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Eight 1,6-O,O-diacetylbritannilactone (OABL) derivatives (compounds 1-8) were synthesized by esterification or reduction of 1-O-diacetylbritannilactone (ABL) isolated from Inula japonica.All derivatives were evaluated for their anti-inflammation activities through the determination of inhibition of nitric oxide (NO) production in lipopolysaccharide (LPS)-induced macrophages.As results,compounds 5-8 (IC50 ＜ 2 μmol/L) exhibited more potent inhibition of NO production activities than the lead compound OABL.
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AIM: To analyze the effect of pigment epithelium derived factor (PEDF) on nitrogen monoxide (NO) and expression of cysteine-containing, aspartate-specific proteases-3 (caspase-3) in retinal tissues of model rats with optic nerve crush injury.METHODS: A total of 60 SD rats were randomly divided into the blank control group, model group and PEDF group, with 20 rats in each group.Except the blank control group, the optic nerve crush injury rat models were established in the other groups, and left eyeballs were taken as samples.After successfully modeling, the model group were treated with intravitreal injection of 5μL of balanced salt solution while PEDF group were treated with intravitreal injection of 5μL of PEDF (0.2μg/μL).Two weeks later, the retinal tissues were collected, and changes of shape were observed under microscope after HE staining.The changes of NO level were measured by colorimetry assay, the expression of caspase-3 mRNA and caspase-3 protein was detected by reverse transcription-polymerase chain reaction (RT-PCR) and Western-blot.RESULTS: HE staining showed that retinal tissues of the blank control group arranged neatly and clearly.Retinal ganglion cells (RGCs) arranged in a monolayer, and cells were oval, uniform in size and distribution, the cell nuclei were clear, closely arranged, with clear boundaries.The retinal tissues of the model group were sparse in shape, RGCs showed vacuolar changes, the overall number of cells was reduced, and cell nuclei of residual RGCs showed pyknosis and uneven staining.RGCs in PEDF group were with slightly edema and arranged closely, and the degree of injury was significantly milder than that in the model group.Levels of Caspase-3 mRNA and protein and NO levels in the three groups showed the model group > PEDF group > blank control group (all P < 0.05).CONCLUSION: The application of PEDF can down regulate the expression of Caspase-3 and NO in rates with optic nerve injury and reduce RGCs injury.
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Objective: To explore the high dose atorvastatin reducing contrast induced nephropathy (CIN) rate in patiens with emergent percutaneous coronary intervention (PCI) via improveing heat shock protein-90 (HSP90) expression with its possible mechanism. Methods: A total of 158 STEMI patients with emergent PCI in our hospital were studied. The patients were randomly divided into 2 groups: High dose atorvastatin group, the patients received pre-operative atorvastatin 40 mg,n=80 and Control group, the patients received pre-operative placebo,n=78. The serum creatinin (Scr), creatinine clearance rate (Ccr), blood urea nitrogen (BUN), superoxide dismutase (SOD), malondialdehyde (MDA), nitrogen monoxide (NO), HSP90 mRNA expression and protein concentration and urine α1-microglobulin were examined in all patients and the incidence rates of CIN were compared between 2 groups. Results: Compared with Control group, High dose atorvastatin group had drcreased Scr (68.92 ± 8.80) μmol/L vs (77.25 ± 13.36) μmol/L, MDA (3.88 ± 0.53) nmol/L vs (4.08 ± 0.52) nmol/L and urine α1-micrglobulin (1.38 ± 0.36) mg/dl vs (1.89 ± 1.13 ) mg/dl; increased Ccr (89.71 ± 9.85) ml/min vs (77.28 ± 13.78) ml/ min, SOD (129.52 ± 30.63) U/ml vs (117.66 ± 27.98) U/ml, NO (66.23 ± 29.26) μmol?gprot vs (55.12±27.43) μmol?gprot, allP<0.05. Compared with Control group, High dose atorvastatin group presented higher post-operative HSP90 mRNA expression (0.466 ± 0.158) vs (0.224 ± 0.278 ) and protein concentration (1259.83 ± 121.17) pg/ml vs (1195.0 ± 127.65) pg/ml, allP<0.05. The incidence rate of CIN was lower in High dose atorvastatin group (2.5%) than Control group (10.3%),P<0.05. Conclusion: A high dose atorvastatin administration before emergent PCI may decrease CIN occurrence rate. Atorvastatin may promote HSP90 expression, increase NO produciton, then improve the vascular endothelial function and anti-oxidative ability to protect the renal function in STEMI patients.
