Synthesis of 6-benzyl-1-[ (benzyloxy) methyl ]-3-hydroxy-5-(hydroxymethyl) pyrimi-dine-2,4(1H,3H)-dione / 北京大学学报(医学版)

Objective:To find the best synthesis method of 6-benzyl-1-[ ( benzyloxy ) methyl ]-3-hydro-xy-5-(hydroxymethyl)pyrimidine-2,4(1H,3H)-dione e for observing the change of its biological activity after N-3 hydroxylation .Methods:After trying some N-hydroxylation methods , the target compound was successfully synthesized via one-pot oxidizing process by sodium hydride ( NaH) and 3-chloroperbenzoic acid( m-CPBA);the anti-HIV reverse transcriptase ( RT) activity and integrase ( IN) activity of the tar-get compound was assayed via enzyme-linked immunesorbent assay ( ELISA) and phosphorylation of DNA package method .Results:The target compound could be obtained through the improved m-CPBA oxida-tive method by only one step , and the yield of the reaction could reach 60%-70%.And the structure of this compound was identified by 1 H NMR, 13 C NMR and MS;The activity result showed it added the an-ti-HIV IN activity after N-3 hydroxylation as well as retained the anti-HIV RT activity.Conclusion:The improved m-CPBA oxidative method is a convenient and efficient way to prepare the compound 6-benzyl-1-[(benzyloxy)methyl]-3-hydroxy-5-(hydroxymethyl)pyrimidine-2,4(1H,3H)-dione e which has both anti-HIV RT and IN activity .

The value of myocardial enzymes and cerebrospinal fluid examination in diagnosis of hand, foot and mouth disease complicated with SIRS and MODS / 重庆医学

Objective To investigate the value of myocardial enzymes and cerebrospinal fluid examination in diagnosis of hand , foot and mouth disease(HFMD) complicated with systemic inflammatory response syndrome (SIRS) and multi-organ dysfunction syndrome(MODS) .Methods During April 2010 to January 2013 ,204 cases were retrospectively analyzed and checked myocardial enzymes and cerebrospinal fluid examination of the children to analyze the correlation between inspection results and incidence of SIRS and MODS .Results The incidence of SIRS and MODS and mortality rate of severe and critical group was significantly higher than ordinary group(P<0 .05) .CSF protein ,CK-MB ,LDH and cTnT content of SIRS group were significantly higher than non-SIRS group(P<0 .05) .CSF protein ,CK-MB ,LDH and cTnT content of MODS group were significantly higher than non-MODS group(P<0 .05) .Spearman rank correlation analysis showed that CSF protein ,CK-MB and cTnT was positively correlated to inci-dence of SIRS and MODS(P<0 .05 ,P<0 .05) .Conclusion Myocardial enzymes and cerebrospinal fluid examination have a higher value in diagnosis of HFMD complicated with SIRS and MODS .

Influence of SGHWJN particles on mediators of inflammation in esophageal tissues of rat with reflux esophagitis / 中国中药杂志

<p><b>OBJECTIVE</b>To study the influence of SGHWJN particles on inflammation and the mediators of inflammation in esophageal tissues of rat with reflux esophagitis.</p><p><b>METHOD</b>Fifty SD rats were randomly divided into 5 groups, namely, a control group, a sham-operated group, a model group, a SGHWJN particles group and a PPI group. Reflux esophagitis was induced by adopting partial pyloric ligation plus cardiomyotomy. One week later, the rats were orally administered twice daily for 28 days. Pathological changes of esophagus mucous membrane were evaluated by using HE staining and Harry S. Cooper's method in every groups. MDA and SOD contents in esophageal tissues were measured by colorimetric method. Expression of TNF-alpha in esophageal tissues were examined by real-time fluorescent quantitative reverse transcriptase polymerase chain reaction (RT-FQ-PCR) with SYBR Green.</p><p><b>RESULT</b>Model group, esophageal inflammation scores, expression of TNF-alpha in esophageal tissues and MDA contents compared with the normal group and sham operation group were significantly higher (P < 0.05). SOD contents in the esophageal tissues of the model group was significantly lower than that of control group and sham-operated group (P < 0.05). SGHWJN particles group and PPI group of esophageal tissue inflammation scores, expression of TNF-a in esophageal tissues and MDA levels than those in model group decreased significantly (P < 0.05). SOD content was significantly higher than that of model group (P < 0.05), SGHWJN particles group and PPI group showed no statistically significant difference between the above-mentioned indicators. The above-mentioned indicators showed no statistically significant difference between the normal group and sham-operated group. MDA content and expression of TNF-alpha in esophageal tissue was positively correlated with inflammatory scores of model group (r = 0.813). Model group esophageal tissue SOD content and inflammation scores were negatively correlated (r = -0.847). Esophageal tissue SOD levels were negatively correlated with MDA levels (r = -0.863).</p><p><b>CONCLUSION</b>SGHWJN particles can effectively inhibit inflammation in rat with reflux esophagitis through regulating TNF-alpha, SOD and MDA.</p>

