An Aspergillus sp. strain F3 was isolated and identified from the rhizosphere soil of mangrove plant, Rhizophora stylosa Griff in Dongzhai harbor mangrove forest conservation in China. In this study, the effects of media salinity and pH on the mycelial biomass and the ability of producing antibacterial metabo- lites from this isolate were carefully analyzed. Results showed that this isolate can grow well on the SDA medium with higher salinity (3%~9%) and higher pH (8~10). Under the modified culturing conditions, this isolate can secret the antibacterial and antitumor metabolites. The extracts of acetic ether were about 448 mg/L of the fermentation broth. The antibacterial activities of the acetic ether extract were analyzed with bacteria and fungus. Results showed this extract can suppress the growth of Staphylococcus aureus、S. epi-dermidis、Sarcina lutea、Bacillus subtilis and Escherichia coli with MIC of 31.3 ?g/mL, 31.3 ?g/mL, 7.8 ?g/mL, 7.8 ?g/mL and 125.0 ?g/mL, respectively. It can also suppress the growth of Candida albicans with MIC of 125.0 ?g/mL. Further studies uncovered the cytotoxicity of this extract against the tumor cells, such as ECV304, Lovo and HepG2 with IC50 of 3.45 ?g/mL, 4.88 ?g/mL and 14.31 ?g/mL respectively.

To investigate the expression changes of Toll-like receptors (TLR) in the lungs of human metapneumovirus infected BALB/c mice, and to explore the effects of PolyI:C on viral replication, HMPV-infected group, PolyI:C+hMPV group, PolyI:C+DMED group and DMEM control group were set up for this study. All mice were sacrificed on day 1, 3, 5, 7, 9 and 16 post inoculation. Lungs were used for viral titration, pulmonary histopathology and detection of TLRs mRNA expression by RT-PCR and real-time PCR. Results showed that the levels of viral replication in the lungs of PolyI:C+hMPV infected mice were significantly decreased and lung inflammation were also lessened compared with those of hMPV infected mice. RT-PCR detection showed that mRNA levels of most TLRs were up-regulated (P < 0.05) in the lungs of hMPV infected group compared with DMEM group. Real time PCR assay showed that TLR7-8 mRNA significantly increased in hMPV infected group in a time-dependent manner. The level of TLR3 mRNA was significantly up-regulated in PolyI:C+hMPV group at the 24 hour after intranasal inoculation. The results showed that hMPV infection up-regulated the expression of TLRs in lungs of BALB/c mice and TLR7/8 pathway might play an important role in the start of natural immune response. PolyI:C was capable of inhibiting viral replication in the lung of mice and reducing lung inflammation probably through the early activation of TLR3.
Animals ; Disease Models, Animal ; Female ; Gene Expression ; Humans ; Lung ; drug effects ; metabolism ; virology ; Metapneumovirus ; drug effects ; genetics ; physiology ; Mice ; Mice, Inbred BALB C ; Paramyxoviridae Infections ; drug therapy ; genetics ; metabolism ; virology ; Poly I-C ; therapeutic use ; Toll-Like Receptors ; genetics ; metabolism ; Virus Replication

Thermodynamic parameters of complexation of naphto-15-crown-5 with four alkaline earth ions in aqueous media was determined using titration microcalorimetry at 298.15 K. The stability of the complexes, thermal effect and entropy effect of the complexation is discussed on the basis of the guest ions structure and the solvent effect. The stability constants tendency to vary with ion radius was interpreted. Complex of naphtha-15-crown-5 with calcium ion is very stable due to the synergism of static electric interaction and size selectivity between the host and the guest.
Calorimetry ; methods ; Crown Ethers ; chemistry ; Ions ; chemistry ; Macromolecular Substances ; analysis ; chemistry ; Metals, Alkaline Earth ; chemistry ; Microchemistry ; methods

OBJECTIVETo investigate the chemical constituents from the rhizomes of Smilax glabra.

METHODThe compounds were isolated by column chromatography with silica gel, Diaion HP-20 and ODS as packing materials, and HPLC. Their structures were determined on the basis of their spectral evidence.

RESULT5 dihydro-flavonol glycosides were identified as: astilbin (1), neoastilbin (2), isoastilbin (3), neoisoastilbin (4), (2R, 3R)-taxifolin-3'-O-beta-D-pyranglucoside (5).

CONCLUSIONCompounds 2, 4, 5 were isolated from this plant for the first time.

