AIMTo explore the effects of interleukin-1beta (IL-1beta) on inducible nitric oxide synthase (iNOS)-nitric oxide (NO) system activity in arginine vasopressin (AVP)-induced rat cardiac fibroblasts (CFs).

METHODSCFs were isolated by trypsin digestion method. Nitric acid reductase method, spectrophotometry and reverse transcription-polymerase chain reaction (RT-PCR) were used to detect NO contents, NOS activity and iNOS mRNA expression.

RESULTSAVP significantly increased iNOS mRNA expressions, NOS activity and NO contents (P < 0.05) in CFs. IL-1beta enhanced the effects of AVP on iNOS-NO system activity in a concentration-dependent manner, moreover the iNOS mRNA expressions, NOS activity and NO contents of AVP + 3 ng/ml, AVP + 5 ng/ml IL-1beta group were both significantly higher than those of AVP group (P < 0.05). But when IL-1beta concentration increased to 5 ng/ml, the iNOS mRNA expressions, NOS activity and NO contents did not increase accordingly, slightly decreased instead.

CONCLUSIONWithin certain range of concentrations IL-1beta cooperates with AVP to increase iNOS-NO system activity in CFs.

Animals ; Arginine Vasopressin ; pharmacology ; Fibroblasts ; drug effects ; metabolism ; Interleukin-1beta ; pharmacology ; Male ; Myocytes, Cardiac ; drug effects ; metabolism ; Nitric Oxide ; metabolism ; Nitric Oxide Synthase Type II ; metabolism ; Rats ; Rats, Sprague-Dawley

The chemical constituents from the fruiting bodies of Lyophyllum decastes (Fr.) Singer were studied in this paper. Thirteen compounds were isolated and purified by column chromatographies on silica gel and Sephadex LH-20. Their structures were identified by MS and NMR data analysis as adenosine (1), 2R, 3S, 4S, 8E)-2-[(2'R)-2-hydroxyheneicosanoylamino]-8-octadecene-1, 3, 4-triol (2), (2R, 3S, 4S, 8E)-2-[(2'R)-2-hydroxypentacosanoylamino]-8-octadecene-1, 3, 4-triol (3), nicotinic acid (4), (4E, 8E) -2-N-2-hydroxytetracosanoyl-1-O-beta-D-glycopyranosyl-9-methyl-4, 8-sphingadienine (5), D-mannitol (6), ergosteryl-3-O-beta-D-glucopyranoside (7), tuberoside (8), (2R, 3S, 4S, 8E)-2-[(2'R)-2-hydroxybehenoylamino]-8-octadecene-1, 3, 4-triol (9),(2R, 3S, 4S, 8E)-2-[(2'R) -2-hydroxytricosanoylamino] -8-octadecene-1, 3, 4-triol (10), (22E, 24R)-ergosta-7, 22-dien-3beta, 5alpha, 6beta-triol (11), (22E, 24R)-ergosta-5, 7, 22-trien-3beta-ol (12), and 5alpha, 8alpha-epidiory-(22E, 24R)-ergosta-6, 22-dien-3beta-ol (13), respectively. All the above compounds are first obtained from the mushroom and compounds 2-10 are reported to be obtained from the Lyophyllum for the first time.
Agaricales ; chemistry ; Drugs, Chinese Herbal ; chemistry ; Fruit ; chemistry

