Febuxostat, as a xanthine oxidase inhibitor, is a classic anti-gout drug with significant therapeutic effects and good tolerability. The structures of febuxostat and its derivatives can be divided into two parts: a substituted phenyl ring and a five-membered or six-membered heterocyclic ring with a carboxyl substitution. This paper reviewed the research progress of febuxostat derivatives in recent ten years and classified the structure-activity relationships of various febuxostat derivatives. Exploring the action mechanisms and structure-activity relationships of xanthine oxidase inhibitors might be significant for the rational design and development of new anti-gout chemical entities.

OBJECTIVETo investigate changes in the adherent ability, the expression of adhesion related proteins Pyk2 and paxillin during HL-60 cells differentiation into granulocyte-monocyte induced by low-dose (LD) bufalin in combination with all-trans retinoic acid (ATRA), and to explore the effects of bortezomib on cellular adhesion and the expression of Pyk2 and paxillin.

METHODSThe expression of CD11b was detected by flow cytometry, cellular adherence ability by MTT assay, and the expressions of Pyk2, paxillin and tubulin by Western blot.

RESULTSThe combination of 5 nmol/L bufalin and 30 nmol/L ATRA induced HL-60 cells differentiation in a time-dependent manner, the percentages of CD11b positive cells treated for 2 d and 4 d being (20.0 +/- 2.8)% and (75.0 +/- 5.3)%, respectively, with the increasing of cellular adherence ability. Meanwhile the expressions of Pyk2 and Paxillin were also up-regulated in a time-dependent manner. Bortezomib suppressed HL-60 cell adhesion in a dose-dependent manner. At concentrations of 1 nmol/L and 10 nmol/L the adherence level were (7.8 +/- 0.1)% and (5.3 +/- 0.3)%, respectively, with down-regulation of Pyk2 but not Paxillin.

CONCLUSIONPyk2 is involved in the regulation of cellular adherence function. Bortezomib might inhibit HL-60 cells adhension function by down-regulation of Pyk2 expression.

Boronic Acids ; pharmacology ; Bortezomib ; Bufanolides ; pharmacology ; Cell Adhesion ; drug effects ; Cell Proliferation ; drug effects ; Focal Adhesion Kinase 2 ; metabolism ; HL-60 Cells ; Humans ; Paxillin ; metabolism ; Pyrazines ; pharmacology ; Tretinoin ; pharmacology

OBJECTIVETo evaluate the effect of Qufeng Zhidong Recipe (QZR) on the head tic behavior, and the mRNA expressions of Notch1 and dopamine D2 receptor (D2R) in tic disordered mice.

METHODSMouse model like wet-dog shake head tic disorder was established by peritoneal injection of 5-HT2A/C agonist DOI for 14 successive days. The model mice were divided into three groups, the model group, the Chinese medicine (CM) treated group and the Western medicine (WM) treated group, they were intervened respectively with distilled water, QZR (10 g/kg) and haloperidol (1 mg/kg). Besides, a normal control group was set up and gastrogavaged with distilled water. The effect of intervention was evaluated 2 weeks later by estimating the head tic and the creeping distance of animals, and the mRNA expressions of D2R and Notch1 in corpus striatum and prefrontal cortex regions were detected using Real-time PCR.

RESULTSThe wet-dog shake response and the creeping distance of mice were significantly reduced after intervention in both intervened groups, showing insignificant difference between the effects of CM and WM (P > 0.05). The expression of D2R mRNA in corpus striatum was higher than that in the prefrontal cortex (P < 0.01), at the prefrontal cortex, it was 151 +/- 30 in the CM group and 180 +/- 41 in the WM group, and at the corpus striatum, 710 +/- 64 and 850 +/- 80 respectively, all higher than those in the model group (P < 0.05). While the Notch1 mRNA expression in model mice were lower at the prefrontal cortex than at the corpus striatum (P < 0.05). After intervention it was 55 +/- 20 in the CM group and 48 +/- 23 in the WM group at the prefrontal cortex, all significantly lower than that in the model group (P < 0.05).

CONCLUSIONDOI-induced wet-dog shake response could well simulate the clinical characteristics of tic disorder; QZR could improve the tic behavior and creeping distance in the model mice. The up-regulation of D2R mRNA expression after QZR intervention may be related with the down-regulation of Notch1 expression, this findings is worthy of further studies.