Flavonols ; chemistry ; isolation & purification ; Glucosides ; chemistry ; isolation & purification ; Plants, Medicinal ; chemistry ; Quercetin ; analogs & derivatives ; chemistry ; isolation & purification ; Rhizome ; chemistry ; Smilax ; chemistry ; Stereoisomerism

Numerous studies have indicated that human metapneumovirus (hMPV) is an important viral pathogen in acute respiratory infections in children, presenting similar manifestations with respiratory syncytial virus (RSV). HMPV infection peaks in the winter-spring season and is more prevalent in younger ages, especially in children less than 1 year old. Host innate immune response has been implicated in recognition of pathogen-associated molecular patterns (PAMPs) of the virus. This recognition occurs through host pattern recognition receptors (PRRs). Toll like receptors (TLRs) are one of the largest class of PRRs which initiate and regulate adaptive immune responses. Some studies have indicated that TLR 3 and TLR 4 may play critical roles in hMPV infection. Construction of recombinant mutant viruses lacking one or two N-linked glycosylation sites in the F protein by using site-directed mutagenesis and reverse genetics may be helpful for developing attenuated live vaccines.
Humans ; Metapneumovirus ; immunology ; Paramyxoviridae Infections ; etiology ; prevention & control ; Vaccines, Attenuated ; immunology ; Vaccines, Synthetic ; immunology ; Viral Vaccines ; immunology

A rapid, sensitive and simple liquid chromatography-tandem mass spectrometric (LC-MS/MS) method was developed for the simultaneous determination of yogliptin and its metabolite in Wistar rat plasma. Linagliptin and dexamethasone were chosen as the internal standards of yogliptin and its metabolite, (R)-8-(3-hydroxypiperidine- -yl)-7-(but-2-yn-1-yl)-1-((5-fluorobenzo[d]thiazol-2-yl)methyl)-3-methyl- H-purine-2, 6 (3H, 7H)-dione, respectively. After a simple protein precipitation using acetonitrile as the precipitating solvent, both analytes and ISs were separated on a Grace Altima HP C18 column (2.1 mm x 50 mm, 5 microm) with gradient elution using methanol (containing 0.1% formic acid, 4 mmol x L(-1) ammonium acetate)-0.1% formic acid (containing 4 mmol x L(-1) ammonium acetate) as the mobile phase. A chromatographic total run time of 4.4 min was achieved. Mass spectrometric detection was conducted with electrospray ionization under positive-ion and multiple-reaction monitoring modes. Linear calibration curves for yogliptin and its metabolite were over the concentration range of 0.5 to 500 ng x mL(-1) with a lower limit of quantification of 0.5 ng x mL(-1). The intra- and inter- assay precisions were all below 14%, the accuracies were all in standard ranges. The method was used to determine the concentration of yogliptin and M1 in Wistar rat plasma after a single oral administration of yogliptin (27 mg x kg(-1)). The method was proved to be selective, sensitive and suitable for pharmacokinetic study of yogliptin and M1 in Wistar rat plasma.
Animals ; Chromatography, Liquid ; Dexamethasone ; blood ; Dipeptidyl-Peptidase IV Inhibitors ; blood ; pharmacokinetics ; Linagliptin ; blood ; Rats ; Rats, Wistar ; Tandem Mass Spectrometry

AIMTo investigate the effects of glycyrrhiza decoction on migrating myoelectric complex (MMC) and gastrointestinal hormone in small intestine in rats.

METHODSWe observed MMC cycle,phase Ill duration,fast wave numbers of phase III of MMC in one minute, fast wave numbers of one cluster in phase III of MMC of small intestine of glycyrrhiza group and control group rats with electrophysiology method, and immunohistochemistry to examine relative content of serotonin (5-HT), substance p(SP) and vasoactive intestinal polypeptide (VIP) in small intestinal chromophil (EC) and myenteric nerve plexus in small intestine of control group and glycyrrhiza group rats.

RESULTSCompared glycyrrhiza group with control group,we found that glycyrrhiza was able to decrease fast wave numbers in one minute and fast wave numbers in one cluster in phase III of MMC of small intestine (P < 0.05), and evidently extend small intestinal cycle of MMC (P < 0.05), it also shortened the phase III III duration (P < 0.05) or made the phase III of MMC absent. Compared glycyrrhiza group with control group it was indicated that content of 5-HT in small intestinal mucous membrane and myenteric nerve plexus was evidently decreased (P < 0.05), and content of SP in myenteric nerve plexus of small intestine of rats was evidently decreased (P < 0.05), and content of VIP in small intestine of rats was evidently increased (P < 0.05).

CONCLUSIONGlycyrrhiza is able to inhibit small intestinal motility, this inhibition is related with the amount of 5-HT, SP, VIP secreted by small intestinal mucous membrane of rats.

Animals ; Drugs, Chinese Herbal ; pharmacology ; Electromyography ; Gastrointestinal Motility ; drug effects ; physiology ; Glycyrrhiza ; Intestine, Small ; drug effects ; physiology ; Rats ; Rats, Sprague-Dawley ; Serotonin ; analysis ; Substance P ; analysis ; Vasoactive Intestinal Peptide ; analysis

