To search for bioactive compounds from the flower disc of Helianthus annuus L.,chromatography was used to isolate and purify the chemical constituents, their structures were identified by spectral analysis, MTT method was applied to investigate their cytotoxic activities, some compounds showed moderate cytotoxic activities on SF-268, MCF-7 and HepG2 cell lines. Eleven compounds were obtained from the flower disc of H. annuus, and identified as ent-kaurane-2o, 16α-diol ( 1 ) and entkaurane-15α, 16α-epoxy-17-al-19-oic acid (2), and nine known diterpenes, ent-kaurane-16β-ol (3),phyllocladan-16β-ol (4) , ent-atisan-16α-ol ( 5 ) , grandifloric acid ( 6 ) , angeloylgrandifloric acid ( 7 ) ,ent-kaurane-16-en-19-oic acid (8), ent-kaurane-17-hydroxy-15-en-19-oic acid (9), ent-kaurane-16β,17-dihydroxy-19-oic acid (10), and ciliaric acid (11). Compounds 1 and 2 are new compounds, some compounds showed cytotoxic activities on SF-268, MCF-7 and HepG2 cell lines.

Acclimatization ; physiology ; Animals ; Animals, Newborn ; Chickens ; Cold Temperature ; Endocrine Glands ; physiology ; Female ; Male ; Rats ; Rats, Wistar

The relation of obesity with food components, genetic factors and life style were explored in obesity group (212 cases) and normal group (212 subjects). The result revealed close relationships among food components, life style or genetic factors and obesity. The food components and life style consisted of high fat and sugar, high salt diet, drinking, smoking and sedentary work. Parents with obesity conferred another factor.

Objective·To investigate the effects of interleukin-1β (IL-1β) on neonatal rat alveolar arrest induced by intra-amniotic injection of lipopolysaccharide (LPS). Methods·A neonatal SD rat model of bronchopulmonary dysplasia (BPD) was constructed by intra-amniotic injection of LPS in pregnant rats. The pregnant rats (E19) were randomly assigned to Saline group, LPS group and LPS+anti-IL-1β group. The lungs of the neonatal rats were randomly collected 1, 3 and 7 days after birth. Pathological changes in the lungs were observed by hematoxylin-eosin (H-E) staining, and expression of IL-1β mRNA and protein was detected by real-time PCR and ELISA, respectively. Rat bone marrow derived primary macrophage was cultured in vitro, and given LPS intervention, then genes related with IL-1β were detected through whole transcriptome sequencing. Results·Compared with the Saline group, the alveolar counts and secondary septa counts significantly decreased, and mean liner intercept significantly increased in LPS group. Moreover, the expression of IL-1β mRNA and protein in lungs significantly increased in LPS group. The LPS-induced pathological changes of lung tissues in neonatal rats were improved by anti-IL-1β. LPS could up-regulate the expression of genes including Gbp5, Ccl3, Nod2, Ccr5, Mefv, Casp4 and Ifnar1, but down-regulate Lgals9 and Gstp1. Among these genes Gbp5, Ccl3, Nod2, Ccr5, Casp4, Ifnar1 and Lgals9 could positively regulate IL-1βproduction. Conclusion·LPS can induce alveolar arrest through up-regulating the expression of IL-1β in macrophages in neonatal rat BPD model. Whole transcriptome sequencing reveals that LPS can regulate the expression of IL-1β in macrophages through several paths.

AIM To substantiate the therapeutic effects of carbonate buffer mixture on naturally occurring gastrointestinal atony in cattle. METHODS Therapeutic effects of carbonate buffer mixture (Na2CO3 50 g, NaHCO3 420 g, KCI 20 g, NaCI 100 g, water 10 L) were observed in 120 cases of gastrointestinal atony including forestomach atony, rumen impaction, rumen acidosis, omasum impaction and intestinal constipation. RESULTS Average cure rate of carbonate buffer mixture on abovementioned diseases was 95 %, and average dose was 1.4-0. 5. CONCLUSION Being a new approach for treatment of gastrointestinal atony in ruminants, the carbonate buffer mixture can eliminate the gastrointestinal atony originated from the over acidity in gastrointestinal canal.

Objective To understand the ammonia pollution level in indoor air in Chengdu city,China.Methods 50 newly decorated houses included resident houses,offices and public places were selected in Chengdu city.The national standard method of China-Berthelot spectrophotometry was used to determine the concentration of ammonia in indoor air.Results The result showed that the average concentration of ammonia was 0.307 mg/m3,the rate of exceed standard limit was 58.33%,the highest concentration was 0.598 mg/m3,which was almost three times of the national standard limit.At 4 months after decoration,the concentration of ammonia decreased near to the national standard limit(0.20 mg/m3).Conclusion As the time goes on,the concentration of ammonia in indoor air shows a downtrend,and in general,it will reach to the safe level in 4 months after decoration,so it is suggested to move in the newly decorated houses after five months since the decoration finished will be better for human health.

