Intestinal Absorption Of Licorice Chemical Composition Based On Caco-2 Cell Model

Licorice is a kind of traditional Chinese medicine.Modern research has shown that licorice is well-known for its physidogical functions,such as anti-inflammation,anti-viral,anti-tumor and anti-allergic activities.The main active ingredients of licorice are triterpenes and flavonoids.The varied structure of licorice compounds,complex metabolic pathways and various metabolic products,which leads that the research methods and pharmacokinetic of licorice require more in-depth research.Caco-2 cell model can get a lot of valuable information quickly and easily,and time-saving than animal experiment economy.It is a rapid screening and important method of early drug development and large-scale evaluation for drug absorption in vitro.There is no system research on intestinal absorption of liquorice triterpene and flavonoids in vitro.Based on this,the intestinal absorption of triterpene and flavonoids compounds in vitro Caco-2 monolayer cell model was studied and antiviral activity of some compounds was screened.We expected to improve the theory basis for new drug design of licorice.The main results are as follows:?1?The Caco-2 cell model was set up and verified in integrity and the ability to transport.?2?Based on Caco-2 cell model,the intestinal absorption of glycyrrhiza triterpene compounds was studied.We found glycyrrhizin?GL?was extremely difficult to absorb,and glycyrrhetinic acid?GA?was well absorbed compound.Glycyrrhetic acid 3-O-mono-?-D-glucuronide?GAMG?was moderately absorbed compound.The absorption mechanism of GA and GAMG in Caco-2 cell model was mainly passive diffusion.In addition,GA and GAMG didn't have accumulation.The total recovery of prototype compounds was in the normal range,which showed that the metabolism,transformation,loss or adsorption on the cells didn't happen during the transfer process.Time dynamics and the relationship between concentration and absorption showed that there was not carrier mediated when compounds through the intestinal wall cells,and it depended on the passive diffusion driven by concentration difference.?3?The article studied the flavonoids of licorice and found liquiritin apioside and isoliquiritin apioside were extremely difficult to absorb,and liquiritigein,licochalcone B,licochalcone C,and echinatin were well absorbed compounds,furthermore,licochalcone A was moderately absorbed compound.The absorption mechanism of these compounds in Caco-2 cell model is mainly passive diffusion.In addition,all the compounds,besides licochalcone A,didn't have accumulation.The total recovery of prototype compounds was in the normal range,which showed that the metabolism,transformation,loss or adsorption on the cells didn't happen during the transfer process.Time dynamics and the relationship between concentration and absorption showed that there was not carrier mediated when compounds through the intestinal wall cells,and it depended on the passive diffusion driven by concentration difference.?4?The inhibition of herpes simplex virus 2?HSV-2?and hepatitis B virus?HBV?by GL,GAMG,GA,saponin G₂,saponin H₂ and D-glucuronic acid were screend.We found that GAMG,GA and D-glucuronic acid had weak inhibitory activity for HSV-2.6 kinds of compounds had no obvious inhibitory activity for HBV.