Table 3.
Inhibition ( IC50) of Danshen's effective components on different CYP450 isozymes in human liver microsomes.
| Components | type of Probe | IC50 ( μM ) | References | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| CYP1A2 | CYP2B6 | CYP2C9 | CYP2C9∗ 1 | CYP2C9∗ 2 | CYP2C9∗ 3 | CYP2C19 | CYP2D6 | CYP3A4 | P450 2J2 | |||
| Tanshinone IIA | 1, 3 - 7, 9 | 1.3- 10.10 | - | > 100 | - | - | - | > 100 | 13.47, > 200 |
> 100 | 2.5 | [43–47] |
| Cryptotanshinone | 1, 3 - 7, 10 | 0.75 - 3.06 | - | 23.86-33 | 1. 74 | 2. 64 | 3. 17 | > 100 | 75 | > 100 | - | [43, 44, 47, 48] |
| Miltirone | 1, 4 - 6, 8 | 1.73 | - | 8.61 | - | - | - | 26.9 | 30.20 | 33.88 | - | [43, 49] |
| Dihydrotanshinone | 1, 2, 4 - 8, 10 | 0.5- 2.25 | 2. 64 | 7.48 | 0. 19 | 0. 56 | 1. 52 | 0.6 | 11.70-35.4 | 0.367-3.22 | - | [43–45, 48, 50] |
| Tanshinone I | 1, 3 - 7 | 0.75-11.61 | - | > 100 | - | - | - | > 100 | > 100 | > 100 | - | [43–45, 47] |
| Salvianolic acid A | 1, 5 | 5. 37 | - | - | - | - | - | - | 11. 53 | - | - | [45] |
| Salvianolic acid B | 1, 3, 5 - 7 | > 100 | - | > 200 | - | - | - | - | > 200 | 12. 35 > 200 |
- | [45, 47] |
| Rosmarinic acid | 1, 7 | 10. 32 | - | - | - | - | - | - | - | 5. 43 | - | [45] |
| Danshensu | 1, 3, 5 - 7 | > 100 | - | 50 | - | - | - | - | > 200 | > 200 | - | [47] |
-, currently not available.
1: Phenacetin; 2: Mephenytoin; 3: Diclofenac; 4: Tolbutamide; 5: Dextromethorphan; 6: Testosterone; 7: Midazolam; 8: Omeprazole; 9: Astemizole; 10: Fluvastatin.