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1.
Braz. oral res. (Online) ; 32: e104, 2018. tab, graf
Article in English | LILACS | ID: biblio-974458

ABSTRACT

Abstract This study evaluated the three-year lifespan of the bond to dentin of experimental self-etch adhesives containing benzodioxole derivatives - 1,3-benzodioxole (BDO) and piperonyl alcohol (PA) - as co-initiator alternative to amines. Adhesive resins were formulated using Bis-GMA, TEGDMA, HEMA, camphorquinone and different co-initiators: BDO, PA or ethyl 4-dimethylamino benzoate (EDAB - amine). An experimental self-etch primer was used to complete the two-step, self-etch adhesive system. Clearfil SE Bond (CSE) was used as commercial reference. Bond strength to human dentin was assessed by microtensile bond strength (µTBS) test, and failure mode was classified. Morphology of the dentin bonding interface was assessed via scanning electron microscopy (SEM). Irrespective of the dental adhesives evaluated, µTBS was higher after 24 hours compared with that after 1.5 and 3 years (p ≤ 0.001). However, adhesives with BDO and PA as co-initiators showed significantly higher bond strength than the bonding resin with EDAB (p ≤ 0.002), independent of the time evaluated. The commercial adhesive CSE showed similar bond strength compared with the other groups (p ≥ 0.05). Mixed failures were mainly observed after 24 hours, while adhesive failures were more frequently observed after 1.5 and 3 years. No notable differences in homogeneity and continuity along the bonded interfaces were detected among the materials in the SEM analysis. In conclusion, benzodioxole derivatives are feasible alternative co-initiators to tertiary amine in camphorquinone-based self-etching dental adhesive formulations.


Subject(s)
Humans , Benzyl Alcohols/chemistry , Dentin-Bonding Agents/chemistry , Resin Cements/chemistry , Dentin/drug effects , Dioxoles/chemistry , Benzodioxoles/chemistry , para-Aminobenzoates/chemistry , Polyethylene Glycols/chemistry , Polymethacrylic Acids/chemistry , Surface Properties , Tensile Strength , Time Factors , Materials Testing , Camphor/analogs & derivatives , Camphor/chemistry , Microscopy, Electron, Scanning , Reproducibility of Results , Dental Bonding/methods , Bisphenol A-Glycidyl Methacrylate/chemistry , Dentin/chemistry , Methacrylates/chemistry
2.
Bol. latinoam. Caribe plantas med. aromát ; 15(1): 1-17, ene. 2016. ilus, graf, tab
Article in English | LILACS | ID: biblio-907513

ABSTRACT

The direct in vitro fungitoxicity and metabolism of safrole and dillapiole (isolated from Piper auritum and Piper holtonii, respectively) by Botryodiplodia theobromae and Colletotrichum acutatum were investigated. Higher values of mycelial growth inhibition for both fungi were obtained for dillapiole, as compared with safrole. B. theobromae was able to metabolize both compounds to their respective vicinal diols, reaching 65 percent relative abundance during the biotransformation of dillapiole; while C. acutatum only transformed safrole to various metabolites with relative abundances under 5 percent. According to the low antifungal activity of the major metabolic products (< 5 percent for vicinal diols), a detoxification process was implied. Studies on the influence of some substituents in the aromatic ring of safrole and dillapiole on the antifungal activity against B. theobromae were also carried out. As result, the safrole nitrated derivative, 6-nitrosafrole, showed a fungitoxicity level similar to that displayed by the commercial fungicide Carbendazim® under the conditions used. In light of this, safrole and dillapiole could be suggested as feasible structural templates for developing new antifungal agents.


