Table 2.
Anti-HBV activity and cytotoxicity of caudatin derivatives in Vitro.a
| Compd | CC50b (μM) | HBsAgc |
HBeAgd |
DNA replication |
|||
|---|---|---|---|---|---|---|---|
| IC50e (μM) | SIf | IC50e (μM) | SIf | IC50e (μM) | SIf | ||
| 1 | 244.58 | 142.67 | 1.7 | >183.44 | <1.3 | 40.62 | 6.0 |
| 6 | >1417.59 | 48.33 | >29.3 | 94.24 | >15.0 | 5.91 | >239.9 |
| 7 | 1371.12 | 81.06 | 16.9 | 230.32 | 6.0 | 7.20 | 190.4 |
| 8 | >1390.35 | 25.44 | >54.7 | 132.40 | >10.5 | 7.22 | >192.6 |
| 9 | 549.95 | 108.25 | 5.1 | >549.95 | –g | 11.95 | 46.0 |
| 10 | 40.24 | 23.51 | 1.7 | 19.19 | 2.1 | 6.34 | 6.3 |
| 11 | 8.49 | 16.06 | – | >567.21 | – | 9.10 | – |
| 12 | >2366.24 | 64.04 | >36.9 | 752.90 | >3.1 | 7.30 | >324.1 |
| 13 | >1075.57 | 10.54 | >102.0 | 24.86 | >43.3 | 4.46 | >241.2 |
| 14 | >1382.87 | 107.56 | >12.9 | 568.51 | >2.4 | 10.88 | >127.1 |
| 15 | >1602.23 | 22.05 | >72.7 | 85.25 | >18.8 | 11.82 | >135.6 |
| 16 | >1023.11 | 29.59 | >34.6 | 379.86 | >2.7 | 11.70 | >87.4 |
| 17 | >1548.49 | 12.39 | >125.0 | 27.98 | >55.3 | 21.06 | >73.5 |
| 18 | >1821.75 | 5.52 | >330.0 | 5.52 | >330.0 | 2.44 | >746.6 |
| 19 | >1655.88 | 9.37 | >176.7 | 43.72 | >37.9 | 6.45 | >256.7 |
| 20 | >1726.56 | 40.56 | >42.6 | 403.52 | >4.3 | 12.01 | >143.8 |
| 21 | >2139.74 | 24.92 | >85.9 | 140.57 | >15.2 | 9.30 | >230.1 |
| 22 | <6.96 | <6.96 | – | 230.83 | – | 3.42 | <2.0 |
| 23 | <9.97 | <9.97 | – | 653.10 | – | 4.39 | <2.3 |
| 24 | 584.11 | 235.59 | 2.5 | >584.11 | – | 5.71 | 102.3 |
| 25 | 522.81 | 71.95 | 7.3 | 21.62 | 24.2 | 7.68 | 68.1 |
| 26 | >1064.00 | 8.40 | >126.7 | 12.56 | >84.7 | 4.75 | >224.0 |
| 27 | >1290.15 | 45.62 | >28.3 | 39.54 | >32.6 | 10.41 | >123.9 |
| 28 | >1146.42 | 28.38 | >40.4 | 550.21 | >2.1 | 22.89 | >50.1 |
| 29 | >1318.31 | 18.81 | >70.1 | 359.00 | >3.7 | 12.72 | >103.6 |
| 30 | 701.24 | 119.29 | 5.9 | >701.24 | – | 16.26 | 43.1 |
| 31 | 428.76 | 14.36 | 29.9 | 12.47 | 34.4 | 4.42 | 97.0 |
| 32 | >1291.76 | 36.42 | >35.5 | 484.88 | >2.7 | 16.03 | >80.6 |
| 33 | 117.84 | 13.15 | 9.0 | 16.36 | 7.2 | 2.86 | >41.2 |
| 34 | >1290.96 | 15.61 | >82.7 | 69.18 | >18.7 | 4.66 | >277.0 |
| 35 | >1340.81 | 20.32 | >66.0 | 90.72 | >14.8 | 18.62 | >72.0 |
| 36 | 396.82 | <5.58 | >71.1 | 14.04 | 28.3 | 2.83 | 140.2 |
| 37 | <8.22 | 26.30 | – | 353.14 | – | 9.90 | – |
| 38 | >1894.52 | 215.88 | >8.8 | 1182.02 | >1.6 | 14.54 | >130.3 |
| 39 | >1424.45 | 111.85 | >12.7 | 949.32 | >1.5 | 14.08 | >101.2 |
| 40 | 1764.54 | 46.94 | 37.6 | >1278.48 | <1.4 | 5.00 | 352.9 |
| 41 | 717.98 | 112.33 | 6.4 | >1191.31 | – | 14.88 | 48.3 |
| 42 | >1267.64 | 60.19 | >21.1 | 1267.64 | >1.0 | 10.07 | >125.9 |
| 43 | >1283.31 | 432.57 | >3.0 | 611.68 | >2.1 | >320.83 | – |
| 44 | >1332.81 | 71.58 | >18.6 | 797.70 | >1.7 | 8.93 | >149.2 |
| 45 | >1548.13 | 36.96 | >41.9 | 52.74 | >29.4 | 21.67 | >71.4 |
| 46 | >1593.22 | 50.32 | >31.7 | 206.56 | >7.7 | 56.71 | >28.1 |
| 47 | 450.03 | 9.52 | 47.3 | 79.52 | 5.7 | 6.31 | 71.3 |
| 48 | >1367.03 | >1367.03 | – | >1367.03 | – | >341.76 | – |
| 49 | >1206.31 | 528.48 | >2.3 | 631.88 | >1.9 | >307.12 | – |
| 50 | >1160.94 | >290.24 | – | >290.24 | – | >290.24 | – |
| 51 | >1737.37 | 116.06 | >15.0 | 521.70 | >3.3 | >434.34 | – |
| TFh | >1740.95 | 1450.11 | >1.2 | 1160.23 | >1.5 | 0.68 | >2560.2 |
a
Values are means determined from at least two experiments.
b
CC50 is 50% cytotoxicity concentration in HepG 2.2.15 cells.
c
HBsAg: hepatitis B surface antigen.
d
HBeAg, hepatitis B e antigen.
e
IC50 is 50% inhibitory concentration.
f
SI (selectivity index) = CC50/IC50.
g
No SI can be obtained.
h
Tenofovir as the positive control.