Explaining the mechanism of the cochlear active phonosensitive amplification has been a major problem in medicine.The basilar membrane(BM)is the key infrastructure.In 1960,Nobel Laureate von B′ek′esy first discovere...Explaining the mechanism of the cochlear active phonosensitive amplification has been a major problem in medicine.The basilar membrane(BM)is the key infrastructure.In 1960,Nobel Laureate von B′ek′esy first discovered BM's traveling wave motion.Since that time,BM's models only have considered the traveling wave but not the biological activity.Therefore,a new model considering changes of BM's stiffness in space and time is established based on the immersed boundary method to describe its biological activity.It not only reproduces the results of traveling wave motion but also explains the mechanization on the generation of traveling wave.An important discovery is that changes of BM's stiffness in space and time will cause the unstable global resonance,which will induce amplification of sounds in cochlea.An important inference is that biological activity shall be included in the application of mechanical principles to the analysis of life,which is the essential difference between biomechanics and general mechanics.展开更多
Citral is a monoterpene aldehyde,which is the main chemical component of essential oils from Litsea cubeba and Cymbopogon citratus,as well as one of the most important representatives of open-chain monoterpene compoun...Citral is a monoterpene aldehyde,which is the main chemical component of essential oils from Litsea cubeba and Cymbopogon citratus,as well as one of the most important representatives of open-chain monoterpene compounds.The lemon flavor released by citral is very strong,and thus,it is widely used in essence,spices,manufacturing of various foods and beauty and other industries.It has antibacterial,anti-inflammatory,antioxidant,anti-tumor,insecticidal and other biological activity.This paper reviewed citral in Lauraceae plants and its biological activity,in order to provide reference for the development and utilization of citral in Lauraceae plants and its diversified applications.展开更多
Lentinula edodes is the second largest edible mushroom in the world and is widely used as food and medicine.Modern research shows that lentinan(LNT)is the main active component of L.edodes.It has anti-cancer,treatment...Lentinula edodes is the second largest edible mushroom in the world and is widely used as food and medicine.Modern research shows that lentinan(LNT)is the main active component of L.edodes.It has anti-cancer,treatment of diabetes,intestinal protection,anti-inflammatory,anti-oxidation,anti-aging,hepatoprotective,immune-regulating effects.In this review,the biological activity,action mechanism and structure-activity relationship of LNT in recent years are reviewed.On this basis,the existing problems were discussed,and the future research and application of LNT were prospected.Finally,it is hoped that this review will promote the in-depth study of LNT and provide a reference for its development as a drug and functional food.展开更多
The compounds have been synthesized and characterized by routine MS, IR and NMR spectrometry methods. The compounds are all active on bacterial strains with the exception of Salmonella typhimirium, with a MIC value of...The compounds have been synthesized and characterized by routine MS, IR and NMR spectrometry methods. The compounds are all active on bacterial strains with the exception of Salmonella typhimirium, with a MIC value of 7.5 mg/mL. They show a percentage of anti-radical activity of 75.476 ± 5.070 for the compound DAN-S and of 68.142 ± 6.539 for the compound DAN-OV. The compounds are sensitive to the two champions used. DAN-S compound is then the most active.展开更多
DAPTMGY(DTY)is an oligopeptide derived from marine microalgae with proven potential to combat oxidative stress in previous research.The composition,ordering,and active sites of amino acids play a key role in activity ...DAPTMGY(DTY)is an oligopeptide derived from marine microalgae with proven potential to combat oxidative stress in previous research.The composition,ordering,and active sites of amino acids play a key role in activity studies and are also the research trends in recent years.As an oligopeptide with a molecular weight of less than 1000 Da,DTY is of great significance to explore the active site and structure-activity relationship.This study used quantum mechanics to optimize DTY’s structure and predict the active site through molecular orbits,energy,and charge.In addition,an LPS-treated HUVEC cell was established as an oxidative-stress model.DTY could reduce mitochondrial oxidative stress and inhibit ROS production by enhancing the antioxidant enzymes SOD,GPX,and HO-1.Moreover,it was confirmed to inhibit inflammation and apoptosis through the NF-κB and MAPK signaling pathways.Lastly,the correlation of the oligopeptide DTY’s active site and antioxidative-stress activity was verified by molecular docking,showing that hydrogen bonding is the main force,which was also the main factor for antioxidant activity.展开更多
Daphnoretin,belonging to coumarin compounds,is the main active ingredient of Wikstroemia indica,and has anti-inflammatory,anti-depression,anti-tumor and other pharmacological activities.This article reviews the extrac...Daphnoretin,belonging to coumarin compounds,is the main active ingredient of Wikstroemia indica,and has anti-inflammatory,anti-depression,anti-tumor and other pharmacological activities.This article reviews the extraction and purification process,content determination methods and pharmacological activity of daphnoretin,in order to provide a theoretical reference for optimization of purification process,improvement of content determination technique and further clinical application of daphnoretin.展开更多
The title compound N-(1-(2,4-dichlorophenyl)-1 H-pyrazolo[3,4-d]pyrimidin-4-yl)-4-(N,N-dipropylsulfamoyl)benzamide was synthesized by the condensation of 4-(dipropylsulfamoyl)benzoic acid with 1-(2,4-dichlorophenyl)-1...The title compound N-(1-(2,4-dichlorophenyl)-1 H-pyrazolo[3,4-d]pyrimidin-4-yl)-4-(N,N-dipropylsulfamoyl)benzamide was synthesized by the condensation of 4-(dipropylsulfamoyl)benzoic acid with 1-(2,4-dichlorophenyl)-1 H-pyrazolo[3,4-d]pyrimidin-4-amine. This intermediate was prepared from 5-amino-1-(2,4-dichlorophenyl)-1 H-pyrazole-4-carbonitrile by the condensation with triethyl orthoformate and then cyclisation with ammonium hydroxide solution in tetrahydrofuran at room temperature. The crystal structure of the title compound was determined. The optimized geometric bond lengths and bond angles obtained by using density functional theory(DFT) have been compared with X-ray diffraction values. In addition, the preliminary biological test showed that the compound possesses distinct effective inhibition on the proliferation of some cancer cell lines.展开更多
