Anti-diabetic effects of linarin from Chrysanthemi Indici Flos via AMPK activation

Objective:The purpose of this study is to investigate the anti-diabetic effects of linarin,a flavonoid extracted from Chrysanthemi Indici Flos(CIF),and its potential mechanisms.Methods:The effects of linarin on cell viability and glucose consumption in Hep G2 cells were measured.Meanwhile,monosodium glutamate(MSG) mouse model was constructed to monitor the changes of insulin tolerance,glucose tolerance,triglyceride and cholesterol.The protein expression levels of pAMPK,p-ACC,PEPCK and p-GS were detected by Western blot.Results:Linarin could increase the relative glucose consumption of Hep G2 cells,improve insulin tolerance and glucose tolerance,and decrease the levels of triglyceride and cholesterol of MSG mice.Simultaneously,the expression levels of p-AMPK and p-ACC in Hep G2 cells and the liver tissue of MSG mice were increased,while the expression levels of PEPCK and p-GS were decreased after treatment with linarin.Conclusion:Insulin resistance could be ameliorated by linarin in type 2 diabetes,and its mechanism may be related to AMPK signaling pathway.

Preparation and pharmacokinetics in vivo of linarin solid dispersion and liposome

Objective:The current investigation aimed to determine the appropriate dosage form by comparing solid dispersion and liposome to achieve the purpose of improving the solubility and bioavailability of linarin.Methods:Linarin solid dispersion(LSD)and linarin liposome(LL)were developed via the solvent method and the thin film hydration method respectively.The Transwell chamber model of Caco-2 cells was established to evaluate the absorption of drug.The pharmacokinetics of linarin,LSD and LL in rats after ig administration were carried out by high performance liquid chromatography(HPLC)method.Results:The solubility of LSD and LL was severally 3.29 times and 3.09 times than that of linarin.The permeation coefficients of LSD and LL were greater than 10^(-6),indicating that the absorption of LSD and LL were both better than linarin.The bioavailability of the LSD was 3.363 times higher than that of linarin,and the bioavailability of LL was 0.9886 times higher than that of linarin.Conclusion:The linarin was more suitable for making solid dispersion to enhance its solubility and bioavailability.