Purpose:To investigate the effect of antineoplastic polypeptide from Buthus martensii venom (APBMV) on the cultured human promyelocytic leukemia cells HL 60 and hepatoma cell line SMMC 7721 and hepatoma H 22 bearing mice.Methods:MTT colorimetric method, growth inhibiting test and colony formation assay were used in the in vitro test. H 22 bearing mice were applied in the in vivo experiment. Through measuring tumor growth inhibitory rate(IR),white blood cell (WBC) number and spleen index (SI) ,we explored the influence of APBMV on H 22 bearing mice.Results:APBMV possessed stronger cytotoxicity on HL 60 cells and SMMC 7721 cells, and IC 50 was 10.74 ?g/ml and 11.33 ?g/ml , respectively. APBMV could dramatically inhibit their growths. There were obvious dosage response correlations. The IC 50 of HL 60 and SMMC 7721 at 24h, 48h and 96h were 19.41 ?g/ml, 9.90 ?g/ml, 11.41 ?g/ml and 15.87 ?g/ml, 13.05 ?g/ml, 8.70 ?g/ml, respectively. When the concentration of APBMV exceeded 8 ?g/ml, the colony formation rate of SMMC 7721 cells decreased dramatically ( P 0.05).Tumor growth of H 22 bearing mice was markedly inhibited by APBMV,the growth inhibiting rate was reached 40.30% ( P

AIM: To observe the growth inhibiting effect of antineoplastic polypeptide from Buthus Martensii venom(APBMV)on liver neoplasm METHODS: MTT calorimetric method, trypin blue exclusion,colony formation and H 22 -bearing mouse model RESULTS: The ability to metabolize MTT of SMMC-7721 cells was lower than control distinctly after the cells were treated by APBMV The IC 50 of APBMV was 11 3 ?g/mL The growth of SMMC-7721 cells was inhibited obviously by APBMV and the dose-response relationship was clear, the IC 50 were 15 87 ?g/mL,13 05 ?g/mL and 8 70 ?g/mL respectively The colony formation rate of SMMC-7721 cells was also decreased evidently compared with control when treated concentrations of APBMV were higher than 8 ?g/mL Tumor growth of H 22 -bearing mice was inhibited by APBMV evidently, the growth inhibiting rate was reached 37 31%( P

The interaction of drug and target protein is a critical part of new drug discovery. It is the premise for drugs to exert therapeutic effects by targeting specific binding sites of target proteins and thereby affecting its pharmacological activity. Currently, a variety of techniques are exploited to detect the interaction between drug ligands and target proteins. For example, cellular thermal shift assay (CETSA) and differential scanning fluorimetry (DSF) based on thermodynamics, mass spectrometry and nuclear magnetic resonance technology, etc. In addition, high-throughput ligand screening technology provides technical convenience for the search of specific ligand, and is a powerful tool to efficiently identify the interaction between drug ligand and target protein. Here, we summarize the detection techniques of interaction between small molecules and target proteins, and discuss the application of high-throughput ligand screening technology in drug research.

Target identification and verification of natural products is an important and challenging work in the field of chemical biology. It is also an important job for researchers to apply chemical proteomics technology to biomedicine in order to identify target proteins of natural products. Target identification is critical to understanding its mechanisms and developing natural products as molecular probes and potential therapeutic drugs. Traditional approaches of small molecule target identification based on affinity have been shown to be successful, such as click-chemical probes, radioisotope labeling or photosensitized small-molecule probes. Nevertheless, these technologies require purified candidate target proteins, and modified small molecules with probes or linkers, such as adding agarose beads, biotin labels, fluorescent labeling or photo-affinity labeling. Many structure-activity relationship studies should be performed to ensure that the addition of small molecule labels undisturbed the original biological activity of the small molecules. Unfortunately, all these modifications are likely to alter their biological activity or binding specificity. To overcome the bottleneck of "target recognition", researchers have developed a series of new techniques for unmodified drug target identification. In this article, we reviewed the target identification techniques of natural product without structural modification in order to provide reference for the development of natural products.