In the modern science, priority is given for the search of biological active compounds with specific properties. As a result of experimental data, it was found that in the reaction between N-(<em>β</em>-D...In the modern science, priority is given for the search of biological active compounds with specific properties. As a result of experimental data, it was found that in the reaction between N-(<em>β</em>-D-glycopyranosyl)-semicarbazide and the Lawesson reagent (2,4-bis(p-methoxyphenyl)-1,3-dithiadiphosphetane 2,4-disulfide) at the ratio 1:1 in pyridine when boiling under reflux in a water bath for 20 - 35 minutes, a new synthetic compound N-(<em>β</em>-D-glycopyranosyl)-thiosemicarbazide is formed. The individuality and structure of the target products were confirmed by 13C NMR spectroscopy, 1H NMR spectroscopy, IR spectroscopy, and elemental analysis. For the synthesized new compounds of N-(<em>β</em>-D-glycopyranosyl)-thiosemicarbazides, the probability of pharmacological and toxic effects were predicted by the computer method in silico. From the synthesized compounds N-(<em>β</em>-D-galactopyranosyl)-thiosemicarbazide, the probability of antibacterial (antibacterial) activity is predicted (<em>Pa</em>/<em>Pi</em> 0.544/0.013). The antibacterial activity of the compound (4) was confirmed in a test for salmonella infection of lambs, salmonellosis of calves, and colipathogenic E. coli serotypes. An experimental study by the in vitro method made it possible to conclude that the new synthetic compound N-(<em>β</em>-D-galactopyranosyl)-thiosemicarbazide in the studied concentrations has a pronounced bactericidal and bacteriostatic effect. The synthetic new compound N-(<em>β</em>-D-glyco- pyranosyl)-thiosemicarbazide is a promising compound for further study.展开更多
<p> <span style="font-family:Verdana;">This work aims to characterize, synthesize and evaluate the biological activity of sodium barbitone and their metal chelates Ni(II), Pd(II) and Pt(II). The ...<p> <span style="font-family:Verdana;">This work aims to characterize, synthesize and evaluate the biological activity of sodium barbitone and their metal chelates Ni(II), Pd(II) and Pt(II). The new synthesized metal chelates are investigated by elemental analysis, IR, mass spectra, thermal analysis and biological activity. Square planer structure of the prepared complexes obtained from the result of analysis. The antibacterial and antifungal of sodium barbitone ligand and its conforming metal chelates were screened against bacterial species Gram positive (<em>Staphylococcus aureus</em>), Gram negative bacteria (<em>Escherichia coli</em>) and fungi <em>Aspergillus flavus</em> and <em>Candida albicans</em> fungi. Ampicillin and amphotericin were used as references for antibacterial and antifungal studies. The activity data show that the plati</span><span style="font-family:Verdana;">num group metals chelates have activity data show that some of the platinum group metals (viz. Pt(II) and Pd(II)) chelates have a promising biological activity comparing to sodium barbitone parent free ligand against bacterial and fungal species.</span> </p>展开更多
Objective To investigate the expression of neuroprotective peptide [Gly14]-Humanin (HNG) in eukaryotic cells by gene engineering technique and analyze its biological activity. Methods By means of asymmetrical primer/t...Objective To investigate the expression of neuroprotective peptide [Gly14]-Humanin (HNG) in eukaryotic cells by gene engineering technique and analyze its biological activity. Methods By means of asymmetrical primer/template,double stranded cDNA of HNG with FLAG in its C-terminal was obtained,which was cloned into the plasmid pcDNA3.1(-),and the resultant recombinant vector pcDNA3.1(-)/HNG-FLAG was transfected into PC12 cells. At the same time,the recombinant vector pcDNA3.1(-)/EGFP was transfected to control the efficiency of transfection. The expression of HNG in the cells was determined by immunocytochemistry. In order to analyze the biological activity of the expressed HNG,25μM Aβ25-35 peptide was added to the culture medium of the transfected cells for 24h,then cell morphology,MTT assay and Hoechst 33258 staining were observed. Results The eukaryotic expression vector of pcDNA3.1(-)/HNG-FLAG was identified by enzyme digestion and sequencing. HNG was highly expressed in PC12 cells. After exposure of PC12 cells to 25μM Aβ25-35 for 24h,cell viability decreased to (65.8±5.3)%,and the dystrophic changes of neuritis and nuclei condensation were obvious. When cells were pre-transfected with pcDNA3.1(-)/HNG-FLAG,Aβ25-35-induced cell death and morphological changes of cells and nuclei were suppressed. In contrast,pre-transfected with empty vector did not protect cells from Aβ25-35-induced toxicity. Conclusion The eukaryotic expression vector for FLAG-tagged HNG was successfully constructed and expressed in PC12 cells. Expressed HNG has biological activity.展开更多
A derivative of Brevianamide F,(3 S,8 a R)-3-((1-allyl-1 H-3-indolyl)methyl)-hexahy-dropyrrolo[1,2-a]pyrazine-1,4-dione, was synthesized and characterized by 1 H NMR, 13 C NMR and confirmed by X-ray crystal structure ...A derivative of Brevianamide F,(3 S,8 a R)-3-((1-allyl-1 H-3-indolyl)methyl)-hexahy-dropyrrolo[1,2-a]pyrazine-1,4-dione, was synthesized and characterized by 1 H NMR, 13 C NMR and confirmed by X-ray crystal structure analysis. This compound crystallizes in orthorhombic system, space group P212121 with a = 9.59590(10), b = 12.70430(10), c = 14.5425(2)A, V = 1772.86(3)A^3, Z = 4, μ(CuK α) = 0.712 mm^-1, Dc = 1.279 g/cm^3, 16019 reflections measured(9.24°≤2θ≤147.28°), 3524 unique(Rint = 0.0309, Rsigma = 0.0175) which were used in all calculations. The final R = 0.0567(I > 2σ(I)) and wR = 0.1411(all data). The structure exhibits intermolecular hydrogen bonds typed O–H…O, leading to the formation of one-dimensional chains. The title compound was tested for inhibitory activity toward B-16, C6, RM-1 and BV-2 cancer cell lines.展开更多
SYP-260 is one of the novel pyrimidine structure chemicals.The biological activity of new compound SYP-260 was tested in this paper using different bioassay methods in the laboratory.Experimental results indicated tha...SYP-260 is one of the novel pyrimidine structure chemicals.The biological activity of new compound SYP-260 was tested in this paper using different bioassay methods in the laboratory.Experimental results indicated that the values of median lethal concentration(LC50,72 h)of new compound SYP-260 against broad bean aphid,green peach aphid and cotton aphid were 0.1708,0.2455 and 0.2632 mg·L-1,respectively.The LC50 of new compound SYP-260 was 0.8892 mg·L-1 against adult mite and the ovicidal activity of new compound SYP-260 was 0.7166 mg·L-1.The LC50 of new compound SYP-260 was 22.1991,71.6915,79.6149 and 42.5698 mg·L-1 against oriental armyworm,diamondback moth,corn borer and beet armyworm,respectively.And at the concentration of 50 mg·L-1,the bioassay result showed that new compound SYP-260 could be absorbed by host plant roots.The temperature bioassay result indicated that new compound SYP-260 was a positive temperature coefficient chemical.So new compound SYP-260 had excellent biological activity against nine different insect targets,such as broad bean aphid,green peach aphid and carmine spider mite.Moreover,this new compound had systemic action,too.Therefore,new compound SYP-260 had good bioactivity against many kinds of insect targets with novel chemical structures.展开更多