Se investigó la fungitoxicidad directa in vitro y el metabolismo de safrol y dilapiol (obtenidos desde Piper auritum and Piper holtonii, respectivamente) por Botryodiplodia theobromae y Colletotrichum acutatum. Los valores mayores de inhibición del crecimiento micelial de ambos hongos se obtuvieron para dilapiol, en comparación con safrol. B. theobromae metabolizó ambos compuestos a sus respectivos dioles vecinales, alcanzando abundancias relativas del 65 por ciento durante la biotransformación del dilapiol; mientras que C. acutatum solo transformó safrol en varios metabolitos con abundancias relativas menores al 5 por ciento. De acuerdo con la baja actividad antifúngica de los productos metabólicos mayoritarios (< 5 por ciento para los dioles vecinales), se sugiere un proceso de desintoxicación. Adicionalmente, se evaluó la influencia de algunos sustituyentes en el anillo aromático de safrol y dilapiol sobre la actividad antifúngica contra B. theobromae. Como resultado, el derivado nitrado del safrol, el 6–nitro safrol, presentó un nivel de fungitoxicidad similar al exhibido por el fungicida comercial Carbendazim® bajo las condiciones usadas. A la luz de lo anterior, safrol y dilapiol podrían ser sugeridos como plantillas estructurales adecuadas para el desarrollo de nuevos agentes antifúngicos.


Subject(s)
Antifungal Agents/pharmacology , Dioxoles/pharmacology , Mitosporic Fungi , Safrole/pharmacology , Antifungal Agents/metabolism , Biotransformation , Colletotrichum , Dioxoles/metabolism , In Vitro Techniques , Safrole/metabolism
3.
Chinese Medical Journal ; (24): 2040-2044, 2016.
Article in English | WPRIM | ID: wpr-307471

ABSTRACT

<p><b>BACKGROUND</b>Bronchiolitis obliterans syndrome (BOS) often develops in transplant patients and results in injury to the respiratory and terminal airway epithelium. Owing to its rising incidence, the pathogenesis of BOS is currently an area of intensive research. Studies have shown that injury to the respiratory epithelium results in dysregulation of epithelial repair. Airway epithelial regeneration is supported by stromal cells, including fibroblasts. This study aimed to investigate whether the supportive role of lung fibroblasts is altered in BOS.</p><p><b>METHODS</b>Suspensions of lung cells were prepared by enzyme digestion. Lung progenitor cells (LPCs) were separated by fluorescence-activated cell sorting. Lung fibroblasts from patients with BOS or healthy controls were mixed with sorted mouse LPCs to compare the colony-forming efficiency of LPCs by counting the number of colonies with a diameter of ≥50 μm in each culture. Statistical analyses were performed using the SPSS 17.0 software (SPSS Inc., USA). The paired Student's t-test was used to test for statistical significance.</p><p><b>RESULTS</b>LPCs were isolated with the surface phenotype of CD31-CD34-CD45- EpCAM+Sca-1+. The colony-forming efficiency of LPCs was significantly reduced when co-cultured with fibroblasts isolated from patients with BOS. The addition of SB431542 increased the colony-forming efficiency of LPCs to 1.8%; however, it was still significantly less than that in co-culture with healthy control fibroblasts (P < 0.05).</p><p><b>CONCLUSION</b>The epithelial-supportive capacity of fibroblasts is impaired in the development of BOS and suggest that inefficient repair of airway epithelium could contribute to persistent airway inflammation in BOS.</p>


Subject(s)
Animals , Humans , Mice , Benzamides , Pharmacology , Bronchiolitis Obliterans , Metabolism , Pathology , Cells, Cultured , Coculture Techniques , Dioxoles , Pharmacology , Fibroblasts , Cell Biology , Metabolism , Physiology , Flow Cytometry , Stem Cells , Cell Biology , Metabolism
4.
Journal of Gynecologic Oncology ; : e53-2016.
Article in English | WPRIM | ID: wpr-115236

ABSTRACT

In 2015, fourteen topics were selected as major research advances in gynecologic oncology. For ovarian cancer, high-level evidence for annual screening with multimodal strategy which could reduce ovarian cancer deaths was reported. The best preventive strategies with current status of evidence level were also summarized. Final report of chemotherapy or upfront surgery (CHORUS) trial of neoadjuvant chemotherapy in advanced stage ovarian cancer and individualized therapy based on gene characteristics followed. There was no sign of abating in great interest in immunotherapy as well as targeted therapies in various gynecologic cancers. The fifth Ovarian Cancer Consensus Conference which was held in November 7–9 in Tokyo was briefly introduced. For cervical cancer, update of human papillomavirus vaccines regarding two-dose regimen, 9-valent vaccine, and therapeutic vaccine was reviewed. For corpus cancer, the safety concern of power morcellation in presumed fibroids was explored again with regard to age and prevalence of corpus malignancy. Hormone therapy and endometrial cancer risk, trabectedin as an option for leiomyosarcoma, endometrial cancer and Lynch syndrome, and the radiation therapy guidelines were also discussed. In addition, adjuvant therapy in vulvar cancer and the updated of targeted therapy in gynecologic cancer were addressed. For breast cancer, palbociclib in hormone-receptor-positive advanced disease, oncotype DX Recurrence Score in low-risk patients, regional nodal irradiation to internal mammary, supraclavicular, and axillary lymph nodes, and cavity shave margins were summarized as the last topics covered in this review.