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Objective: To evaluate the in vitro effects of different combinations of the active fractions in Yaotongning Capsule (YTNC) on anti-inflammation, immunity, and activating blood circulation, and the interactions among these active fractions. Methods: Six samples were prepared by adding flavonoids, saponins, volatile oils/aqueous extracts, and polysaccharides, which were extracted from the material medicines in YTNC, to the alkaloids of Strychnos nux-vomica (Ma Qian Zi) and Ephedra sinica (Ma Huang) in turn according to the formulating principle of YTNC, combination chemistry concept, and their importance in the formula. The effects of the six samples on the production of lipopolysaccharide (LPS)-induced prostaglandin E2 (PGE2) in Ana-1 cells, concanavalin (ConA)- induced interleukin-2 (IL-2) in splenocyte, and nitrogen monoxide (NO) in human umbilical vein endothelial cells (HUVEC) were explored by detecting their half-maximal inhibitory concentration (IC50) or half-maximal effective concentration (EC50). An innovative method based on least square optimization was applied to calculate the additive IC50/EC50 value of each sample. The interactions of the active fractions in these samples were investigated by comparing the additive IC50/EC50 values with the corresponding experimental IC50/EC50 values. Results: All the six samples could inhibit the production of PGE2 and promote the secretion of IL-2 in the investigated concentration range. Only sample III consisting of the alkaloids, flavonoids, and saponins from YTNC had the EC50 value of promoting NO production. Moreover, the sample also displayed excellent activities in the three models of LPS-induced PGE2 production, ConA-induced IL-2 production, and NO production, which could reflect the capability of anti-inflammation, enhancing the body's immunity, and activating blood circulation, respectively. Different combination of the active fractions from YTNC produced the different interaction types in the three models. And the active fractions in sample III, i.e., the alkaloids, flavonoids, and saponins from YTNC, generated high synergistic effects in all the three models. Conclusion: All the six samples derived from the different combination of the active fractions from YTNC show the good activity of inhibiting PGE2 production and promoting IL-2 secretion. Therefore, the YTNC formula is reasonable and has good activity of anti-inflammation and immunity. However, the YTNC formula still could be improved by reducing the categories of its active fractions because the combination of the alkaloids, flavonoids, and saponins exerted better activities than the other samples and the three kinds of active fractions produced an excellent synergistic effect in all the three models. Synthetically evaluating various activities of YTNC in the present work may lead to develop new Chinese materia medica for rheumatic arthralgia treatment, which is more effective and easily controllable in quality.
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Objective To set up the molecular cytobiological model of endogenous coagulation factor Ⅷ (FⅧ) re-expressing in human liver cells L02,and to study the regulation pathway and molecular basis of the re-expression of FⅧ in L02 cells activated by NO signal.Methods The L02 cells at logarithm growth phase were selected and randomly divided into blank control group and experimental group, inhibitor group and inhibitor control group;they were cultured for 0,12,24,36,48,and 60 h.Flow cytometry was used to detect the expression of human FⅧ protein in L02 cells after treated for 48 h.Griess experiment was performed to detect the levels of NO in L02 cells at different time points;the transcription levels of human FⅧ gene,iNOS gene,NF-κB1 gene and I-κB alpha gene were detected by RT-PCR method.Western blotting method was used to detect the expression levels of human phosphorylated I-kappaB (phosphorylated I-κB)in L02 cells.Results The results of flow cytometry showed that the expression of human L02 FⅧ protein was found after treated with L-arginine for 48 h. The Griess results showed that the levels of NO in L02 cells in experimental group were significantly increased at 3,6,12,and 24 h (P<0.05)and the levels of NO in blank control group,inhibitor group and inhibitor control group had no changes. The RT-PCR results showed that the transcription of human FⅧ mRNA in L02 cells was found in experimental group,but there was no transcription of human FⅧ mRNA in blank control group,inhibitor group and inhibitor control group;the transcription levels of iNOS,NF-κB1 and I-κB alphain experiment group were increased(P<0.05)and the transcription levels of these genes in blank control group,inhibitor group and inhibitor control group had no changes. The Western blotting results showed that after adding L-arginine the expression level of phosphorylated I-κB was significantly increased (P < 0.05 ), other groups had no such change. Conclusion L-arginine can activate the phosphorylation of I-κB by NO signal pathway to lead to the changes in the expression of human FⅧ gene promoter upstream regulatory-related transcription factors NF-κB to activate the expression of human FⅧ in human liver cells L02.
