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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.
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Objective To observe the value of CE-MRA in differentiating secondary vascular tortuosity of the spinal cord caused by spinal vascular malformations (SCVM) or non-vascular malformations.Methods A retrospective analysis was performed on 30 patients suspected as SCVM.Based on the results of DSA or surgery,the patients were divided into SCVM group (n=16) or non-vascular malformation group (n=14).CE-MRA features were compared between the two groups,including the number,length,position,tortuosity degree of spinal cord tortuous vascular and whether the abnormal feeding artery existed surrounding tortuous vascular.Results Compared with non-vascular malformation group,SCVM group showed more average number of tortuous vascular [(1.38 ± 0.16) vs 1,P=0.012],longer tortuous vascular lengthy [similar lengthy of (9.68 ± 1.18) vertebral body vs(4.14±0.62) vertebral body,P＜0.001),higher score of tortuosity degree [(2.23 ± 0.22) scores vs (0.86±0.10) scores,P＜0.001] and more easier to appear abnormal feeding artery surrounding tortuous vascular [75.00％(12/16) vs28.57％(4/14),P=0.014].Furthermore,only2 cases (2/16,12.50％) of tortuous vascular located in and limited to lower thoracic vertebra (T7 T12 vertebrae) in SCVM group,while 11 cases (11/14,78.57％) in non-vascular malformation group (P=0.020).Conclusion Spinal cord secondary vascular tortuosity of SCVM can be well distinguished from that caused by non-vascular malformation with CE MRA spinal angiography.
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Objective:To investigate the generative condition of situational forgiveness in college students.Methods:Totally 208 college students were selected and randomly divided into 8 experimental treatment groups,using 8 different experimental conditions as stimuli,using 2 (behavioral intention:intentional/unintentional) × 2 (level of harm:high/low) × 2 (sincere apology:sincerity/insincerity) subjects experimental design,examining the subjects'cognitive appraisals of behavior intention,the degree of injury and sincere apology toward situational stories,to investigate the generative condition of situational forgiveness.Results:The forgiveness scores were significantly higher in the unintentional injury situation than in the intentional injury situation [(5.1 ± 1.8) vs.(4.0 ±1.5),P ＜ 0.001].The forgiveness scores were significantly higher than in low damage situation that in high damage situation [(5.0 ± 1.7) vs.(4.2 ± 1.7),P ＜0.001].The forgiveness scores were significantly higher in the situation of sincere apology than in the situation of insincerity [(5.4 ± 1.7) vs.(3.8 ± 1.3),P ＜0.001].Conclusion:It suggests that one'evaluation on the offend situation may affect the occurrence of situational forgiveness.Low damage and sincere apology are more likely to produce situational forgiveness
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AIM:To remark the effect of Qingguang'an Ⅱ on expression of PAX6, Ngn1, and Ngn2 mRNA of rats with chronic high intraocular pressure.METHODS:Totally 40 male SD rats were randomly divided into 6 groups, that was:A:blank group, B:model group, C:Qingguang'an Ⅱ low dose group, D:Qingguang'an Ⅱ moderate dose group, E:Qingguang'an Ⅱ high dose group, F:Yimaikang disket group.B, C, D, E, F groups of experimental rats were established the model of chronic high intraocular pressure (IOP) by cauterizing of superficial scleral vein.Animal model was established successfully by using monitoring IOP consistently keep above 25mmHg for 8wk as cut-off criterion.Tissues of Eyes were obtained after intragastric administration for 2wk and 4wk.The expressions of PAX6, Ngn1, and Ngn2 mRNA were investigated by Real-time PCR.RESULTS:At the time-point of 2wk, PAX6, Ngn1, and Ngn2 mRNA in group B were statistically expressed in lower level comparing with other groups (P0.05).CONCLUSION:In summar, Qingguang'an Ⅱ and Yimaikang disket can remarkably increase the expressions of PAX6, Ngn1, and Ngn2, which suggest protecting the optic nerve of rats caused by chronic high IOP.What's more, this study indicated that, in the protection of optic nerve of rats with chronic high IOP, the high dose of Qingguang'an Ⅱ at the time-point of 4wk was the better choice.
