Canadian Journal of Physiology and Pharmacology. Oct, 2017, Vol. 95 Issue 10, p1091, 9 p.
Fibrosis -- Physiological aspects, Fibrosis -- Care and treatment, Heart diseases -- Physiological aspects, Heart diseases -- Care and treatment, and Cardiac patients -- Physiological aspects
Cardiac fibrosis is a significant global health problem that is closely associated with multiple forms of cardiovascular disease, including myocardial infarction, dilated cardiomyopathy, and diabetes. Fibrosis increases myocardial wall stiffness due to excessive extracellular matrix deposition, causing impaired systolic and diastolic function, and facilitating arrhythmogenesis. As a result, patient morbidity and mortality are often dramatically elevated compared with those with cardiovascular disease but without overt fibrosis, demonstrating that fibrosis itself is both a pathologic response to existing disease and a significant risk factor for exacerbation of the underlying condition. The lack of any specific treatment for cardiac fibrosis in patients suffering from cardiovascular disease is a critical gap in our ability to care for these individuals. Here we provide an overview of the development of cardiac fibrosis, and discuss new research directions that have recently emerged and that may lead to the creation of novel treatments for patients with cardiovascular diseases. Such treatments would, ideally, complement existing therapy by specifically focusing on amelioration of fibrosis. Key words: cardiac fibrosis, extracellular matrix, fibrosis therapy, fibroblast, myofibroblast. A l'echelle mondiale, la fibrose cardiaque est un important probleme de sante etroitement lie a diverses formes de maladies cardiaques, y compris l'infarctus du myocarde, la cardiomyopathie dilatee et le diabete. La fibrose entraine une augmentation de la rigidite de la paroi myocardique en raison du depot d'un exces de matrice extracellulaire, ce qui affecte les fonctions systolique et diastolique et qui favorise l'arythmogenese. En consequence, les taux de morbidite et de mortalite des patients sont souvent considerablement plus eleves qu'en absence de fibrose manifeste, ce qui montre que la fibrose elle-meme est a la fois une reaction pathologique a une maladie existante et un important facteur de risque de l'exacerbation de l'affection sous-jacente. Le manque de tout traitement specifique de la fibrose cardiaque chez les patients atteints de maladie cardiovasculaire constitue une lacune cruciale dans notre capacite de soigner ces personnes. Nous presentons ici un apercu de la formation de fibrose cardiaque, et nous discutons de nouvelles avenues de recherche emergentes qui pourraient mener au developpement de nouveaux traitements pour les patients atteints de maladies cardiovasculaires. Idealement, de tels traitements pourraient apporter un complement aux traitements existants en se centrant specifiquement sur des ameliorations en matiere de fibrose. [Traduit par la Redaction] Mots-cles: fibrose cardiaque, matrice extracellulaire, traitement de la fibrose, fibroblaste, myofibroblaste.
Al-Shamary, Danah S., Al-Alshaikh, Monirah A., Kheder, Nabila Abdelshafy, Mabkhot, Yahia Nasser, and Badshah, Syed Lal
Chemistry Central Journal. May 31, 2017, Vol. 11 Issue 1
Organic compounds -- Research, Cancer -- Care and treatment, and Cancer -- Research
Background The quinazoline are an important class of medicinal compounds that possess a number of biological activities like anticancer, anticonvulsant and antioxidant etc. Results We evaluated the previously synthesized quinazoline derivatives 1-3 for their anticancer activities against three cancer cell lines (HepG2, MCF-7, and HCT-116). Among the tested compounds, quinazolines 1 and 3 were found to be more potent than the standard drug Vinblastine against HepG2 and MCF-7 cell lines. All the tested compounds had less antioxidant activity and did not exhibit any anticonvulsant activity. Also, molecular docking studies were performed to get an insight into the binding modes of the compounds with human cyclin-dependent kinase 2, butyrylcholinesterase enzyme, human gamma-aminobutyric acid receptor. These compounds showed better docking properties with the CDK2 as compared to the other two enzymes. Conclusions The overall study showed that thioxoquinazolines are suitable antitumor agents and they should be explored for other biological activities. Modification in the available lot of quinazoline and synthesis of its novel derivatives is essential to explore the potential of this class of compounds. The increase in the threat and with the emergence of drug resistance, it is important to explore and develop more efficacious drugs. Keywords: Thioxoquinazolin-4(3H)-one, Anticancer activity, Antioxidant activity, Anticonvulsant activity, Molecular docking
Privacy issue, Company Web site/Web page, Company business management, Computer services industry, Web sites -- Safety and security measures, Computer services industry -- Safety and security measures, Computer services industry -- Management, and Privacy -- Reports
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