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

In Vitro Enzyme Inhibition Experiment

Screening of kratom extracts as inhibitors of CYP3A activity in HLM

Inhibition was detected.  Cutoff used —

50% inhibition at the highest tested concentration

midazolam 708298

methanolic extract of kratom

1'-hydroxymidazolam

  • CYP3A

Cell fraction Pooled human liver microsomes -7999662

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

Results

Mitragynine and kratom extracts showed concentration-dependent inhibition of CYP activity in HLM. Mitragynine at 10 µM inhibited CYP2C9, CYP2D6, and CYP3A activity by 42%, 87%, and 50%, respectively. Kratom extracts at 20 µg/mL inhibited these activities by 81-88%, 87-93%, and 86-89%, respectively.  

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

1010191

400 µL

2 min

NADPH

Available

Available

2 µM

2, 10, and 20 µg/ml