The aim of this paper was to investigate the mechanism of the active peptide DP17 of Eupolyphaga steleophaga in the treatment of hyperlipidemia rats. HPLC and MADIL-TOF/TOF-MS were used for the amino acid sequence analysis and solid-phase synthesis on the active peptide of E. steleophaga which were obtained by biomimetic enzymatic hydrolysis, separation and purification. The hyperlipidemia model was established by feeding with high-fat diet.Twenty days later, the rats in the blank group and the model group were given the saline and the rats in remaining groups were given the corresponding drugs by oral administration. After administration for 4 weeks, the levels of triglyceride(TG), total cholesterol(TC) and low density lipoprotein(LDL) in serum, the levels of TG, TC, adenosine monophosphate(AMP), adenosine triphosphate(ATP) in liver tissues and TG in feces were detected, respectively. Hematoxylin-eosin(HE) staining was used to observe the pathological changes of liver tissues. The Real-time fluorescence quantitative PCR method was used to detect the expression of acetyl coa carboxylase(ACC) and hydroxymethylglutaryl-coa reductase(HMGCR) mRNA in liver tissues. The expression of mammalian target of rapamycin(mTORC1) protein and adenosine 5'-monophosphate-activated protein kinase(AMPK) in liver tissues were detected by Western blot. The analysis showed that the amino acid sequence of active peptide from E. steleophaga was DAVPGAGPAGCHPGAGP(DP17). The results of pharmacological experiments showed that after oral administration of DP17 in rats, the levels of TG, TC and LDL in serum as well as TG and TC levels in liver tissues were significantly decreased(P<0.05), while the levels of AMP, ATP in liver tissues and TG content in feces were significantly increased(P<0.05); the liver steatosis of rats was significantly relieved; the expression of ACC, HMGCR mRNA and mTORC1 protein in liver tissues were significantly reduced, while the expression of AMPK phosphorylated protein was significantly increased(P<0.05). DP17, the active peptide of E. steleophag can significantly reduce lipid accumulation in liver tissues, and it may play a role in reducing blood lipids by regulating the energy metabolism balance in the body and activating AMPK/mTOR signaling pathway.
Animals ; Diet, High-Fat/adverse effects* ; Hyperlipidemias/genetics* ; Lipids ; Liver ; Peptides ; Rats ; Triglycerides

AIM To establish an HPLC method for the simultaneous content determination of seven constituents in Gnaphalium affine D.Don.METHODS The analysis of 80％ methanol of G.affine was performed on a 30 ℃ Atlantis (C) T3 column (4.6 mm× 250 mm,5 μm),with the mobile phase comprising of acetonitrile-formic acid flowing at 1.0 mL/min in a gradient elution manner,and the detection wavelength was set at 288 nm.RESULTS Seven constituents showed good linear relationships within their own ranges (R2 ≥0.999 8),whose average recoveries were 98.58％-103.8％ with the RSDs of 0.88％-1.74％.CONCLUSION This accurate,stable and reproducible method can be used for the quality control of G.affine.

Objective To evaluate in vitro synergy between palmatine and commonly used antibiotic against main clinical isolated strains in recent three years.Methods All of 118 strains isolated in recent three years and 2 standard strains were studied.Minimal inhibition concentrations (MIC) were tested by agar dilution method and combination effects were measured by checkerboard method.Results Palmatine showed moderate in vitro activity against Staphylococcus.Synergy was detected with palmatine in combination with levofloxacin against gram-positive and negative strains,though synergistic rate less than 20％.Synergy was not show between palmatine and linezolid.Additive effect was found widely between palmatine and two agents against almost all tested species.Conclusion The results of in vitro synergy tests may be different sometimes on account of various strains,methods,etc.So,more deeper understanding of action mechanism of traditional Chinese medicine and correlation between in vitro test and clinical outcomes will help medical to select antibiotic more suitablly.