The fungitoxicity of five Malagasy essential oils (Eos)<span style="font-family:;" "=""> </span><span style="font-family:Verdana;">against</span><span styl...The fungitoxicity of five Malagasy essential oils (Eos)<span style="font-family:;" "=""> </span><span style="font-family:Verdana;">against</span><span style="font-family:;" "=""> </span><i><span style="font-family:Verdana;">Colletotrichum asianum</span></i><i><span style="font-family:;" "=""> </span></i><span style="font-family:Verdana;">was assessed in terms of conidial germination and mycelia</span><span style="font-family:Verdana;">l</span><span style="font-family:" color:red;"=""> </span><span style="font-family:Verdana;">growth. Their effect on defense-related compounds content, physicochemical properties</span><span style="font-family:;" "=""> </span><span style="font-family:Verdana;">and anthracnose lesions</span><span style="font-family:;" "=""> </span><span style="font-family:;" "=""><span style="font-family:Verdana;">in mango fruits was also determined. Four of the tested </span><span style="font-family:Verdana;">Eos w</span></span><span style="font-family:Verdana;">ere</span><span style="font-family:;" "=""><span style="font-family:Verdana;"> from </span><i><span style="font-family:Verdana;">Ravensara aromatica </span></i><span style="font-family:Verdana;">leaves,</span></span><span style="font-family:;" "=""> </span><span style="font-family:;" "=""><span style="font-family:Verdana;">and the last Eo was extracted from clove leaves. Their chemical compositions were then determined through GC-MS analysis and the active compound of the most fungitoxic Eo was determined by testing the toxicity of its major component to </span><i><span style="font-family:Verdana;">C</span></i><span style="font-family:Verdana;">.</span></span><i><span style="font-family:;" "=""> </span></i><i><span style="font-family:Verdana;">asianum</span></i><span style="font-family:Verdana;">s</span><span style="font-family:Verdana;"> s</span><span style="font-family:Verdana;">pore germination, mycelia</span><span style="font-family:Verdana;">l</span><span style="font-family:;" "=""><span style="font-family:Verdana;"> growth and its ability to inhibit anthracnose development on mango fruits. The </span><i><span style="font-family:Verdana;">R</span></i><span style="font-family:Verdana;">.</span><i><span style="font-family:Verdana;"> aromatica</span></i></span><i><span style="font-family:;" "=""> </span></i><span style="font-family:;" "=""><span style="font-family:Verdana;">Eos tested were fungistatic to </span><i><span style="font-family:Verdana;">C</span></i><span style="font-family:Verdana;">.</span><i><span style="font-family:Verdana;"> asianum</span></i><span style="font-family:Verdana;">,</span></span><i><span style="font-family:;" "=""> </span></i><span style="font-family:;" "=""><span style="font-family:Verdana;">whereas clove Eo was fungitoxic and the 4 chemotypes of </span><i><span style="font-family:Verdana;">R</span></i><span style="font-family:Verdana;">.</span><i><span style="font-family:Verdana;"> aromatica</span></i><span style="font-family:Verdana;"> Eo exhibited variable inhibiting capabilities: </span></span><span style="font-family:Verdana;">1</span><span style="font-family:Verdana;">)</span><span style="font-family:;" "=""> </span><span style="font-family:Verdana;">all tested doses of all Eos</span><span style="font-family:;" "=""> </span><span style="font-family:Verdana;">(112.5 and 225</span><span style="font-family:;" "=""> </span><span style="font-family:Verdana;">μL/L of air) were effective against</span><span style="font-family:;" "=""> </span><i><span style="font-family:Verdana;">C</span></i><span style="font-family:;" "=""><span style="font-family:Verdana;">.</span><i><span style="font-family:Verdana;"> asianum </span></i><span style="font-family:Verdana;">mycelial growth (10</span></span><span style="font-family:Verdana;">% </span><span style="font-family:Verdana;">-</span><span style="font-family:;" "=""> </span><span style="font-family:Verdana;">100% inhibition) but doses of 225</span><span style="font-family:;" "=""> </span><span style="font-family:Verdana;">μL/L were more inhibitory than those of</span><span style="font-family:;" "=""> </span><span style="font-family:Verdana;">112.5</span><span style="font-family:;" "=""> </span><span style="font-family:Verdana;">μL/L, </span><span style="font-family:Verdana;">2</span><span style="font-family:Verdana;">) Conidial germination was more resistant to Eos toxicity since only 225</span><span style="font-family:;" "=""> </span><span style="font-family:Verdana;">μL/L of methyl eugenol</span><span style="font-family:;" "=""> </span><span style="font-family:;" "=""><span style="font-family:Verdana;">chemotype of </span><i><span style="font-family:Verdana;">R</span></i><span style="font-family:Verdana;">.</span><i><span style="font-family:Verdana;"> aromatica</span></i></span><i><span style="font-family:;" "=""> </span></i><span style="font-family:Verdana;">Eo, all tested doses of the sabinene</span><span style="font-family:;" "=""> </span><span style="font-family:;" "=""><span style="font-family:Verdana;">chemotype of </span><i><span style="font-family:Verdana;">R</span></i><span style="font-family:Verdana;">.</span><i><span style="font-family:Verdana;"> aromatica</span></i></span><i><span style="font-family:;" "=""> </span></i><span style="font-family:Verdana;">Eo and</span><span style="font-family:;" "=""> </span><span style="font-family:;" "=""><span style="font-family:Verdana;">clove Eo were found inhibitory toward conidial germination of </span><i><span style="font-family:Verdana;">C</span></i><span style="font-family:Verdana;">.</span><i> <span style="font-family:Verdana;">asianum</span></i><span style="font-family:Verdana;">.</span></span><i><span style="font-family:;" "=""> </span></i><span style="font-family:Verdana;">30</span><span style="font-family:;" "=""> </span><span style="font-family:Verdana;">μL/L of sprayed clove Eoweretested on inoculated mangoes and were found to be effective against anthracnose development</span><span style="font-family:;" "=""> </span><span style="font-family:;" "=""><span style="font-family:Verdana;">without affecting the resorcinol content in mango peel and the physicochemical properties of mango pulp. Tests on the major components of clove Eo showed fungitoxic activities against mycelial growth and conidial germination of </span><i><span style="font-family:Verdana;">C</span></i><span style="font-family:Verdana;">.</span><i><span style="font-family:Verdana;"> asianum</span></i></span><i><span style="font-family:;" "=""> </span></i><span style="font-family:Verdana;">similar to those of</span><span style="font-family:;" "=""> </span><span style="font-family:Verdana;">clove Eo.</span>展开更多
Binary orotic acid metal complexes of Fe(III), Co(II), Ni(II), Cu(II), Zn(II), Cd(II), Hg(II), and two mixed metals complexes of (Co(II), Ni(II)) and (Ni(II), Cu(II)) were synthesized and characterized by elemental an...Binary orotic acid metal complexes of Fe(III), Co(II), Ni(II), Cu(II), Zn(II), Cd(II), Hg(II), and two mixed metals complexes of (Co(II), Ni(II)) and (Ni(II), Cu(II)) were synthesized and characterized by elemental analysis, IR, electronic spectra, magnetic susceptibility, and ESR spectra. The Analysis proved that the ligand has different coordination modes and the complexes were of octahedral, tetrahedral, and trigonal bipyramidal geometries. Molecular modeling techniques and quantum chemical methods have been performed for orotic acid to calculate charges, bond lengths, bond angles, dihedral angles, electronegativity (χ), chemical potential (μ), global hardness (η), softness (σ) and the electrophilicity index (ω). The thermal decomposition of the complexes was monitored by TGA, DTA, and DSC techniques under the N2 atmosphere. The thermal decomposition mechanisms of the complexes were suggested. The biological activity of orotic acid and some of the complexes are tested against antibacterial and antifungal organisms.展开更多
