title: Folic acid-conjugated 4-amino-phenylboronate, a boron-containing compound designed for boron neutron capture therapy, is an unexpected agonist for human neutrophils and platelets.
abstract: Boron neutron capture therapy (BNCT) is an anticancer treatment based on the accumulation in the tumor cells of (10) B-containing molecules and subsequent irradiation with low-energy neutrons, which bring about the decay of (10) B to very toxic (7) Li(3+) and (4) He(2+) ions. The effectiveness of BNCT is limited by the low delivery and accumulation of the used (10) B-containing compounds. Here, we report the development of folic acid-conjugated 4-amino-phenylboronate as a novel possible compound for the selective delivery of (10) B in BNCT. An extensive analysis about its biocompatibility to mature blood cells and platelet progenitors revealed that the compound markedly supports platelet aggregation, neutrophil oxidative burst, and inhibition of megakaryocyte development, while it does not have any manifest effect on red blood cells.
authors.affiliation: Laboratories of Biochemistry, Department of Biology and Biotechnology, University of Pavia, via Bassi, 21, Pavia, 27100, Italy.
authors.forename: Cesare
authors.initials: C
authors.lastname: Achilli
authors.forename: Sushilkumar A
authors.initials: SA
authors.lastname: Jadhav
authors.forename: Gianni F
authors.initials: GF
authors.lastname: Guidetti
authors.forename: Annarita
authors.initials: A
authors.lastname: Ciana
authors.forename: Vittorio
authors.initials: V
authors.lastname: Abbonante
authors.forename: Alessandro
authors.initials: A
authors.lastname: Malara
authors.forename: Maurizio
authors.initials: M
authors.lastname: Fagnoni
authors.forename: Mauro
authors.initials: M
authors.lastname: Torti
authors.forename: Alessandra
authors.initials: A
authors.lastname: Balduini
authors.forename: Cesare
authors.initials: C
authors.lastname: Balduini
authors.forename: Giampaolo
authors.initials: G
authors.lastname: Minetti
mesh_terms: D001792:Blood Platelets / Q000166:cytology / Q000187:drug effects; D016754:Boron Neutron Capture Therapy; D001897:Boronic Acids / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D002454:Cell Differentiation / Q000187:drug effects; D005492:Folic Acid / Q000737:chemistry*; D006801:Humans; D008533:Megakaryocytes / Q000166:cytology; D009504:Neutrophils / Q000187:drug effects*; D010974:Platelet Aggregation / Q000187:drug effects
chemical_list: D001897:Boronic Acids; D005492:Folic Acid; C010686:benzeneboronic acid
keywords: biocompatibility; blood cells; boron neutron capture therapy; erythrocytes; granulocytes; inflammation; megakaryocytes; platelets; thrombosis; toxicology