Objective:To investigate the effects of Processing on antioxidation of Radix et Rhizoma Rhei and Rhizoma Polygoni Cuspidati. Method: The oxygen free radicals generation system and mouse liver homogenate lipid peroxidation in vitro were used. Result:The processed products of Radix et Rhizoma Rhei and Rhizoma Polygoni Cuspidati could scavenge superoxide radical （O2*）generated through hypoxanthine-oxidase system and (*OH) generated through Fenton action, and inhibit lipid peroxidation induced by hydroxyl radical generation system, respectively. There existed significant differences among the different processed products. Conclusion:After Radix et Rhizoma Rhei and Rhizoma Polygoni Cuspidati were processed, their effects became weaker.

OBJECTIVETo observe the effect of Tiaozhi Jiangtang Tablet (TJT) on insulin resistance (IR) in rats with diebetes mellitus type 2.

METHODSThe model rats of diebetes mellitus were induced by intraperitoneal injection of streptozotocin (30mg/kg) and feeding with high lipid forage. The rats in the TJT group were treated with TJT and those in the metformin group treated with metformin as positive controls. The glucose infusion rate (GIR) was detected by glucose clamp technique after treatment for 8 weeks. At the same time, fasting blood glucose ( FBG), fasting insulin ( FINS), free fatty acids ( FFA), total cholesterol ( TC), triglyceride (TG), and high-density lipoprotein cholesterol (HDL-C) were measured respectively, and insulin sensitivity index (ISI) and HDL-C/TC calculated. The changes of insulin sensitivity and lipid metabolism were evaluated.

RESULTSTC, TG, HDL-C/TC, FINS, and FFA significantly reduced in the TJT group as compared with those in the control group, while ISI and GIR significantly increased, the effects of TJT were similar to those of metformin.

CONCLUSIONTJT is effective in increasing insulin sensitivity and improving glucose and lipid metabolisms in rats with diebetes mellitus type 2.

Animals ; Blood Glucose ; Cholesterol ; blood ; Cholesterol, HDL ; blood ; Diabetes Mellitus, Experimental ; blood ; drug therapy ; Diabetes Mellitus, Type 2 ; blood ; drug therapy ; Drugs, Chinese Herbal ; therapeutic use ; Fatty Acids, Nonesterified ; blood ; Hypoglycemic Agents ; therapeutic use ; Insulin ; blood ; Insulin Resistance ; Rats ; Tablets ; Triglycerides ; blood

Objective:To investigate the effects of different processing products of Cortex Phellodendri on scavenging oxygen free radicals and anti-lipidperoxidation. Method:The oxygen free radicals generation system and mouse liver homogenate lipid peroxidation in vitro were used. Result:The aqueous and 80% alcohol extracts of raw,stir-fried,stir-fried with salt,stir-fried with yellow alcohol products of Cortex Phellodendri could scavenge superoxide radical(O2*)generated through hypoxanthine-oxidase system and(*OH)generated through Fenton action,and inhibit lipid peroxidation induced by hydroxyl radical generation system,respectively.But the carbonized product has no effect.There are differences among these processed products.Conclusion:80% alcohol extract of stir-fried with yellow alcohol products of Cortex Phellodendri was more intense.

OBJECTIVETo summarize and analyze the clinical indication, surgical techniques and results of percutaneous antegrade Kirschner pinning in the treatment of proximal fracture of humerus.

METHODSThirty-two patients with displaced fractures of the proximal humerus were treated with 2 to 3 Kirschner wires by percutaneous antegrade transfixation. Among 32 casas, there were 7 male and 25 female, with a mean age of 49.25 years (range, from 28 to 75 years). According to the Neer fracture classification, there were 20 cases of 2-part, 9 of 3-part, and 3 of 4-part fractures.

RESULTSAll patients were followed up for 8 to 34 months with an average of 13.5 months. According to Constant-Murley evaluation, the results were excellent in 21 cases, good in 9, fair in 2.

CONCLUSIONPercutaneous antegrade transfixaton is a good technique for the management of displaced 2-part fractures of the proximal humerus and also alternative to 3-part or 4-part fractures.

Adult ; Aged ; Bone Wires ; Female ; Fracture Fixation, Internal ; methods ; Humans ; Humeral Fractures ; surgery ; Male ; Middle Aged

OBJECTIVETo investigate the occupational exposure levels of dust in new suspension preheated dry process (NSP) cement production line and put forward rectification measures for dust-exposed posts, and to provide ideas for the modern cement production enterprises in dust control and occupational health management.