Cigu Xiaozhi pills's influence on lipid peroxidation and TNF-alpha expression in liver tissues of rats with nonalcoholic steatohepatitis / 中国中药杂志

<p><b>OBJECTIVE</b>To investigate the effect of Cigu Xiaozhi pills on expression of tumor necrosis factor alpha (TNF-alpha) in rat with nonalcoholic steatoheptatitis (NASH).</p><p><b>METHOD</b>Fifty male SD rats were divided randomly into five groups: the normal group (n = 10), the model group (n = 10), the high dosage group (n = 10) and the little dosage group of the treatment (n = 10), Dongbao Gantai group (n = 10). Rats in normal control group were fed with standard diet. Rats in other four groups were established models of nonalcoholic steatohepatitis and were treated simultaneously with traditional Chinese medicine and positive medicine. Histopathological changes in the liver were observed. The serum ALT, AST, TG, TC and hepatic MDA, SOD, GPX were detected histologically. The expression of TNF-alpha in the liver was determined using the immunohistochemical technique and RT-PCR.</p><p><b>RESULT</b>In model group, extensive adipose degeneration and inflammatory cell infiltration were found in the liver. In treatment groups steatohepatitis were markedly alleviated. Compared with model group, TG, TC, ALT, AST of the serum and MDA of liver tissue were reduced significantly, and SOD, GPX were increased significantly in treatment groups and positive control group (P < 0.05). TNF-alpha was not expressed almost in normal rat liver and was expressed highly in model rat liver. Compared with model group, the TNF-alpha mRNA and protein expression were significantly lower in liver of treatment groups and positive control group (P < 0.05). And the effects of high dosage group surpass than those of Dongbao Gantai group (P < 0.05).</p><p><b>CONCLUSION</b>TNF-alpha plays an important role in NASH pathogenesis. Cigu Xiaozhi pills can effectively treat experimental nonalcoholic steatohepatitis in rats, and its mechanism may be associated with ameliorating hepatocellular steatosis, removing the free radicals and enhancing the capability of anti-oxidation and anti-inflammatory.</p>

Logistic regression analysis on relationships between traditional Chinese medicine constitutional types and overweight or obesity / 中西医结合学报

To explore the relationships between traditional Chinese medicine (TCM) constitutional types and overweight or obesity so as to provide evidence for adjusting constitutional bias and preventing and treating obesity.

Protective and therapeutic effects of Sagittara Sagittifolia L. Xiao-Zhi Pills on nonalcoholic steatohepatitis in rats / 西安交通大学学报(医学版)

Objective To observe the preventive and therapeutic effects of Sagittara Sagittifolia L. Xiao-Zhi Pills on nonalcoholic steatohepatitis (NASH) in rats. Methods Rat NASH models were established and the rats were divided randomly into five groups: the normal group, model group, high-dosage group and low-dosage groups of the treatment, and Dongbao Gantai positive drug group. Histopathological changes of the liver were observed. The levels of MDA, superoxide dismutase (SOD), and NO (nitric oxide) in the liver homogenate were determined. Expressions of cyclooxygenase-2 (cox-2) and inducible nitric oxide synthase (iNOS) in the liver were determined with immunohistochemical technique. Results In model group, extensive adipose degeneration and inflammatory cell infiltration were found in the liver. Compared with those in normal group, SOD activities in model group were obviously decreased (P<0.01), the contents of MDA and NO were obviously increased (P<0.01), and the expressions of cox-2 and iNOS proteins were obviously increased (P<0.01). Compared with those in model group, the activities of SOD in treatment groups were obviously increased (P<0.01), the contents of MDA and NO were obviously decreased (P<0.01), and the expressions of COX-2 and iNOS proteins were obviously decreased (P<0.01). The effect of high-dosage group was more obvious than that of Dongbao Gantai group (P<0.05). Conclusion Sagittara Sagittifolia L. Xiao-Zhi Pills can effectively prevent and treat nonalcoholic steatohepatitis in rats, and its mechanism may be associated with ameliorating hepatocellular steatosis, removing the free radicals and enhancing the anti-oxidation and anti-inflammation capability.