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Invigorating blood and dissolving stasis method is a kind of unique therapy of Traditional Chinese Medicine(TCM) treatment, which efficacy has become increasingly prominent in the treatment of ophthalmology.With the further studies of blood stasis and invigorating blood and dissolving stasis therapy, it is widely used in clinical ophthalmology, and get good effects beyond thought, especially when western medicine has no curative effects.It improved the cure rate of fundus oculi disease from the eyelids, conjunctiva, lacrimal sac, vitreous body to the choroid and retina, optic nerve and macula lutea, from surface to fundus, or pathological changes related to inflammation, degeneration, necrosis, atrophy, hyperplasia of fibrous tissue hyperplasia.This paper is aim to explain the definition of invigorating blood and dissolving stasis and make a review of basic research and clinical application about it in several diseases.
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Objective To establish an experimental model of acute cerebral schistosomiasis japonica and explore the MRI manifestations of acute cerebral schistosomiasis. Methods Rabbits were divided into 3 groups with 10 rabbits in each group. The rabbits in the experimental group were directly injected with suspension fluid of Schistosoma japonicum eggs(0.9 mg,1 ml) by the cranial drilling method,those in the negative control group were given saline(1 ml)by the same method above-men-tioned,and those in the blank control group were not given any treatment. Antibiotic was given to the first two groups after the op-eration. The clinical manifestations of the 3 groups were observed,and the magnetic resonance imaging(MRI)was performed in 30 days post-operation,and then the brain tissues were taken for pathological examinations. Results All the rabbits in the ex-perimental group exhibited inappetence,various neurological symptoms including hemiplegia,and weight loss after the opera-tion;while those in the negative control group showed inappetence in 3 days after the operation,and 1 week later,the symptom disappeared;there were no adverse reactions in the blank control group. MRI of the experimental group showed nodular or patchy enhancement on T1WI enhancement,brain edema,abnormal ventricular dilatation,and needle augmentation. SWI dis-played hypointense in the abnormal enhanced nodules and flaky hypointense on the operation brain. In the negative control group,2 rabbits showed abnormal enhancement of the needle canal,and 1 showed mild dilatation of the ventricle. The blank control group showed normal manifestations. The pathological examinations showed abnormal appearances in 10 rabbits of the ex-perimental group,including 6 with S. japonicum egg granuloma nodules,nonspecific granuloma nodules coexisted with perivas-cular inflammation;no granuloma nodules were found in the negative control group,but 2 rabbits showed vascular inflamma-tion;the blank control group showed the normal brain tissue. Conclusions An experimental model of acute cerebral schistoso-miasis is successfully established in rabbits by intracranial injection of schistosome eggs. The MRI examination combined with the clinical manifestations can improve the accuracy of early diagnosis of cerebral schistosomiasis.
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Objective To explore the correlation between CT perfusion imaging parameters and differentiation degree of gastric cancer.Methods Fifty patients with gastric cancer proved by surgery and pathology underwent 64-slice spiral CT perfusion imaging before surgery,and the CT perfusion parameters were obtained including blood flow(BF),blood volume(BV),mean transit time (MTT)and permeability surface(PS).The patients were divided into 3 groups (well,moderate and poor differentiation)according to the degree of cell differentiation.Statistical analysis was performed by using the SPSS 17.0 statistics software.Results The perfusion parameters of BF (mL·min-1 ·100 g-1 ),BV (mL/100 g),MTT (s)and PS (mL·min-1 ·100 g-1 )were as follows:75.28±6.81,9.01± 0.94,9.89±1.65 and 10.05±0.71 in well differentiation group with 10 patients (20%),110.01±31.90,18.18±5.62,9.81±3.69 and 40.08±1 5.82 in moderate differentiation group with 24 patients (48%),138.59±38.09,21.08±4.1 1,9.47 ±1.80 and 57.50± 13.28 in poor differentiation group with 1 6 patients (32%)respectively.Among three groups,there were statistic differences in BF, BV and PS between well differentiation group and moderate differentiation group or low differentiation group (P 0.05).Conclusion The BF,BV and PS values may be regarded as the evaluation index for malignant degree of gastric cancer.