Subject(s)
Female , Humans , Biomedical Research/trends , Breast Neoplasms/therapy , Combined Modality Therapy , Dioxoles , Endometrial Neoplasms/therapy , Genital Neoplasms, Female/genetics , Immunotherapy , Neoadjuvant Therapy , Neoplasm Recurrence, Local , Ovarian Neoplasms/prevention & control , Papillomavirus Vaccines , Precision Medicine , Tetrahydroisoquinolines , Uterine Cervical Neoplasms/prevention & control , Uterine Neoplasms/therapy
5.
Braz. j. microbiol ; 46(1): 293-299, 05/2015. tab, graf
Article in English | LILACS | ID: lil-748267

ABSTRACT

The effect of fludioxonil + metalaxyl-M on the mycelial morphology, sporulation and fumonisin B1 production by Fusarium verticillioides 103 F was evaluated. Scanning electron microscopy analysis showed that the fungicide caused inhibition of hyphal growth and defects on hyphae morphology such as cell wall disruption, withered hyphae, and excessive septation. In addition, extracellular material around the hyphae was rarely observed in the presence of fludioxonil + metalaxyl-M. While promoting the reduction of mycelial growth, the fungicide increased sporulation of F. verticillioides compared to the control, and the highest production occurred on the 14th day in the treatments and on the 10th day in the control cultures. Fumonisin B1 production in the culture media containing the fungicide (treatment) was detected from the 7th day incubation, whereas in cultures without fungicide (control) it was detected on the 10th day. The highest fumonisin B1 production occurred on the 14th day, both for the control and for the treatment. Fludioxonil + metalaxyl - M can interfere in F. verticillioides mycelial morphology and sporulation and increase fumonisin B1 levels. These data indicate the importance of understanding the effects of fungicide to minimize the occurrence of toxigenic fungi and fumonisins.


Subject(s)
Fumonisins/metabolism , Fungicides, Industrial/pharmacology , Fusarium/drug effects , Fusarium/metabolism , Hyphae/drug effects , Hyphae/ultrastructure , Alanine/analogs & derivatives , Alanine/pharmacology , Dioxoles/pharmacology , Fusarium/growth & development , Fusarium/ultrastructure , Hyphae/growth & development , Microscopy, Electron, Scanning , Pyrroles/pharmacology , Spores, Fungal/growth & development
6.
Chinese journal of integrative medicine ; (12): 846-854, 2015.
Article in English | WPRIM | ID: wpr-267150

ABSTRACT

<p><b>OBJECTIVE</b>To study the effect of oral administration of dimethyl dimethoxy biphenyl dicarboxylate (DDB) on adjusting angiogeneic/inflammatory mediators and ameliorating the pathology of bones in rats with collagen-induced arthritis (CIA).</p><p><b>METHODS</b>Wistar rat model of CIA was set up using bovine collagen type II. Fifty rats were divided into five groups randomly: normal, CIA model, DDB treatment, methotrexate (MTX) treatment, and combined DDB+MTX treatment. Ankle joints of rats were imaged with digital X-ray machine to show the destruction of joints. Fore and hind paw and knee joints were removed above the ankle joint then processed for haematoxylin and eosin staining. Plasma levels of vascular endothelial growth factor (VEGF), platelet derived growth factor, interleukin-8 (IL-8), IL-4, tumor necrosis factor α (TNF-α), and cyclooxygenase-2 (COX-2) were quantified by enzyme-linked immunosorbent assay. Nitric oxide levels were detected by Griess reagent.</p><p><b>RESULTS</b>Compared with the CIA model group, a remarkable reduction in various angiogenic (VEGF and IL-8) and inflammatory mediators (TNF-α, IL-4 and COX-2) after treatment with DDB either alone or combined with MTX P<0.05 or P<0.01). Histopathological and X-ray findings were confirmatory to the observed DDB anti-arthritic effect. The DDB-treated group showed amelioration in signs of arthritis which appeared essentially similar to normal.</p><p><b>CONCLUSION</b>Our data shed light on the therapeutic efficacy of DDB in experimental rheumatoid arthritis (RA) compared with a choice drug (MTX) and it may be offered as a second-line drug in the treatment of RA.</p>


