Administration, Oral ; Animals ; Mice ; Nanoparticles ; toxicity ; Particle Size ; Titanium ; toxicity ; Toxicity Tests, Acute

Digoxin ; poisoning ; Heart Aneurysm ; Humans ; Male ; Middle Aged ; Rupture ; chemically induced

OBJECTIVE:To study the protective effects of soluble ornithine cyclase activator cinaciguat(called CIN for short) on human umbilical vein endothelial cells (HUVECs) under the condition of high glucose. METHODS:HUVECs were treated with glucose 33.3 mmol/L to induce oxidative stress injury model. HUVECs were divided into normal group,high glucose group and high glucose+CIN 0.01,0.1,1 and 10 μmol/L groups. The cell viability was detected by MTT assay,and the survival rate of cells was callulated. Besides,HUVECs were divided into normal group,normal+CIN 1 μmol/L group,high glucose group,high glucose+CIN 1 μmol/L group. MDA content and SOD activity were determined by TBA method and xanthine oxidase method;mRNA expression of ICAM-1 and VCAM-1 were determined by RT-PCR. RESULTS:Compared with normal group,survival rate decreased in high glucose group(P<0.05);compared with high glucose group,that increased in high glucose+CIN 0.01,0.1,1 and 10 μmol/L groups,in concentration-dependent manner;there was no statistical significance in survival rate between high glu-cose+CIN 1 μmol/L group and high glucose+CIN 10 μmol/L group (P>0.05). Compared with normal group,MDA content and mRNA expression of ICAM-1 and VCAM-1 increased in high glucose group,while SOD activity decreased(P<0.05);above indi-cators had no significant change in normal+CIN 1 μmol/L group(P>0.05). Compared with high glucose group,MDA content and mRNA expression of ICAM-1 and VCAM-1 decreased in high glucose+CIN 1 μmol/L group,while SOD activity increased(P<0.05). CONCLUSIONS:CIN can protect high glucose-induced HUVECs injury in vitro. The mechanism may be associated with in-hibition of oxidative stress and inflammatory response.

OBJECTIVETo screen antifungal activity of endophytes from Pseudolarix kaempferi.

METHODEndophytes from P. kaempferi were separated. By means of microdilution method, antifungal active endophytes were fast screened by Pyricularia oryzae P-2b model, and activity of endophytes against pathogenic fungus was studied.

RESULT44.8% of endophytes showed activity against P. oryzae P-2b in Pseudolarix kaempferi. Among them JJ314, JJ323 introduced formation of characteristic beads and swellings on the growing hyphae, JJ324 inhibited the conidia germination. They all showed activity against Trichophyton rubrum, Cryptococcus neoformans and Candida albicans.

CONCLUSIONEndophytes from P. kaempferi are a potential resource for the development of antifungal agent.

Antifungal Agents ; isolation & purification ; pharmacology ; Candida albicans ; drug effects ; Cryptococcus ; drug effects ; Fungi ; chemistry ; classification ; isolation & purification ; Mitosporic Fungi ; drug effects ; Pinaceae ; microbiology ; Plants, Medicinal ; microbiology ; Symbiosis ; Trichophyton ; drug effects

To study the effect of pulchinenoside (PULC) on the Frizzled (FZD) expression of adjuvant arthritis ( AA) rats. AA rats were prepared through the toe injection with complete Freund's adjuvant to culture fibroblast-like synoviocytes (FLS). The effect of the oral administration with PULC on the FZD8 expression was detected by the real time qPCR. The effect of FZD8 knockout on the expressions of IL-1, IL-6, IL-8 were detected by MTT and ELISA. The role of miR-375 in the abnomal expression of FZD8 was detected by the real time qPCR. The results showed signfiicant decrease in the FZD8 expression among AA rats, FLS proliferation ater FZD8 knockout and IL-1, IL-6, IL-8 expressions and notable increase in miR-375 expression after the oral administration with PULC. The up-regulated miR-375 expression can inhibit the FZD8 expression. PULC may inhibit the FZD8 expression by up-regulating the miR-375 expression.
Animals ; Arthritis, Experimental ; drug therapy ; genetics ; metabolism ; Disease Models, Animal ; Drugs, Chinese Herbal ; administration & dosage ; Humans ; Male ; Rats ; Rats, Sprague-Dawley ; Receptors, Cell Surface ; genetics ; metabolism ; Saponins ; administration & dosage

AIMTo investigate the effects of Angelica sinensis polysaccharide fraction AP-3 on IL-2 and IFN-gamma induction and its further immunomodulatory feature.

METHODSThe percentage of CD4+ lymphocyte was detected by flow cytometric method, the production of IL-2 and IFN-gamma in cell culture supernatant were determined by ELISA, mRNA expressions of IL-2 and IFN-gamma cytokines were detected by RT-PCR.