Animals ; Corpus Striatum ; metabolism ; Drugs, Chinese Herbal ; therapeutic use ; Male ; Mice ; Mice, Inbred C57BL ; Phytotherapy ; RNA, Messenger ; genetics ; metabolism ; Random Allocation ; Receptor, Notch1 ; genetics ; metabolism ; Receptors, Dopamine D2 ; genetics ; metabolism ; Signal Transduction ; drug effects ; Tic Disorders ; drug therapy

Objective To understand the treatment compliance and its influence factors in patients with liver cirrhosis, and provide scientific reference for nursing. Methods A survey was conducted using a questionnaire on 84 hospitalized patients with liver cirrhosis. Results Total score of treatment compliance in patients with liver cirrhosis is (39.42 ± 9.03) ,and the main impact factors are economy conditions, knowledge of liver disease, and social support. Conclusions Better understanding of disease in patients and a quicker rehabilitation will be achieved if we pay more attention to the poor treatment compliance in patients with liver cirrhosis.

Objective To explore the effect of dietary categories on effectiveness of the intestinal cleanliness before the colonoscopy,patients' acceptance of dietary changes and adverse reactions in bowel preparation.Methods Totals of 94 patients who underwent colonoscopy were divided into normal diet group (n =30),semi-liquid food group (n =32) and fasting group (n =32) according to the dinner diet styles the day before the colonoscopy.Observed three groups of adverse reactions,patients' acceptance and intestinal cleanliness.Results No significant difference was found in the medicine dosage,water intake,intestinal cleanliness among the three groups (P ＞ 0.05).The cases of fatigue phenomenon and discomfort on dietary changes in normal diet group were 4 and 1,in semi-liquid food group were 14 and 8,in fasting group were 13 and 5,and the difference was statistically significant (x2 =7.765,20.623,respectively; P ＜ 0.05).While no significant difference was found in the incidence of other adverse reaction among the three groups (P ＞ 0.05).Conclusions Dietary categories are no effect on the intestinal cleanliness of the colonoscopy.However,according to the conditions of the patients before taking laxatives poly would increase their comfort under certain dietary restrictions.

Objective To explore the role of maternal physiology, mentality and prenatal health care on low birth weight (LBW). Methods A LBW-small for gestation age (SGA)-control group retrospective study was conducted based upon a population of infants born from November 2004 to June 2006. 896 cases involved in this study were entirely under voluntary participation and subject could withdraw their consent at any point. All subject recruitment and enrollment took place at Fujian Provincial Maternal and Children Hospital at the time of delivery. Using χ2 test for single factor analysis and logistic regression for multiple analyses Results There were 15 out of 22 single factors having statistical significances, including 2 maternal psychological, 4 physiological, 6 pathological and 3 prenatal health care factors respectively. When multi-factorial stepwise regression analyses was performed, there were 9 factors for main relative factors of LBW ,including women's height, number of prenatal examination, in-normal non-stress test, umbilical cord around the neck, retardation of the umbilical blood flow, week of gestation when the first examination was performed, premature rupture of membrane, preference on the sex of the infant, abnormal family history etc.were influencing the existence of LBW. Awareness on health information appeared to be a protective factor,suggesting that LBW could be prevented during the pregnant period. Conclusion Multiple factors seemed to be contributing to the incidence of low birth weight.

Objective To observe the therapeutic effect of ankle bath by traditional Chinese medicine associated with chiropractic technique on the patients with ankle fractures in later period so as to explore the nursing and its influencing factors.Methods From June 2009 to December 2011,a total of 76 cases with ankle fractures were selected and radomly divided into control group and observation group.Control group took medicine that could activate blood circulation to dissipated blood stasis,bathed ankle in warm water and took functional exercise,while the observation group received Chinese medicine bath and massage followed by functional exercise.Results After 10 days,the difference between observation group and control group in the degree of pain and activity of ankle and joint function appeared ( 14.86 ±7.21vs 8.68 ± 8.98,7.18 ± 1.91vs 4.34 ± 1.66,2.84 ± 1.46 vs 1.97 ± 1.17 ) and the difference was statistically significant ( t =3.31,6.90,2.85 ;P＜0.05).And 20 days later,the improvement rate of observation group was 92.1％ and 71.06％ of control group,and the difference was statistically significant ( u =2.07,P ＜ 0.05).Conclusions Bath foot by traditional Chinese medicine associated with chiropractic technique can make qi and blood be unobstructed,activate blood circulation to dissipate blood stasis,promote ankle joint swelling and analgetic,and finally enhance joint function to recover.