Changes of endocrine and immune function in subjects of yang deficiency constitution / 中西医结合学报

To investigate the changes of endocrine, cyclic nucleotide and immune systems in subjects of yang deficiency constitution, and to explore the relationship among characteristics and causes of yang deficiency constitution, the physiological and biochemical parameters.

Effects of fuzheng yiliu granules on apoptotic rate and mitochondrial membrane potential of hepatocellular carcinoma cell line H22 from mice / 中西医结合学报

OBJECTIVE: To evaluate the effects of Fuzheng Yiliu Granules (FZYLG) on apoptotic rate and mitochondrial membrane potential (Delta psi m) of hepatocellular carcinoma cell line H22 from mice. METHODS: Forty-eight mice inoculated with H22 cells were randomly divided into four groups: untreated group, cyclophosphamide-treated group, high-dose FZYLG-treated group and low-dose FZYLG-treated group. After 14 days of corresponding treatment, H22 cells in each group were stained with propidium iodide, and the apoptotic rates were detected by flow cytometry (FCM). The rhodamine 123 was used as a fluorescence probe to label the H22 cells, and the fluorescence intensities were observed with laser scanning confocal microscope. The fluorescence intensity of H22 cells indicated the Delta psi m of H22 cells. RESULTS: FZYLG could significantly increase the apoptotic rate while reduce the Delta psi m of H22 cells from mice as compared with those in the untreated group. CONCLUSION: The antitumor effects of FZYLR on H22 cells from mice are related to decreasing the Delta psi m and then inducing the apoptosis of the H22 cells.

Experimental study on anti-tumor activity of total hedysarum polybotrys saccharide in vivo / 中华中医药杂志

Objective:To investigate the suppressed e ects of total hedysarum polybotrys saccharide(THPS) alone and THPS combined with Cytoxan(CTX) on tumor-bearing mice and its mechanisms.Method:Kunming mice inoculated with S180 were given low,moderate and high dose THPS and THPS combined with CTX by intraperitoneal injection.Fourteen day later,tumor weight,inhibition rate,thymus index and spleen index were observed.CD4+ and CD8+ lymphocyte were counted though the ow cytometer.Results:Compared with the control,the moderate dose THPS showed signi cantly suppressed e ect on the growth of S180 tumor(P

Effects of Fuzheng Yiliu Granule-medicated serum on apoptosis of liver cancer cells from mice and its mechanism / 中西医结合学报

OBJECTIVE: To study the effects of Fuzheng Yiliu Granule (FZYLG)-medicated serum on apoptosis of liver cancer cells H22 from mice and its mechanism. METHODS: Liver cancer cells H22 from mice were incubated in culture media containing sera from rabbits medicated with different doses of FZYLG. Flow cytometry was used to examine the cell cycle and analyze the apoptotic rate of the H22 cells. The morphological changes of the H22 cells were observed by transmission electron microscope and the apoptosis related proteins Bcl-2 and Bax were examined by streptavidin-biotin peroxidase complex (SABC) method. RESULTS: FZYLG-medicated serum could influence the cell cycle and stop the proliferation of H22 cells at the G(1)/G(0) phase with apoptotic peak being detected. In culture media with FZYLG-medicated sera, the expression of Bcl-2 decreased while that of Bax increased as compared with that in culture medium with non-medicated serum (P<0.05). CONCLUSION: FZYLG-medicated serum can induce apoptosis of the liver cancer cells H22 by influencing the cell cycle, down-regulating the expression of Bcl-2 and up-regulating the expression of Bax.

