Current Bioactive Compounds - Volume 6, Issue 3, 2010

The Vesicular Acetylcholine Transporter (VAChT) is found throughout the cholinergic nervous system and is responsible for transporting Acetylcholine (ACh) into synaptic vesicles for storage. Deterioration of cholinergic neurotransmission is a known pathophysiological hallmark of Alzheimer's disease (AD). Ligands that bind to VAChT - particularly in the brain and CNS where cholinergic neurotransmission is vital for memory and cognitive function - may facilitate the study of cholinergic pathway regulation in the CNS and serve as useful diagnostic agents for AD. Vesamicol was the first VAChT ligand identified, however its poor selectivity has prompted the search for more potent and selective compounds. Numerous structural modifications to the vesamicol scaffold have been explored and several classes of VAChT ligands are highlighted in this review. The affinity and selectivity of these ligands for VAChT and σ-receptors are discussed.

Several investigations have unveiled multiple effects of the ployphenol curcumin on immune responses, both in physiological and in pathological conditions. Here we review the biochemistry of this compound in the context of its potential and limitations as possible therapeutic modulator of immune responses.

Ellagic acid is a polyphenol antioxidant found in numerous fruits and vegetables including raspberries, strawberries, cranberries, walnuts, pecans, pomegranates and other plant foods. The antiproliferative and antioxidant properties of ellagic acid have spurred several researches into the potential health benefits of its consumption, leading to its marketing as a dietary supplement. Recently, ellagic acid was shown to display interesting and usable antimalarial activity. However, the relatively insolubility of this compound in water and organic solvents, and its low bioavailability tend to disqualify it as a potential drug candidate. In this review, we will discuss the potential of ellagic acid and derivatives as antimalarial drug candidates. While highlighting their numerous biological and pharmacological activities against other human ailments, we will evaluate the possibility of developing this family of compounds as antimalarial drugs, and discuss strategies and related challenges to achieve that goal.

In this review we cover the names, structures, and occurrence of all the scalaranes since their discovery in 1972. We have given special attention to the biological properties of these polycyclic terpenoids of exclusive marine origin.