Four New Groups of Aza-Macrolides from the Madagascar Sponge Fascaplysinopsis Sp.

A large variety of  unique N-atom containing compounds ( alkaloids ) without terrestrial counterparts , have been isolated from marine  invertebrates mainly sponges and  ascidians. Many of these compounds display interesting biological activities.  four groups of secondary metabolites ,  salarins , tulearins , taumycins and tausalarin have been isolated from the Madagascr sponge Fascaplysinopsis sp.. Several salarin C derivatives have been synthesized for  SAR , e.g. glycosidation of  a desoctanoyl derivative. 

We have found that salarins and tulearins inhibit cell proliferation, and modulate the cycle of cultured cell lines from both mouse and human origins ( D. Neumann , N. Ben-Califa  , 2010 , 2012 ). The novelty regarding these compounds stems from the fact that the "effect size" on proliferation and on cell cycle parameters that they manifest is different for each one of the tested cell lines. These features may be reflected in differential effects/potency of the compounds on transformed cells versus normal cell lineages, thus placing these new compounds as attractive candidates for further development as “custom-designed” anti-cancer agents. Our research plans are thus focused on resolving the molecular mechanisms underlying the activity of these compounds and pinpointing functional groups that are responsible for their differential bio-activity.