Objective To observe the antibacterial activity of artificial antimicrobial peptides (AMPs) to Blastomyces albicans, E. coli and Staphylococcus aureus in oral infection in vitro. Methods The AMPs were dissolved into PBS or sterilized saliva, then the inhibi-tion of different concentration AMPs to E. coil was evaluated by tube testing. The inhibition effect of different concentration of AMPs to Staph-ylococcus aureus and Blastomyces albicans were evaluated by antibiotic-susceptive test paper. Results When the concentration of AMPs added to broth of E. coli is from 150μmol/L to 300μmol/L , the bacterium count is 0 while the number in control is 6700 ～ 9200cfu/ml. At 100μg/tablet AMPs, the diameter of inhibitor zones of Staphylococcus aureus and Blastomyces albicans are 13mm and 11 mm. At 300μg/ tablet, the diameter are 16 mm and 17mm. AMPs dissolved in PBS and saliva have similar antimicrobial activity. Gonclusions The AMPs is effective to prevent Blastomyces albicans, E. coli and Staphylococcus aurcus in oral infection in vitro.

Objective To investigate the effect of an oral calcium load on serum electrolytes and PTH concentrations in healthy apheresis donors.Methods Forty-five apheresis donors were divided into two groups: calcium group(11 donors,taking oral calcium before apheresis) and no calcium group(34 donors).Serum parathyroid hormone(PTH),total calcium(Ca),phosphorus(P),potassium(K),sodium(Na) and magnesium(Mg) were measured before and after the apheresis process.Twenty-four whole blood donors served as controls.Results After the apheresis process,PTH concentrations in calcium group and mean P in no calcium group increased significantly(P

OBJECTIVETo observe the effect of Zhenqing Recipe (ZQR) on non-alcoholic fatty liver (NAFL), and the expression of hepatic salt-inducible kinase 1 (SIK1) and sterol-regulatory element binding protein-ic (SREBP-lc) in type 2 diabetes rats.

METHODSA rat model of type 2 diabetes was established by high fat/sucrose diet combined with intraperitoneal injection of small dose streptozotocin (STZ) . Modeled rats were randomly divided into the model group, the ZQR group, and the metformin group, 8 in each group. Eight rats were recruited as a normal control group. ZQR at the daily dose of 12 g crude drugs/kg was administered to rats in the ZQR group by gastrogavage. Metformin suspension at the daily dose of 150 mg/kg was administered to rats in the metformin group by gastrogavage. Equal volume of distilled water was administered to rats in the normal control group and the model group. All medication lasted for 12 weeks. The levels of fasting blood glucose (FBG), free fatty acid (FFA), serum triglyceride (TG), serum total cholesterol (TC), serum alanine aminotransferase (ALT), and aspartate aminotransferase (AST) were detected. The body weight and wet liver weight were weighed, and the liver weight index calculated. The liver TG content was measured. The pathological changes of liver and the expression of SIK1 were observed by HE staining and immunohistochemistry. The mRNA and protein expression of SIK1 and SREBP-1c were detected using RT-PCR and Western blot.

RESULTSCompared with the normal control group, FBG, FFA, TG, TC, ALT, AST, liver weight index, and liver TG contents significantly increased (P < 0.01); liver steatosis was severe, the mRNA and protein expression of SIK1 obviously decreased (P < 0.01); mRNA and protein expression of SREBP-1c increased (P < 0.01). After drug therapy, compared with the model group, FBG, FFA, TG, TC, ALT, AST, and liver weight index significantly decreased, liver TG contents significantly decreased, the mRNA and protein expression of SIK1 obviously increased, while mRNA and protein expression of SREBP-1c obviously decreased (P < 0.05, P < 0.01) in the ZQR group and the metformin group (P < 0.05, P < 0.01); and the pathological changes were also improved. All the indices were improved more in the ZQR group (all P < 0.05).