Computer analysis of N-(β-D-galactopyranosyl)-thiosemicarbazide compounds by in silico method revealed high probability of antibacterial (antimycobacterial), anti-tuberculosis (antituberculosic), antiviral (Influenza...Computer analysis of N-(β-D-galactopyranosyl)-thiosemicarbazide compounds by in silico method revealed high probability of antibacterial (antimycobacterial), anti-tuberculosis (antituberculosic), antiviral (Influenza), antitumor (antineoplastic) 9 > Pa > 0.5 and with a low probability of cytotoxic/cytostatic (cytostatic/cytotoxic) activities. An experimental study by in vitro and in vivo methods allowed us to conclude that studied new synthetic compound N-(β-D-galactopyranosyl)-thiosemicarbazide in the studied concentrations has a pronounced bactericidal and bacteriostatic effects.展开更多
Schiff<sup> </sup>base synthesis is usually acid catalyzed and it usually requires refluxing the mixture of aldehydes and amine in ethanolic solution. Synthesis and characterization of Schiff base ligands ...Schiff<sup> </sup>base synthesis is usually acid catalyzed and it usually requires refluxing the mixture of aldehydes and amine in ethanolic solution. Synthesis and characterization of Schiff base ligands derived from substituted amine and salicylaldehyde and their complexes (Cu<sup>2+</sup>, Co<sup>2+</sup>) are reported. The ligands and ligand-complexes were characterized by melting point, FTIR, CHN-elemental analysis and UV-Visible analysis. The UV-Visible and elemental analysis of complexes established (1:2) mole ratio (M:L). The stability constant and thermodynamic parameters (K, ΔG, ΔH, ΔS) were determined at different temperature (30 - 40)°C which established that the metal-complexes were very stable. The review describes the promising biological<sup> </sup>activities of Schiff base and their metal complexes.展开更多
A 3-Dimension-Quantitative Structure-Activity Relationship</span></span><span><span><span style="font-family:""> (</span></span></span><span><spa...A 3-Dimension-Quantitative Structure-Activity Relationship</span></span><span><span><span style="font-family:""> (</span></span></span><span><span><span style="font-family:"">3D-QSAR</span></span></span><span><span><sup><span style="font-family:"">1</span></sup></span></span><span><span><span style="font-family:"">) </span></span></span><span><span><span style="font-family:"">approach is applied for the prediction of accurate chemical</span></span></span><span><span><span style="font-family:""> products made from biological activity and toxicity. Quantum chemical technique allows the construction of the molecular descriptors. The molecular quantum descriptors are classified into five principal component factors. Various linear <span>regression equations are obtained using the statistical technique. In this</span> study, the researchers propose the three best regression equations based on quantum molecular descriptors discussed earlier in this study. The observed EC50 vs calculated EC50 is plotted using the best fitting with the quantum descriptors.展开更多
Hepatocyte growth factor (HGF) is a renotropic, antifibrotic and regenerative factor with cytoprotective effects that is produced by mesenchymal cells and shows high affinity to components of extra cellular matrix, su...Hepatocyte growth factor (HGF) is a renotropic, antifibrotic and regenerative factor with cytoprotective effects that is produced by mesenchymal cells and shows high affinity to components of extra cellular matrix, such as heparan sulphate proteoglycan (HS-PG), in healthy. Patients with chronic renal failure (CRF) suffer from a chronic inflammatory disorder. In order to assess the underlying mechanisms for development of CRF we aimed to assess the amounts and affinity of HGF in this patient group. Elisa, western blot and surface plasmon resonance (SPR) were used to study HGF in blood samples, as well as in isolated neutrophils, in CRF patients compared to healthy controls. Patients with CRF showed higher HGF levels in serum (P P < 0.0001), compared to healthy controls. Addition of protease inhibitors decreased the difference between patients with CRF compared to healthy individuals. HGF with potent regenerative function during injury lacks affinity to HSPG in patients with CRF that may depend on production of proteases from activated immune cells. This information might be used to highlight underlying mechanisms for chronicity and leading to new strategies for treatment of chronic injuries.展开更多
BACKGROUND: The proliferation and metastasis of cancers depend on angiogenesis. This property provides the feasibility for the treatment of cancer by inhibition of angiogenesis, and many angiogenic inhibitors have bee...BACKGROUND: The proliferation and metastasis of cancers depend on angiogenesis. This property provides the feasibility for the treatment of cancer by inhibition of angiogenesis, and many angiogenic inhibitors have been demonstrated to effectively inhibit angiogenesis and consequently the growth of solid cancer. As for the newly identified angiogenesis inhibitor, arresten, some studies have found its high activity on restrainting tumor vessel. This study was to assess the anti-angiogenic activity of arresten. METHODS: The arresten gene was obtained from a healthy puerpera’s placenta tissue by the reverse transcriptase-polymerase chain reaction （RT-PCR） method, and molecular cloning to prokaryotic expression plasmid pBV220 by recombination strategy. The prokaryotic expression plasmid pBV220/arr was identified by restriction enzyme digestion and sequenced. The pBV220/arr was transformed into E. coli JM109, DH5α, BL21 and BL21 （DE3） by the CaCl<sub>2</sub> transformation method. The arresten expression level was detected by SDS-PAGE. The expressed product was purlfled, re-naturalized and detected for its biological activity of inhibiting the angiogenesis of chorioallantoic membrane （CAM）. RESULTS: The arresten gene was cloned and pBV220/arr was constructed. The arresten expression level of protein was highly increased after pBV220/arr was transformed into E. coli BL21 （DE3）. SDS-PAGE showed that the expressed arresten proteins were mainly inclusion bodies and had a molecular weight of 26 kDa. The expressed arresten protein showed evident biological activities. CONCLUSIONS: The successful construction of recombinant plasmid pBV220/arr and the effective expression in E. coil have laid a foundation for further study of its anti-angiogenic function and may pave the way for future antitumor application.展开更多
基金Project supported by the Key Projects of National Natural Science Foundation of China(No.11932010)。
文摘Explaining the mechanism of the cochlear active phonosensitive amplification has been a major problem in medicine.The basilar membrane(BM)is the key infrastructure.In 1960,Nobel Laureate von B′ek′esy first discovered BM's traveling wave motion.Since that time,BM's models only have considered the traveling wave but not the biological activity.Therefore,a new model considering changes of BM's stiffness in space and time is established based on the immersed boundary method to describe its biological activity.It not only reproduces the results of traveling wave motion but also explains the mechanization on the generation of traveling wave.An important discovery is that changes of BM's stiffness in space and time will cause the unstable global resonance,which will induce amplification of sounds in cochlea.An important inference is that biological activity shall be included in the application of mechanical principles to the analysis of life,which is the essential difference between biomechanics and general mechanics.