Objective To observe the clinical efficacy and safety of ilaprazole enteric-coated tablets combined with clarithromycin tablets and furazolidone tablets in the treatment of elderly peptic ulcer.Methods Ninety-six elderly patients with peptic ulcer were randomly divided into control and treatment groups with 48 cases per group.Control group was treated with omeprazole enteric-coated capsules 40 mg per time,bid,orally + clarithromycin tablets 0.5 g per time,bid,orally + furazolidone tablets 100 mg per time,qd,orally,continuous treatment for 10 days.Treatment group was treated with ilaprazole enteric-coated tablets 5 mg per time,bid,orally + clarithromycin tablets 0.5 g per time,bid,orally,continuous treatment for 5 days,then treated with ilaprazole enteric-coated tablets 5 mg per time,bid,orally + furazolidone tablet 100 mg per time,qd,orally,continuous treatment for 5 days.The clinical efficacy,Helicobacter Pylori (Hp) positive rate,serum vascular endothelial cell growth factor (VEGF),basic fibtroblast growth factor (bFGF),nitric oxide (NO) and adverse drug reactions were compared between two groups.Results After treatment,the total effective rates of treatment and control groups were 95.83％ (46 cases/48 cases) and 72.92％ (35 cases/48 cases) with significant difference (P ＜0.05).After treatment,the main indexes in treatment and control groups were compared:the Hp positive rates were 4.17％ (2 cases/48 cases) and 20.83％ (10 cases/48 cases),the VEGF were(167.28 ± 12.94) and (145.26 ± 17.87) pg · mL-1,the bFGF were (144.38 ± 14.80) and (123.29 ± 14.46) pg · mL-1,the NO were (31.81 ± 3.50) and (40.92 ± 6.32) μmol · L-1,the differences were statistically significant (all P ＜ 0.05).The adverse drug reactions in the treatment group were dizziness,vomiting and constipation,which in control group were dizziness,rash and diarrhea.The total incidences of adverse drug reactions in treatment and control groups were 8.33％ and 16.67％ without significant difference (P ＞ 0.05).Conclusion Ilaprazole enteric-coated tablets combined with clarithromycin tablets and furazolidone tablets have a definitive clinical efficacy in the treatment of elderly peptic ulcer,which can regulate the levels of serum VEGF,bFGF and NO,without increasing the incidence of adverse drug reactions.

Objective To investigate the metabolic effects of glucose dependent insulinotropic peptide receptor antagomst pro3 (GIP) in induced diabetes mice about blood glucose,triglyceride,cholesterol,leptin and fatty issue.Methods 27 C57 mice were randomly divided into normal group and diabetes mice group,and the mice in diabetes group were fed with high fat food and intraperitoneal injected streptozocin.Then 1 mouse that random blood giucose lower than 16.9 mmol/L was deleted in diabetes group.The rest mice in diabetes group were divided into two groups,diabetes control group,pro3 (GIP) group.Pro3 (GIP) group was given drug pro3 (GIP).The bloodglucose and glucose tolerance were measured.After treatment for 6 weeks,all mice were sacrificed and fatty tissues were collected.Results After 6 weeks,the blood glucose of the pro3 (GIP) group was obviously lower than diabetes control group (t=8.43,P＜0.01),and insulin levers in 0,30,60 and 120 min were obviously lower than diabetes control group (t =3.90,2.60,6.88 and 3.33,P＜0.05).There was significant difference between pro3 (GIP) group and diabetes control group about inflammatory cells.Moreover,leptin in pro3 (GIP) group was obviously lower than in diabetes control group (t =5.04,P＜0.01),but triglyceride,cholesterol,and adiponectin had no significant difference between two groups.Conclusion Pro3 (GIP) can significantly reduce blood glucose,insulin level,leptin of diabetes mice,and attenuate the inflammatory cells infiltration in fatty issue.

AIM To study the chemical constituents from Illicium brevistylum A.C.Smith and to evaluate their anti-inflammatory activities.METHODS The n-BuOH fraction of 80％ ethanol extract from I.brevistylum was isolated and purified by silica,ODS and Sephadex LH-20,the structures of obtained compounds were identified by spectral data.Then their anti-inflammatory activities were screened.RESULTS Nine compounds were isolated and identified as (7S,8R)-3,3',5-trimethoxy-4',7-epoxy-8,5'-neolignan-4,9,9'-triol (1),methylabieta-8,11,13,15-tetraen-18-oate (2),majusanin A (3),pubeside C (4),(+)-lyoniresinol-3a-O-α-L-rhamnopyranoside (5),junipercomnoside D (6),lyoniside (7),nudiposide (8),rhyncoside A (9).The inhibition rates of compounds 2,6,9 on NF-κB were 47.81％,37.33％,33.37％,respectively.CONCLUSION Compounds 1,5,7-9 are isolated from genus Illicium for the first time,and compounds 2,6,9 exhibit good anti-inflammatory activities.

