ABSTRACT
Acute stress is a feature of our daily events that affects cardiovascular system and predisposes to hypertension. H2S is now considered as a vasorelaxant gasotransmitter although it was considered as a toxic agent. In present work we studied the effect of H2S releasing Na2S in acute stress induced hypertension and cardiac damage. Rats were divided into five groups: control, Na2S, acute stress, half dose of Na2S (6 mg/kg), and finally full dose of Na2S (12 mg/kg) to acute stressed rats. BP was measured then blood samples were taken for estimation of cortisol, cardiac enzymes markers, IL-6 and H2S. Finally, animals were sacrificed, hearts and thoracic aortae were excised for histological assessment, estimation of MDA, SOD and RNA extraction of CSE. Acute stress significantly elevated BP, cortisol, cardiac enzymes markers, IL-6, and tissue levels of MDA. It also, induced cardiac cell damage with congested B.V., extravasation of blood and decreased eNOs. Moreover, acute stress reduced H2S levels, RNA expression of CSE and SOD in cardiac tissues. Na2S significantly decreased BP, serum levels of cortisol, cardiac enzymes markers, IL-6, and tissue levels of MDA. Also, Na2S elevated serum H2S, RNA expression of CSE, SOD in cardiac tissue and increased eNOs activity.
Subject(s)
Hydrogen Sulfide/pharmacology , Hypertension/enzymology , Hypertension/etiology , Nitric Oxide Synthase Type III/metabolism , Protective Agents/pharmacology , Stress, Psychological/complications , Sulfides/pharmacology , Animals , Aorta, Thoracic/pathology , Biomarkers/metabolism , Blood Pressure/drug effects , Cystathionine gamma-Lyase/genetics , Cystathionine gamma-Lyase/metabolism , Gene Expression Regulation, Enzymologic/drug effects , Hydrocortisone/metabolism , Hypertension/blood , Interleukin-6/blood , Interleukin-6/metabolism , Myocardium/enzymology , Oxidative Stress , Rats , Stress, Psychological/blood , Systole/drug effectsABSTRACT
The pyrimidine thione derivatives 2a-d were prepared by the reaction of thiourea, ethyl cyanoacetate and several aromatic aldehydes. The acyclic thioglycosides 4a-7d were prepared by the reaction of the synthesized pyrimidine thiones 2a-d with different alkyl halides, whereas the reaction of 2a-d with 2,3,4,6-tetra-O-acetyl-alpha-D-glucopyranosyl bromide afforded the cyclic thioglycosides 8a-d whose deprotection afforded 9a-d. The obtained compounds were tested for their antischistosomal and antiviral activity against hepatitis B virus (HBV). Compounds 5a, 5d, 7a showed high activity against HBV using the MTT assay; moreover compounds 5c, 6d, 7a, 9a, 9c exhibited high activity as antischistosomal agents.
Subject(s)
Antiviral Agents/chemical synthesis , Schistosomicides/chemical synthesis , Thioglycosides/chemical synthesis , Animals , Antiviral Agents/pharmacology , Carcinoma, Hepatocellular , Cell Line, Tumor/drug effects , Enzyme-Linked Immunosorbent Assay , Humans , Lamivudine/pharmacology , Liver Neoplasms , Pyrimidines/chemical synthesis , Pyrimidines/pharmacology , Schistosoma mansoni/drug effects , Schistosomicides/pharmacology , Spectrophotometry, Infrared , Thioglycosides/pharmacology , Thiones/chemical synthesis , Thiones/pharmacologyABSTRACT
Six new examples of intercalating nucleic acids were synthesized in order to evaluate the dependence of the length of the linker between oligo and intercalator on the thermal stability of their corresponding duplexes and triplexes.