基金Supported by Changsha Science and Technology Program (kh2101007).
文摘Citral is a monoterpene aldehyde,which is the main chemical component of essential oils from Litsea cubeba and Cymbopogon citratus,as well as one of the most important representatives of open-chain monoterpene compounds.The lemon flavor released by citral is very strong,and thus,it is widely used in essence,spices,manufacturing of various foods and beauty and other industries.It has antibacterial,anti-inflammatory,antioxidant,anti-tumor,insecticidal and other biological activity.This paper reviewed citral in Lauraceae plants and its biological activity,in order to provide reference for the development and utilization of citral in Lauraceae plants and its diversified applications.
基金Supported by National Natural Science Foundation of China (82360716).
文摘Lentinula edodes is the second largest edible mushroom in the world and is widely used as food and medicine.Modern research shows that lentinan(LNT)is the main active component of L.edodes.It has anti-cancer,treatment of diabetes,intestinal protection,anti-inflammatory,anti-oxidation,anti-aging,hepatoprotective,immune-regulating effects.In this review,the biological activity,action mechanism and structure-activity relationship of LNT in recent years are reviewed.On this basis,the existing problems were discussed,and the future research and application of LNT were prospected.Finally,it is hoped that this review will promote the in-depth study of LNT and provide a reference for its development as a drug and functional food.
文摘The compounds have been synthesized and characterized by routine MS, IR and NMR spectrometry methods. The compounds are all active on bacterial strains with the exception of Salmonella typhimirium, with a MIC value of 7.5 mg/mL. They show a percentage of anti-radical activity of 75.476 ± 5.070 for the compound DAN-S and of 68.142 ± 6.539 for the compound DAN-OV. The compounds are sensitive to the two champions used. DAN-S compound is then the most active.
基金The research was funded by the 2020 Shenzhen International Scientific and Technological Cooperation R&D Project(No.GJHZ20190823111601682)the Natural Science Foundation of Guangdong Province(No.2020A 1515011075)+2 种基金It was supported by the Special Funds for the‘Cultivation of Guangdong College Students’Scientific and Technological Innovation(‘Climbing Program’Special Funds No.pdjh2022a0232)The study also was funded by the Postgraduate Education Innovation Project of Guangdong Ocean University(No.2021148)Innovative Training Program for College Students of Guangdong Ocean University(No.S202210566067)。
文摘DAPTMGY(DTY)is an oligopeptide derived from marine microalgae with proven potential to combat oxidative stress in previous research.The composition,ordering,and active sites of amino acids play a key role in activity studies and are also the research trends in recent years.As an oligopeptide with a molecular weight of less than 1000 Da,DTY is of great significance to explore the active site and structure-activity relationship.This study used quantum mechanics to optimize DTY’s structure and predict the active site through molecular orbits,energy,and charge.In addition,an LPS-treated HUVEC cell was established as an oxidative-stress model.DTY could reduce mitochondrial oxidative stress and inhibit ROS production by enhancing the antioxidant enzymes SOD,GPX,and HO-1.Moreover,it was confirmed to inhibit inflammation and apoptosis through the NF-κB and MAPK signaling pathways.Lastly,the correlation of the oligopeptide DTY’s active site and antioxidative-stress activity was verified by molecular docking,showing that hydrogen bonding is the main force,which was also the main factor for antioxidant activity.
基金Supported by Central Government Supports Local College Reform and Development Fund Talent Training Projects(2020GSP16)。
文摘Daphnoretin,belonging to coumarin compounds,is the main active ingredient of Wikstroemia indica,and has anti-inflammatory,anti-depression,anti-tumor and other pharmacological activities.This article reviews the extraction and purification process,content determination methods and pharmacological activity of daphnoretin,in order to provide a theoretical reference for optimization of purification process,improvement of content determination technique and further clinical application of daphnoretin.
基金Supported by the Youth National Natural Science Foundation of China(No.21373132,21603133)Basic science research project of Shaanxi Province(No.2015JM2060)+2 种基金the local special projects of education department of Shaanxi province 15JF013)the projects of social science and technology development of Shaanxi provincial science and Technology Department(2015SF270)the project of Shaanxi University of technology(SLGQD2017-14)
文摘The title compound N-(1-(2,4-dichlorophenyl)-1 H-pyrazolo[3,4-d]pyrimidin-4-yl)-4-(N,N-dipropylsulfamoyl)benzamide was synthesized by the condensation of 4-(dipropylsulfamoyl)benzoic acid with 1-(2,4-dichlorophenyl)-1 H-pyrazolo[3,4-d]pyrimidin-4-amine. This intermediate was prepared from 5-amino-1-(2,4-dichlorophenyl)-1 H-pyrazole-4-carbonitrile by the condensation with triethyl orthoformate and then cyclisation with ammonium hydroxide solution in tetrahydrofuran at room temperature. The crystal structure of the title compound was determined. The optimized geometric bond lengths and bond angles obtained by using density functional theory(DFT) have been compared with X-ray diffraction values. In addition, the preliminary biological test showed that the compound possesses distinct effective inhibition on the proliferation of some cancer cell lines.
