Humans ; Paraffin Embedding ; methods ; Periodontium ; pathology ; Tooth ; pathology

Objective To investigate the roles and significances of MMP-2 and MMP-9 in diffuse proliferative lupus nephritis by repeated renal biopsy.Methods Seventeen patients diagnosed by renal biopsy as WHO typeⅣlupus nephritis were analyzed by immunohistochemistry staining for MMP-2 and MMP-9. Double staining for MMP-2 and MT1-MMP,MMP-9 and CD68 were also performed.Patients had repeated renal biopsy after followed up for 2.5 years.The relationship between expressions of gelatinases and pathological activity index and clinical data were studied.Results MMP-2 immunoreactivity was detected in normal controls and was increased in diffuse proliferative lupus nephritis.MMP-9 staining,which was almost negative in normal giomeruli,was increased much more significantly in diffuse proliferative lupus nephritis. The immunoreactivity of MMP-2 and MMP-9 was positive in MT1-MMP staining and CD68-positive macrophages, respectively.The expression of MMP-2 and MMP-9 was reduced by 70% and 62% in 10 patients whose clinical condition was partially alleviated,while the expressions in 7 patients whose clinical condition was not alleviated,were only reduced by 27% and 32%.The staining for MMP-2 and MMP-9 were correlated with activity index of lupus nephritis and proteinuria.Conclusion Up-regulation of gelatinases expression in diffuse proliferate lupus nephritis is correlated to activity index of the disease.

Objective To explore the role of tissue inhibitor of metalloproteinase-1(TIMP-1) during renal senescence by using human TIMP-1 transgenic mice.Methods Renal histological changes of wild type mice and transgenic mice at the age of 3,12,24 months were observed by periodic acid-schiff(PAS)staining of paraffin sections.The numbers of F4/80 positive cells were detected by immunofluoreseence.The protein expressions of TIMP-1,TIMP-2,matrix metalloproteinase(MMP)-9,MMP-2,intercellular adhesion molecule-1(ICAM-1),transforming growth factor?1(TGF-?1),collagenⅢand collagenⅣwere detected by Western blot.The activities of gelatinases and TIMP-1 were examined by gelatin zymography and reverse zymography respectively.Results Focal renal fibrosis was found in two genotypes with aging.At the age of 24 months,compared with wild type,in kidneys of transgenic type,the expressions and activities of gelatinases were dowregulated (MMP-2:2.08?0.20 vs.3.39?0.43;MMP-9:4.02?0.82 vs.6.72?1.40,all P＜0.05);the expressions of collagenⅢ,collagenⅣ,ICAM-1,and TGF-?1 were upragulated(0.72+0.11 vs.0.57?0.09;0.84?0.13 vs.0.6?0.11,0.72?0.12 vs.0.53?0.07; 0.69?0.12 vs.0.45?0.09,all P＜0.05),and the numbers of F4/80 positive cells were increased (18.8?4.4 vs.12.7?3.6,P＜0.05)with the upregulated expression and activity of TIMP-1(1.10?0.18 vs.0.62?0.09;50.75?7.25 vs.20.64?3.50,P＜0.05).Conclusions TIMP-1 could promote age-related renal fibrosis through enhancing inflammation reaction by ICAM-1 upregulation.

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

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

OBJECTIVE: To evaluate the application of MSCT and post-processing images to fractures of nasal bone in forensic identification. METHODS: 134 cases were examined by thin slice scanning with MSCT and all of the data were sent to workstation for MPR and SSD. The result of MSCT was compared with that of X-ray. RESULTS: There are 55 (41.04%) cases of linear fracture, 46 (34.33%) cases of comminuted fracture, 27 (20.15%) cases of depressed fracture and 6 (4.48%) cases of no fracture in this sample. With X-ray or CR, 48 (35.82%) cases were misdiagnosed or underdiagnosed. 133 (99.25%) cases were confirmed by MSCT. Significance difference was found between X-ray and MSCT (chi2= 45.0816, P<0.001). CONCLUSION MSCT and post-processing images might be the chief evidence for nasal fractures in forensic identification.
Adolescent ; Adult ; Chromatography, Thin Layer ; Female ; Forensic Medicine/methods* ; Fractures, Comminuted/diagnostic imaging* ; Humans ; Imaging, Three-Dimensional ; Male ; Middle Aged ; Nasal Bone/injuries* ; Skull Fractures/diagnostic imaging* ; Tomography, Spiral Computed/methods* ; Young Adult

ObjectiveTo investigate the effect of out-patient training combined with family training under doctor's instructions on children with cerebral palsy (CP).Methods80 CP children were selected as treatment group and trained one to three months by therapists at out-patient department, then continually trained at family by parents who received doctor's instructions 30 min once every two or three months. 60 CP children in hospital were selected as control group. Rehabilitative effects of two groups were compared.ResultsIn the first and third month after training completed, movement growth of treatment group was not different from that of control group (P>0.05), but in the sixth month, was significant different from that of control group (P<0.05). The effect of treatment group was better than that of control group.ConclusionOut-patient training combined with family training under doctor's instructions can decrease treatment expenses, and is convenient and effective for CP children.

