Study On Chemical Consittutens, Hepatoprotective And Antihyperglycemic Effect Of Lysimachia Paridiformis Van Stenophylia And Lysimachia Ckthroides

The plants of genus Lysimachia are abundant in resource and widely distributed in China. Reports forgenus Lysimachia are full as folk-medicines widely used in China. This paper include antioxidant andα-glucosidase inhibitory activity of two species that screened in thirteen species of Lysimachia genus invitro. Then, active compounds, hepatoprotective and antihyperglycemic effect of L. paridiformis var.stenophylla and L. clethroides on liver injury and alloxan-induced diabetic mice are evaluated in vivo. Thisthesis provides the theoretical basis for medicine development, introduction and cultivation and utilizationof this genus. As part of systematic and deep research, this thesis has innovative results as follows:1. Antioxidant activity of L. clethroides. and L. paridiformis var. stenophylla is evaluated for the firsttime in vitro, and antioxidant activity of n-BuOH extracts (LPFBU and LCBU) are the highest than that ofother extracts. In DPPH assay, the antioxidant activity of LCBU and LPFBU (IC₅₀=9.86and15.69μg/mL,respectively) were both higher than that of BHT (IC₅₀=18.71μg/mL). In ABTS assay, the antioxidantactivity of LCBU (IC₅₀=7.43μg/mL) was higher than that of BHT (IC₅₀=7.72μg/mL). In ABTS assay, theantioxidant activity of LPFEA (IC₅₀=10.31μg/mL) and LPFBU (IC₅₀=10.97μg/mL) were lower than thatof three positive control, and far higher than that of LPFPE (IC₅₀=109.32μg/mL). In FARP assay, LPFEAand LPFBU (RACT₅₀=695.2and765.4μmol/g, respectively) ferri ion reduction capacity were lower thanthat of three positive control, but far higher than that of LPFPE (RACT₅₀=156.55μmol/g).The levels of GOT and GPT in serum are significantly decreased by intragastric administration ofthree extracts of LPF compared with positive control of bifendate on CCl4-induced acute liver injury inmice, LPFBU (600mg/kg) showed the highest activity in decreasing the level of GOT in serum, and thecontent of MDA in liver for each treatment group is significantly decreased, and the level of SOD issignificantly increased. Administration each dose group of LCPE, LCEA and LCBU respectively weresignificantly decreased in the level of GOT and GPT, and LCEA (600and300mg/kg, respectively) andLCBU (300and1₅₀ mg/kg, respectively) tend to bring the level to near normal compared with positivecontrol of bifendate (70mg/kg). Results showed that intragastric administration of LCPE, LCEA andLCBU was similar to bifendate and LCEA showed dose dependence. The conent of MDA in liver for eachtreatment group is significantly decreased, and the level of SOD in liver is significantly increased except LCBU(1₅₀ mg/kg). LPFBU(600and300mg/kg, respectively) showed the highest activity. Results showedthat LC and LPF are useful to protect CCl4-induced acute liver injury and hepatoprotective mechanisms isrelated to improve the antioxidant capacity of liver cells. It can be used to protect and treatment of liverdisease.2. The LPFPE, LPFEA and LPFBU have strong α-glucosidase inhibitory activity in vitro which arereported for the first time. They showed stronger inhibitory activity against a-glucosidase (IC₅₀=38.97,42.62and20μg/mL, respectively) than that of acarbose (IC₅₀=1103.01μg/mL) as positive control. Resultsshowed that α-glucosidase inhibitory activities of LPFPE, LPFEA and LPFBU exhibited strong activity indose dependent manner.Administration of LPF and LC to diabetic rats resulted in no significant decrease in level ofpost-prandial blood glucose. The intragastric administration of LPFEA (1000and500mg/kg, respectively)to diabetic rats resulted in a significant decrease in level of fasting blood glucose (p<0.001). The level ofTG and TC in administration of LPF in serumon Alloxan-induced diabetic mice was significantly decreased.This can improve concurrent hyperlipidemia of ALX-induced diabetic mice, and correct the abnormal lipidmetabolism. Through improving liver glycogen synthesis can decrease glycogen breakdown and bloodsugar. By reducing the content of MDA and increasing activity of SOD to enhance antioxidant capabilityand protect the body from further oxidative damage which is caused by free radicals in diabetic mice,which play the role of hypoglycemic effect. Therefore, LPF has effective prevention and treatment on thedevelopment for diabetes and its complications.3. Active compounds in L. clethroides are isolated and identified using all kinds of columnchromagraphy and spectral technology.14compounds are isolated and7are identified as β-daucosterin(1), kaempferol (2), sitosterol (3), quercetin (4), soybeansterol (5), β-fragrant resin (6) and betulinic acid(7). Results showed that the compound2and4had the highest antioxidant activity(IC₅₀=14.78and6.94μg/mL, respectively) and stronger inhibitory activity against a-glucosidase(IC₅₀=73.69and8.86μg/mL,respectively) in vitro. Based on the results, it can be concluded that the compound2and4are activeingredients of L. clethroides.4. The volatile constituents of five species of genus Lysimachia were analyzed by head-space solidmicro-extraction,coupled with GC-MS (HS-SPME-GC-MS) for the first time. The consequence has shown that the plant of genus Lysimachia essential oils has great value both in the medical industry and the spicesindustry, however, more research should be carried out on the mechanism of action in the future.5. The paper summarized the progress of chemical compounds and pharmacology of genusLysimachia, to provide reference for further studies on the bioactive constituents and medicinal use of thisgenus．...