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Synthesis of dolutegravir derivatives modified by 1,2,3-triazole structure and their anti-inflammatory activity in LPS-induced BV2 cells.
Bioorg Med Chem Lett
December 2024
Key Laboratory of Green Chemical Media and Reactions (Ministry of Education), Collaborative Innovation Center of Henan Province for Green Manufacturing of Fine Chemicals, School of Chemistry and Chemical Engineering, Henan Normal University, Xinxiang, Henan 453007, PR China. Electronic address:
Given the promising anti-inflammatory activity of the HIV integrase inhibitor dolutegravir and the widespread use of the 1,2,3-triazole structure in anti-inflammatory drug development, this study aimed to enhance dolutegravir's efficacy by introducing a 1,2,3-triazole group. As a result, four series of dolutegravir derivatives were synthesized. Screening these derivatives for anti-inflammatory activity in microglial cells revealed that compound 6k demonstrated the most potent anti-inflammatory effect without significant cytotoxicity.
View Article and Find Full Text PDFProtective Effects of the Food Supplement Flexovital in a Model of Cardiovascular-Kidney-Metabolic Syndrome in Mice.
Nutrients
November 2024
Department of Physiology and Pharmacology, Karolinska Institutet, 17165 Solna, Sweden.
The prevalence of cardiovascular-kidney-metabolic (CKM) syndrome is increasing rapidly, and cardiovascular complications pose significant risks in individuals with kidney disease and metabolic dysfunction. Understanding the mechanisms of CKM disorders is crucial, as is the discovery of novel preventive treatments. This study aimed to examine the therapeutic effects of a specially formulated nitric oxide-enhancing food additive in a mouse model of CKM syndrome induced by unilateral nephrectomy (UNX) in combination with chronic Western diet (WD) feeding.
View Article and Find Full Text PDFSelectively targeting the AdipoR2-CaM-CaMKII-NOS3 axis by SCM-198 as a rapid-acting therapy for advanced acute liver failure.
Nat Commun
December 2024
Key Laboratory of Spine and Spinal Cord Injury Repair and Regeneration of Ministry of Education, Department of Orthopedic, Tongji Hospital affiliated to Tongji University, School of Life Sciences and Technology, Tongji University, Shanghai, China.
Acute liver failure (ALF) is a hepatology emergency with rapid hepatic destruction, multiple organ failures, and high mortality. Despite decades of research, established ALF has minimal therapeutic options. Here, we report that the small bioactive compound SCM-198 increases the survival of male ALF mice to 100%, even administered 24 hours after ALF establishment.
View Article and Find Full Text PDFHypoxia Microenvironment Preconditioning Attenuated Myocardial Ischemia-Reperfusion Injury via Stc1-Mediating Cardiomyocyte Self-Protection and Neutrophil Polarization.
Adv Sci (Weinh)
December 2024
Department of Cardiology, State Key Laboratory of Organ Failure Research, Nanfang Hospital, Southern Medical University, 1838 North Guangzhou Avenue, Guangzhou, 510515, China.
Ischemic preconditioning (IPC) therapy application to attenuate myocardial ischemia-reperfusion (MI/R) injury in clinical practice remains challenging. The secretome, derived from hypoxia-preconditioned cardiomyocytes (SHPC), potentially mimics the IPC microenvironment and facilitates IPC clinical translation. This study aims to determine whether SHPC can be a feasible alternative to IPC for attenuating MI/R injury, and to identify the functional factor of SHPC.
View Article and Find Full Text PDFAlleviation of lipopolysaccharide-induced heart inflammation in poultry treated with carnosic acid via the NF-κB and MAPK pathways.
J Anim Sci
December 2024
College of Veterinary Medicine, Nanjing Agricultural University, Nanjing 210095, China.
In intensive poultry farming, environmental stress, pathogen infections, and noise can negatively impact growth or cause sudden death, leading to economic losses. The prevalent use of antibiotics as feed additives to prevent diseases in broilers has raised concerns about antibiotic resistance and highlighted the need for safer and more effective alternatives. Carnosic acid (CA), a bioactive compound derived from rosemary, exhibits notable pharmacological properties, including anti-inflammatory and antioxidant effects.
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