Screening of kratom extracts as inhibitors CYP3A activity in HIM CSV JSON

In Vitro Enzyme Inhibition Experiment

Screening of kratom extracts as inhibitors CYP3A activity in HIM

Inhibition was detected.  Cutoff used —

50% inhibition at the highest tested concentration

midazolam 708298

mitragynine

1'-hydroxymidazolam

  • CYP3A

Cell fraction Pooled human intestinal microsomes -7999663

Three methanolic Kratom extracts were tested, K-50, K-51 and K-52.

Results

Mitragynine and kratom extracts showed concentration-dependent inhibition of CYP3A activity in HIM. Mitragynine at 10 µM inhibited CYP3A activity by 44%. Kratom extracts at 20 µg/mL inhibited CYP3A activity by 82-90%. 

Sample Compound measured Value Measurement Study sequence Additional information N replicates

Experimental Conditions

Methanol (0.8 % v/v) served as solvent control. Sulphaphenazole (1 µM), quinidine (2 µM), and ketoconazole (0.01 µM) served as positive control inhibitors of CYP2C9, CYP2D6, and CYP3A, respectively.

NA

0.05 mg/mL

Commercially available

1610314

400 µL

10 min

NADPH

Available

Available

2 µM

2, 10, 20 µg/mL