CONCLUSIONIn this experiment, we found that the expression of SIK1 decreased in NAFL rats with type 2 diabetes. ZQR could alleviate lesion of NAFL type 2 diabetes rats possibly by up-regulating hepatic SIK1 expression at mRNA and protein levels.

Animals ; Diabetes Mellitus, Type 2 ; complications ; drug therapy ; metabolism ; Disease Models, Animal ; Drugs, Chinese Herbal ; therapeutic use ; Fatty Liver ; complications ; drug therapy ; metabolism ; Liver ; metabolism ; Male ; Protein-Serine-Threonine Kinases ; metabolism ; Rats ; Rats, Wistar ; Sterol Regulatory Element Binding Protein 1 ; metabolism

Objective To investigate the ex pr ession of squamous cell carcinoma antigen (SCC-Ag) and carcinoembryanic antigen (CEA) and its clinical significance in patients with lung cancer. Meth ods The pre-treatment serum from 134 patients with lung cancer from 1998 to 2002 were analyzed for the SCC-Ag level and CEA level by IMX, and the correlation of the SCC-Ag level and CEA level with the clinicopathologic charac teristics were also detected. Results Significant correlations were found between the pre -treatment SCC-Ag level, and CEA level and the pathologic classification, clin ical stage, the positive rate of diagnosing lung cancer was raised by combined a ssay with serum SCC-Ag and CEA. Conclusion Pre-treatment and after-treatment measurement of serum SCC-Ag level and CEA level can be used for diagnosis, prediction of pr ognosis and monitor of after-treatment recurrence in patients with lung cancer.

Objective To investigate the clinical significa nc e and the relationship between the serum squamous cell carcinoma antigen (SCC-A g) levels and the biological characteristics in patients with cervical carcinoma . Methods The pre-post-treatment sera from 500 patients w ith cervical carcinoma from 1998 to 2002 were analyzed for the SCC-Ag levels by IMX; and the correlation between the SCC-Ag level and the clinicopathologic ch aracteristics were also detected. Results Significant corre lation was found between the pre-treatment SCC-Ag level and pathologic classif ication, and clinical stage (P0.05); The pre-treatm ent SCC-Ag level is significantly higher than that of post-treatment (P

Objective: To study the influence of high cell incubating temperature on AMP-activated protein kinase(AMPK) activity and lipid metabolites of piglets hepatocytes in vitro.Method: Primary hepatocytes of piglets about age 55d were separated and cultured under 37 ℃(control) or 42 ℃(heat stress).The anabolic and catabolic products of [14C]-oleic acid were detected for hepatocytes and culture media at 60min,120min and 180min.There were 9 replicates per time point.Result: Heat stress activated AMPK activity and enhanced fatty acid oxidation.The production of [14C]-CO2 and [14C]-acid soluble metabolites(ASM) was higher in heat stress group than in the control.At the same time,heat stress depressed the incorporation of [14C]-oleate into phospholipids,monoglycerides,triglycerides,cholesterol and cholesteryl ester.Conclusion: Heat stress activated AMPK activity and enhanced the formation of anabolic products and depressed catabolic products in piglets hepatocytes in vitro.

