ABSTRACT
Objective: To screen and evaluate PXR/CYP3A4-induced lipid-regulating quality marker in propolis with precise and quantitative method. Methods: The LS174T cell was given certain amount of midazolam injection, along with different dosage of known components found in propolis, after incubation and extraction, the samples were determined for 1’-OH-midazolam, and each compound was evaluated to discover the PXR/CYP3A4 pathway regulatory activity according to the results; Then, compounds selected were used as indexes for UHPLC-MS-MS content determination, and their own values were regarded as a preliminary step of confirming PXR/CYP3A4-induced lipid-regulating quality markers of propolis. Results: In all components tested, chrysin, galangin, heterochlorogenic acid A, quercetin, and caffeic acid phenethylester significantly affected the 1’-OH-midazolam yield compared with blank and positive control, indicating their obvious influence on PXR/CYP3A4 expression; The UHPLC-MS-MS determination showed that except galangin, heterochlorogenic acid A, and quercetin, all the other compounds had adequate content in propolis to take effect. Conclusion: Chrysin, galangin, caffeic acid phenethylester, and quercetin were probably defined as PXR/CYP3A4-induced lipid-regulating quality marker in propolis, which inhibited the expression of such targets to down-regulate blood lipid level; Additionally, the method used for quality marker screening and evaluation in this study was fast, effective and quantitative, and capable of carrying out high throughput active component screening for PXR/CYP3A4 regulatory activities.
ABSTRACT
Objective To study protective effect and mechanism of caffeic acid phenethyl ester ( CAPE ) in rats with doxorubicin-induced myocardial injury.Methods Sixty male SD rats were randomly divided into control group, model group and CAPE ( 12、24、48 mg/kg ) groups.The models of doxorubicin-induced myocardial injury were established by injection of 2.5 mg/kg doxorubicin every other day for 6 times.After the last injection, model group was given distilled water and CAPE ( 12、24、48 mg/kg ) groups were fed with CAPE, one time a day for 8 weeks.After consecutive 8 weeks, serum creatine kinase, lactate dehydrogenase and BNP were assessed , NO concentration, MDA,GSH,SOD,NOS,LPO and CAT contents in the heart were determined and histopathological changes were detected.Results serum creatine kinase、lactate dehydrogenase and BNP of CAPE 48 mg/kg group decreased significantly(P<0.05), while the activity of NO,NOS,GSH,CAT and SOD increased in the CAPE 48 mg/kg group significantly ( P<0.05 ) .Histopathology showed caffeic acid phenethyl ester could improve the doxorubicin-induced myocardium injury. Conclusion caffeic acid phenethylester has the protective effects in rats with doxorubicin-induced myocardial injury.Protective effect may be related to improve myocardial against oxidative stress damage.