AIMTo study the synthesis and anti alpha-adrenoceptor activity of 1,2-dihydro-quinoline-2-one compounds.

METHODSAcylation, bromination and cyclization, and substitute reactions were used in the synthesis of the title compounds IV. A proposed mechanism was showed to explain the unusual compounds 5 and 6 in the route C. The inhibition activity of the six target compounds were tested.

RESULTSTwelve new compounds were synthesized (II1-6 and IV1-6). Among them, six new compounds (IV1-6) are the title compounds. Structure of the title compounds were determined by IR, 1HNMR, MS and HRMS.

CONCLUSIONCompounds IV3, IV4 and IV6 showed inhibitiion activity, and were worth further studying.

Adrenergic alpha-Antagonists ; chemical synthesis ; pharmacology ; Animals ; Aorta ; drug effects ; In Vitro Techniques ; Molecular Structure ; Phenethylamines ; chemical synthesis ; pharmacology ; Quinolones ; chemical synthesis ; pharmacology ; Rabbits ; Receptors, Adrenergic, alpha ; drug effects ; metabolism ; Technology, Pharmaceutical

OBJECTIVETo compare the clinical efficacy on upper limb motor impairment in stroke between the interactive dynamic scalp acupuncture therapy and the traditional scalp acupuncture therapy.

METHODSThe randomized controlled trial and MINIMIZE layering randomization software were adopted. Seventy patients of upper limb with III to V grade in Brunnstrom scale after stroke were randomized into an interactive dynamic scalp acupuncture group and a traditional scalp acupuncture group, 35 cases in each one. In the interactive dynamic scalp acupuncture group, the middle 2/5 of Dingnieqianxiexian (anterior oblique line of vertex-temporal), the middle 2/5 of Dingniehouxiexian (posterior oblique line of vertex-temporal) and Dingpangerxian (lateral line 2 of vertex) on the affected side were selected as the stimulation areas. Additionally, the rehabilitation training was applied during scalp acupuncture treatment. In the traditional scalp acupuncture group, the scalp stimulation areas were same as the interactive dynamic scalp acupuncture group. But the rehabilitation training was applied separately. The rehabilitation training was applied in the morning and the scalp acupuncture was done in the afternoon. The results in Fugl-Meyer for the upper limb motor function (U-FMA), the Wolf motor function measure scale (WM- FT) and the modified Barthel index in the two groups were compared between the two groups before treatment and in 1 and 2 months of treatment, respectively.

RESULTSAfter treatment, the U-FMA score, WMFT score and the score of the modified Barthel index were all apparently improved as compared with those before treatment (all P < 0.01). The improvement in the U-FMA score after treatment in the interactive dynamic scalp acupuncture group was better than that in the traditional scalp acupuncture group (P < 0.05). For the patients of IV to V grade in Brunnstrom scale, WMFT score in 2 months of treatment and the score of Barthel index after treatment in the interactive dynamic scalp acupuncture group were improved apparently as compared with those in the traditional scalp acupuncture group (P < 0.05, P < 0.01). But, for the patients of III grade in Brunnstrom scale, WMFT score and the score of Barthel index after treatment in the interactive dynamic scalp acupuncture group were not different significantly as compared with those in the traditional scalp acupuncture group (both P > 0.05).

CONCLUSIONFor the patients of IV to V grade in Brunnstrom scale in stroke, the interactive dynamic scalp acupuncture therapy achieves the superior improvements of the upper limb motor function and the activity of daily life as compared with the traditional scalp acupuncture therapy, and the longer the treatment lasts, the more apparent the improvements are. For the patients of III grade in Brunnstrom scale, the interactive dynamic scalp acupuncture therapy achieves the similar improvement in the upper limb motor impairment as compared with the traditional scalp acupuncture therapy.

Activities of Daily Living ; Acupuncture Points ; Acupuncture Therapy ; Adult ; Aged ; Female ; Humans ; Male ; Middle Aged ; Occupational Therapy ; Scalp ; Stroke ; physiopathology ; therapy ; Stroke Rehabilitation ; Treatment Outcome ; Upper Extremity ; physiopathology

Aneurysm, False ; etiology ; surgery ; Blood Loss, Surgical ; Carcinoma ; Carotid Arteries ; Carotid Artery Diseases ; etiology ; surgery ; Humans ; Nasopharyngeal Neoplasms ; radiotherapy ; Rupture

OBJECTIVETo investigate the protective effects of carnosine against experimental closed head injury (CHI) in mice.

