Pharmacokinetic interaction between rhynchopylline and pellodendrine via CYP450 enzymes and P-gp

Figures & data

Figure 1. The pharmacokinetic profiles of rhynchopylline (A) and pellodendrine (B) in different groups. Group A: orally administration of 30 mg/kg rhynchopylline; Group B: pre-treatment of 20 mg/kg pellodendrine for 7 days followed by 30 mg/kg rhynchopylline; Group C: orally administration of 20 mg/kg pellodendrine; Group D: pre-treatment of 30 mg/kg rhynchopylline followed by 20 mg/kg pellodendrine.

Table 1. Corresponding pharmacokinetic parameters of rhynchopylline (Group A and B) and pellodendrine (Group C and D) in different groups.

	Unit	Group A	Group B	Group C	Group D
AUC (0-t)	μg/L*h	1728.08 ± 220.598	3080.14 ± 454.54*	1416.58 ± 362.93	1914.68 ± 259.94
t1/2	h	4.81 ± 0.42	9.74 ± 2.94*	10.25 ± 2.88	11.02 ± 2.56
Tmax	h	1.83 ± 0.22	0.87 ± 0.24*	1.03 ± 0.26	0.94 ± 0.13
Cl/F	L/h/kg	11.39 ± 1.37	5.67 ± 1.42*	12.34 ± 2.76	8.44 ± 1.59
Cmax	μg/L	249.1 ± 16.20	395.1 ± 18.58*	188.9 ± 16.22	214.07 ± 18.67

*p < 0.05.

Figure 2. The metabolic stability of rhynchopylline in the presence or absence of pellodendrine.

Figure 3. The transport of rhynchopylline and pellodendrine in the Caco-2 cell model in different groups. *p < 0.01, **p < 0.001 relative to Group A; ^#p < 0.05 relative to Group A or Group C.

Figure 4. Effect of pellodendrine and rhynchopylline on the activity of CYP1A2 and CYP2C9. (A) pellodendrine inhibited the activity of CYP1A2 and CYP2C9 in a dose-dependent manner with the IC₅₀ values of 22.99 and 16.23 μM. (B) Rhynchopylline did not affect the activity of CYPs.

Data availability statement

Corresponding authors may provide relevant data if appropriate.