Table 1.
Targets in cellular and animal models of Milk Thistle’s Active Components.
Compound | Target | Cellular or Animal Model | Reference | ||
---|---|---|---|---|---|
Inhibition | Silybin, dehydrosilybin | Phase I enzymes | Ethoxyresorufin O-dealkylase (EROD) (P450 1A1) | human keratinocytes (HaCaT), human hepatoma cells (HepG2) | [16] |
Silybin, silibinin | P450 1A1, methoxyresorufin O-dealkylase (MROD) (P450 1A2), pentoxy-O-dealkylase (PROD) (P450 2B) | mouse liver microsomes | [18] | ||
Silymarin | P450 1A1 | Wistar rats, Syrian hamsters | [19,20] | ||
Silymarin | CYP3A4 | LS180 colon adenocarcinoma cells | [22] | ||
Silibinin | Phase III transporters | Organic Anion Transporters (OAT)P1B1, OATP1B3, OATP2B1, MRP2 | Chinese hamster ovary cells | [31] | |
Silymarin and silibinin | OATP1B1, OATP1B3 and OATP2B1 | human hepatocytes | [32] | ||
Silymarin | P-glycoprotein (P-gP) | Madin–Darby canine kidney II cells, MCF-7 | [33,34] | ||
Silibinin | MDR1, MRP3, MRP2, MRP1, MRP5, MRP4, ABCG2, ABCB11, MRP6 and MRP7 | K562 and KCL22 cell lines | [35] | ||
Silibinin | P-gP | Rats | [36,37] | ||
Silymarin | MRP1 | human pancreatic adenocarcinoma cell Panc-1 | [38] | ||
Silibinin | Phase I enzymes | cytochrome P4503A4 | rats | [37] | |
Activation | Silymarin | Phase II enzymes | glutathione S-transferase (GST), glutathione reductase (GR), glutathione peroxidase (GPO) | mouse liver | [23] |
Silymarin | GST, UDP-glucuronosyltransferases (UGT), epoxide transferase, sulfotransferase | Wistar rats | [19] |