Coupling to a glioblastoma-directed antibody potentiates antitumor activity of curcumin- Global Medical Discovery

The paper entitled [Coupling to a glioblastoma-directed antibody potentiates antitumor activity of curcumin] is now featured on Global Medical Discovery as a Key Scientific Article. See the link: 

https://globalmedicaldiscovery.com/key-drug-discovery-articles/coupling-to-a-glioblastoma-directed-antibody-potentiates-antitumor-activity-of-curcumin/

Recognition of the anticancer properties of the food-derived agent curcumin has resulted in an explosion of literature on curcumin.  Although it is hydrophobic and can cross the blood-brain barrier, attempts to use it clinically have been thwarted by its poor solubility in the aqueous body fluids and also its rapid degradation in the body.  Alteration of its functional groups has been attempted, but such attempts either compromises curcumin’s anticancer activity or converts it into a toxic agent.  The referenced studies published in International Journal of Cancer in 2012 (131, E569-E578) and 2014 (135, 710-719) tackle this “poor bioavailability” of curcumin by coupling it in a releasable form to a glioblastoma-specific antibody.  This antibody-curcumin adduct gets rapidly concentrated in the cancer cells in vitro and in vivo. Once endocytosed by cancer cells, the curcumin molecule is released from the adduct by the action of intracellular esterases, thereby causing rapid elimination of the targeted cancer cells.  This versatile approach causes a hundred to two-hundred-fold increase in the anticancer activity of curcumin and can be used for any cancer cell that expresses a specific antigen molecule in excess over other cells.  Because curcumin targets multiple cancer cell-specific pathways and does not kill normal cells, any off-target delivery of curcumin does not eliminate normal cells. These two landmark publications in the International Journal of Cancer have initiated important follow-up studies, which have demonstrated that the relatively non-invasive intranasal route is effective in delivering the antibody-curcumin adduct into the brain. This has now improved the complete rescue rates to 50% in glioblastoma-implanted mice.