ABSTRACT
The present work proposed the preparation of triazolic analogues of tyrosol, a biophenol found in olive oil and whose wide range of bioactivities has been the target of many studies. We obtained fifteen novel tyrosol derivatives and the compounds of the series were later evaluated as acetylcholinesterase (AChE) inhibitors. The study of AChE inhibition is important for the development of new drugs and pesticides, and especially the research for managing Alzheimer's disease. The most active compound, namely 7-({1-[2-(4-hydroxyphenyl)ethyl]-1H-1,2,3-triazol-4-yl}methoxy)-4-methyl-2H-chromen-2-one (30), showed IC50 value of 14.66⯱â¯2.29⯵mol L-1. Docking experiments corroborated by kinetic assay are suggestive of a competitive inhibition mechanism. Derivatives interacted with amino acids from the AChE active site associated to the development of Alzheimer's disease. The results indicate that the compounds synthesized have a high potential as prototypes for the development of new acetylcholinesterase inhibitors.
Subject(s)
Acetylcholinesterase/metabolism , Cholinesterase Inhibitors/pharmacology , Triazoles/pharmacology , Animals , Cholinesterase Inhibitors/chemical synthesis , Cholinesterase Inhibitors/chemistry , Electrophorus , Molecular Docking Simulation , Molecular Structure , Triazoles/chemical synthesis , Triazoles/chemistryABSTRACT
Euphorbia heterophylla L. is regarded as a major weed worldwide. Its high aggressiveness in agricultural environment prompted us to investigate the allelopatic activity and chemical constitution of extracts from roots of this plant. Hexane extract showed low phytotoxic activity. Methanol extract at 2.0 mg mL-1 inhibited 100% of germination, root and shoot growth of the indicator plants Sorghum bicolor and Lactuca sativa. ß-sitosterol, stigmasterol, and esters of lupeol, germanicol, taraxasterol, pseudotaraxasterol, α-amyrin and ß-amyrin were isolated from the hexane extract and their structures elucidated on the basis of MS and 1H, 13C and DEPT-135 NMR data. GC-MS analysis of the derivatized methanol extract allowed for identifying a series of allelopathic organic acids potentially involved in allelopathic interactions of E. heterophylla. This is the first study on the allelopathic activity of extracts and identification of metabolites from roots of E. heterophylla.
Subject(s)
Euphorbia/chemistry , Pheromones/pharmacology , Plant Extracts/chemistry , Plant Extracts/pharmacology , Allelopathy , Gas Chromatography-Mass Spectrometry , Germination/drug effects , Hexanes/chemistry , Lactuca/drug effects , Lactuca/growth & development , Magnetic Resonance Spectroscopy , Methanol/chemistry , Molecular Structure , Oleanolic Acid/analogs & derivatives , Oleanolic Acid/analysis , Pheromones/chemistry , Plant Roots/chemistry , Plant Roots/drug effects , Plant Roots/growth & development , Sorghum/drug effects , Sorghum/growth & development , Sterols/analysis , Sterols/chemistry , Triterpenes/analysis , Triterpenes/chemistryABSTRACT
O tratamento endovascular dos aneurismas de artéria renal tem sido descrito como alternativa à cirurgia convencional. Relatamos o caso de uma paciente com um aneurisma de artéria renal complexo à direita que apresentava hipertensão arterial de difícil controle. O tratamento endovascular foi realizado com a técnica de remodelagem de colo (técnica de Moret), ou técnica de embolização assistida por balão. A paciente obteve normalização da pressão arterial após o procedimento sem recidiva dos sintomas ou necessidade do uso de drogas anti-hipertensivas.
Endovascular treatment of renal artery aneurysms has been described as an alternative to conventional surgery. We report the case of a patient with complex renal artery aneurysm on the right kidney who had hard-to-control arterial hypertension. Endovascular treatment was performed with the aneurysm neck remodeling technique (Moret technique), or balloon-assisted coil embolization. The patient achieved blood pressure normalization after the procedure without recurrence of symptoms or need for antihypertensive drugs.
