Silibinin

Biological Activity

Silibinin, the main flavonoid extracted from the milk thistle Silybum marianum, displays hepatoprotective properties in acute and chronic liver injury. Silibinin is an effective SARS-CoV-2 main protease (Mpro) inhibitor. Silibinin can significantly reduce tumor cell proliferation, angiogenesis as well as insulin resistance.

In vivo experiments (for reference only)

Male C57BL/6 (8 weeks old, weight 20–23 g) were housed under temperature- and light- controlled condi tions (21–23 °C under a 12 h light/dark cycle), being allowed for free access to food and water. Animals were acclimatized for 1 week before the experiments.
All mice were divided randomly into the following six groups: control group, MPTP (30 mg/kg in saline) group, MPTP and silibinin-treated groups (70, 140, and 280 mg/ kg in 0.5% sodium carboxymethyl cellulose) or meman tine-treated group (3 mg/kg in 0.5% sodium carboxymethyl cellulose). MPTP was administered intraperitoneally (i.p.) at 30 mg/kg daily for 7 days. Silibinin or memantine was intragastrically (i.g.) administrated into mice on the same 7 days (1 h after every MPTP injection) and additional 17 days thereafter during the behavioral tests. Mice in the control group and in the MPTP vehicle group were administered with the same volume of 0.5% sodium carboxymethyl cel lulose as vehicle.

https://pubmed.ncbi.nlm.nih.gov/34097239/

Kunming mice (weighing 18–22 g, 6–8 weeks old, either sex) were housed in a temperature controlled room (22 ± 2°C) on a 12/12-hr day/night cycle. The animals were randomized into specified experimental groups and allowed to acclimatize for 1 week before the experiment. Food and water were provided ad libitum.
Mice were separated into five groups (n=12 each): control+vehicle, CUMS+vehicle, CUMS+silibinin (100 mg/kg), CUMS+silibinin (200 mg/kg), CUMS+silibinin (400 mg/kg), and CUMS+fluoxetine (20 mg/kg). Doses were based on body weight. Silibinin was suspended in a 0.3% carboxymethylcellulose (CMC) solution and provided by oral gavage. Mice were subjected to various mild stressors for 5 weeks and then administered silibinin for 3 weeks.
https://pmc.ncbi.nlm.nih.gov/articles/PMC4428717/

Product Citations

• 

  J Adv Res. 2022 May 13;S2090-1232(22)00117-5.

  Combination of natural polyphenols with a precursor of NAD+ and a TLR2/6 ligand lipopeptide protects mice against lethal γ radiation
  Silibinin purchased from AbMole

Protocol (for reference only)

Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time

Animal Experiment
Animal models	Athymic (nu/nu) male nude mice s.c. injected with 6 × 106 DU145 cells
Formulation	0.5% CMC (w/v) in saline
Dosages	200 mg/kg
Administration	oral gavage just before the first dose of IR and continued for 5 days/week

Chemical Information

Molecular Weight	482.44
Formula	C25H22O10
CAS Number	22888-70-6
Solubility (25°C)	DMSO 96 mg/mL
Storage	Powder -20°C

References

[1] Nambiar DK, et al. Mol Cancer Ther. Silibinin Preferentially Radiosensitizes Prostate Cancer by Inhibiting DNA Repair Signaling.

[2] Abdul Quaiyoom Khan, et al. Nutr Cancer. Silibinin inhibits tumor promotional triggers and tumorigenesis against chemically induced two-stage skin carcinogenesis in Swiss albino mice: possible role of oxidative stress and inflammation

[3] Khaled Khazim, et al. Am J Physiol Renal Physiol. The antioxidant silybin prevents high glucose-induced oxidative stress and podocyte injury in vitro and in vivo