METHODSOccupational health field investigation combined with field test were used to measure the time-weighted average concentration (C(TWA)) of the dust in the workplace. Rectification measures were taken for the dust-exposed posts with unqualified dust concentration, and the protective effects of dustproof facilities in the rectified workplace were evaluated.

RESULTSThe field investigation revealed incompletely closed dustproof facilities, improperly set dust hoods, excess of dust leakage points, and other problems in the dust-exposed posts of an NSP cement production line before rectification, and the dustproof facilities could hardly exert dust removal effect. The field test showed that the vast majority of dust-exposed posts had the dust concentrations exceeding the occupational exposure limits (OELs), with a qualified rate as low as 31.8%. A series of rectification measures were taken for these posts. After the rectification, the dust-exposed posts demonstrated dramatically dropped C(TWA), and the qualified rate of dust concentration in the dust-exposed posts rose to 90.9%.

CONCLUSIONThe dust hazards in NSP cement production line cannot be ignored. Taking appropriate protective measures are critical for curbing dust hazards in modern cement production.

Air Pollutants, Occupational ; analysis ; Construction Materials ; Dust ; analysis ; Humans ; Occupational Exposure ; analysis ; prevention & control ; Workplace

The effects of mangiferin on uric acid excretion, kidney function and related renal transporters were investigated in hyperuricemic mice induced by potassium oxonate. Mice were divided into normal control group, and 5 hyperuricemic groups with model control, 50, 100, and 200 mg x kg(-1) mangiferin, and 5 mg x kg(-1) allopurinol. Mice were administered by gavage once daily with 250 mg x kg(-1) potassium oxonate for seven consecutive days to create the model. And 3 doses of mangiferin were orally initiated on the day 1 h after potassium oxonate was given, separately. Serum uric acid, creatinine and urea nitrogon levels, as well as urinary uric acid creatinine levels were measured. Mouse uromodulin (mUMOD) levels in serum, urine and kidney were determined by ELISA method. The mRNA and protein levels of related renal transporters were assayed by RT-PCR and Western blotting methods, respectively. Compared to model group, mangiferin significantly reduced serum uric acid, creatinine and urea nitrogon levels, increased 24 h uric acid and creatinine excretion, and fractional excretion of uric acid in hyperuricemic mice, exhibiting uric acid excretion enhancement and kidney function improvement. Mangiferin was found to down-regulate mRNA and protein levels of urate transporter 1 (mURAT1) and glucose transporter 9 (mGLUT9), as well as up-regulate organic anion transporter 1 (mOAT1) in the kidney of hyperuricemic mice. These findings suggested that mangiferin might enhance uric acid excretion and in turn reduce serum uric acid level through the decrease of uric acid reabsorption and the increase of uric acid secretion in hyperuricemic mice. Moreover, mangiferin remarkably up-regulated expression levels of renal organic cation and carnitine transporters (mOCT1, mOCT2, mOCTN1 and mOCTN2), increased urine mUMOD levels, as well as decreased serum and kidney mUMOD levels in hyperuricemic mice, which might be involved in mangiferin-mediated renal protective action.
Animals ; Blood Urea Nitrogen ; Carrier Proteins ; genetics ; metabolism ; Creatinine ; blood ; Glucose Transport Proteins, Facilitative ; genetics ; metabolism ; Hyperuricemia ; blood ; chemically induced ; physiopathology ; urine ; Kidney ; metabolism ; physiopathology ; Male ; Membrane Proteins ; genetics ; metabolism ; Mice ; Octamer Transcription Factor-1 ; genetics ; metabolism ; Organic Anion Transport Protein 1 ; genetics ; metabolism ; Organic Anion Transporters ; genetics ; metabolism ; Organic Cation Transport Proteins ; genetics ; metabolism ; Organic Cation Transporter 2 ; Oxonic Acid ; Protective Agents ; pharmacology ; RNA, Messenger ; metabolism ; Random Allocation ; Solute Carrier Family 22 Member 5 ; Uric Acid ; blood ; urine ; Uromodulin ; blood ; urine ; Xanthones ; pharmacology