Cannabis (Cannabis sativa)
Interaction of plant cannabinoids with the multidrug transporter ABCC1 (MRP1)
CSV
JSON
The ATP-binding cassette (ABC) transporter ABCC1, or multidrug resistance-related protein 1 (MRP1) is implicated in Phase II metabolism and multidrug resistance as it effluxes substrate anticancer drugs. As cannabinoids inhibit two related ABC transporters, P-glycoprotein and ABCG2, here we examined whether they also inhibit ABCC1. Indeed, the cannabinoids enhanced the intracellular accumulation of two ABCC1 substrates, Fluo3 and vincristine, in ovarian carcinoma cells over-expressing ABCC1 (2008/MRP1) with a rank order of potency: cannabidiol>cannabinol>Delta(9)-tetrahydrocannabinol. Cannabinoid inhibition of ABCC1 was confirmed using insect cell membrane MRP1 ATPase assays. These results demonstrate that cannabinoids inhibit ABCC1.
1 . Inhibition of ABCC1 by Cannabidiol (id=NPDI-PWUeog)
In Vitro Transporter Inhibition Experiment
Inhibition was detected. Cutoff used —
NA
- ABCC1
Cell system Human ovarian carcinoma cell line
Results
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
24 well plates
90 min
37 C
1 µg/ml
2, 10, 50 and 100 µM
2 . Inhibition of ABCC1 by Cannabinol (id=NPDI-7RWWrg)
In Vitro Transporter Inhibition Experiment
Inhibition was detected. Cutoff used —
NA
- ABCC1
Cell system Human ovarian carcinoma cell line
Results
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
24 well plates
90 min
37 C
1 µg/ml
2, 10, 50 and 100 µM
3 . Negligible inhibition of ABCC1 by Cannabidiol (id=NPDI-qeGJYg)
In Vitro Transporter Inhibition Experiment
Non-inhibition was detected. Cutoff used —
Not provided. A common convention is that IC50 > 100 micM signals negligible inhibition
- ABCC1
Cell system Human ABCC1 transduced subline (MRP1)
Results
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
incubation time with two phases, cells and natural products for 30 min and then with Fluo3 for another 60 min.
24 well plates
60 min
37 C
1 µg/ml
0.08, 0.4, 2, 10, 50, 100 and 200 µM
4 . Negligible inhibition of ABCC1 by Cannabinol (id=NPDI-JnMHww)
In Vitro Transporter Inhibition Experiment
Non-inhibition was detected. Cutoff used —
Not provided. A common convention is that IC50 > 100 micM signals negligible inhibition
- ABCC1
Cell system Human ABCC1 transduced subline (MRP1)
Results
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
24 well plates
60 min
37 C
1 µg/ml
0.08, 0.4, 2, 10, 50, 100 and 200 µM
5 . Negligible inhibition of ABCC1 by THC (id=NPDI-lNsNoQ)
In Vitro Transporter Inhibition Experiment
Non-inhibition was detected. Cutoff used —
Not provided. A common convention is that IC50 > 100 micM signals negligible inhibition
- ABCC1
Cell system Human ABCC1 transduced subline (MRP1)
Results
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
24 well plates
60 min
37 C
1 µg/ml
0.08, 0.4, 2, 10, 50, 100 and 200 µM
6 . Negligible inhibition of ABCC1 by THC (id=NPDI-uUyadQ)
In Vitro Transporter Inhibition Experiment
Non-inhibition was detected. Cutoff used —
Not provided. A common convention is that IC50 > 100 micM signals negligible inhibition
- ABCC1
Cell system Human ovarian carcinoma cell line
Results
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
24 well plates
90 min
37 C
1 µg/ml
2, 10, 50, 100 and 200 µM