, SC, United States of America; Department of Pathology & Laboratory Medicine, Medical University of South Carolina, Charleston, SC, United States of America.
Diabetes is a major risk factor for all types of dementia. The underlying reasons are not fully understood, and preventive therapeutic strategies are lacking. Previously we have shown that diabetic but not control rats developed a progressive cognitive decline in a microemboli (ME) model of vascular contributions to cognitive impairment & dementia (VCID).
View Article and Find Full Text PDFNew Skin-Relevant Cell Coculture Model With Stratum Corneum-Like Layer.
Biomed Res Int
June 2024
Department of Dermatological Research Sunny BioDiscovery Inc., 972 E. Main Street, Santa Paula, California, USA.
Two-dimensional (2D) cell culture is an important tool in the discovery of skin-active agents. Fibroblasts and keratinocytes, more rarely fibroblast-keratinocyte cocultures, are usually used for that purpose, where test compounds are added by mixing with the overlaying growth medium. However, such an approach is suboptimal because it lacks the component.
View Article and Find Full Text PDFEvaluation of the safety and efficacy of skin penetration enhancer Putocrin®.
J Cosmet Dermatol
October 2024
Vitargent (International) Biotechnology Limited, Hong Kong, China.
Background: Substances that can efficiently enhance skin penetration while exerting no adverse effect are useful for drug and cosmetics formulation.
Objective: To investigate the safety and enhance skin penetration efficacy of Putocrin®, a combination containing 2% isosorbide dimethyl ether, 1% pentanediol, and 0.5% inositol.
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