Table 6.
Pharmacokinetics, toxicities and receptor binding properties of resveratrol, naringenin, zingiberene, β-caryophyllene, citronellol, eugenol, and gallic acid
| Parameters | Resveratrol | Naringenin | Zingiberene | β-caryophyllene | Citronellol | Eugenol | Gallic acid |
|---|---|---|---|---|---|---|---|
| Absorption | |||||||
| Human intestinal absorption | + | + | + | + | + | + | + |
| Caco-2 | + | + | + | + | + | + | – |
| Human oral bioavailability | – | – | – | + | – | – | + |
| Water solubility | − 2.778 | − 3.19 | − 4.937 | − 4.687 | − 2.78 | − 1.918 | − 1.097 |
| Distribution | |||||||
| Subcellular localization | Mitochondria | Mitochondria | Lysosomes | Lysosomes | Lysosomes | Mitochondria | Mitochondria |
| Blood Brain Barrier penetration | – | – | + | + | + | + | – |
| Plasma protein binding | 0.677 | 1.001 | 1.038 | 0.832 | 0.769 | 0.94 | 0.668 |
| P-glycoprotein inhibitior | – | – | – | – | – | – | – |
| P-glycoprotein substrate | – | – | – | – | – | – | – |
| Metabolism | |||||||
| OATP2B1 inhibitior | – | – | – | – | – | – | – |
| OATP1B1 inhibitior | + | + | + | + | + | + | + |
| OATP1B3 inhibitior | + | + | + | + | + | + | + |
| MATE1 inhibitior | – | – | – | – | – | – | – |
| OCT2 inhibitior | – | – | – | – | – | – | – |
| BSEP inhibitior | – | – | – | – | – | – | – |
| CYP3A4 substrate | – | – | – | + | – | – | – |
| CYP2C9 substrate | – | – | – | – | – | – | – |
| CYP2D6 substrate | – | – | – | – | – | + | – |
| CYP3A4 inhibition | + | + | – | – | – | – | – |
| CYP2C9 inhibition | + | + | – | – | – | – | – |
| CYP2C19 inhibition | + | + | – | – | – | – | – |
| CYP2D6 inhibition | – | – | – | – | – | – | – |
| CYP1A2 inhibition | + | + | – | – | – | – | – |
| CYP inhibitory promiscuity | + | + | – | – | – | – | – |
| Toxicity | |||||||
| Carcinogenicity | – | – | – | – | – | – | – |
| Human either-à-go-go inhibition | – | – | + | + | – | – | – |
| Hepatotoxicity | + | + | – | – | – | – | – |
| Acute Oral Toxicity (kg/mol) | 2.644 | 1.87 | 1.827 | 2.366 | 2.077 | 1.645 | 1.552 |
| Receptor binding | |||||||
| Estrogen receptor binding | + | + | – | – | – | – | – |
| Androgen receptor binding | + | + | – | – | – | – | + |
| Thyroid receptor binding | + | + | – | – | – | – | – |
| Glucocorticoid receptor binding | + | + | – | – | – | – | – |
| Aromatase binding | + | + | – | – | – | – | – |
| PPAR gamma | + | + | – | – | – | – | – |
OATP2: organic anion-transporting polypeptide; OCT2: organic cation transporter 2; BSEP: bile salt export pump; CYP: cytochrome P450; Human ether-a-go-go-related Gene (hERG); (–): absence of activity; ( +): presence of activity