TY - JOUR
T1 - Outstanding plasmodicidal properties within a small panel of metallic compounds
T2 - Hints for the development of new metal-based antimalarials
AU - Gabbiani, Chiara
AU - Messori, Luigi
AU - Cinellu, Maria A.
AU - Casini, Angela
AU - Mura, Pasquale
AU - Sannella, Anna R.
AU - Severini, Carlo
AU - Majori, Giancarlo
AU - Bilia, Anna R.
AU - Vincieri, Franco F.
N1 - Funding Information:
A.C. and C.G. wish to thank AIRC for providing them with research fellowships. Ente Cassa di Risparmio di Firenze and Toscana Life Sciences are gratefully acknowledged for financial support.
PY - 2009/2
Y1 - 2009/2
N2 - A variegate group of metallodrugs was evaluated in vitro for antimalarial activity through the pLDH test. The panel comprised one mononuclear gold(III) complex, (Aubipy), three dinuclear gold(III) compounds (Auoxo4, Auoxo5 and Auoxo6), three ruthenium(III) complexes (NAMI A, PMRU20, PMRU27), one ruthenium(II) complex (PMRU52), one bismuth(III) compound (Bismuth citrate), antimony trichloride (SbCl3) and arsenic trioxide (As2O3). This panel, although relatively small, was built up in such a way to include a variety of metal centers, structural motifs and metal coordination environments. In general, the tested compounds turned out to contrast effectively Plasmodium falciparum growth in vitro. In two cases, i.e. NAMI A and antimony trichloride, IC50 values in the high nanomolar range were measured. Notably, the antiplasmodial effects appear not to be correlated to in vitro anticancer properties. The mechanistic and pharmacological implications of the obtained results are discussed.
AB - A variegate group of metallodrugs was evaluated in vitro for antimalarial activity through the pLDH test. The panel comprised one mononuclear gold(III) complex, (Aubipy), three dinuclear gold(III) compounds (Auoxo4, Auoxo5 and Auoxo6), three ruthenium(III) complexes (NAMI A, PMRU20, PMRU27), one ruthenium(II) complex (PMRU52), one bismuth(III) compound (Bismuth citrate), antimony trichloride (SbCl3) and arsenic trioxide (As2O3). This panel, although relatively small, was built up in such a way to include a variety of metal centers, structural motifs and metal coordination environments. In general, the tested compounds turned out to contrast effectively Plasmodium falciparum growth in vitro. In two cases, i.e. NAMI A and antimony trichloride, IC50 values in the high nanomolar range were measured. Notably, the antiplasmodial effects appear not to be correlated to in vitro anticancer properties. The mechanistic and pharmacological implications of the obtained results are discussed.
KW - Gold(III) complexes
KW - Malaria
KW - Plasmodium falciparum
KW - Ruthenium complexes
UR - http://www.scopus.com/inward/record.url?scp=58149507982&partnerID=8YFLogxK
U2 - 10.1016/j.jinorgbio.2008.10.004
DO - 10.1016/j.jinorgbio.2008.10.004
M3 - Article
C2 - 19027959
AN - SCOPUS:58149507982
SN - 0162-0134
VL - 103
SP - 310
EP - 312
JO - Journal of Inorganic Biochemistry
JF - Journal of Inorganic Biochemistry
IS - 2
ER -