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Objective To research photoelectric facial blood flow volume characteristic of premature coronary heart disease of heart blood stasis syndrome (HBSS) and phlegm syndrome (PS), and its relation with NO and ET. Methods Patients of premature coronary heart disease of HBSS (36 cases) and PS (35 cases) were selected, with 31 health people as control. The parameter of photoelectric facial blood flow volume was detected with GD-3 photoelectric blood stream plethysm (PBSP) of the facial color-diagnosis. NO was determined by nitrate reductase method and ET was determined by RIA. Results Hb, He, Hf, Hb/Tab and Hf/Hb of HBSS decreased obviously compared with the control (P
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Objective To study the influence of Yin-nourishing Qi-tonifying and blood-activating recipe(养阴益气活血方) on anticoagulation and fabrinolysis of cultured human umbilical vein endothelial cells(HUVEC).Methods Yin-nourishing Qi-tonifying blood-activating recipe was composed of three equal proportions of Radix Rehmanniae(生地黄),Radix Astragali(黄芪) and Rhizoma Chuanxiong(川芎);blood-activating recipe(活血方)contains Rhizoma Chuanxiong only.Serology pharmacology method was used to observe the effects of Yin-nourishing Qi-tonifying and blood-activating recipe on anticoagulation and fabrinolysis of cultured endotheliocytes of human umbilical vein.Results Compared with control group,both Yin-nourishing Qi-tonifying blood-activating and blood-activating recipes could obviously increase the content of 6-keto-prostacyclin 1?(6-keto-PGF1?) in HUVEC((412.5?42.7)ng/L and(231.7?30.1)ng/L vs.(137.6?13.5)ng/L),promote the activity of tissue plasminogen activator(t-PA)((0.920?0.072)kU/L and(0.679?0.062)kU/L vs.(0.516?0.052)kU/L),and inhibit the activity of tissue plasminogen activator inhibitor(PAI)((0.622?0.071)kAU/L and(0.851?0.085)kAU/L vs.(0.934?0.076)kAU/L),decrease the content of endothelin(ET)((35.7?4.9)ng/L and(46.8?5.1)ng/L vs.(58.6?6.2)ng/L),and increase the content of nitrogen monoxide(NO)((21.68?2.26)mmol/L and(15.15?1.73)mmol/L vs.(8.67?1.24)mmol/L) of cultured HUVEC(P
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Objective: To investigate the protective effect and its mechanisms of Jiusuyu on gastric mucosa of acute alcoholism mice.Methods: Acute alcoholism mouse models were set up by intragastric administration of 56? Hongxing Erguotou wine,compared with Gehuajiecheng liquid,the effect of Jiusuyu on gastric mucosa pathological histology,SOD、MDA、NO and ET-1 of acute alcoholism mice were observed.Results: The gastric mucosa of mice in model group appeared obvious bleeding,fester and ulcer;a lot of phlegmonosis cells infiltrating could be seen below mucosa.At the same time the activity of SOD and level of NO in gastric mucosa were decreased(P
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Objective:To compare the effect between benazepril and candesartan combination and single medication in either one of them for treatment of hypertension-combined with microalbuminuria(MCA). Methods:A total of 95 patients were divided into three groups.Benazepril group(n=31),patients were treated with Benazepril 10～20 mg/day;Candesartan group(n=32),patients were treated with Candesartan 4～8 mg/day;and Combination group (n=32),patients were treated with benazepril 10 mg/day and candesartan 4 mg/day.The medication lasted for 8 weeks.Blood pressure(BP),plasma urinary albumin and creatinine ratio(A/C),endothelin-1(ET-1),nitrogen monoxide(NO)and potassium were examined and compared before and after the medication respectively. Results:The levels of BP,plasma A/C and ET-1 were decrease and NO was increased in all three groups(P0.05,respectively). Conclusion:Effect of benazepril and candesartan combination in patients with hypertension-combined microalbuminuria was better than single medication in either benazepril or candesartan.
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AIM:To study the effects of isoproterenol (Iso) on cardiac fibrosis and related cytokines in rats. METHODS:20 SD rats were divided into control and Iso group in random, with 10 rats each group. After injected Iso, cardiac histology was observed and cardiac function, collagen volume fraction (CVF), content of collagen protein and the concentrations of Angiotensin Ⅱ (Angll) and nitrogen monoxide (NO) were measured in the two groups. RESULTS:Compared with control group, microscopic examination showed that fibrosis increased in Iso group. Iso did decrease cardiac function and NO levels and increase CVF, content of collagen protein and AngII levels. Left ventricular pressure maximal rate of rise (+ dp/dt_(max)) and left ventricular systolic pressure (LVSP) were not significantly different from that of control group. CONCLUSIONS:Iso can induce myocardial fibrosis and change levels of related cytokines in rats.