Objective To identify changes in the occurrence of endemic fluorosis in order to provide scientific basis for making countermeasures. Methods Five villages from 14 counties of mild, moderate and severe fluorosis affected areas were selected by stratified cluster sampling every year in the whole province during 2006 - 2010. Water and urinary fluorine were determined by ion selective electrode method(GB/T 8538-1995); dental fluorosis of children 8-12 years old was diagnosed with Dean method; skeletal fluorosis was diagnosed according to "clinical indexing standards of endemic skeletal fluorosis "(GB 16396-1996), between 2006 and 2008, and "clinical diagnosis standard of endemic skeletal fluorosis"(WS 192-2008) between 2009 and 2010. Results A total of 25 diseased villages were surveyed, 14 with water sources changed, covered a resident population of 8005 people, beneficiary population 7154, and accounting for 89.37% of the resident population; not changed villages 11. In accordance with the "State drinking water health standards", in the 14 changed villages the fluoride in drinking water was qualified (≤ 1.20 mg/L), there were 3 schools whose water fluorine content exceeded the standard; among the 11 villages that did not change water sources 7 drinking water samples fluorine content exceeded the standard. Of the 8 to 12 years old children in villages with changed water sources, 363 of them were checked and 142 dental fluorosis were found, the detection rate of dental fluorosis was 39.12% (142/363); in villages with water sources not changed, 303 children were checked, the detection rate of dental fluorosis was 43.89%(133/303). Of sixteen and elder adults in water source changed villages, 6424 people were checked and 403 skeletal fluorosis were found, skeletal fluorosis detection rate was 6.27% (403/6424); 3572 people were checked in not changed villages, the detection rate of skeletal fluorosis was 13.89%(496/3572). In water sources changed areas, geometric mean of urinary fluoride was in the normal reference value(WS/T 256-2005, 1.40 mg/L)or less. Conclusions Endemic fluorosis is decreased in water improved areas, but in unimproved areas the disease is still severe, and control of endemic fluorosis is still an arduous task.

Animals ; Hindlimb ; blood supply ; Intestine, Small ; metabolism ; Ischemia ; metabolism ; prevention & control ; Ischemic Preconditioning ; Lung Injury ; metabolism ; Male ; Muscle, Skeletal ; metabolism ; Rats ; Rats, Wistar ; Reperfusion Injury ; metabolism

Objective To investigate the status of anxiety-depression and the relevant factors in puerpera be- fore delivery.Methods The emotion of anxiety and depression in puerpera before delivery was evaluated by self-rat- ing anxiety scale(SAS)and self-rating depression scale(SDS)which had satisfactory validity and reliability.Results The values of anxiety and depression in puerpera were higher than those of general crowd(P

Objective To study the changes and correlation of serum interleukin-17,-6 and-8 (IL-17,IL-6 and IL-8),c-reactive protein (CRP),tumor necrosis factor alpha (TNF-α) of patients with chronic obstructive pulmonary diseases (COPD),and discuss the role and clinical significance of these factors in the occurrence and development of COPD.Methods 100 COPD patients were selected (COPD group),and 50 healthy elderly people in the same period in outpatient medical examination were served as control (control group).The levels ofIL-17,IL-6 and IL-8,CRP,TNF-α in serum were detected with ELISA method.Results The serum levels of IL-17,IL-6,IL-8,CRP and TNF-α of patients in COPD group were higher than those in the control group (P ＜ 0.01),and of patients with acute aggravating period were higher than those of patients with stable period (P ＜ 0.05 or P ＜ 0.01).Pearson correlation analysis showed there were positive correlations among IL-17,IL-6,IL-8,CRP and TNF-α (P ＜ 0.05) Conclusion The serum levels of IL-17,IL-6,IL-8,CRP and TNF-α of COPD patients have abnormal increased,and will increase with the rise of the illness severity.The above factors may be involved in the airway in patients with acute inflammatory reaction and the development process.

The methyl group plays an important role in the rational drug design. Introducing methyl into small molecules has become an important strategy of lead compound optimization. The application of methyl in drug design is reviewed in this paper. Methyl can modulate the physicochemical, pharmacodynamic, and pharmacokinetic properties by ortho effect, inductive effect, and conformational effect. It also improves the metabolic stability as a soft metabolic point. In addition, introducing methyl into drug molecules can also be applied as a strategy in new uses of old drugs and generate me-too drugs.
Drug Design ; Hydrophobic and Hydrophilic Interactions ; Lipid Metabolism ; Methylation ; Pharmaceutical Preparations ; chemical synthesis ; chemistry ; metabolism ; Solubility ; Stereoisomerism ; Structure-Activity Relationship

OBJECTIVEThe study was aimed to investigate the inhibitory effect and mechanism of astragaloside IV (ASI) on the activation of microglial cells.