RESULTSAt the range of 0. 6 - 2 micromol x L(-1), AP-3 significantly enhanced the percentage of CD4+ lymphocytes in total splenocytes. At the range of 2 - 6 micromol x L(-1), the treatment of AP-3 augmented both productions of IL-2 in cell culture supernatant and cell IL-2 mRNA transcription level in a time and dose dependent manner. While in the case of IFN-gamma, AP-3 stimulated at early time after exposure but down-regulated thereafter.

CONCLUSIONAngelica sinensis polysaccharide could regulate the immune response through upregulating IL-2, IFN-gamma expression and activating Th1 cell.

Angelica sinensis ; chemistry ; Animals ; CD4-Positive T-Lymphocytes ; cytology ; Cell Proliferation ; drug effects ; Cells, Cultured ; Female ; Interferon-gamma ; biosynthesis ; genetics ; Interleukin-2 ; biosynthesis ; genetics ; Lymphocyte Activation ; drug effects ; Male ; Mice ; Mice, Inbred BALB C ; Plants, Medicinal ; chemistry ; Polysaccharides ; isolation & purification ; pharmacology ; RNA, Messenger ; biosynthesis ; genetics ; Spleen ; cytology ; metabolism

Ten compounds were isolated from the barks of Jasminum giraldii by means of various of chromatographic techniques such as silica gel, Sephadex LH-20 and Rp-HPLC. Their structures were identified by spectroscopic data analysis as (+)-medioresinol (1), (+) -syringaresinol (2), syringaresinol-4'-O-beta-D-glucopyranoside (3), oleanic acid (4), 3-methoxy-4-hydroxy-trans-cinnamaldehyde (5), trans-sinapaldehyde (6), syringaldehyde (7), 1-(4-methoxy -phenyl) -ethanol (8), trans-cinnamic acid (9), and 4-(1-methoxyethyl) -phenol (10). Among them, compounds 1-3, 5-8 and 10 were isolated from the J. genus for the first time and compounds 4 and 9 were obtained from J. giraldii for the first time. In the DPPH free radical scavenging assay, compound 1 exhibited significant activity (IC50 55.1 micromol x L(-1)), compared with vitamin C(IC50 59.9 micromol x L(-1)); and compound 2 showed moderate activity (IC50 79.0 micromol x L(-1)), compared with 2, 6-di-tert-butyl4-methylphenol (IC50 236 micromol x L(-1)).
Antioxidants ; chemistry ; isolation & purification ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; Jasminum ; chemistry ; Magnetic Resonance Spectroscopy ; Molecular Structure ; Spectrometry, Mass, Electrospray Ionization

Ten compounds were isolated from the leaf of Eucommia ulmoides by means of recrystallization and chromatographic techniques such as D-101 macroporous resin, MCI resin, ODS gel, Sephadex LH-20 and Rp-HPLC. Their structures were identified by NMR spectral analyses as kaempferide 3-O-beta-D-glucoside (1), quercetin-3-O-beta-D-glucoside (2), quercetin (3), quercetin-3-O-beta-D-xylosyl-(1-->2)-beta-D-galactoside (4), kaempferol-3-O-alpha-L-rhamnosyl-(1-->6)-beta-D-glucoside (5), (2S,3S)-taxifolin 3-O-beta-D-glucoside (6) ,4-hydroxy cinnamic acid (7), (+)-cycloolivil (8), pinoresinol beta-D-glucoside (9), squalene (10). Among them compounds 1,5-7,10 were isolated from the Eucommia genus for the first time. In the DPPH free radical scavenging assay, compound 2 exhibited significant activity (IC50 13.7 micromol x L(-1)), compared with vitamin C (IC50 59.9 micromol x L(-1)); compounds 1, 3 and 9 showed moderate activity (IC50 161,137, 214 micromol x L(-1)), compared with 2,6-di-tert-butyl-4-methylphenol (IC50 236 micromol x L(-1)); compound 4 and 6 showed weak activity (IC50 264, 299 micromol x L(-1)).
Antioxidants ; chemistry ; Chromatography, High Pressure Liquid ; Drugs, Chinese Herbal ; chemistry ; Eucommiaceae ; chemistry ; Magnetic Resonance Spectroscopy ; Molecular Structure ; Plant Leaves ; chemistry

Aim To explore the novel anti-fatigue a-gents targeting AMPA receptor. Methods Three ben-zoic acids of different methoxy substitutions were em-ployed, including piperonylic acid, 3,4,5-trimethoxy benzoic acid and 3,4-dimethoxy benzoic acid, which as mother nucleus and cyclic aliphatic amine or pheny-lpiperazine derivatives were introduced to modify the nitrogen atoms connecting to amino bonds. Forty-three compounds were synthesized and identified by 1 H-NMR. MTT assay, then pentobarbital induced hypno-sis experiment and mice burden swimming experiment were applied respectively to evaluate the new synthesized compounds’ cytotoxicity, CNS excitability and anti-fatigue activity. Results Compound 2j had low cytotoxicity,presenting certain central excitability and significant advantages on anti-fatigue. Conclusion The further development of compounds 2j with good anti-fatigue activities could be cultivated in further study.

Anal Canal/surgery* ; Humans ; Rectal Fistula/surgery* ; Treatment Outcome