Table 1.
Inhibition of β-hematin formation, partition coefficient and antiplasmodial activities of complex 1 and CQDP
Complexes | Inhibition of β-hematin formation | HAI50 (mM) in buffera | HAI50 (mM) in interfaceb | Log Kc | Effect on the in vitro growth strains of P. falciparum (IC50 nM)d | |
---|---|---|---|---|---|---|
FCB1 | FCB2 | |||||
[Au(CQ)(PPh3)]PF6 | + | 3.42 ± 1.89 (0.1) | 0.64 ± 0.02 (5) | 7.69 ± 0.01 | 5.1 | 23 |
CQDP | + | 0.35 ± 0.09 (1) | 3.38 ± 0.13 (1) | 5.84 ± 0.01 | 47 | 110 |
HAI50 is the drug-to-hemin ratio required to inhibit 50% of heme aggregation against a control experiment in the absence of drugs.
Values in parentheses are the relative activity with respect to CQDP.
After 24-h reaction.
After 2 h reaction.
At 25°C.