METHODAfter pre-incubated with ASI for 2 h, microglial cells BV-2 were stimulated with interferon-γ (IFN-γ) for 1. 5 h and 24 h, respectively. Secretion of nitric oxide (NO) in the medium was measured by Griess method. Production of tumor necrosis factor alpha (TNF-α) was detected by ELISA approach. Cellular gene expressions of CD11b, TNF-α, interleukin 1β (IL-1β) and induced nitric oxide synthase (iNOS) were examined by quantitative-PCR analysis. Total and phosphorylation of STAT1, IκB and NF-κB was analyzed by Western blot method.

RESULTASI could significantly inhibit the increased secretion of TNF-α and NO from BV-2 cells upon IFN-γ stimulation (P < 0.001). Further study showed that ASI significantly down-regulated gene expression of IL-1β and TNF-α (P < 0.01, P < 0.05) and exhibited a trend to reduce that of iNOS. IFN-γ and ASI have no obvious effect on gene expression of CD11b. Moreover, ASI inhibited the phosphorylation of STAT1, IκB and NF-κB elicited by IFN-γ stimulation.

CONCLUSIONASI could restrain microglial activation through interfering STAT1/IκB/NF-κB signaling pathway, reducing gene expres- sion of IL-1β and TNF-α, and thus inhibiting the production of proinflammatory mediators such as NO and TNF-α.

Animals ; Astragalus Plant ; chemistry ; Drugs, Chinese Herbal ; pharmacology ; I-kappa B Proteins ; genetics ; metabolism ; Interferon-gamma ; genetics ; metabolism ; Mice ; NF-kappa B ; genetics ; metabolism ; Nitric Oxide ; metabolism ; Nitric Oxide Synthase Type II ; genetics ; metabolism ; STAT1 Transcription Factor ; genetics ; metabolism ; Saponins ; pharmacology ; Signal Transduction ; drug effects ; Triterpenes ; pharmacology

Objective To investigate the expression of caspase-10 in differentiated thyroid carcinoma and association with its development and metastasis. Methods Thyroid samples from 37 patients in a period from January 2006 to December 2007, with differentiated thyroid carcinoma were retrospectively analyzed for caspase-10 by immunohistocbemistry(streptavidin-perosidase, S-P), compared to control group of 46 cases with nodtdar goiter. The relationship between the expression of caspase-10 and the clinical pathologic characteristics of thyroid carcinoma were also explored simultaneously. Results caspase-10 were observed as brown or yellow particles located in the cytoplasm or cell membrane of nodular goiter but there were no significant evidence for its positive expression in thyroid carcinoma, caspase-10 expression was markedly down-regulated in differentiated thyroid carcinoma(29.73%,11/37) compared with benign nodules(71.74%,33/46, χ2=14.528, P<0.01). The positive expression in 18 cases with lymph node metastasis(11.11%,2/18) was significantly lower than those in 19 patients without lymph node metastasis(47.37%,9/19; χ2=4.210, P<0.01). There was no significant correlation(P> 0.05) between the expression of caspase-10 and the clinical pathologic characteristics including male, age, TNM stage and pathologic type. Conclusion Down-regulation of caspase-10 may play a critical role in carcinogenesis and development of differentiated thyroid carcinoma.

OBJECTIVETo explore the influence of the DNA repair gene ERCC2 single nucleotide polymorphisms (SNPs) rs13181, rs1618536, and rs1799793 on male idiopathic infertility in Ningxia, China.

METHODSUsing MassArray, we conducted a case-control study and genotyped three ERCC2 SNPs rs13181, rs1618536, and rs1799793 for 351 males (aged 31.0 +/- 4.2 years) with idiopathic infertility and another 327 normal fertile men (aged 33.0 +/- 5.9 years) as controls.

RESULTSThe ERCC2 AnyG-anyA-anyA genotypes were significantly associated with an increased risk of idiopathic infertility (OR 0.414, 95% CI 0.176 - 0.970), while the three single ERCC2 SNPs rs13181, rs1618536, and rs1799793 showed no significant differences between the cases and controls (P > 0.05).

CONCLUSIONThe ERCC2 SNPs rs13181, rs1618536, and rs1799793 play a role of interaction in male idiopathic infertility in Ningxia, contributing to the risk of the disease.

Adult ; Case-Control Studies ; China ; DNA Repair ; Genotype ; Humans ; Infertility, Male ; genetics ; Male ; Polymorphism, Single Nucleotide ; Xeroderma Pigmentosum Group D Protein ; genetics