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Objective To explore the relationship of neuron injury and its severity with the cause and the duration of convulsion Methods Patients were divided into 5 groups or 3 groups according to the causes of convulsion or duration of convulsion in children The levels of neuron specific enolase(NSE) and nitrogen monoxide and nitricoxide synthase(NO/NOS) in serum and cerebrospinal fluid(CSF) were tested by ELISA and spectrophotography at different time points after convulsion in children Results The levels of NSE and NO/NOS in serum and CSF of all objective groups except the febrile convulsion group were apparently higher than those in control group( t =15 4～47 7, P
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AIM: To study the protective effect and mechanism of melatonin on learning and memory in mice with repeated cerebral ischemia and reperfusion and its mechanism. METHODS: The models of repeated cerebral ischemia reperfusion were established in mice. The function of learning and memory was tested by the electric mare method, and the concentrations of MDA and NO were measured by colorimetric method and nitric reduction method in brain tissue. RESULTS: MT could obviously improve the function of learning and memory of model mice, inhibit cerebral dropsy, and lower the content of MDA and NO in cerebral tissue. CONCLUSION: MT shows significantly protective effect against repeated ischemia reperfusion injury in mice, and the mechanism might be related to inhibit the rise of MDA and NO in brain tissue.
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Objective To investigate effect of Irbesartan on plasma endothelin-1 (ET-1) and nitrogen monoxide (NO) in elderly patients with moderate to severe essential hypertension.Methods Forty patients with essential hypertension who were ≥60 years of age and had been treated with two or more antihypertensive drugs but whose systolic pressure were ≥160 mmHg and or whose diastolic pressure were ≥100mmHg,entered into the present study. Irbesartan 150mg daily was added to their original treatment for 6 week. ET-1 and NO were measured before and 6 week after treatment.used forty-two healthy adults as controls. Results In the treatment group,ET-1 was significantly decreased and NO was significantly increased after 6 weeks,addition of Irbesartan.As compared with controls,ET-1 of treatment group was higher both before and after addition of Irbesartan ( P
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0.05). Compared with the sham operative group, NO content in model group was obviously lower( P
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Objective To explore the effects of alcohol on NO concentration in plasma and activity of ATP enzyme in erythrocytes of rabbits. Methods 32 rabbits were divided into groups and treated with alcohol, injected intravenously, at the doses of 0.5 g/kg, 1.0 g/kg and 1.5 g/kg, 15 minutes after treatment, the blood samples were collected and NO concentration in plasma, activity of ATP enzyme in erythrocytes were determined. Results NO concentration in plasma of rabbits significantly decreased in 0.5 g/kg and 1.0 g/kg groups, but increased in 1.5 g/kg group (P
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AIM: To study the effect of puerarin (Pue) on related cytokines in myocardial hypertrophy induced by isoproterenol (Iso) in rats. METHODS: 40 SD rats were randomly divided into 4 treatments groups: control group, Iso group, Iso+Pue group (Pue group) and Iso+Captoril (Cap) group (Cap group), with 10 rats each group. Ratio of ventricle weight to heart weight, cardiomyocyte diameter, plasma and myocardial tissue NO, ET and Ang Ⅱ levels were measured. RESULTS: Compared with the control group, Iso did induce significant changes in cardiac hypertrophy (P
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OBJECTIVE:To investigate the influence of nitrogen monoxide(NO) donor,sodium nitroprusside(SNP),on mRNA expression of sodium/iodide symporter(NIS) in thyrocyte membrane cultured in vitro in order to interpret molecular mechanism that NO inhibits the uptake of iodide.METHODS:The effect of SNP at different concentrations(0,10-6,10-5,10-4,10-3 mmol?L-1) on mRNA expression of NIS in thyrocyte by using cell culture method and RT-PCR with optical density ratio of NIS/?-actin as index.RESULTS:Optical density ratio of NIS/?-actin in each group decreased in order after treated with SNP(0,10-6,10-5,10-4,10-3 mmol?L-1).NO inhibited mRNA expression of NIS in a dose-dependent manner(P
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Objective To observe the effect of PM2.5 on the secretion of NO, ET-1 and the proliferation of rat vascular smooth muscle cell(VSMC) in vitro.Methods VSMCs were treated with PM2.5 collected from urban area of Zhanjiang,at the doses of 10,20,50,100 and 200 ?g/ml.After 24 hours of treatment, the levels of NO and ET-1 in the VSMCs were detected by nitrate reductase method and radioimmunoassay respectively, the proliferation of VSMCs was detected by MTT.Results At the concentrations of 10-200 ?g/ml, with PM2.5 increased, the level of NO in VSMCs decreased from(43.53 ?3.46)?mol/L to(29.28?2.28)?mol/L(F=18.89,P