Goldenseal (Hydrastis canadensis) 43525850
Organic anion-transporting polypeptides contribute to the hepatic uptake of berberine CSV JSON

  1. The purpose of this study was to investigate the mechanism of hepatic uptake of berberine. Berberine accumulation in hepatocytes was found to be highly dependent on active uptake, which could not be explained by liver organic cation transporter (OCT) alone.

  2. Our studies indicated that berberine uptake was significantly suppressed by rifampicin, cyclosporine A and glycyrrhizic acid, which act as specific inhibitors of different Oatp isoforms (Oatp1a1, Oatp1a4 and Oatp1b2) in rat hepatocytes. The combination of OCT and OATP inhibitors further reduced berberine accumulation in both rat and human hepatocytes. The uptake of berberine could be increased in human HEK293-OATP1B3 but not in OATP1B1-transfected HEK 293 cells.

  3. Rifampicin could reduce the berberine liver extraction ratio (ER) and double its concentration in the effluent in isolated rat livers. Further in vivo study indicated that berberine plasma exposure could be significantly increased by co-administration of the OATP inhibitor rifampicin or the substrate rosuvastatin.

  4. In conclusion, this study demonstrated that both OCT and OATP contribute to the accumulation of berberine in the liver. OATPs may have important roles in berberine liver disposition and potential clinically relevant drug–drug interactions.

PMID: 26068524

26068524

1 . Transport of Berberine by OAT1B3 (id=NPDI-kt6jEg)

In Vitro Transporter Kinetics Experiment

Transport Activity was detected.  Cutoff used — not specified

berberine 19012197

  • OATP1B3 (SLCO1B3)

Transfected / siRNA knock-out / injected cells HEK293 transfected cells

Results

Fig 5 p value compared to mock control

Sample Compound measured Measurement Value Study sequence Additional information N replicates

Experimental Conditions

Cell Culture Conditions

1.5 x 10^5

12 well

Assay Conditions

15 min

37 deg C

10 μM

2 . BBR-OATP1B1 (id=NPDI-mUlTOw)

In Vitro Transporter Kinetics Experiment

No Transport Activity was detected.  Cutoff used — not specified

berberine 19012197

  • OATP1B1 (SLCO1B1)

Transfected / siRNA knock-out / injected cells HEK293 transfected cells

Results

Fig 5 - presented as concentration of BBR - in 1B1 there was no difference between control and transfected (thus 1 fold ratio)

Sample Compound measured Measurement Value Study sequence Additional information N replicates

Experimental Conditions

Cell Culture Conditions

1.5 x 10^5

12 well

Assay Conditions

15 min

37 deg C

10 μM