文摘In the modern science, priority is given for the search of biological active compounds with specific properties. As a result of experimental data, it was found that in the reaction between N-(<em>β</em>-D-glycopyranosyl)-semicarbazide and the Lawesson reagent (2,4-bis(p-methoxyphenyl)-1,3-dithiadiphosphetane 2,4-disulfide) at the ratio 1:1 in pyridine when boiling under reflux in a water bath for 20 - 35 minutes, a new synthetic compound N-(<em>β</em>-D-glycopyranosyl)-thiosemicarbazide is formed. The individuality and structure of the target products were confirmed by 13C NMR spectroscopy, 1H NMR spectroscopy, IR spectroscopy, and elemental analysis. For the synthesized new compounds of N-(<em>β</em>-D-glycopyranosyl)-thiosemicarbazides, the probability of pharmacological and toxic effects were predicted by the computer method in silico. From the synthesized compounds N-(<em>β</em>-D-galactopyranosyl)-thiosemicarbazide, the probability of antibacterial (antibacterial) activity is predicted (<em>Pa</em>/<em>Pi</em> 0.544/0.013). The antibacterial activity of the compound (4) was confirmed in a test for salmonella infection of lambs, salmonellosis of calves, and colipathogenic E. coli serotypes. An experimental study by the in vitro method made it possible to conclude that the new synthetic compound N-(<em>β</em>-D-galactopyranosyl)-thiosemicarbazide in the studied concentrations has a pronounced bactericidal and bacteriostatic effect. The synthetic new compound N-(<em>β</em>-D-glyco- pyranosyl)-thiosemicarbazide is a promising compound for further study.
文摘<p> <span style="font-family:Verdana;">This work aims to characterize, synthesize and evaluate the biological activity of sodium barbitone and their metal chelates Ni(II), Pd(II) and Pt(II). The new synthesized metal chelates are investigated by elemental analysis, IR, mass spectra, thermal analysis and biological activity. Square planer structure of the prepared complexes obtained from the result of analysis. The antibacterial and antifungal of sodium barbitone ligand and its conforming metal chelates were screened against bacterial species Gram positive (<em>Staphylococcus aureus</em>), Gram negative bacteria (<em>Escherichia coli</em>) and fungi <em>Aspergillus flavus</em> and <em>Candida albicans</em> fungi. Ampicillin and amphotericin were used as references for antibacterial and antifungal studies. The activity data show that the plati</span><span style="font-family:Verdana;">num group metals chelates have activity data show that some of the platinum group metals (viz. Pt(II) and Pd(II)) chelates have a promising biological activity comparing to sodium barbitone parent free ligand against bacterial and fungal species.</span> </p>
基金supported by Youth Foundation of Medical School of Xi an Jiaotong University (No.YQNO8O7)
文摘Objective To investigate the expression of neuroprotective peptide [Gly14]-Humanin (HNG) in eukaryotic cells by gene engineering technique and analyze its biological activity. Methods By means of asymmetrical primer/template,double stranded cDNA of HNG with FLAG in its C-terminal was obtained,which was cloned into the plasmid pcDNA3.1(-),and the resultant recombinant vector pcDNA3.1(-)/HNG-FLAG was transfected into PC12 cells. At the same time,the recombinant vector pcDNA3.1(-)/EGFP was transfected to control the efficiency of transfection. The expression of HNG in the cells was determined by immunocytochemistry. In order to analyze the biological activity of the expressed HNG,25μM Aβ25-35 peptide was added to the culture medium of the transfected cells for 24h,then cell morphology,MTT assay and Hoechst 33258 staining were observed. Results The eukaryotic expression vector of pcDNA3.1(-)/HNG-FLAG was identified by enzyme digestion and sequencing. HNG was highly expressed in PC12 cells. After exposure of PC12 cells to 25μM Aβ25-35 for 24h,cell viability decreased to (65.8±5.3)%,and the dystrophic changes of neuritis and nuclei condensation were obvious. When cells were pre-transfected with pcDNA3.1(-)/HNG-FLAG,Aβ25-35-induced cell death and morphological changes of cells and nuclei were suppressed. In contrast,pre-transfected with empty vector did not protect cells from Aβ25-35-induced toxicity. Conclusion The eukaryotic expression vector for FLAG-tagged HNG was successfully constructed and expressed in PC12 cells. Expressed HNG has biological activity.
基金financially sponsored by the Natural Science Foundation of Hebei Province(No.B2015208134)
文摘A derivative of Brevianamide F,(3 S,8 a R)-3-((1-allyl-1 H-3-indolyl)methyl)-hexahy-dropyrrolo[1,2-a]pyrazine-1,4-dione, was synthesized and characterized by 1 H NMR, 13 C NMR and confirmed by X-ray crystal structure analysis. This compound crystallizes in orthorhombic system, space group P212121 with a = 9.59590(10), b = 12.70430(10), c = 14.5425(2)A, V = 1772.86(3)A^3, Z = 4, μ(CuK α) = 0.712 mm^-1, Dc = 1.279 g/cm^3, 16019 reflections measured(9.24°≤2θ≤147.28°), 3524 unique(Rint = 0.0309, Rsigma = 0.0175) which were used in all calculations. The final R = 0.0567(I > 2σ(I)) and wR = 0.1411(all data). The structure exhibits intermolecular hydrogen bonds typed O–H…O, leading to the formation of one-dimensional chains. The title compound was tested for inhibitory activity toward B-16, C6, RM-1 and BV-2 cancer cell lines.