Objective To explore the regularity of time-dependent changes in morphology and biomechanical properties of brain tissues in pigs,and value the feasibility of deducing the postmortem interval (PMI).Methods Brain tissues were taken from 42 pigs and kept in an artificial climate chamber with the temperature of 25 ℃ and humidity of 75％.The samples were collected from telencephalon at sequential time intervals (0,12,24,36,48,60 h;n =6) according to the principle of predefined time,position,direction,ratio,quantity and shape.The samples fixed with formaldehyde were then immediately tested by mechanical testing machine to obtain their biomechanical parameters and the histological sections were prepared.Results With the extension of PMI (0-60 h),brain tissues gradually became discolored,weak,mudding and liquefied under the influence of autolysis and putrefaction.Both clearance area of the white matter and its integrated optical density (IOD) significantly increased during 0-48 h.Biomechanical properties of brain tissues including the limit load,average force,elastic modulus and fracture energy all presented a declining tendency at the interval of 12-60 h.The limit load was considered highly statistically significant,and statistical differences were found in average force,elastic modulus and fracture energy.Conclusions There exists a significantly negative structure-activity relationship between the morphology of brain tissues and biomechanical properties.The limit load of postmortem brain tissues in 60 h is the optimum in the window period,which can be used as a new method for estimating PMI.

A new hexaketide acid esterified by the 17-hydroxyl group of 16,17-dihydroxycyclooctatin, namely 17-[16,17-dihydroxycyclooctatinyl]-hexaketide ester (1), a member of the group of rare bacterial diterpenes with a fused 5-8-5 ring system was isolated from strain Streptomyces sp. SR107. The structure was determined on the basis of its spectral data (H NMR, C NMR, H-H COSY, HSQC, HMBC, NOESY, IR and HR-ESI-MS). The antibacterial activity was also evaluated in this paper.
Anti-Bacterial Agents ; chemistry ; pharmacology ; Bacteria ; drug effects ; Diterpenes ; chemistry ; metabolism ; pharmacology ; Esters ; chemistry ; pharmacology ; Magnetic Resonance Spectroscopy ; Molecular Structure ; Streptomyces ; chemistry

Objective To investigate the role of antigen-processing machinery (APM) component defects in HLA class Ⅰ antigen down-regulation in laryngeal squamous cell carcinoma (SCC) and to assess the clinical significance of these defects. Methods Fifty-one formalin-fixed,paraffin-embedded SCC specimens were examined for the expressions of APM component transporter associated with antigen processing (TAP1) and low molecular weight polypeptide (LMP-7) and HLA class Ⅰ antigen by immunohistochemistry.Results HLA class Ⅰ antigens,TAP-1 and LMP-7 expressions were downregulated in 56.9％ (29/51),39.2 ％ (20/51) and 45.1％ (23/51) of the tested specimens respectively,whereas HLA class Ⅰ antigens,TAP-1 and LMP-7 expressions lost in 21.6 ％ ( 11/51 ),33.3％ ( 17/51 )and 27.5 ％ ( 14/51 ) of the tested specimens respectively.TAP-1 and LMP-7 expressions were significantly correlated with HLA class Ⅰ antigen expression (r =0.460,P < 0.05 and r =0.685,P < 0.05,respectively).HLA class Ⅰ antigens down-regulation was significantly correlated with T stage( x2 =8.61,P ＜ 0.05).Both TAP-1 and LMP-7 down-regulations were significantly correlated with T stage ( x2 valueswere 9.72 and 8.97 respectively,P ＜ 0.05 ) and TNM stage( x2 values were 9.18 and 7.70 respectively,P ＜0.05 ).TAP-1,LMP-7 and HLA class Ⅰ antigen down-regulations were significantly associated with reduced patients' overall survival ( P ＜ 0.05 ) and disease-free survival ( P ＜ 0.05 ).Multivariate analysis showed lymph node metastasis,recurrence and HLA class I antigen down-regulation were unfavorable prognostic factors(P ＜ 0.05).Conclusions Down-regulated expressions of HLA class Ⅰ antigen and APM component TAP-1 and LMP-7 occur frequently in laryngeal squamouss cell carcinoma,by which cancer cells could avoid immune surveillance,while HLA class Ⅰ antigen down-regulation is a major contributing factor to tumour progression and mortality.