Background Scarring of the filtering bleb is a main cause of filtering surgical failure in glaucoma.It has been reposed that tetrandrine could suppress the proliferation of cultured human fibroblast of Tenons capsule in vitro and thus has the potential effect to prevent scarring after the filtering surgery. Objective Present study was to investigate the anti-cicatricial effect of tetrandrine drug delivery system(Tet DDS)during filtration surgery. Methods Filtration surgery was performed in bilateral eyes of 18 New Zealand white rabbits.The Tet DDS with 0.3 mg Tet,0.2 mg Tet or free-Tet were implanted subcunjunctially during the surgery.The filtering blebs were scored in 1 day,4,7,10,14 days after referring to the corneal thickness and bleb range under the slit-lamp biomicroscopy.The morphology of filtering bleb was assessed by in vivo confocal microscopy in 7 and 14 days after operation.The filtering bleb specimen was prepared in 7 and 14 days for the histopathological examination. Results The filtering bleb scores in Tet DDS implantation groups were significantly higher than those in free-Tet DDS group from 4 days through 14 days after trabeculectomy(P＜0.01),and the scores showed a considerably increase in 0.3 mg Tet DDS group compared with 0.2 mg Tet DDS group from 7 days through 14 days after trabeculectomy(P＜0.05).The filtering blebs of Tet DDS implantation groups were found with distinct subepithelial cystic spaces under the light microscopy and in vivo confocal microscopy on the 7th day and 14th day after surgery.Compared with free-Tet DDS group,the numbers of subepithelial mierocysts were much more(P＜0.01)and the area of microcysts was larger(P＜0.01)in Tet DDS group.The filtering tissue presented with more subepithelial microcysts and larger microcysts range in 0.3 mg Tet DDS group than 0.2 mg Tet DDS group in 7 and 14 days after operation(P＜0.05).The inflammatory cell infiltration wag milder in 0.3 mg Tet DDS group in comparison with 0.2 mg Tet DDS group and free-Ted DDS group.Conclusion Tet DDS has strong inhibitory effects on inflammatory cells activity and fibroblagt activity the early stage after filtering surgery and therefore improve the surgery success rate.

Protein tyrosine phosphatase (PTP) 1B is a potential target for the treatment of diabetes and obesity. We have previously identified the benzoyl sulfathiazole derivative II as a non-competitive PTP1B inhibitor with in vivo insulin sensitizing effects. Preliminary SAR study on this compound series has been carried out herein, and thirteen new compounds have been designed and synthesized. Among them, compound 10 exhibited potent inhibition against human recombinant PTP1B with the IC50 value of 3.97 micromol x L(-1), and is comparable to that of compound II.
Humans ; Protein Tyrosine Phosphatase, Non-Receptor Type 1 ; antagonists & inhibitors ; Structure-Activity Relationship ; Sulfathiazoles ; chemistry ; pharmacology

Humans ; Infant ; Lead Poisoning, Nervous System, Childhood ; diagnosis ; therapy ; Male

The chemical constituents from the fruiting bodies of Lyophyllum decastes (Fr.) Singer were studied in this paper. Thirteen compounds were isolated and purified by column chromatographies on silica gel and Sephadex LH-20. Their structures were identified by MS and NMR data analysis as adenosine (1), 2R, 3S, 4S, 8E)-2-[(2'R)-2-hydroxyheneicosanoylamino]-8-octadecene-1, 3, 4-triol (2), (2R, 3S, 4S, 8E)-2-[(2'R)-2-hydroxypentacosanoylamino]-8-octadecene-1, 3, 4-triol (3), nicotinic acid (4), (4E, 8E) -2-N-2-hydroxytetracosanoyl-1-O-beta-D-glycopyranosyl-9-methyl-4, 8-sphingadienine (5), D-mannitol (6), ergosteryl-3-O-beta-D-glucopyranoside (7), tuberoside (8), (2R, 3S, 4S, 8E)-2-[(2'R)-2-hydroxybehenoylamino]-8-octadecene-1, 3, 4-triol (9),(2R, 3S, 4S, 8E)-2-[(2'R) -2-hydroxytricosanoylamino] -8-octadecene-1, 3, 4-triol (10), (22E, 24R)-ergosta-7, 22-dien-3beta, 5alpha, 6beta-triol (11), (22E, 24R)-ergosta-5, 7, 22-trien-3beta-ol (12), and 5alpha, 8alpha-epidiory-(22E, 24R)-ergosta-6, 22-dien-3beta-ol (13), respectively. All the above compounds are first obtained from the mushroom and compounds 2-10 are reported to be obtained from the Lyophyllum for the first time.
Agaricales ; chemistry ; Drugs, Chinese Herbal ; chemistry ; Fruit ; chemistry