CHENG Long, WANG Lan, WANG Yan-li, et al. Influence of Jinglingzi Powder with Different Compatibility on the Activity of Cytochrome P450 3A4 from Rat Liver Microsomes[J]. Chinese journal of experimental traditional medical formulae, 2011, 17(22): 117-122.
DOI:
CHENG Long, WANG Lan, WANG Yan-li, et al. Influence of Jinglingzi Powder with Different Compatibility on the Activity of Cytochrome P450 3A4 from Rat Liver Microsomes[J]. Chinese journal of experimental traditional medical formulae, 2011, 17(22): 117-122. DOI: CNKI:11-3495/R.20110920.1429.002.
Influence of Jinglingzi Powder with Different Compatibility on the Activity of Cytochrome P450 3A4 from Rat Liver Microsomes
Objective: To illustrate the compatibility of Jinglingizi powder by investigating the influence of Jinglingzi powder with different compatibility on the enzymatic activity of cytochrome P450 3A4(CYP 3A4) from rat liver microsome. Method: The different compatibility of Jinglingizi powder was designed based on the orthogonal array L9(34). In vitro test
rat liver microsome incubation system was applied to detect the 50% inhibitory concentration of Jinglingzi powder with different compatibility. In vivo experiment
rats were administered orally with the different compatibility of Jinglingizi powder (dose: 9.75 g·kg-1) from day 1 to day 5
then injected probe drug testosterone. The biosamples from liver tissue were obtained by microdialysis probe
then to be analysed by HPLC. The concentration of 6-β-testosterone and testosterone were accurately determined. The ratio hepatic concentration of 6-β-testosterone to hepatic concentration of testosterone
was applied to describe the CYP 3A4 enzyme activity. Result: The half maximal inhibitory concentrations (IC50) of the extract of Toosendan fruit
Rhizoma Corydalis and Jinlingzi Powder(formula.1-9) on the enzymatic activity of CYP3A4 were (2.59±0.33)
(0.87±0.30)
(1.14±0.20)
(1.00±0.13)
(1.19±0.10)
(2.33±0.15)
(1.39±0.19)
(1.14±0.20)
(1.29±0.14)
(1.43±0.32)
(1.49±0.28) mg·L-1
respectively. In vivo test
the CYP3A4 enzyme activity was inhibited by the different compatibility of Jinglingizi powder
compared with the normal control group. The inhibited intensity of Jinglingizi powde followed the order: formula 1 (formula 4)> formula 7 > formula 2(formula 5) > formula 8> formula 3> formula 9. Conclusion: The CYP3A4 enzyme activity is inhibited by the different compatibility of Jinglingizi powder
compared with the normal control group. Compatibility of Jinglingizi powder synergetically down-regulate the the CYP3A4 enzyme activity.