OBJECTIVETo explore the norms of treatment of acute organophosphorus pesticide poisoning (AOPP), and observe the curative effect.

METHODSOn basis of the pre-research, the norms of treatment of AOPP were summarized, and a multi-center clinical trial was performed in 6 hospitals selected from high incidence of AOPP in Shandong Province.

RESULTS422 patients of AOPP in 6 hospitals in observation period were treated and observed by the norms of treatment. Among them, the proportion of oral poisoning was 97.16%, middle and severe degree were 87.44%. Compared with themselves 2 years ago before standard treatment, the curative effect of the norms of treatment for AOPP was much better than before. The mortality rate of AOPP declined from 9.87% to 1.66% (Chi2 = 27.92, P < 0.01), that was much better than the average therapeutic effect level of all our province in the same period (the mortality rate: 8.92%) (Chi2 = 26.05, P < 0.01). The average amount of atropine [(37.54 +/- 17.76) mg], dropped greatly [(1280.70 +/- 69.22) mg] (U = 439.22, P < 0.01).The usage of atropine by continuous intravenous injection with venous pump was better than ordinary intravenous injection. The mean dosage of pralidoxime chloride increased twice than the previous (U = 19.48, P < 0.01). There was no drug poisoning.

CONCLUSIONThe standard treatment of AOPP is urgently needed in our country, especially in rural area. By this trial, the satisfactory effect of the norms of treatment for AOPP summarized is observed and it reduces the fatality rate remarkably.

Adolescent ; Adult ; Aged ; Child ; Female ; Humans ; Male ; Middle Aged ; Organophosphate Poisoning ; Pesticides ; poisoning ; Poisoning ; therapy ; Standard of Care ; standards ; Young Adult

This study was aimed to investigate the immunomodulatory ability of human umbilical cord mesenchymal stem cells (UB-MSC) along with prolonging of culture time and increasing of passages in vitro. Mesenchymal stem cells (MSC) were isolated from human umbilical cord and cultured in vitro. The morphological changes and nucleocytoplasmic ratio of MSC were observed using Giemsa staining. MSC of the 5th passage were selected as control group, and MSC of the 13th passage were taken as senile group. The degree of cell senescence was detected by aging cells in situ test kit. Cell Counting Kit-WST-8 was used to determine the proliferation of lymphocytes in mixed lymphocytes coculture system with different passages of MSC. The expression of immunomodulation-related genes was detected by RT-PCR. The results showed that the length-breadth ratio of MSC increased and nucleocytoplasmic ratio decreased along with the increasing of passages. The senium degree of cells of the 13th passage was higher than that of the 5th passage cells. The capacity of suppressing lymphocyte proliferation of the 13th passage MSC was enhanced, compared with the 5th passage. Moreover, the expression of immunosuppression-related genes of senile MSC increased and the expression of most anti-inflammation associated genes declined as compared with young MSC by RT-PCR. It is concluded that the degree of MSC senescence gradually develops with increasing of culture passage, but the immunosuppressive ability of MSC strengthens with continuous culture.
Cell Differentiation ; Cell Proliferation ; Cells, Cultured ; Cellular Senescence ; Humans ; Lymphocytes ; cytology ; immunology ; Mesenchymal Stromal Cells ; cytology ; immunology ; Umbilical Cord ; cytology

OBJECTIVETo describe a HPLC method for assessing betaine in Fufang Guilu granule.

METHODThe content of betainephenaxcyl bromide in Fufang Guilu granule was determined by HPLC. The analytical column was a shim-pack CLC-ODS (6.0 mm x 150 mm) filling a 5 microm stationary phase; The mobile phase consisted of acetonitrile-water(35:65) with 0.1 mol x L(-1) NaClO4; The flow-rate was 1 mL x min (-1); The detector was set at 254 nm.

RESULTThe calibration curve was linear over the range of 0.09-0.585 microg (r = 0.9997). The average recovery of the method was 98.4%, RSD 2.5% (n = 5).

CONCLUSIONThe results showed that this method was reliable and accurate, and can be used for quality control of Fufang Guilu granule.

Betaine ; analysis ; Chromatography, High Pressure Liquid ; methods ; Codonopsis ; chemistry ; Drug Combinations ; Drugs, Chinese Herbal ; chemistry ; Lycium ; chemistry ; Plants, Medicinal ; chemistry ; Quality Control ; Reproducibility of Results