TABLE 1.
BBIQ alkaloid (compound no.) | IC50 (μM) against P. falciparum straina,d: |
CC50 (μM) against cancer cell line(s): |
SIf |
||||
---|---|---|---|---|---|---|---|
Dd2 | W2 | D6 | KBb or HCTc | HOEe | KB/W2 | HOE/Dd2 | |
Cycleanine (1) | 17.7 ± 2.0 | 0.25b; 4.5c | 0.07b | >33.7b; 531 (HCT)c | 35.0 ± 0.1 | >133 | 2.0 |
Isochondodendrine (2) | 6.1 ± 1.3 | 0.2c | NDd | 29 (HCT)c | 10.5 ± 1.2 | 116 | 1.7 |
2′-Norcocsuline (3) | 7.0 ± 1.6 | 0.28b | 0.048b | 3.8b | 8.0 ± 0.2 | 14 | 1.1 |
5-[(Dimethylamino)methyl]cycleanine (4) | 0.7 ± 0.1 | ND | ND | ND | 10.0 ± 0.2 | ND | 14.3 |
5-[(Propargylamino)methyl]cycleanine (5) | 1.8 ± 0.2 | ND | ND | ND | 32.0 ± 1.6 | ND | 17.8 |
Chloroquine | 0.18 ± 0.03 | 0.135b | 0.006b | 33.7b | ND | 250 | ND |
In vitro 50% inhibitory concentration (IC50) values of BBIQ alkaloids (compounds 1 to 5) against P. falciparum chloroquine-resistant strains (Dd2 and W2 strains) and the chloroquine-sensitive strain (D6). IC50 values are expressed as mean ± SD for n = 3 independent biological repeats.
IC50 data against P. falciparum W2 and D6 strains and 50% cytotoxic concentration (CC50) values for human oral epidermoid carcinoma (KB) cells were sourced from a previous report (16).
IC50 data against chloroquine-resistant P. falciparum strain W2 and CC50 values for HCT-116 human colon carcinoma cells were sourced from a previous report (18).
ND, not determined.
CC50 data for human ovarian epithelial (HOE) cells. Data in this column for compounds 1 to 5 were sourced from our previous reports (13, 15).
This selectivity index (SI) was calculated as CC50 /IC50 against P. falciparum.