The effectiveness and safety of acupuncture combined with western medicine for angina of coronary artery disease are evaluated. Databases including Pubmed, Embase, Cochrane Library, CBMDisk,. CNKI, Wanfang, Chinese Clinical Trial Registry, etc. are searched with search time from beginning of the database establishment to January of 2014. As a result, totally 15 articles of acupuncture for angina of coronary artery disease that met the inclusive criteria were collected, involving 11 researches and 1 232 patients. The results of Meta-analysis indicate that based on regular western medicine, additional use of acupuncture could further improve symptoms of angina, increase efficacy of electrocardiogram (ECG) and reduce the dosage of nitroglycerin, in the meanwhile the hemorheology could be ameliorated, and the contents of C reactive protein (CRP), malondialdehyde (MDA), lipid peroxide (LPO), endothelin (ET) could be reduced, while the contents of superoxide dismutase (SOD) and nitric oxide (NO) could be increased; besides, the occurrence rate of cardiovascular event could be reduced without causing obvious adverse events. Except for certain outcomes (including dynamic ECG and blood viscosity) those have no statistical significance between treatment group and control group, the differences of remaining outcomes are: statistically significant. It is believed that acupuncture combined with regular treatment of western medicine are effective treatment plan for angina of coronary artery disease, which are superior to regular treatment of western medicine, but the results of this systematic review be taken with caution, and more clinical trials with high quality are looking forward to be included into Meta-analysis to increase the level of evidence.
Acupuncture Therapy ; Combined Modality Therapy ; Coronary Artery Disease ; drug therapy ; therapy ; Female ; Humans ; Treatment Outcome

Objective To determine if pregnancy affects the toxicity of bupivacaine and to investigate the effect of Shenfu injectio,a preparation of Chinese herbal medicine,on central nervous system and cardiac toxicity of bupivacaine in pregnant rats.Methods Twenty-four SD rats weighing 320-360 g were assigned to 3 groups(n =8 each):Ⅰ non-pregnant control group,Ⅱ pregnant control group and Ⅲ Shenfu injectio pretreatment group. The animals were anesthetized with isoflorane(2%-4%)-O_2 inhalation which was stopped before bupivacaine infusion was started.Femoral artery was canunlated for MAP monitoring and blood sampling and femoral vein was cannulated for bupivacaine infusion.MAP,HR and ECG were continuously monitored.All animals in the 3 groups received continuous infusion of 5% bupivacaine at 2 mg?kg~(-1).min~(-1).In group Ⅲ Shenfu injectio 10 ml?kg~(-1) was injected intraperitoneally(IP)30 min before bupivacaine infusion whereas in the two control groups(group Ⅰ and Ⅱ)equal volume of normal saline was injected IP instead of Shenfu injectio.The duration between the beginning of bupivacaine infusion and onset of convulsion/arrhythmia(QRS≥90 ms)/asystol was recorded and the amount of bupivacaine infused was calculated.Results There was no significant difference in the amount of bupivacaine causing convulsion and asystol between group Ⅰ and Ⅱ but the amount of bupivacaine causing arrhythmia was significantly larger in group Ⅰ(non-pregnant) than in group Ⅱ(pregnant control group)(P＜0.05).The amount of bupivacaine causing convulsion,arrhythmia and asystole was significantly larger in Shenfu injectio pretreatment group(group Ⅲ)than in pregnant control group(group Ⅱ)(P＜0.05 or 0.01).Conclusion Bupivacaine- induced cardiotoxicity is increased in pregnant rats and Shenfu injectio pretreatment can reduce the systemic toxicity of bupivacaine in pregnant rats.

A series of novel sorafenib analogues were designed and synthesized. The cytotoxic activities of these compounds were tested in four tumor cell lines. Some of the compounds showed potent antiproliferative activity against the tested cell lines with IC50 = 4-20 micromol x L(-1). Some compounds demonstrated competitive antiproliferative activities to sorafenib against tested cancer cell lines. Among them, compound 7c demonstrated significant inhibitory activities on ACHN, HCT116 and MDA-MB-231 cell lines with IC50 values of 9.01, 4.97, 6.61 micromol x L(-1), respectively.
Antineoplastic Agents ; chemical synthesis ; chemistry ; pharmacology ; Cell Line, Tumor ; Cell Proliferation ; drug effects ; Humans ; Inhibitory Concentration 50 ; Molecular Structure ; Niacinamide ; analogs & derivatives ; chemical synthesis ; chemistry ; pharmacology ; Phenylurea Compounds ; chemical synthesis ; chemistry ; pharmacology ; Structure-Activity Relationship

The aim of this study is to evaluate anti-tumor activities and mechanism of a novel kinase inhibitor ZLJ213 which targeted Aurora A and vascular endothelial growth factor receptor (VEGFR) in vitro and in vivo against human colon cancer. Results showed that ZLJ213 inhibited cell proliferation and induced cell cycle arrest and apoptosis of HCT1 16 and SW48 cell lines. In HCT116-derived xenograft, ZLJ213 dosed at 100 mg · kg(-1) inhibited tumor growth by 73.24%. The IC50 of ZLJ213 on the expression of p-Aurora A was 0.258 µmol · L(-1) analyzed by ELISA. Under the concentration of 0.08 µmol · L(-1), ZLJ213 could inhibit the activities of Aurora A, Histone H3 and VEGFR of HCT116 and SW48 cell lines. Simultaneously, ZLJ213 induced activation of Caspase 3 and PARP cleavage. Above data suggested that ZLJ213 had the ability to inhibit cell proliferation and induce cell apoptosis both in vitro and in vivo in colon cancer, and down-regulate the expression of p-Aurora A and p-VEGFR. ZLJ213 might be a potential therapeutic agent against colon cancer.
Animals ; Apoptosis ; Aurora Kinase A ; antagonists & inhibitors ; Cell Cycle Checkpoints ; Cell Line, Tumor ; drug effects ; Cell Proliferation ; Colonic Neoplasms ; pathology ; Humans ; Protein Kinase Inhibitors ; pharmacology ; Receptors, Vascular Endothelial Growth Factor ; metabolism ; Xenograft Model Antitumor Assays