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PURPOSE: To investigate the blood pharmacokinetics and bio-distribution of DTPA-bis-amide (L3) Gd(III) complexes. MATERIALS AND METHODS: The pharmacokinetics and bio-distribution of Gd (L3)(H2O).nH2O were investigated in Sprague-Dawley rats after intravenous administration at a dose of 0.1 mmol Gd/kg. The Gd content in the blood, various tissues, and organs was determined by ICP-AES. Blood pharmacokinetic parameters were calculated using a two-compartment model. RESULTS: The half-lives of alphaphase and betaphase Gd (L3)(H2O).nH2O were 2.286+/-0.11 min and 146.1+/-7.5 min, respectively. The bio-distribution properties reveal that the complex is mainly excreted by the renal pathway, and possibly excreted by the hepatobiliary route. The concentration ratio of Gd (III) was significantly higher in the liver and spleen than in other organs, and small amounts of Gd (III) ion were detected in the blood or other tissues of rats only after 7 days of intravenous administration. CONCLUSION: The MRI contrast agent Gd (L3)(H2O).nH2O provides prolonged blood pool retention in the circulation and then clears rapidly with minimal accumulation of Gd(III) ions. The synthesis of gadolinium complexes with well-balanced lipophilicity and hydrophilicity shows promise for their further development as blood pool MRI contrast agents.
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Animals , Rats , Administration, Intravenous , Contrast Media , Gadolinium , Hydrophobic and Hydrophilic Interactions , Ions , Liver , Magnetic Resonance Imaging , Models, Animal , Pharmacokinetics , Rats, Sprague-Dawley , SpleenABSTRACT
<p><b>OBJECTIVE</b>In order to explore the role of toll-like receptors 2 (TLR2) in initiating inflammatory response, the expression of TLR2 of the liver and IL-18, TNF-alpha and IFN-gamma of plasma in fulminant hepatic failure was analysed.</p><p><b>METHODS</b>D-galactosamine (D-Gal, 900 mg/kg) and lipopolysaccharide (LPS, 10 microg/kg) were administered intraperitoneally into the BALB/C mice. To evaluate the hepatic injury, serum transaminase (ALT and AST) and plasma IL-18, TNF-alpha and IFN-gamma were determined and the mortality was observed at various time points following the intraperitoneal injection. The level of TLR2 mRNA was measured by semiquantitative RT-PCR. The protein expression of TLR2 in the liver was detected by immunohistochemistry. The data was analyzed by SAS software.</p><p><b>RESULTS</b>After 4 hours of intraperitoneal injection of D-Gal/LPS, the serum transaminase and plasma IL-18, TNF-alpha and IFN-gamma levels were elevated. The treated mice began to die at 7 hours. The mortality reached up to 80% at 10 h. TLR2 mRNA was expressed at a low level in liver tissues of normal mice, while it was significantly increased and maintained at a higher level following intraperitoneal injection with D-Gal/LPS. The expression of TLR2 protein was similar to that of the TLR2 mRNA, and the expression of TLR2 mRNA was positively correlated with the concentration of plasma IL-18, TNF-alpha and IFN-gamma (r=0.36, P=0.02; r = 0.48, P 0.003; r = 0.72, P<0.001) at different time points.</p><p><b>CONCLUSIONS</b>Our results showed that TLR2 was involved in initiating and inducing the expression of proinflammation cytokines in this model of fulminant hepatic failure. The results suggest that adjusting the expression of TLR2 might be a new strategy in preventing the development of infectious diseases</p>