The expression and significance of IL-23/IL-17 axis in esophageal tissues of rats with reflux esophagitis / 西安交通大学学报(医学版)

Objective To detect the expressions of interleukin-17(IL-17) and interleukin-23(IL-23) in esophageal tissues of rats with reflux esophagitis(RE) and explore the role of IL-23/IL-17 axis in the pathogenesis of RE.Methods Thirty SD rats were randomly divided into 3 groups,namely,control group,sham-operated group and model group.RE was induced by adopting partial pyloric ligation plus cardiomyotomy.Then rats in each group were fasted for 24 h but had free access to water.They were fed 24 h after operation.Four weeks later,rats were killed and pathological changes of esophagus mucous membrane were observed by HE staining in each group.The expressions of IL-23p19 and IL-17 mRNA in esophageal tissues were examined by real-time fluorescent quantitative reverse transcriptase polymerase chain reaction(RT-FQ-PCR).IL-17 protein content in esophageal tissues was measured by ELISA.Results After four weeks,compared with control group,model group had significant pathological changes of esophagus mucous membrane.Expressions of IL-23p19 and IL-17 mRNA in the esophageal tissues of model group were significantly higher than those of the other two groups;the content of IL-17 protein was significant higher in model group than in the other two groups.There were no significant differences between control group and sham-operated group.Conclusion IL-23/IL-17 axis is an important cellular factor involved in the pathogenesis of RE and may be involved in the chronic inflammation of RE.

Effects of Fuzheng Yiliu Granule on expression of CD44v6 and nm23-H1 in esophageal carcinoma treated with radiotherapy / 中西医结合学报

OBJECTIVE: To evaluate the effects of Fuzheng Yiliu Granule on the expression of CD44v6 and nm23-H1 in esophageal carcinoma treated with radiotherapy. METHODS: Sixty-three cases of esophageal carcinoma were randomly divided into two groups: Fuzheng Yiliu Granule plus radiotherapy treated group (n=30) and radiotherapy treated group (n=33). The carcinoma specimens were obtained through endoscopic biopsy before and after twenty-one days of treatment. The expression of CD44v6 and nm23-H1 was determined in the sixty-three specimens of esophageal carcinoma by immunohistochemical SABC methods. RESULTS: After twenty-one days of treatment, the positive rates of CD44v6 in the Fuzheng Yiliu Granule plus radiotherapy treated group and the radiotherapy treated group were 40.0% and 69.7%, respectively, and there was significant difference between the two groups (P0.05). CONCLUSION: Fuzheng Yiliu Granule can lower the expression of CD44v6 in esophageal carcinoma, and may prevent infiltration and lymph node metastasis of esophageal carcinoma.

Protective and therapeutic effects of Sagittara Sagittifolia L.Xiao-Zhi Pills on nonalcoholic steatohepatitis in rats / 西安交通大学学报(医学版)

Objective To observe the preventive and therapeutic effects of Sagittara Sagittifolia L.Xiao-Zhi Pills on nonalcoholic steatohepatitis(NASH) in rats.Methods Rat NASH models were established and the rats were divided randomly into five groups: the normal group,model group,high-dosage group and low-dosage groups of the treatment,and Dongbao Gantai positive drug group.Histopathological changes of the liver were observed.The levels of MDA,superoxide dismutase(SOD),and NO(nitric oxide) in the liver homogenate were determined.Expressions of cyclooxygenase-2(cox-2) and inducible nitric oxide synthase(iNOS) in the liver were determined with immunohistochemical technique.Results In model group,extensive adipose degeneration and inflammatory cell infiltration were found in the liver.Compared with those in normal group,SOD activities in model group were obviously decreased(P

Protection of ultra-filtration extract mixture from Angelica sinensis and Hedysarum polybotrys on oxidative damage in cardiomyocytes of neonatal rats and its mechanism / 中草药

Objective To investigate whether the administration of the ultra-filtration extract mixture from Angelica sinensis and Hedysarum polybotrys is able to protect cardiomyocytes from oxidative injury of rats induced by H2O2 and its potential mechanism. Methods Myocardial cells from 2—3 d neonatal rats were cultured in DF medium and the cellular injury was induced by H2O2. The ultra-filtration extract mixture from A. sinensis and H. polybotrys was given in three doses of 3.75,7.5,and 15 mg/mL. Morphological changes of cardiomyocytes were observed by microscope. Survival rate of myocardial cells was assessed using MTT. The cardiomyocyte damages were estimated by detecting lactate dehydrogenase (LDH) and creatine kinase (CK) releases in the medium,superoxide dismutase (SOD) activities and intracellular malondialdehyde (MDA),and myeloperoxidase (MPO) contents. The levels of caspase-3 and hsp70 expression in cardiomyocytes were measured by RT-PCR. Results The ultra-filtration extract mixture could protect the cardiomyocytes from H2O2 injury in a dose-dependent manner (3.75,7.5,and 15 mg/mL). The ultra-filtration extract mixture could significantly decrease LDH and CK leakages and intracellular MDA and MPO contents,increase SOD activity,upregulate hsp70 expression,and downregulate caspase-3 expression. Conclusion The ultra-filtration extract mixture has protection on cardiomyocytes injured by H2O2 through improving cell antioxidant ability,upregulating hsp70 expression,and inhibiting caspase-3 activity.