Subject(s)
Animals , Female , Rats , Arthritis, Experimental , Diagnostic Imaging , Drug Therapy , Pathology , Arthritis, Rheumatoid , Diagnostic Imaging , Drug Therapy , Pathology , Collagen , Cyclooxygenase 2 , Blood , Dioxoles , Therapeutic Uses , Enzyme-Linked Immunosorbent Assay , Interleukin-4 , Blood , Interleukin-8 , Blood , Methotrexate , Therapeutic Uses , Nitric Oxide , Platelet-Derived Growth Factor , Radiography , Rats, Wistar , Tumor Necrosis Factor-alpha , Blood , Vascular Endothelial Growth Factor A , Blood
7.
Acta Pharmaceutica Sinica ; (12): 191-198, 2015.
Article in Chinese | WPRIM | ID: wpr-251796

ABSTRACT

A series of [1,3]dioxolo[4,5-f]isoindolone derivatives were designed, synthesized and evaluated as inhibitors of acetylcholinesterases (AChE). Furthermore, their effects on memory impairment of mice induced by scopolamine were investigated with step-through test. The results suggested that most of the target compounds exhibited potential inhibition on AChE with IC50 values at micromolar range. Compounds I1 (IC50 value of 0.086 μmol · L(-1)) and I2 (IC50 value of 0.080 μmol · L(-1)) showed the strongest AChE inhibitory activity, which are equipotent to donepezil (IC50 value of 0.094 μmol · L(-1)). Moreover, compounds I1-I4 could improve the memory impairment induced by scopolamine in mice.


Subject(s)
Animals , Mice , Cholinesterase Inhibitors , Chemistry , Dioxoles , Chemistry , Drug Design , Indans , Inhibitory Concentration 50 , Isoindoles , Chemistry , Memory Disorders , Drug Therapy , Piperidines , Scopolamine
8.
China Journal of Chinese Materia Medica ; (24): 1355-1361, 2015.
Article in Chinese | WPRIM | ID: wpr-246096

ABSTRACT

<p><b>OBJECTIVE</b>To observe the effect of sesamin (Ses) on pulmonary vascular remodeling in rats with monocrotaline ( MCT)-induced pulmonary hypertension (PH).</p><p><b>METHOD</b>Totally 48 male Sprague-Dawley (SD) rats were fed adaptively for one week and then divided into the normal control group, the MCT group, the MCT +Ses (50 mg x kg(-1)) group and the MCT + Ses (100 mg x kg(-1)) group, with 12 rats in each group. The PH rat model was induced through the subcutaneous injection with MCT(60 mg x kg(-1)). After the administration for four weeks, efforts were made to measure the right ventricular systolic pressure( RVSP) and mean pulmonary artery pressure (mPAP) through right jugular vein catheterization, and isolate right ventricle( RV) and left ventricle( LV) +septum (S) and measure their length to calculate RV/ ( LV + S) and ratio of RV to tibial length. Pathologic changes in arterioles were observed by HE staining. Masson's trichrome stain was used to demonstrate changes in collagen deposition of arterioles. The alpha-smooth muscle actin (alpha-SMA) expression in pulmonary arteries was measured by immunohistochemisty. The total antioxidative capacity (T-AOC) and malondialdehyde (MDA) content in pulmonary arteries were determined by the colorimetric method. The protein expressions of collagen I, NOX2 and NOX4 were analyzed by Real-time PCR and Western blot.</p><p><b>RESULT</b>After the administration for 4 weeks, Ses could attenuate RVSP and mPAP induced by MCT, RV/ (LV + S) and ratio of RV to Tibial length, alpha-SMA and collagen I expressions and remodeling of pulmonary vessels and right ventricle. Meanwhile, Ses could obviously inhibit the expressions of NOX2, NOX4 and MDA content and increase T-AOC.</p><p><b>CONCLUSION</b>Sesamin could ameliorate pulmonary vascular remodeling induced by monocrotaline in PH rats. Its mechanism may be related to expressions of NOX2 and NOX4 expression and reduction in oxidative stress injury.</p>


