From the marine sponge Reniera sarai 3-alkylpyridinium oligomers and polymers have been isolated. 3-Alkylpyridinium polymers are potent anticholinesterase agents; in addition, they show hemolytic and cytotoxic activities. Oligomers with a molecular weight lower than 3000 Da do not possess any significant activity. We report structural characterization of 3-alkylpyridinium polymers and their beh...

A novel series of meta-substituted ethanediamide and 2-butenediamide derivatives were synthesized and tested for their ability to inhibit electric eel acetylcholinesterase (AChE) and equine serum butyrylcholinesterase (BuChE). The synthesized compounds were evaluated against ChE enzymes using the colorimetric method described by Ellman et al. (Biochem. Pharmacol., 7, 1961). It was revealed that...

Five sesquiterpene coumarin ethers: umbelliprenin, umbelliprenin-10',11'-monoepoxide, conferone, mogoltacin and feselol were isolated from the fruits of Heptaptera cilicica. Their structures were identified by means of spectroscopic methods. AChE and BuChE inhibitory activities of the compounds were determined by molecular docking method which were confirmed by in vitro experiments. According t...

Nerve agents are organophosphate compounds similar to those used as pesticides but with much higher toxicity. They all block the activity of the enzyme acetylcholine esterase. Victims are intoxicated by absorption of the toxin via exposed skin or, more commonly, via inhalation of the poisonous gas. The resultant clinical picture is of hyperstimulation of both the nicotinic and muscarinic cholin...

In this study, novel N'-(3-cyclohexyl/phenyl-4-(substituted phenyl)thiazole-2(3H)-ylidene)-2-[(5,6,7,8-tetrahydronaphthalen-2-yl)oxy]acetohydrazide (4a-4k) derivatives were synthesized and their anticancer potency were evaluated on human breast adenocarcinoma cell line (MCF-7), human lung carcinoma cell line (A549) and mouse embryoblast cell line (NIH/3T3) using the MTT method, DNA synthesis in...

Huperzine A (HupA), isolated originally from a traditional Chinese medicine Qiang Ceng Ta, whole plant of Huperzia serrata (Thunb. ex Murray) Trev., a member of the Huperziaceae family, has attracted intense attention since its marked anticholinesterase activity was discovered by Chinese scientists. Several members of the Huperziaceae (Huperzia and Phlegmariurus species) have been used as medic...

Centella asiatica (CA), commonly named gotu kola, is an Ayurvedic herb used to enhance memory and nerve function. To investigate the potential use of CA in Alzheimer's disease (AD), we examined the effects of a water extract of CA (GKW) in the Tg2576 mouse, a murine model of AD with high β-amyloid burden. Orally administered GKW attenuated β-amyloid-associated behavioral abnormalities in these ...