Studies On Processing Mechanism Of Herba Epimedii From Intestinal Absorption And Metabolism Kinetics Of Main Constituents

This project was designed to study the intestinal absorption and metabolism kineticsof main constituents including icariin, epimedin A, epimedin B, epimedin C,baohuosideâ… and total flavonoids in herba epimedii of crude and processing sample, andexplain the processing mechanisms of herba epimedii from the aspect of absorption andmetabolism kinetics of active components.We had prepared icariin(1), icarisideâ… (2), Hexandraside E(3), icaritin(4),desmethylicariin(5), baohuosideâ… (6), these compounds provide elementary andnecessary qualification to the study.The studies on intestinal absorption and metabolism kinetics of main constituentswas performed by using in situ perfused rat intestinal model and intestinal bacteriametabolism experiment, compared the difference of icariin, epimedin A, epimedin B,epimedin C, baohuosideâ… and total flavonoids in the aspect of intestinal absorption andmetabolism kinetics. The absorption characteristics and mechanism of active compoundsfor various intestinal segments in rats showed that icariin was metabolized quickly in theintestine. Some constituents of the total flavonoids showed metabolic transformation, andicariin showed obviously metabolism. Studies on the metabolism of flavonoid compoundsin Herba Epimedii by intestinal flora were described. Icariin,epimedin A,epimedin B andepimedin C were all metabolized quickly in vitro by rat intestinal flora, and icariin couldbe metabolized in vivo by rat intestinal flora. Some metabolites were observed in ratserum samples,urine samples and feces samples. We found that the main metabolite isbaohuosideâ… in both experiments of intestinal absorption and metabolism kinetics. Themethod used for metabolites analysis was HPLC and HPLC-MS. The results of Caco-2cell model showed that the permeability coefficient(P^*_eff) of baohuosideâ… was higherthan icariin and the permeability coefficient(P^*_eff) of icariin was higher than epimedin A,epimedin B and epimedin C, so the absorption of baohuosideâ… was best in all thesecompounds.Studies on the variation of active compounds in herba epimedii about the differenceof heating temperature and heating time, it could establish a basis to make a standard ofprocessing. The traditional processing method is to roast by adding quantitive meltedadept ovillus, and the leaves of the herb were heating in course of processing, but thestructure of these flavonoids was destroyed easily by light, heat and so on. To standard theprocess method, it is necessary to study the influence of active compounds in herba epimedii due to the temperature and time about heat.These conclusions authenticated previous hypothesis: processing would alter relativeratio of flavonoids in harba epimedii, the content of polycose glycoside was degrade, butthe content of deutero-polycose glycoside was increased. The permeability coefficient ofdeutero-polycose glycoside is higher than polycose glycoside, so the absorption ofpolycose glycoside is much better. And then, we draw a conclusion that processing canelevate the absorption of flavonoids in herba epimedii in vivo.