METHODSThe CHI model was established by free-falling weight-drop. Carnosine (250 mg/kg or 500 mg/kg) was administered intraperitoneally 30 min before brain trauma, then q.d for 7 d; while normal saline was administrated for control group. The neurological defect was evaluated by neurological severity score (NSS) within 7 d; the survival rate and the histological alternations were observed.

RESULTSCarnosine prevented the body weight loss of mice at dose of 500 mg/kg; significantly increased the survival rate, and reduced the neurological defect and histological damage at dose of 250 and 500 mg/kg.

CONCLUSIONCarnosine can attenuate closed head injury in mice.

Animals ; Carnosine ; therapeutic use ; Disease Models, Animal ; Head Injuries, Closed ; drug therapy ; pathology ; Male ; Mice ; Mice, Inbred ICR

Objective The present study was conducted to identify the Vibrio cholera type and to analyze its antibiotic resistance in an epidemic of cholera in Haiyan County in 2018, which would provide the references for prevention and control of cholera. Methods Stool samples of the patient and his close contacts as well as the food and environmental samples were collected for identification of the type of Vibrio cholerae and the toxin gene. The resistance of identified Vibrio cholerae to 20 different common antibiotics were tested. Results A total of 176 samples were collected, including 101 stool samples from the case and his close contacts, 35 environmental samples and 40 food samples. Among those samples, only one strain of V. cholerae, O139, was isolated from the patient's first feces sample. It was detected as a toxin gene of ctxA positive by real-time fluorescence PCR. Antibiotic resistance test showed that the strain was sensitive to norfloxacin, levofloxacin, ciprofloxacin, cefotaxime, cephalothin, ampicillin, and amoxicillin. It was 100% resistant to tetracycline, doxycycline, neomycin, kanamycin, streptomycin, and rifampicin. Conclusion V. cholerae O139 strain with ctxA is detected in an epidemic of cholera. Norfloxacin, levofluoxacin and some other antibiotics could be used for clinical treatment and prevention. It should pay attention to this strain of V. cholera regarding the multiple drug resistance and the change of antibiotic resistance.

A quantitative real-time PCR assay was developed to measure the proviral load of human T-lymphotropic virus type I (HTLV-I) in peripheral blood. The technology utilizes special primers and Taqman MGB fluorescence probe to measure amplification products from the gag-pro-pol polyprotein gene of HTLV-I. HTLV-I copy number was normalized to the amount of cellular DNA by quantitation of the beta-actin gene, The amplification system was sensitive to detect 5 copy/microL. The standard curve had a good linearity when the quantity for the gene was between 10(3) and 10(7) copy/microL (R2 = 0.999). Good reproducibility was observed in each intra- and inter-assay. We also measured proviral load in peripheral blood in 12 HTLV-I seropositive former blood donors. Proviral load for HTLV-I infected donors ranged from 0.015 to 12.819 copy/cell in WBC with the mean of 3.116 copy/cell.
Gene Products, gag ; genetics ; Gene Products, pol ; genetics ; Human T-lymphotropic virus 1 ; genetics ; isolation & purification ; Humans ; Molecular Probes ; Polymerase Chain Reaction ; methods ; Viral Proteins ; genetics

Bone Diseases ; etiology ; surgery ; Chronic Disease ; Epidermal Cyst ; etiology ; surgery ; Femur ; Humans ; Male ; Middle Aged ; Osteomyelitis ; complications

OBJECTIVETo determine the correlation of the CYP1A1 (rs4646422) gene polymorphisms with male infertility in the Chinese Han population.

METHODSUsing the Mass ARRAY iPLEX GOLD technique, we conducted a case-control study on theCYPlA1 (rs4646422) gene polymorphisms in 636 infertile males aged 21-49 years (case group) and 442 normal healthy men aged 23-47 years (control group) of the Chinese Han population. We analyzed the genotypes and allele frequencies in the two groups ofsubjects with the SPSS 20.0 software.

