Antileishmanial Activities of Aphidicolin and Its Semisynthetic Derivatives

DOI: 10.1128/AAC.45.1.288-292.2001

Article Figures & Data

Open in new tab
Download powerpoint
Fig. 1.
Chemical structures of aphidicolans used in this study.

Table 1.

Antileishmanial activities of aphidicolin and derivatives

Compound^a	EC₅₀ (μg/ml) against parasite:					EC₅₀ (μg/ml) for cytotoxicity to cells:			SI^b
Compound^a	L. major (extracellular)	L. donovani (extracellular)	L. infantum (extracellular)	L. enriettii (extracellular)	L. donovani (intracellular)	BMMφ	KB	SK-Mel	SI^b
1	0.19	0.54	0.14	0.31	0.12	>25.0	>25.0	>25.0	208
2	1.77	2.50	1.70	1.88	0.95	>25.0	>25.0	>25.0	26
3	1.83	0.62	0.99	1.32	0.11	24.9	>25.0	>25.0	226
4	0.40	0.60	0.42	0.42	0.21	>22.4	>25.0	>25.0	106
5	0.09	0.08	0.10	0.10	0.05	18.2	>25.0	>25.0	364
6	0.05	0.04	0.06	0.04	0.20	>25.0	>25.0	>25.0	125
7	0.51	0.31	0.50	0.51	0.36	>25.0	>25.0	>25.0	69
8	1.09	0.63	1.70	1.14	1.11	>25.0	>25.0	>25.0	23
9	0.38	0.31	0.95	0.33	0.20	>25.0	>25.0	>25.0	125
10	0.41	0.32	0.95	0.65	0.25	>25.0	>25.0	>25.0	100
11	0.37	0.27	0.89	0.61	0.24	>25.0	>25.0	>25.0	104
12	0.54	1.25	0.67	3.30	0.56	>25.0	>25.0	>25.0	44
13	>5.0	>5.0	>5.0	>5.0	>5.0	>25.0	>25.0	>25.0	5
14	0.12	0.08	0.12	0.12	0.09	>25.0	>25.0	>25.0	277
15	0.45	0.66	0.44	0.57	0.20	>25.0	>25.0	>25.0	16
16	1.25	>5.0	>5.0	3.30	>5.0	>25.0	>25.0	>25.0	5
17	1.25	1.84	1.88	0.85	1.51	>25.0	>25.0	>25.0	16
18	0.12	0.20	0.21	0.11	0.02	11.3	>25.0	>25.0	565
AMB	0.03	0.03	0.04	0.02	0.025	>25.0	>25.0	>25.0	1,000
MF	0.02	0.05	0.06	0.02	0.002	>25.0	>25.0	>25.0	<12,500