Observation on Gastroscopic and Histopathologic Effect of Chronic Gastritis Treated on the Basis of Differentiation of Zheng ( Syndrome) / 中医杂志

Both Jianpi Wenwei and Shugan Hewei Decoctions can markedly improved the naked eye changes, histopathologic changes inhibition of Hp growth, and bile regurgitation under gastroscopy. Stereo -determination of the thickness of gastricmucosa was made before and after treatment. The result showed that thethickness was markedly increased after treatment.

Chromatography fingerprint of Baitiao Radix Codonopsis in Gansu Province by HPLC / 中成药

AIM To establish chromatography fingerprint of Radix Codonopsis. METHODS HPLC was applyed on a Hypersil ODS column with water-methanol gradient elution, flow-rate of 0.8 ml?min -1 . Determination of content of atractylenodie Ⅲ adopted ELSD and PAD with methanol-water(67∶ 33), flow-rate of 1.0 ml?min -1 , column temperature at 30?C , ELSD:carried-gas flow-rate of 2.2 L?min -1 , drift-tuber temperature was 80?C ;PAD:wavelength was 220 nm. RESULTS 25 common peaks were picked up, their similarity among 10 batchs of samples was more than 98.12 % based on marker composition(Atractylenolide Ⅲ). CONCLUSION The chromatography fingerprint of Baitiao Radix Codonopsis could be used as their characteristic chromatography fingerprint of hydrophobic fraction.

Determination of formononetin and calycosin from Zhengqifuzheng Preparation by HPLC / 中成药

AIM: To establish a method of RP-HPLC for determination of calycosin and formononetin in Zhengqifuzheng Preparation(Radix Astragali, Fructus Ligustri Lucidi, etc.). METHODS: Kromasil ODS column(5?m,4.6mm?250mm) was used to determine two isoflavoniods with water-methanol gradient elution, at column temperature of 25℃, flow-rate of 1.0mL?min -1 and detection wavelength at 254nm. RESULTS: The average recoveries of formononetin and calycosin in Zhengqifuzheng Capsules were 96.53% and 98.34% and RSD were 2.25% and 4.01%, respectively, the average recoveries of formonoenetin and calycosin in Zhengqifuzheng Granules were 97.20% and 95.65% and RSD were 2.66% and 2.32%, respectively. CONCLUSION: The method is sample, reliable, accurate, practical, and can provid a new idea to study the quality standard of this preparation.

Clinical effect of Fuzheng Jiedu Granule combined with western medicine on 60 patients with coronary heart disease long-term exposed to nickel / 中成药

AIM:To evaluate the clinical effect of Fuzheng Jiedu Granule(Radix Hedysari,Poria,Radix Angelicae sinensis,Fructus Forsythiae,Rhizoma Curcumae,Radix et Rhizoma Salviae miltiorrhizae,etc.) on patients with coronary heart disease who have longterm contact with nickel,and observe its influence on the level of Creatine kinase(CK),Lactate dehydrogenase(LDH),Na~+-K~+-ATPase,Ca~(2+)-ATPase in RBC membrane,Nitric oxide(NO),Nitric oxide synthase(NOS),Nickel(Ni) in serum. METHODS: 60 cases were divided into two groups A and B randomly.30 cases in group A were treated with Fuzheng Jiedu Granule combined with western medicine Betaloc and Isosorbide Dinirrate;30 cases in group B were given only western medicine.The period of treatment was 4 weeks.Another 15 healthy cases selected as group C(healthy control group).Before and after treatment,the clinical effects were observed,meanwhile,some biochemical indexes such as CK,LDH,Na~+-K~+-ATPase,Ca~(2+)-ATPase in RBC membrane,NO,NOS,Ni in serum were measured with clinic test methods.Finally,the experimental results were compared and analyzed in the three groups mentioned above. RESULTS: The therapeutic effect of symptoms and signs of group A was superior to that of group B(P