The interest on the Mediterranean sponge Haliclona sarai was raised some years ago by the fact that this
sponge appears free from parasites and fouling organisms present in its environment. The study of such a
feature was at the beginning due to the interest in finding new and efficient anti-fouling substances for
applicative purposes. The characteristic was related to the expression of poly-alkylpyridinium salts (poly-
APs), a mixture of two of 3-octylpyridinium polymers, including 29 and 99 monomeric units. The main
effect of this compound was represented by the strong specific and non-toxic acetylcholinesterase inhibition
in vitro. The substance was first tested for its effect on larval development and settling of incrusting
organisms, such as Amphibalanus amphitrite. The experiments confirmed the ability of Poly-APs to prevent
settlement of sessile organism, by impinging on the AChE activity. Acetylcholinesterase is an enzyme
associated to the cholinergic signal system, but is also involved in cell-to-cell communication driving
embryonic development and in the regulation of several cellular features, such as apoptosis and cell
movements, and is present in some tumour cells and biopsies. Cytotoxicity tests on immortalized and
primary cell lines derived from lung tumour (NSCLC) showed a poly-APS dose-dependent selective
reduction of cell viability, statistically significant. The same cells, exposed to the poly-APS salts exhibited a
loss in the mitochondrial potential, and positive response to apoptosis assays. What makes the poly-APS salts
interesting as anticancer therapy adjuvant is that they, at the concentrations inducing apoptosis in tumour
cells, seem to scarcely affect the viability of lymphocytes isolated from healthy patients. In this promising
frame, the need emerges for the isolation of synthetic homologs of poly-APS molecules, in order to start a
study for the therapeutical application of the drug.
Key words: Lung Cancer, Acetylcholinesterase; Apoptosis; Cell Proliferation; Poly-APS
1 Introduction
Nature has supplied several active anticancer
agents (vinca alkaloids, anthracyclines, epipodophyllotoxin,
and taxanes), which have significantly
improved th