This article was aimed to study effects and mechanisms of Gymnema sylvestre on protein kinase B (PKB) and its phosphorylation in adipose tissues of KKAy mice which were mainly characterized by insulin resistance (IR). A total of 18 KKAy mice were randomly divided into the diabetes model (DM) group and Gymnema sylvestre (GS) group according to body weight levels. And 9 normal C57BL/6J mice were used as the normal control (NC) group. Intragastric administration of medication was given to mice for 8 weeks. At the end of the experiment, all animals were tested for fasting plasma glucose (FPG) and fasting insulin level (Fins) for evaluation of insulin sensitivity index (ISI). Expressions of phosphoinositide-dependent kinase-1 (PDK1), PKB, P-PKB (Ser473), P-PKB (Thr 308) in adi-pose tissues of epididymis were determined. The expression of phosphatase and tensin homolog (PTEN) mRNA was also determined. The results showed that compared with the DM group, the GS group showed lower FPG and Fins, higher ISI. The expression of P-PKB (Ser473) phosphorylation and P-PKB (Thr 308) were increased, and the PDK1 and PTEN mRNA were decreased. It was concluded that GS can improve insulin sensitivity of KKAy mice through activating PKB by up-regulate the expression of P- PKB (Ser473) and its phosphorylation ratio and P- PKB (Thr 308) in adipose tissues.

Objective To observe the effects of genistein(GEN)on oleic acid(OA)induced lipid accumulationin in H4 ⅡE cells and to discuss the possible mechanism of GEN in the pointof AMPK.Methods H4ⅡE cells were cultured in vitro.The control group(NOR),OA treatment group(MOD group)and GEN treatment group were established according to the experimental requirements.The effects of GEN on the proliferation of H4 Ⅱ E cells were measured with MTT assay.The intraeellular TG mass was quantified spectrophotometrically using TG test kit.Cell protein was determined by DCTM Protein Assay kit.The intracellular TG concentration which was used to evaluate lipid accumulation was corrected using protein content as an internal standard.Western blotting was applied to determine the expression of AMPK and P-AMPK (Thr172).Accordingly the phosphorylation levels of AMPK was by means of P-AMPK(Thr172)/AMPK.Results OA treatment can induce lipid accumulation in H4 Ⅱ E cells while GEN treatment can decrease the intracellular TG concentration through up-regulate the phosphorylation levels of AMPK,though the effect was blocked by Compound C that is the inhibitor of AMPK.Conclusion GEN has anti-accumulation of lipid effect in H4ⅡE cell.The mechanism of GEN protective effect is partially due to AMPK.

This study was aimed to improve the drug activity of three kinds of isoflavones from Chickpeas.Biochanin A,formononetin and genistein were used as raw materials.Acetone was used as solvent.Potassium carbonate was used as catalyst.The etherification reaction was with 1,3-dibromopropane,1-bromopropane and 3-bromopropene.The results showed that 9 isoflavone ramifications were synthesized.This method was simple,easy to control with high yield.It was concluded that the product structure was confirmed by 1H-NMR,13C-NMR and ESI-MS analysis.It laid a foundation for the structural study basis in the further research of its drug activity.

To develop a method for determining 3 Xanthone glycosides (1, 5-dihydroxy- 3-methoxyxanthone 8-O-β-D-glucopyranoside(F1), 1-hydroxy-3, 4-dimethoxyxanthon 7-O-β-D-glucopyranoside (F2), 1, 8-dihydroxy-3, 4-dimethoxyxanthone 5-O-β- D-glucopyranoside (F3) of Gentianella acuta by HPLC. The Thermo syncronis C18 (4.6 mmí250 mm, 5 μm) was used for simultaneous determination of 3 Xanthone glycosides in G. acuta. Isocratic elution with water and acetonitrile was 75.5:24.5. The flow rate was 1.0 mL·min-1 and the detection wavelength was set at 254 nm. The column temperature was 35℃. The linear concentration ranges of F1,F2,F3 were 14.06 ~ 281.28 μg·mL-1 (R2=0.999 7),0.56~11.16 μg·mL-1 (R2=0.999 8),0.46~9.20 μg·mL-1 (R2=0.999 9), respectively; The average recov-eries (n = 9) were 99.70% (RSD=1.06%),99.78% (RSD=1.21%),100.28% (RSD=1.15%), respectively. The method is simple, accurate and sensitive, and can be used for the quality control of G. acuta as a reference.

In this paper, three higher content of flavonol glycosides from the stems and leaves of Tribulus terrestris L. were determined by reversed phase HPLC. The results showed that there was good liner relationship between the peak areas and the sample concentration at the ranges of 0.011 2~0.280 0 μg (r=0.999 6), 0.064 8~2.592 0 μg (r=0.999 8) and 0.018 4~0.460 0 μg (r=0.999 8) for isorhamnetin-3-O-β-D-gentiobioside-7-O-β-D-glucoside, quercetin-3-O-β-D-gentiobioside and isorhamnetin-3-O-β-D-gentiobioside respectively. The verage recovery rates (n=9) of three flavonol glycosides compounds were 100.15%(RSD=1.32%), 100.02% (RSD=1.14%), 99.77% (RSD=1.16%), respectively. This method is considered to be simple, accurate, stable, good precision and reproducibility, which is available for the quality control and evaluation of T. terrestris L.

Guava leaf (GL) has been widely used as an herbal medicine for diabetes treatment in tropical and sub-tropical regions. GL has the function of drying dampness and fortifying the spleen, clearing heat and resolving toxins. Modern pharmacological study showed that GL contained flavonoid, phenolic acids, terpene, sesquiterpenoids and other chemical compounds, which regulated hyperglycemia. In recent years, the clinical and basic research on GL has received certain progress. This article reviewed effective components of GL, as well as research progress on clini-cal and basic research of type 2 diabetes.