Protein kinase C beta (PKCbeta) is a multifunctional serine/threonine protein kinase, which plays an important role in many cell signaling pathways. PKCbeta takes part in multiple physiological processes, including regulation of the cell cycle, differentiation, proliferation, apoptosis and angiogenesis. Increased PKCbeta activity has been observed in many human cancers, such as colon, breast and haematological malignancies. At present, Enzastaurin is mostly studied in preclinical and clinical studies, which is a selective PKCbeta inhibitor. This review focuses on the functional properties of PKCbeta, its role played in tumors and Enzastaurin.
Animals ; Antineoplastic Agents ; pharmacology ; therapeutic use ; Cell Line, Tumor ; Cell Proliferation ; drug effects ; Clinical Trials as Topic ; Humans ; Indoles ; pharmacology ; therapeutic use ; Neoplasms ; drug therapy ; metabolism ; pathology ; Protein Kinase C ; antagonists & inhibitors ; chemistry ; metabolism ; Protein Kinase C beta ; Protein Kinase Inhibitors ; pharmacology

The aim of the manuscript was to optimize formulations and preparation technologies of cataplasm of white mustard seed varnish, and to evaluate its anti-asthma effect on rats. The single factor experiments included spreading thickness, types of crosslinking agents, dihydroxyaluminum aminoacetate amount, sodium polyacrylate amount, types of adhesive agents with human sense as the evaluation index. Blank cataplasm matrix was optimized by the orthogonal experiment with the amount of glycerine, citric acid, and sodium carboxymethylcellulose as the major influential factors. Initial adhesive force, peeling strength and human sense were as the evaluation index. The optimized formulation of blank cataplasm were as followings: glycerine-water-ethanol-PEG400-dihydroxyaluminum aminoacetate-citric acid-sodium carboxymethylcellulose-sodium carboxymethylcellulose 2 : 8 : 0.8 : 0.4 : 0.07: 0.15 : 0.1 : 0.5. The active ingredients of white mustard seed, corydalis, and gansui root were extracted by alcohol extraction method. Asiasarum volatile oil was extracted by oil extractor. The optimized drug loading amount was 11% with initial adhesive force, peeling strength and human sense as the evaluation index. Asthma rats model were established by sensitized with ovalbumin and nose-scratching time as the evaluation index. High dose (17%) group of drug-loaded cataplasm had the obvious inhibition effect on nose-scratching time of rats (P = 0.037 < 0.05). In comparison, middle dose (11%), low dose (4%) and positive-control groups had no obvious inhibitive effect on rats. White mustard seed cataplasm supplied a novel choice for anti-asthma therapy. And the overall pharmacodynamics assessment will be carried out on molecular level in near future.
Animals ; Anti-Asthmatic Agents ; administration & dosage ; chemistry ; Asthma ; drug therapy ; Chemistry, Pharmaceutical ; Drugs, Chinese Herbal ; administration & dosage ; chemistry ; Female ; Humans ; Male ; Mustard Plant ; chemistry ; Rats ; Rats, Sprague-Dawley ; Seeds ; chemistry

Objective To investigate the effect of surgical treatment of retrograde A-type aortic dissection after Stanford B-type interstitial vascular repair on the expression of proinflammatory cytokines. Methods One hundred patients with Stanford type B aortic dissection who were treated in our hospital from March 2016 to March 2018 were randomly divided into control group and study group, with 50 cases in each group. The control group was treated with conventional methods. The study group was treated with the surgical treatment of retrograde aortic dissection. And the effects of the two treatments on the expression of proinflammatory cytokines were observed. Results The therapeutic effect of the study group was better than that of the control group (P<0.05). The incidence rate of clinical symptoms in the study group was lower than that of the control group (P<0.05). Conclusion In the treatment of Stanford type B aortic dissection, the use of postoperative retrograde type A aortic dissection can more effectively affect the expression of pro-inflammatory cytokines in patients, and should be further promoted in clinical practice.