The paper is to report the pharmacokinetic character of a series of chemical compounds in vitro and in vivo. Metabolism stability of a series of chemical compounds was screened by using rat liver microsomes. The samples of different chemical compounds were combined and then simultaneously detected by LC-MS/MS. Compounds y13, y12 and y11 were screened out by microstability assay in vitro. The pharmacokinetics of compounds y11, y12 and y13 was evaluated by using SD rat. The plasma samples were pooled at the same time. The plasma concentrations were determined by LC-MS/MS. The pharmacokinetic character of two compounds y13, y11 was good by screening in vivo, so they were developed for further research. High-throughput screening of drug candidates in vitro and in vivo was effective, to provide information for the chemical structure information and lower the drug development risk.
Animals ; Chromatography, Liquid ; methods ; Drug Evaluation, Preclinical ; methods ; Female ; High-Throughput Screening Assays ; methods ; Male ; Microsomes, Liver ; metabolism ; Pharmaceutical Preparations ; administration & dosage ; blood ; metabolism ; Pharmacokinetics ; Random Allocation ; Rats ; Rats, Sprague-Dawley ; Spectrometry, Mass, Electrospray Ionization ; methods

The aim of this study was to find platelet specific autoantibodies against glycoproteins in myelodysplastic syndrome (MDS) and to explore its role in pathogenesis of MDS. The plasma autoantibodies against GP IIb/IIIa and GP Ib/IX were measured by using a modified monoclonal antibody specific immobolization platelet antigens assay (MAIPA). Absorbance greater than mean value plus tripled standard deviation recorded from the normal controls were regarded as positive. The results indicated that the total positive rate in patients with MDS was 16.67% (5/30), the total positive rate in patients with ITP was 46.67% (14/30), the difference between MDS group and ITP group was significant (P < 0.05). It is concluded that partial patients with MDS have plasma specific autoantibodies against platelet GP II b/III a and GP Ib/IX, indicating correlation of thrombocytopenia of patients with immune factors and the autoantibody-mediated platelet destruction may be involved in the pathogenesis of MDS. It provides a new basis for immunosuppression therapy for MDS.
Adolescent ; Adult ; Aged ; Antibodies ; immunology ; Antigens, Human Platelet ; immunology ; Autoantibodies ; biosynthesis ; immunology ; Female ; Humans ; Male ; Middle Aged ; Myelodysplastic Syndromes ; complications ; immunology ; Platelet Glycoprotein GPIIb-IIIa Complex ; immunology ; Platelet Glycoprotein GPIb-IX Complex ; immunology ; Thrombocytopenia ; etiology ; immunology

Objective To explore a more minimally invasive and economical treatment for atrial septal defect (ASD) through comparing the efficacy and safety in percutaneous transcatheter closure of atrial septal defect procedure,guided by transthoracic echocardiography(TTE) and transesophageal echocardiography(TEE).Methods From March 2014 to September 2017,197 patients with ASD who were feasible to treated with percutaneous transcatheter closure procedure evaluated by preoperative ~ were recruited.TTE showed ASD belonged to secundum(central type) with a maximal diameter range from 2 mm to 35mm,including 82 cases of the ASD without aortic rim.There were 106 patients(47males and 59 females including 37 ASD without aortic rim) with a mean age of 14.2 years(6 months-59 years) old and a mean body weight of 29.5(8.5-64.0)kg were performed percutaneous transcatheter closure of ASD guided by TEE under general anesthesia and endotracheal intubation,and 91 patients(41males and 50 females with 45 ASD without aortic rim inside) with a mean age of 13.8 years(9 months-65 years) old and a mean body weight of 30.4 (9.5-61.0)kg were treated with the percutaneous transcatheter procedure guided by TTE when patients in waking state of local anesthesia(general anesthesia were adopted in patients under 12 years old without intubation).The size of the occluder was selected on the basis of the maximal diameter plus 2-6mm.All 197 cases intraoperation and postoperation data were collected,including complications 、operation time 、operation room stay time and total cost.Results 1 patients in 106 cases of the the TEE group were transferred to small incision on the chest performing transthoracic transcatheter closure of ASD because the difficult stuck of the occluder.3 patients in TEE group transferred to repair under cardiopulmonary bypass(CPB) via small incision on the chest because the difficult stuck of the occluder even in using transthoracic transcatheter closure way.86 patiens in TTE group successfully treated with percutaneous transcatheter closure,and there were 5 failed cases including 2 patients who transferred to TEE guided because of the poor imaging of TTE,another 2 cases treated with transthoracic transcatheter closure of ASD because the difficult stuck of the occluder,and 1 patient performed ASD repair procedure under CPB via small incision on the chest because of the huge ASD without aortic rim and difficult stuck of the occluder.All the 197 patients were cured and discharge from hospital,and there were no complications.There was no significant difference in age,weight,and maximum diameter of ASD between TEE group and TTE group (P ＞ 0.05).Follow-ups were conducted by TTE at month 3 post-operation,and all 197 cases performed no residual shunt of ASD,there were no difference between 2 group.The stay time in the operation room was(68.2 ± 17.3) min in group TEE and (34.7 ± 16.8) min in group TTE,there was obviously shortened the stay time in operation room(P ＜0.01).The total cost of the TTE group was(24.2 ± 2.1) thousand yuan,and the group TEE was(29.3 ± 1.4) thousand yuan,and the cost was significantly reduced in TTE group (P ＜ 0.01).Conclusion The treatment of percutaneous transcatheter closure of ASD guided by TTE is effective and safe,and the feature of more non-invasive and socioeconomic benefits show a broad application prospect.