The multifaceted nature of Alzheimer's disease (AD) has led to the development of multi-targeted compounds based on the classical AD drug, tacrine, first known to inhibit the acetylcholine-degrading enzyme acetylcholinesterase (AChE). In the present work, we explore the potentiality of multimers of tacrine in this field. The synthesis using the so-called "click chemistry" and the in vitro study...

A flow-injection pulse amperometric method for determining tacrine, based on ion transfer across a plasticized poly(vinyl chloride) (PVC) membrane, was developed. A four-electrode potentiostat with ohmic drop compensation was used, while a flow-through cell incorporated the four electrodes and the membrane, which contained tetrabutylammonium tetraphenylborate. The influence of the applied poten...

The purpose of this investigation was to explore the potentiality of a novel animal model to be used for the in vivo evaluation of the ability of a drug delivery system to promote the passage through the blood-brain barrier (BBB) and/or to improve the brain localization of a bioactive compound. A Tween 80-coated poly-L-lactid acid nanoparticles was used as a model of colloidal drug delivery sys...

BACKGROUND approximately one-third of patients with Alzheimer's disease (AD) respond favourably to the anticholinesterase tacrine, but the drug's usefulness is marred by a high incidence of side-effects. OBJECTIVE to discover if AD patients with white matter low attenuation (WMLA) represents a subgroup that responds differently to tacrine from those with no WMLA. DESIGN the results come fro...

We have recently reported that phlorofucofuroeckol A isolated from Ecklonia stolonifera showed potential antioxidative and anti-inflammatory properties in LPS-stimulated macrophages. This study aims to investigate the cytoprotective effect of phlorofucofuroeckol A and to characterize its molecular mechanisms using tacrine-treated HepG2 cells. Phlorofucofuroeckol A showed a cytoprotective effect...

The present study investigated the protective effect of the ethanolic extract of Psidium guajava L. against tacrine-induced orofacial dyskinesia in rats. Behavioral assessments such as vacuous chewing movements, tongue protrusions, orofacial bursts, locomotion, and cognition were recorded. Forebrain of tacrine treated animals was assessed for its antioxidant levels. P. guajava (100 and 200 mg/k...

The synthesis of four tetra-tacrine clusters where the tacrine binding units are attached to a central scaffold via linkers variable lengths is described. multivalent inhibition potencies for were investigated acetylcholinesterase. Two displayed small but significant potency in which affinity each increased up 3.2 times when they connected scaffold.

The neuroprotective properties of bis(7)-tacrine, a novel dimeric acetylcholinesterase (AChE) inhibitor, on glutamate-induced excitotoxicity were investigated in primary cultured cerebellar granule neurons (CGNs). Exposure of CGNs to 75 mum glutamate resulted in neuronal apoptosis as demonstrated by Hoechst staining, TUNEL, and DNA fragmentation assays. The bis(7)-tacrine treatment (0.01-1 mum)...

A spectrofluorimetric method to determine tacrine is proposed and applied to the determination of tacrine in human serum and pharmaceuticals. The fluorimetric method allows the determination of 1-70 ng ml-1 of tacrine in aqueous solutions containing acetic acid-sodium acetate buffer (pH 5.6) with lambda exc = 242 nm and lambda em = 362 nm.

OBJECTIVES To determine the effects of cholinesterase inhibition with tacrine hydrochloride for the symptoms of Alzheimer disease in terms of cognitive performance, clinical global impression, behavior, and functional autonomy. DATA SOURCES The Cochrane Dementia Group registry of trials. STUDY SELECTION Unconfounded, randomized, double-blind, placebo-controlled trials in which tacrine had b...