Enhanced cytotoxic activity of bile acid cisplatin derivatives by conjugation with gold nanoparticles.
This article explores the potential cytotoxic activity of bile-acid cisplatin derivatives like bisursodeoxycholate(ethylenediamine)platinum(II), PtU2, when conjugated with gold nanoparticles, being a promising alternative to cisplatin in the treatment of cancer due to their lower toxicity. For our purpose we analyzed the intracellular delivery ability of these compounds after conjugation with 20-nm gold nanoparticles (PtU2-AuNPs) in the MG63 (osteosarcoma) cell line. Same platinum uptake after incubation with PtU2 and PtU2-AuNPs-derivatives is associated with a higher cytotoxic activity in case of the platinum-gold nanoparticle conjugate, the overall IC50 of PtU2 being reduced more than 10 fold for these new conjugates. When conjugated with gold nanoparticles, this bile-acid derivative is more efficient than the platinum compound alone in terms of their cytotoxic activity.
Departamento de Química Analítica, Nutrición y Bromatología, Facultad de Ciencias Químicas, Universidad de Salamanca, Plaza de la Merced s/n, Salamanca 37008, Spain.
Sara
S
Sánchez-Paradinas
Centro de Investigación del Cáncer (CIC; IBMCC CSIC/USAL), Servicio de Citometría, Departamento de Medicina and IBSAL, Universidad de Salamanca, Salamanca 37007, Spain.
Martín
M
Pérez-Andrés
Departamento de Química Analítica, Nutrición y Bromatología, Facultad de Ciencias Químicas, Universidad de Salamanca, Plaza de la Merced s/n, Salamanca 37008, Spain.
María Jesús
MJ
Almendral-Parra
Departamento de Química Inorgánica, Facultad de Farmacia, Universidad de Salamanca, Campus "Miguel de Unamuno", Salamanca 37007, Spain.
Emilio
E
Rodríguez-Fernández
Department of Condensed Matter Physics & Materials Research Institute of Aragón, Universidad de Zaragoza, C/ Pedro Cerbuna 12, E-50009 Zaragoza, Spain.
Angel
A
Millán
Department of Condensed Matter Physics & Materials Research Institute of Aragón, Universidad de Zaragoza, C/ Pedro Cerbuna 12, E-50009 Zaragoza, Spain.
Fernando
F
Palacio
Centro de Investigación del Cáncer (CIC; IBMCC CSIC/USAL), Servicio de Citometría, Departamento de Medicina and IBSAL, Universidad de Salamanca, Salamanca 37007, Spain.
Alberto
A
Orfao
Departamento de Química Inorgánica, Facultad de Farmacia, Universidad de Salamanca, Campus "Miguel de Unamuno", Salamanca 37007, Spain.
Julio J
JJ
Criado
Centro de Investigación del Cáncer (CIC; IBMCC CSIC/USAL), Servicio de Citometría, Departamento de Medicina and IBSAL, Universidad de Salamanca, Salamanca 37007, Spain. Electronic address: mfuentes@usal.es.
Manuel
M
Fuentes
D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology; D001647:Bile Acids and Salts / Q000737:chemistry*; D001859:Bone Neoplasms / Q000188:drug therapy / Q000473:pathology; D045744:Cell Line, Tumor; D002945:Cisplatin / Q000031:analogs & derivatives; D004337:Drug Carriers / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D016503:Drug Delivery Systems / Q000379:methods; D006046:Gold; D006801:Humans; D020128:Inhibitory Concentration 50; D053768:Metal Nanoparticles / Q000737:chemistry*; D009944:Organoplatinum Compounds / Q000737:chemistry* / Q000494:pharmacology*; D012516:Osteosarcoma / Q000188:drug therapy / Q000473:pathology
D000970:Antineoplastic Agents; D001647:Bile Acids and Salts; D004337:Drug Carriers; D009944:Organoplatinum Compounds; C542727:bisursodeoxycholate(ethylenediamine)platinum(II); D006046:Gold; D002945:Cisplatin
Bile-acid cisplatin derivatives; Cytotoxic activity; Drug delivery; Gold nanoparticles