Aspirin ; administration & dosage ; therapeutic use ; Blood Cell Count ; Blood Platelets ; drug effects ; physiology ; C-Reactive Protein ; analysis ; Child, Preschool ; Diagnosis, Differential ; Female ; Humans ; Hydroxyurea ; administration & dosage ; therapeutic use ; Interferons ; administration & dosage ; therapeutic use ; Platelet Count ; Thrombocythemia, Essential ; blood ; diagnosis ; therapy

Adult ; Aged ; Carcinoma, Squamous Cell ; metabolism ; pathology ; Female ; Fibroblast Growth Factor 2 ; metabolism ; Humans ; Laryngeal Neoplasms ; metabolism ; pathology ; Male ; Middle Aged ; Neoplasm Staging ; Receptors, Fibroblast Growth Factor ; metabolism

Objective Research the correlation between expression of MMP-2 in colorectal cancer and patho- logical factors,or biological behaviors in colorectal cancer.Methods The expression of MMP-2 in 68 cases with col- orectal cancer were detected by immunohistochemical staining.Results The expression of MMP-2 in colorectal can- cer was not correlated with tumor region and histologic type,but related with depth of tumor invasion and metasta- sis.The frequency of positive cases in patients with colorectal cancer with of lymph,node metastasis was significantly higher than that in patients without lymph node metastasis(P

The aim of this study was to investigate and evaluate the antitumor effects of a novel poly(ADP-ribose) polymerase (PARP) 1/2 inhibitor, YHP-836, in combination with temozolomide (TMZ) for the treatment of glioblastoma (GBM). The cytotoxicity of YHP-836 was tested alone or in combination with TMZ using MTT assay. Immunoblotting and flow cytometry were also employed to assess the combination activity of YHP-836 and TMZ in multiply GBM cell lines. Further, the antitumor activity of YHP-836 and TMZ was evaluated using subcutaneous and orthotopic mice xenograft tumor models. All procedures were approved by the Ethics Committee for Animal Experiments of the Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College and conducted under the Guidelines for Animal Experiments of Peking Union Medical College. The approval number is 00009138. It was demonstrated that the combination of YHP-836 and TMZ increased the cytotoxicity against GBM cells and upregulated histone H2AX phosphorylation (γH2AX) expression levels compared to TMZ treatment alone. The combination also led to the S-phase cell cycle arrest. Moreover, YHP-836 significantly enhanced TMZ antitumor effects without significantly increasing chemotherapy drug toxicity in vivo, whereas YHP-836 alone showed limited therapeutic efficacy against GBM. In conclusion, the novel PARP1/2 inhibitor, YHP-836, sensitizes TMZ and provides a basis for further investigation into its mechanism of action. These findings suggest that YHP-836 may be a potential candidate for combination therapy with TMZ in patients with TMZ resistance.

Objective To explore the effects of early interventions on growth associated protein-43(GAP-43) and neuron apoptosis in brain of neonatal rats.Methods According to matched-pairs design,30 rats from the same materal rats were divided into two groups:intervention group and control group randomly.The intervention group received the neonatal handling for 14 d and then were kept in an enriched environment for another 14 d.The expression of GAP-43 and the number of neurons apoptosis were detected by immunohistochemistry and TUNEL staining respectively in forehead cortex and hippocampus of rats.The brain functional outcomes of rats were evaluated by water-maze test.Results In prefrontal cortex and hippocampus,the level of GAP-43 immuno-positive response in intervention group was significantly higher than that of control group(P

PARP [poly(ADP-ribose)polymerase] represents a novel potential target in cancer therapy. It is involved in a DNA repair process by catalyzing the transfer of ADP-ribose units from NAD to a number of its substrate proteins. In this work, a series of novel azaindole derivatives was designed and synthesized. Moreover, 16 target molecules were screened and 8 compounds displayed inhibitory activity against PARP-1. It has been demonstrated that these azaindoles bearing cycloamine substituents at 2-position were active to both PARP-1 and PARP-2.
Antineoplastic Agents ; chemical synthesis ; chemistry ; pharmacology ; Aza Compounds ; chemical synthesis ; chemistry ; pharmacology ; Indoles ; chemical synthesis ; chemistry ; pharmacology ; Poly (ADP-Ribose) Polymerase-1 ; Poly(ADP-ribose) Polymerases ; metabolism

OBJECTIVETo study clinical value of shear wave elastography (SWE) in the evaluation of neck-shoulder myofascial pain syndrome.