基金Supported by the Key Projects in the National Science&Technology Pillar Program During the 13th Five-Year Plan Period(2016YFD0300708)。
文摘SYP-260 is one of the novel pyrimidine structure chemicals.The biological activity of new compound SYP-260 was tested in this paper using different bioassay methods in the laboratory.Experimental results indicated that the values of median lethal concentration(LC50,72 h)of new compound SYP-260 against broad bean aphid,green peach aphid and cotton aphid were 0.1708,0.2455 and 0.2632 mg·L-1,respectively.The LC50 of new compound SYP-260 was 0.8892 mg·L-1 against adult mite and the ovicidal activity of new compound SYP-260 was 0.7166 mg·L-1.The LC50 of new compound SYP-260 was 22.1991,71.6915,79.6149 and 42.5698 mg·L-1 against oriental armyworm,diamondback moth,corn borer and beet armyworm,respectively.And at the concentration of 50 mg·L-1,the bioassay result showed that new compound SYP-260 could be absorbed by host plant roots.The temperature bioassay result indicated that new compound SYP-260 was a positive temperature coefficient chemical.So new compound SYP-260 had excellent biological activity against nine different insect targets,such as broad bean aphid,green peach aphid and carmine spider mite.Moreover,this new compound had systemic action,too.Therefore,new compound SYP-260 had good bioactivity against many kinds of insect targets with novel chemical structures.
文摘The fungitoxicity of five Malagasy essential oils (Eos)<span style="font-family:;" "=""> </span><span style="font-family:Verdana;">against</span><span style="font-family:;" "=""> </span><i><span style="font-family:Verdana;">Colletotrichum asianum</span></i><i><span style="font-family:;" "=""> </span></i><span style="font-family:Verdana;">was assessed in terms of conidial germination and mycelia</span><span style="font-family:Verdana;">l</span><span style="font-family:" color:red;"=""> </span><span style="font-family:Verdana;">growth. Their effect on defense-related compounds content, physicochemical properties</span><span style="font-family:;" "=""> </span><span style="font-family:Verdana;">and anthracnose lesions</span><span style="font-family:;" "=""> </span><span style="font-family:;" "=""><span style="font-family:Verdana;">in mango fruits was also determined. Four of the tested </span><span style="font-family:Verdana;">Eos w</span></span><span style="font-family:Verdana;">ere</span><span style="font-family:;" "=""><span style="font-family:Verdana;"> from </span><i><span style="font-family:Verdana;">Ravensara aromatica </span></i><span style="font-family:Verdana;">leaves,</span></span><span style="font-family:;" "=""> </span><span style="font-family:;" "=""><span style="font-family:Verdana;">and the last Eo was extracted from clove leaves. Their chemical compositions were then determined through GC-MS analysis and the active compound of the most fungitoxic Eo was determined by testing the toxicity of its major component to </span><i><span style="font-family:Verdana;">C</span></i><span style="font-family:Verdana;">.</span></span><i><span style="font-family:;" "=""> </span></i><i><span style="font-family:Verdana;">asianum</span></i><span style="font-family:Verdana;">s</span><span style="font-family:Verdana;"> s</span><span style="font-family:Verdana;">pore germination, mycelia</span><span style="font-family:Verdana;">l</span><span style="font-family:;" "=""><span style="font-family:Verdana;"> growth and its ability to inhibit anthracnose development on mango fruits. The </span><i><span style="font-family:Verdana;">R</span></i><span style="font-family:Verdana;">.</span><i><span style="font-family:Verdana;"> aromatica</span></i></span><i><span style="font-family:;" "=""> </span></i><span style="font-family:;" "=""><span style="font-family:Verdana;">Eos tested were fungistatic to </span><i><span style="font-family:Verdana;">C</span></i><span style="font-family:Verdana;">.</span><i><span style="font-family:Verdana;"> asianum</span></i><span style="font-family:Verdana;">,</span></span><i><span style="font-family:;" "=""> </span></i><span style="font-family:;" "=""><span style="font-family:Verdana;">whereas clove Eo was fungitoxic and the 4 chemotypes of </span><i><span style="font-family:Verdana;">R</span></i><span style="font-family:Verdana;">.</span><i><span style="font-family:Verdana;"> aromatica</span></i><span style="font-family:Verdana;"> Eo exhibited variable inhibiting capabilities: </span></span><span style="font-family:Verdana;">1</span><span style="font-family:Verdana;">)</span><span style="font-family:;" "=""> </span><span style="font-family:Verdana;">all tested doses of all Eos</span><span style="font-family:;" "=""> </span><span style="font-family:Verdana;">(112.5 and 225</span><span style="font-family:;" "=""> </span><span style="font-family:Verdana;">μL/L of air) were effective against</span><span style="font-family:;" "=""> </span><i><span style="font-family:Verdana;">C</span></i><span style="font-family:;" "=""><span style="font-family:Verdana;">.</span><i><span style="font-family:Verdana;"> asianum </span></i><span style="font-family:Verdana;">mycelial growth (10</span></span><span style="font-family:Verdana;">% </span><span style="font-family:Verdana;">-</span><span style="font-family:;" "=""> </span><span style="font-family:Verdana;">100% inhibition) but doses of 225</span><span style="font-family:;" "=""> </span><span style="font-family:Verdana;">μL/L were more inhibitory than those of</span><span style="font-family:;" "=""> </span><span style="font-family:Verdana;">112.5</span><span style="font-family:;" "=""> </span><span style="font-family:Verdana;">μL/L, </span><span style="font-family:Verdana;">2</span><span style="font-family:Verdana;">) Conidial germination was more resistant to Eos toxicity since only 225</span><span style="font-family:;" "=""> </span><span style="font-family:Verdana;">μL/L of methyl eugenol</span><span style="font-family:;" "=""> </span><span style="font-family:;" "=""><span style="font-family:Verdana;">chemotype of </span><i><span style="font-family:Verdana;">R</span></i><span style="font-family:Verdana;">.</span><i><span style="font-family:Verdana;"> aromatica</span></i></span><i><span style="font-family:;" "=""> </span></i><span style="font-family:Verdana;">Eo, all tested doses of the sabinene</span><span style="font-family:;" "=""> </span><span style="font-family:;" "=""><span style="font-family:Verdana;">chemotype of </span><i><span style="font-family:Verdana;">R</span></i><span style="font-family:Verdana;">.</span><i><span style="font-family:Verdana;"> aromatica</span></i></span><i><span style="font-family:;" "=""> </span></i><span style="font-family:Verdana;">Eo and</span><span style="font-family:;" "=""> </span><span style="font-family:;" "=""><span style="font-family:Verdana;">clove Eo were found inhibitory toward conidial germination of </span><i><span style="font-family:Verdana;">C</span></i><span style="font-family:Verdana;">.</span><i> <span style="font-family:Verdana;">asianum</span></i><span style="font-family:Verdana;">.</span></span><i><span style="font-family:;" "=""> </span></i><span style="font-family:Verdana;">30</span><span style="font-family:;" "=""> </span><span style="font-family:Verdana;">μL/L of sprayed clove Eoweretested on inoculated mangoes and were found to be effective against anthracnose development</span><span style="font-family:;" "=""> </span><span style="font-family:;" "=""><span style="font-family:Verdana;">without affecting the resorcinol content in mango peel and the physicochemical properties of mango pulp. Tests on the major components of clove Eo showed fungitoxic activities against mycelial growth and conidial germination of </span><i><span style="font-family:Verdana;">C</span></i><span style="font-family:Verdana;">.</span><i><span style="font-family:Verdana;"> asianum</span></i></span><i><span style="font-family:;" "=""> </span></i><span style="font-family:Verdana;">similar to those of</span><span style="font-family:;" "=""> </span><span style="font-family:Verdana;">clove Eo.</span>
文摘Binary orotic acid metal complexes of Fe(III), Co(II), Ni(II), Cu(II), Zn(II), Cd(II), Hg(II), and two mixed metals complexes of (Co(II), Ni(II)) and (Ni(II), Cu(II)) were synthesized and characterized by elemental analysis, IR, electronic spectra, magnetic susceptibility, and ESR spectra. The Analysis proved that the ligand has different coordination modes and the complexes were of octahedral, tetrahedral, and trigonal bipyramidal geometries. Molecular modeling techniques and quantum chemical methods have been performed for orotic acid to calculate charges, bond lengths, bond angles, dihedral angles, electronegativity (χ), chemical potential (μ), global hardness (η), softness (σ) and the electrophilicity index (ω). The thermal decomposition of the complexes was monitored by TGA, DTA, and DSC techniques under the N2 atmosphere. The thermal decomposition mechanisms of the complexes were suggested. The biological activity of orotic acid and some of the complexes are tested against antibacterial and antifungal organisms.