This paper was aimed to study the albiflorin activity of Tang-Bi-Kang (TBK) granules in protecting Schwann cells (SCs) of rat's sciatic nerve.The establishment of SCs oxidative stress model was the condition of 150 mmol×L-1 Dglucose with different concentrations.And the incubation time was 48 h.The experiment groups were the high-dose,middle-dose and low-dose (100 μM,20 μM,4 μM) albiflorin group,the model group,the vitamin C (100 μM) group,and the normal group.Flow cytometry was used to detect the content of ROS in SCs.Fluorescence microscope was used to observe the condition of ROS fluorescence in SCs.And CCK-8 was used to detect the cell activity.The results showed that by using CCK-8 to detect cell proliferation,after 48 h,there was a significant difference between the model group and the normal group (P＜0.01);the albiflorin group compared with the model group (P＜0.01).It indicated that albiflorin can promote the proliferation of SCs.Detecting the ROS fluorescence content,it showed that compared with the model group (Glu 150 mM),the 100 μM,20 μM,and 4 μM albiflorin group,it was P＜0.01 for each group.It showed that albiflorin could relieve the ROS in SCs and alleviate oxidative stress.It was concluded that albiflorin can increase the proliferation of SCs and improve the state of oxidative stress with the protection of SCs.

Through comprehensively characterizing components in blood after oral administration of Tang-Bi-Kang (TBK) granules by UPLC-ESI-MSn,this study was aimed to explain the pharmaceutical material basis of TBK initially.UPLC-LTQ-Orbitrap was used under both positive and negative ion modes of electrospray ionization.The blank serum and rat serum after oral administration of TBK were analyzed.Components in rat serum were identified and characterized based on ion fragment information,evenelectron law,nitrogen rule and so on.Reference data was used to establish the UPLC-ESI-MSn method.The results showed that after oral administration of TBK granules,15 components were detected in the serum,of which 13 components were taken as the prototype to blood and 2 metabolites.It was concluded that constituents of TBK granules in rat serum were generated from compatibility of all herbal medicines.In rat serum,most of the components had been absorbed by rat's metabolism;a few were absorbed as the prototype.This research provided references for pharmacodynamic material basis and metabolism of TBL granules in vivo.

This paper was aimed to study the effect of ethyl acetate extracts of Gentianella acuta on the gene and protein of insulin significant signal IRS-1 and Akt in insulin resistance (IR) HepG2 cells.The CCK-8 method was used to detect the HepG2 cell activity.HepG2 cells of human liver cancer were cultured with high concentration insulin (10-6 mol· L-1)for 36 hours to establish IR cell model.According to the results of CCK-8,the control group,model (IR) group,ethyl acetate extracts of Gentianella acuta IR + 50 μg· mL-1,IR + 500 μg· mL-1 group,and the metformin group were divided.Glucose consumption was measured with a glucose assay kit.The expressions of IRS-1 and Akt gene in IR HepG2 cells were detected by RT-PCR after 6-hour using of ethyl acetate extracts of Gentianella acuta.Western blot was used to detect the expression of IRS-1 and Akt protein after 6-hour using of ethyl acetate extracts of Gentianella acuta.The results showed that when the concentration of ethyl acetate extracts of Gentianella acuta was 500 μg· mL-1,the survival rate reached 95％.When the concentration was higher than 500 μg· mL-1,the survival rate decreased.Compared with the IR group,the IR + 50 μg· mL-1 group and the IR + 500 μg· mL-1 group promoted glucose consumption of IR HepG2 cells,but its effect was less than that of the metformin hydrochloride group.The expression of IRS-1 and Akt in IR HepG2 cells was significantly increased by using RT-PCR in the group of IR + 50 μg· mL-1 and IR + 500 μg·mL-1 compared with the IR group after 6-hour using of ethyl acetate extracts of Gentianella acuta.The expression of IRS-1 and Akt protein in the group of IR + 50 μg· mL-1 and IR + 500 μg· mL-1 was significantly higher than that in the IR group after 6-hour medication detected by western blot.It was concluded that the ethyl acetate extracts of Gentianella acuta can increase the expression of IRS-1,Akt gene,the expression of IRS-1 and Akt protein in HepG2 cells,which may be the mechanism of IR improvement.

Through the ethoxylation structure modification of three isoflavones which were genistein, biochanin A and formononetin in chickpea, the hypoglycemic activity and the synergistic hypoglycemic activity were studied. Ethoxylation structure modification was given on three kinds of isoflavones. The hypoglycemic activity of three kinds of isoflavones and their derivatives were studied. The synergistic hypoglycemic activity of the compounds was also studied. The insulin-resistance HepG2 cell was selected as the model of hypoglycemic activity screening. The results showed that four ethoxylation products were synthesized. And the hypoglycemic activity of genistein was better than biochanin A and formononetin with significant difference (P < 0.05). The maximum dosage of three isoflavones was compared with the positive drug metformin hydrochloride. And the effect was not as good as metformin hydrochloride. There was significant difference (P < 0.05, orP < 0.01). There was no significant difference of effect between the compound a and the compound d (P > 0.05). Effects of the compound b and compound c were not as good as the compound a and compound d. There was statistical difference (P < 0.05). The activity of compound d was significantly improved than the parent compound (P < 0.05). There was no statistical difference on the hypoglycemic activity between combination 5 and metformin hydrochloride (P > 0.05). It was concluded that the combinations of compounds played synergistic effects with better hypoglycemic effect. It provided a basis for developing hypoglycemic agents with the intellectual property rights.