METHODSFrom December 2013 to July 2014,30 patients diagnosed as neck-shoulder myofascial pain syndrome were in the treatment group,including 17 males and 13 females, with an average age of (44 ± 3) years old. Thirty healthy people were in the control group, including 22 males and 8 females, with a mean age of (37 ± 5) years old. The patients in the treatment group were treated with manipulation, once every other day, total 7 times. The SWE was used to detect tension part of trapezius muscle of patients in the treatment group before and after treatment, as well as to detect muscle belly at the descending part of trapezius muscle in the control group. The tissue elasticity and Yang's modulus value were recorded and compared.

RESULTSThe tissue elasticity chart of patients in the treatment group before treatment was mainly greenish blue with the score of 3.70 ± 1.53, and the Yang's modulus was (43.4 ± 15.6) kPa. The tissue elasticity figure after treatment was mainly blue with the score of 2.40 ± 0.87, and the Yang's modulus was (29.0 ± 5.9) kPa. Whereas in the control group, the tissue elasticity figure was mainly blue with the score of 1.60 ± 0.72, and the Yang's modulus was (24.0 ± 7.6) kPa. These were statistical differences between the two groups (P = 0.000).

CONCLUSIONSWE can be used as an evaluation method of manipulation treatment for neck-shoulder myofascial pain syndrome, which is an objective and sensitive detection method.

Adult ; Elasticity Imaging Techniques ; methods ; Female ; Humans ; Male ; Middle Aged ; Musculoskeletal Manipulations ; Myofascial Pain Syndromes ; diagnosis ; therapy ; Neck ; Shoulder

Poly(ADP-ribose) polymerase-1 (PARP-1) has emerged as a promising anticancer drug target due to its key role in the DNA repair process. It can polymerize ADP-ribose units on its substrate proteins which are involved in the regulation of DNA repair. In this work, a novel series of para-substituted 1-benzyl-quinazoline-2, 4 (1H, 3H)-diones was designed and synthesized, and the inhibitory activities against PARP-1 of compounds 7a-7e, 8a-8f, 9a-9c and 10a-10c were evaluated. Of all the tested compounds, nine compounds displayed inhibitory activities with IC50 values ranging from 4.6 to 39.2 micromol x L(-1). In order to predict the binding modes of the potent molecules, molecular docking was performed using CDOCKER algorithm, and that will facilitate to further develop more potent PARP-1 inhibitors with a quinazolinedione scaffold.
Antineoplastic Agents ; chemical synthesis ; chemistry ; pharmacology ; Drug Design ; Enzyme Inhibitors ; chemical synthesis ; chemistry ; pharmacology ; Molecular Docking Simulation ; Molecular Structure ; Poly (ADP-Ribose) Polymerase-1 ; Poly(ADP-ribose) Polymerases ; Quinazolinones ; chemical synthesis ; chemistry ; pharmacology ; Structure-Activity Relationship

Poly(ADP-ribose)polymerase-1 (PARP-1) plays a significant role in the DNA repair process by catalyzing the transfer of ADP-ribose from NAD+ to its receptors. It is a promising anticancer drug target and many PARP-1 inhibitors have been developed and used in the clinical trial. In this work, a series of 3-(2-oxo-2-substituted acetamido)benzamides have been synthesized and their inhibitory activities against PARP-1 were evaluated. Of all the tested compounds, six compounds displayed inhibitory activities with IC50 values ranging from 0.23 to 5.78 µmol.L-1 . The binding pose of compound 5a was predicted using molecular docking to facilitate further structural modification.
Antineoplastic Agents ; Benzamides ; chemistry ; DNA Repair ; Drug Design ; Humans ; Molecular Docking Simulation ; Poly(ADP-ribose) Polymerase Inhibitors ; chemical synthesis ; chemistry ; Poly(ADP-ribose) Polymerases

This paper presents the detail methods which innovation activities are in harmony for fundamental medical physics ex- periment teaching without increasing course period and new equipment.