ABSTRACT
Among the cardiotonics (agents against congestive heart failure), the most important group is of the digitalis cardiac glycosides, but since these compounds suffer from a low therapeutic index, attention has been paid to investigating safer cardiotonic agents through the inhibition of Na+,K+-ATPase, the mechanism by which the digitalis cardiac glycosides elicit their action. Recently, a series of perhydroindenes were studied for their Na+,K+-ATPase inhibition activity. We report here a QSAR study on them to investigate the physicochemical and structural properties of the molecules that govern their activity in order to rationalize the structural modification to have more potent drugs. A multiple regression analysis reveals a significant correlation between the Na+,K+-ATPase inhibition activity of the compounds and Kier’s first order valence molecular connectivity index of their R5-substituents and some indicator parameters, suggesting that the R5-substituents of the compounds containing atoms with low valence and high saturation and the R1-substituents having =N−O− moiety will be conducive to the activity.
Subject(s)
Cardiotonic Agents/chemical synthesis , Cardiotonic Agents/chemistry , Digitalis/chemistry , Digitalis Glycosides/antagonists & inhibitors , Digitalis Glycosides/chemistry , Enzyme Inhibitors/chemistry , Quantitative Structure-Activity Relationship , Regression Analysis , Sodium-Potassium-Exchanging ATPase/antagonists & inhibitorsABSTRACT
Antimicrobial activity of the methanolic extracts of leaves and flowers of D. lamarckii Ivan, (Scophulariaceae), an endemic plant species of Turkey, was tested on ten bacterial and four yeast strains. Effective antibacterial activity was observed in four bacterial strains. Minimum inhibitory concentration (MIC) was calculated by use of liquid culture tests and in all the four effective bacterial strains, the MIC was found to be > or = 199.5 mg/ml. The minimum bactericidal concentration (MBC) of B. subtilis, S. aureus, and L. monocytogenes was calculated to be > or = 199.5 mg/ml, and MBC value for Shigella was calculated as > or = 399 mg/ml.
Subject(s)
Anti-Bacterial Agents/isolation & purification , Anti-Bacterial Agents/pharmacology , Antifungal Agents/isolation & purification , Antifungal Agents/pharmacology , Digitalis/chemistry , Digitalis/growth & development , Methanol , Microbial Sensitivity Tests , Plant Extracts/isolation & purification , Plant Extracts/pharmacology , TurkeyABSTRACT
Se presentan aspectos históricos, fitoquímicos, farmacológicos, toxicológicos y referentes a la utilidad medicinal de Digitalis spp., género con gran valor ornamental y comercial, sobre todo para elaborar purpureaglucósidos, digitoxina y gitoxina, compuestos utilizado en el tratamiento de enfermedades cardiacas. Digitalis purpurea fue utilizada desde el siglo XI y experimentada científicamente por W. Whitering en 1785, Inglaterra. Se le cultiva en Europa y en Estados Unidos de América del Norte, al igual que otras especies como Digitalis lanata Ehrh. y Digitalis lutea L.; actualmente son objeto de numerosos estudios y cultivos in vitro