Objective: To screen the potential inhibitor for human epidermal growth factor receptor (EGFR) from four kind compounds including shikonin

acetylshikonin

β-acetoxyisovalerylshikonin and β

β-dimethylacrylshikonin contained in Arnebia euchroma. Method: Through adsorption experiment

the best conditions of the pH and concentration for immobilization of EGFR were determined by using the surface plasmon resonance (SPR) method to construct EGFR biochip. The interactions between EGFR and four compounds were studied on real time after the EGFR immobilization on the chip with PBST (10 mmol·L-1

pH 7.4

including 0.005% tween 20) as the interaction buffer. The kinetic parameters were calculated by software

and the inhibitors were then screened based on the combination with kinetic constant. Result: The optimal immobilization conditions were as follows:with 10 mg·L-1 acetate buffer (10 mmol·L-1

pH 4.5)

and was immobilized with a 250 response unit finally. The interaction results showed that only β

β-dimethylacrylshikonin had good interaction with EGFR among them

and other three compositions had no clear response. The kinetic parameters were calculated further

with binding rate constant ka=1.27×104 L·mol-1·s-1

dissociation rate constant kd=2.92×10-2 s-1

dissociation equilibrium constant KD=2.31×10-6 mol·L-1 and Chi square value (Chi2) of 3.25. KD<1×10-5 mol·L-1

suggesting that they had a strong affinity. Conclusion: It was indicated that the β

β-dimethylacrylshikonin could be a potential EGFR inhibitor.