| Extract/constituent | Enzyme/transporter | Substrate | (μM) | Reference | HLMs | Purified | Inhibition type |
| Tanshinone I | CYP1A1 | 7-Ethoxyresorufin | | | | [39] | CYP1A2 | 7-Ethoxyresorufin | | | | [39] | CYP1A2 | Phenacetin | 0.48–2.16 | 0.11 | com | [36, 37] | CYP2C9 | Tolbutamide | 51.2 | 73.4 | com | [36] | Diclofenac | >20 | | | [37] | CYP2D6 | Dextromethorphan | 12 | | | [37] | CYP2E1 | Chlorzoxazone | 3.67 | ND | non | [36] | CYP3A4 | Testosterone | 86.9 | 92.5 | com | [36] | Testosterone | >20 | | | [37] | Midazolam | >20 | | | [37] | CE1 | o-Nitrophenyl acetate | | 26.3 | | [44] | CE2 | o-Nitrophenyl acetate | | 14.6 | | [44] | Irinotecan | | 1.4 | | [44] | P-gp | Digoxin | (Caco-2 cells) | | [60] |
| Tanshinone IIA | CYP1A | 7-Ethoxyresorufin | | | | [39] | CYP1A | 7-Methoxyresorufin | | | | [39] | CYP1A1 | 7-Ethoxyresorufin | | | | [39] | CYP1A2 | 7-Ethoxyresorufin | | | | [39] | CYP1A2 | Phenacetin | 1.0–1.45 | 0.05 | com | [36, 37] | CYP2C9 | Diclofenac | >20 | | | [37] | CYP2C9 | Tolbutamide | 61.6 | 88.6 | com | [36] | CYP2D6 | Dextromethorphan | >20 | | | [37] | CYP2E1 | Chlorzoxazone | — | — | | [36] | CYP3A4 | Midazolam | >20 | | | [37] | Testosterone | >20 | | | [37] | Testosterone | 219 | 141 | com | [36] | CE1 | o-Nitrophenyl acetate | | 6.9 | | [44] | CE2 | o-Nitrophenyl acetate | | 2.5 | | [44] | Irinotecan | | 0.07 | | [44] |
| Cryptotanshinone | CYP1A1 | 7-Ethoxyresorufin | | | | [39] | CYP1A2 | 7-Ethoxyresorufin | | | | [39] | CYP1A2 | Phenacetin | | | com | [38] | Phenacetin | 0.45–1.88 | 0.27 | com | [36, 37] | CYP2C9 | Diclofenac | 8 | | mixed | [37] | Tolbutamide | 22.9 | 9.90 | com | [36] | CYP2D6 | Dextromethorphan | 68 | | mixed | [37] | CYP2E1 | Chlorzoxazone | 10.87 | ND | com | [36] | CYP3A4 | Midazolam | >20 | | | [37] | Testosterone | >20 | | | [37] | Testosterone | 120 | 59.9 | com | [36] | CE1 | o-Nitrophenyl acetate | | 0.54 | | [44] | CE2 | o-Nitrophenyl acetate | | 0.14 | | [44] | Irinotecan | | 0.29 | | [44] |
| Dihydrotanshinone I | CYP1A2 | Phenacetin | 0.53 | 0.02 | com | [36] | CYP2C9 | Tolbutamide | 1.92 | 3.14 | com | [36] | CYP2E1 | Chlorzoxazone | — | ND | un | [36] | CYP3A4 | Testosterone | 2.11 | 2.98 | non | [36] | Midazolam | | | | [33] | CE1 | o-Nitrophenyl acetate | | 0.40 | | [44] | CE2 | o-Nitrophenyl acetate | | 0.12 | | [44] | CE2 | Irinotecan | | 1.83 | | [44] |
| Miltirone | CE1 | o-Nitrophenyl acetate | | 2.53 | | [44] | CE2 | o-Nitrophenyl acetate | | 0.04 | | [44] | CE2 | Irinotecan | | 0.08 | | [44] |
| Tanshinone IIA sulfonate | CYP2A6 | Coumarin | >10 | | | [31] | CYP2C9 | Tolbutamide | >10 | | | | CYP2C19 | s-mephenytoin | >10 | | | | CYP2D6, | Metoprolol | >10 | | | | CYP2E1 | Chlorzoxazone | >10 | | | | CYP3A4 | Midazolam | 3.2 | | com | | CE1 | o-Nitrophenyl acetate | | >100 | | [44] | CE2 | o-Nitrophenyl acetate | | 3.9 | | | CE2 | Irinotecan | | 28.8 | | |
