TABLE 1.
Summary of cytotoxicity, immunosuppressive activity, and antifungal activity of FK506 structural analogsa
| FK506 analog | Concn for 50% cytotoxicity (μg/ml) | Concn for 50% immunosuppression (ng/ml) |
Cryptococcus neoformans |
Candida albicans |
Aspergillus fumigatus |
|||
|---|---|---|---|---|---|---|---|---|
| IC50 (μg/ml) | Avg IC50 (μg/ml) | IC50 (μg/ml) | Avg IC50 (μg/ml) | IC50 (μg/ml) | Avg IC50 (μg/ml) | |||
| FK506 | ≃0.001 | 0.027 | 0.001 | 0.0007 | 0.005 | 0.01208 | 0.015 | 0.0313 |
| 9DP-FK506 | >1 | 268.300 | 4.813 | >12.5 | 322.000 | >10 | >50.000 | >50 |
| 9D-FK506 | 1 | 0.513 | 0.039 | 0.0016 | 0.963 | 1.410 | 24.190 | 4.6340 |
| 31OD-FK506 | >1 | 0.246 | 0.007 | 0.0018 | 0.106 | 0.08696 | 0.165 | 0.1797 |
| 9D31OD-FK506 | >1 | 15.090 | 0.175 | 0.0026 | 2.796 | 3.239 | 29.770 | 19.5500 |
a
Abbreviations: 9DP-FK506, 9-deoxo-prolyl-FK506; 9D-FK506, 9-deoxo-FK506; 31OD-FK506, 31-O-demethyl-FK506; 9D31OD-FK506, 9-deoxo-31-O-demethyl-FK506; IC50, 50% inhibitory concentration.