文摘Computer analysis of N-(β-D-galactopyranosyl)-thiosemicarbazide compounds by in silico method revealed high probability of antibacterial (antimycobacterial), anti-tuberculosis (antituberculosic), antiviral (Influenza), antitumor (antineoplastic) 9 > Pa > 0.5 and with a low probability of cytotoxic/cytostatic (cytostatic/cytotoxic) activities. An experimental study by in vitro and in vivo methods allowed us to conclude that studied new synthetic compound N-(β-D-galactopyranosyl)-thiosemicarbazide in the studied concentrations has a pronounced bactericidal and bacteriostatic effects.
文摘Schiff<sup> </sup>base synthesis is usually acid catalyzed and it usually requires refluxing the mixture of aldehydes and amine in ethanolic solution. Synthesis and characterization of Schiff base ligands derived from substituted amine and salicylaldehyde and their complexes (Cu<sup>2+</sup>, Co<sup>2+</sup>) are reported. The ligands and ligand-complexes were characterized by melting point, FTIR, CHN-elemental analysis and UV-Visible analysis. The UV-Visible and elemental analysis of complexes established (1:2) mole ratio (M:L). The stability constant and thermodynamic parameters (K, ΔG, ΔH, ΔS) were determined at different temperature (30 - 40)°C which established that the metal-complexes were very stable. The review describes the promising biological<sup> </sup>activities of Schiff base and their metal complexes.
文摘A 3-Dimension-Quantitative Structure-Activity Relationship</span></span><span><span><span style="font-family:""> (</span></span></span><span><span><span style="font-family:"">3D-QSAR</span></span></span><span><span><sup><span style="font-family:"">1</span></sup></span></span><span><span><span style="font-family:"">) </span></span></span><span><span><span style="font-family:"">approach is applied for the prediction of accurate chemical</span></span></span><span><span><span style="font-family:""> products made from biological activity and toxicity. Quantum chemical technique allows the construction of the molecular descriptors. The molecular quantum descriptors are classified into five principal component factors. Various linear <span>regression equations are obtained using the statistical technique. In this</span> study, the researchers propose the three best regression equations based on quantum molecular descriptors discussed earlier in this study. The observed EC50 vs calculated EC50 is plotted using the best fitting with the quantum descriptors.
文摘Hepatocyte growth factor (HGF) is a renotropic, antifibrotic and regenerative factor with cytoprotective effects that is produced by mesenchymal cells and shows high affinity to components of extra cellular matrix, such as heparan sulphate proteoglycan (HS-PG), in healthy. Patients with chronic renal failure (CRF) suffer from a chronic inflammatory disorder. In order to assess the underlying mechanisms for development of CRF we aimed to assess the amounts and affinity of HGF in this patient group. Elisa, western blot and surface plasmon resonance (SPR) were used to study HGF in blood samples, as well as in isolated neutrophils, in CRF patients compared to healthy controls. Patients with CRF showed higher HGF levels in serum (P P < 0.0001), compared to healthy controls. Addition of protease inhibitors decreased the difference between patients with CRF compared to healthy individuals. HGF with potent regenerative function during injury lacks affinity to HSPG in patients with CRF that may depend on production of proteases from activated immune cells. This information might be used to highlight underlying mechanisms for chronicity and leading to new strategies for treatment of chronic injuries.
基金This work was supported by a grant from Science and Technology Fund of Shanxi Province, China (No. 042082).
文摘BACKGROUND: The proliferation and metastasis of cancers depend on angiogenesis. This property provides the feasibility for the treatment of cancer by inhibition of angiogenesis, and many angiogenic inhibitors have been demonstrated to effectively inhibit angiogenesis and consequently the growth of solid cancer. As for the newly identified angiogenesis inhibitor, arresten, some studies have found its high activity on restrainting tumor vessel. This study was to assess the anti-angiogenic activity of arresten. METHODS: The arresten gene was obtained from a healthy puerpera’s placenta tissue by the reverse transcriptase-polymerase chain reaction （RT-PCR） method, and molecular cloning to prokaryotic expression plasmid pBV220 by recombination strategy. The prokaryotic expression plasmid pBV220/arr was identified by restriction enzyme digestion and sequenced. The pBV220/arr was transformed into E. coli JM109, DH5α, BL21 and BL21 （DE3） by the CaCl<sub>2</sub> transformation method. The arresten expression level was detected by SDS-PAGE. The expressed product was purlfled, re-naturalized and detected for its biological activity of inhibiting the angiogenesis of chorioallantoic membrane （CAM）. RESULTS: The arresten gene was cloned and pBV220/arr was constructed. The arresten expression level of protein was highly increased after pBV220/arr was transformed into E. coli BL21 （DE3）. SDS-PAGE showed that the expressed arresten proteins were mainly inclusion bodies and had a molecular weight of 26 kDa. The expressed arresten protein showed evident biological activities. CONCLUSIONS: The successful construction of recombinant plasmid pBV220/arr and the effective expression in E. coil have laid a foundation for further study of its anti-angiogenic function and may pave the way for future antitumor application.