RESULTSCompared with the wild homozygous genotype GG, the heterozygous genotype AG (OR = 1.06, 95% CI 0.81-1.38) and homozygous genotype AA (OR = 1.11, 95% CI 0.56-2.21) showed no correlation with male infertility, nor did the mutant allele A (OR = 1.06, 95% CI 0.85-1.32) in comparison with the wild allele G.

CONCLUSIONThe CYP1A1 (rs4646422) gene polymorphisms might not be correlated with male infertility in the Chinese Han population.

Adult ; Alleles ; Case-Control Studies ; China ; Cytochrome P-450 CYP1A1 ; genetics ; Gene Frequency ; Genotype ; Homozygote ; Humans ; Infertility, Male ; genetics ; Male ; Middle Aged ; Polymorphism, Genetic ; Young Adult

Purpose To investigate the expression of RSK4 (ribosomal S6 protein kinase 4),CD44 and MMP-9 protein in primary renal cell carcinoma (pRCC) and metastatic renal cell carcinoma (mRCC),and to explore the level of expression as well as the association with clinicopathologic features and clinical outcome.Methods The expression of RSK4,CD44 and MMP-9 in 52 pRCC and 48 mRCC samples was detected by immunohistochemistry and its relationship with clinicopathologic features as well as prognosis was analyzed by statistical methods.Results In the 48 mRCC samples,there were 36 (75％,36/48),33(68.75％,33/48) and 44 (91.7％,44/48) positive for RSK4,CD44 and MMP-9,respectively,while the positive rate in 52 pRCC samples were 23 (44.2％,23/52),18 (34.6％,18/52) and 36 (69.2％,36/52),respectively.Statistical analysis showed that the expression of RSK4,CD44 and MMP-9 in mRCC samples was higher than the pRCC samples (PRsK4 =0.002,PMMP-9 =0.002,PcD44 =0.001).Furthermore,the expression of RSK4,CD44 and MMP-9 in mRCC samples was not correlated with ages,genders,Fuhrman grading and the metastatic sites (P ＞ 0.05).Further analysis showed that there was positive correlation among the three proteins (P =0.008),particularly,the expression of RSK4 and CD44 (P =0.019),MMP-9 and CD44 (P =0.05) were positively correlated,while the expression of RSK4 and MMP-9 (P =1.00) had no significance of correlation.Conclusion The expression of RSK4,CD44 and MMP-9 in mRCC samples is significantly higher than pRCC samples,suggesting that the three may mediate the metastasis of renal cell carcinoma,and its specific mechanism of action remains to be further studied.

Background: In acute and chronic renal inflammatory diseases, the activation of inflammatory cells is involved in the defect of erythropoietin (EPO) production. Ras guanine nucleotide-releasing protein-4 (RasGRP4) promotes renal inflammatory injury in type 2 diabetes mellitus (T2DM). Our study aimed to investigate the role and mechanism of RasGRP4 in the production of renal EPO in diabetes. Methods: The degree of tissue injury was observed by pathological staining. Inflammatory cell infiltration was analyzed by immunohistochemical staining. Serum EPO levels were detected by enzyme-linked immunosorbent assay, and EPO production and renal interstitial fibrosis were analyzed by immunofluorescence. Quantitative real-time polymerase chain reaction and Western blotting were used to detect the expression of key inflammatory factors and the activation of signaling pathways. In vitro, the interaction between peripheral blood mononuclear cells (PBMCs) and C3H10T1/2 cells was investigated via cell coculture experiments. Results: RasGRP4 decreased the expression of hypoxia-inducible factor 2-alpha (HIF2A) via the ubiquitination–proteasome degradation pathway and promoted myofibroblastic transformation by activating critical inflammatory pathways, consequently reducing the production of EPO in T2DM mice. Conclusion RasGRP4 participates in the production of renal EPO in diabetic mice by affecting the secretion of proinflammatory cytokines in PBMCs, degrading HIF2A, and promoting the myofibroblastic transformation of C3H10T1/2 cells.