| Tanshinol | CYP1A2 | Phenacetin | | | | [37] | CYP2C9 | Diclofenac | 35 | | com | | CYP2D6 | Dextromethorphan | >20 | | | | CYP3A4 | Midazolam | >20 | | | | Testosterone | >20 | | | | OAT1 | p-Aminohippuric acid | | 40.4 | | [54] | | | | [56] | OAT2 | Prostaglandin F2α | | | | [56] | OAT3 | Estrone sulfate | | 8.6 | | [54] | | | | [56] | OAT4 | Estrone sulfate | | | | [56] |
| Protocatechuic aldehyde | CYP1A2 | Phenacetin | >20 | | | [37] | CYP2C9 | Diclofenac | >20 | | | | CYP2D6 | Dextromethorphan | >20 | | | | CYP3A4 | Midazolam | | | | | Testosterone | | | | |
| Protocatechuic acid | CYP1A2 | Phenacetin | >20 | | | [37] | CYP2C9 | Diclofenac | >20 | | | | CYP2D6 | Dextromethorphan | >20 | | | | CYP3A4 | Midazolam | >20 | | | | Testosterone | >20 | | | |
| Salvianolic acid B | CYP1A2 | Phenacetin | | | | [37] | CYP2C9 | Diclofenac | >20 | | | | CYP2D6 | Dextromethorphan | >20 | | | | CYP3A4 | Midazolam | >20 | | | | Testosterone | >20 | | | | OAT1 | p-Aminohippuric acid | | 22.2 | | [54] | OAT3 | Estrone sulfate | | 19.8 | | |
| Salvianolic acid A | OAT1 | p-Aminohippuric acid | | 5.6 | | [54] | OAT3 | Estrone sulfate | | 0.16 | | |
| Lithospermic acid | OAT1 | p-Aminohippuric acid | | 20.8 | | [54] | OAT3 | Estrone sulfate | | 0.59 | | |
| Rosmarinic acid | OAT1 | p-Aminohippuric acid | | 0.35 | | [54] | OAT3 | Estrone sulfate | | 0.55 | | |
| Danshen | CYP1A2 | Phenacetin | | | | [64] |
| Danshen | CYP3A4 | Testosterone | | | com | [35] |
| Danshen ethanol | CYP1A2 | Phenacetin | | | com | [34] | CYP3A4 | Testosterone | | | com | |
| Danshen ethanol | CYP3A4 | Midazolam | | | | [33] |
| | CYP1A2, | Phenacetin | >10 | | | [32] | CYP2A6 | Coumarin | >10 | | | | CYP2C9 | Tolbutamide | >10 | | | | CYP2C19 | s-mephenytoin | >10 | | | | CYP2D6, | Metoprolol | >10 | | | | CYP2E1 | Chlorzoxazone | >10 | | | | CYP3A4 | Midazolam | | | non | |
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com, competitive; non, noncompetitive; un, uncompetitive. , IC50 (μM). #, μg/mL. tanshinol 3.1, salvianolic acid B 37.3, rosmarinic acid 1.8 and protocatechuic aldehyde 0.16 mg/g, and dihydrotanshinone I 12.7, cryptotanshinone 34.6, tanshinone I 10.4, and tanshinone IIA 22.6 μg/g. tanshinol 31, salvianolic acid B 41, rosmarinic acid 6.1, and protocatechuic aldehyde 2.8 mg/g, dihydrotanshinone I 98, cryptotanshinone 70, tanshinone I 32, and tanshinone IIA 21 μg/g. tanshinol 2.68, salvianolic acid B 209, rosmarinic acid 14.9, and protocatechuic aldehyde 0.64, dihydrotanshinone I 9.3, cryptotanshinone 36.8, tanshinone I 17.9, and tanshinone IIA 118 mg/g. tanshinone IIA 106.2, cryptotanshinone 88.0, tanshinone I 53.1, and dihydrotanshinone I 13.5 mg/g. salvianolic acid B (≥85%), rosmarinic acid (≥10.1%), and lithospermic acid (≥1.9%).
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