Subject(s)
Animals , Humans , Male , Rats , Dioxoles , Disease Models, Animal , Drugs, Chinese Herbal , Hypertension, Pulmonary , Drug Therapy , Genetics , Lignans , Lung , Metabolism , Membrane Glycoproteins , Genetics , Metabolism , Monocrotaline , NADPH Oxidase 2 , NADPH Oxidase 4 , NADPH Oxidases , Genetics , Metabolism , Pulmonary Artery , Metabolism , Rats, Sprague-Dawley , Vascular Remodeling
9.
Chinese Journal of Oncology ; (12): 804-809, 2015.
Article in Chinese | WPRIM | ID: wpr-286719

ABSTRACT

<p><b>OBJECTIVE</b>To investigate the effect of transforming growth factor-β1 (TGF-β1) on the differentiation of bone marrow-derived mesenchymal stem cells (MSCs) into cancer-associated fibroblasts(CAFs).</p><p><b>METHODS</b>MSCs were cultured in α-MEM with recombinant human TGF-β1 or in tumor-conditioned medium.The expression of CAFs markers were detected by immunofluorescence and quantitative RT-PCR.</p><p><b>RESULTS</b>The qRT-PCR assay showed that the expression of CAFs markers FAP, ACTA, CAV, CCL5, CXCR4, FSP1, SDF-1 and vimentin were 9.92±2.16, 7.76±1.28, 3.04±0.95, 3.28±2.16, 2.13±0.71, 1.41±0.66, 2.25±0.86 and 1.38±0.56, respectively, significantly upregulated in the MSCs co-cultured with TGF-β1 or TCM. The relative levels of FAP, ACTA, CAV, CCL5, CXCR4, FSP1, SDF-1 and vimentin mRNA in the TCM group were 7.52±1.76, 5.02±1.18, 1.98±1.19, 1.82±1.19, 2.95±0.86, 1.44±0.67, 2.08±0.74 and 1.47±0.55, respectively, indicating that MSCs can express CAFs phenotype.TGF beta signaling pathway inhibitor SB-431542 could inhibit the differentiation. Both immunofluorescence and Western blot confirmed the above results.</p><p><b>CONCLUSIONS</b>TGF-β1 induces differentiation of local MSCs to CAFs by upregulating the expression of pSmad3, so as to further promote the growth of cancer cells.</p>


Subject(s)
Humans , Benzamides , Pharmacology , Bone Marrow Cells , Cell Biology , Cell Differentiation , Cell Line, Tumor , Chemokine CXCL12 , Metabolism , Coculture Techniques , Culture Media, Conditioned , Dioxoles , Pharmacology , Fibroblasts , Cell Biology , Mesenchymal Stem Cells , Cell Biology , Organic Chemicals , Receptors, CXCR4 , Metabolism , Recombinant Proteins , Pharmacology , Smad3 Protein , Metabolism , Transforming Growth Factor beta1 , Pharmacology , Vimentin , Metabolism
10.
Chinese Journal of Cancer ; (12): 41-49, 2015.
Article in English | WPRIM | ID: wpr-349613

ABSTRACT

Epithelial ovarian cancer (OC) is a common gynecologic malignancy in women. The standard treatment for OC is maximal cytoreductive surgical debulking followed by platinum-based chemotherapy. Despite the high response rate to primary therapy, approximately 85% of patients will develop recurrent ovarian cancer (ROC). This review identifies the clinical use of trabectedin in the treatment algorithm for ROC, with specific emphasis on platinum-sensitive ROC, for which trabectedin in combination with pegylated liposomal doxorubicin has been approved as a treatment protocol. The main mechanisms of action of trabectedin at the cellular level and in the tumor microenvironment is also discussed as bases for identifying biomarkers for selecting patients who may largely benefit from trabectedin-based therapies.


Subject(s)
Female , Humans , Antineoplastic Agents, Alkylating , Therapeutic Uses , Clinical Trials as Topic , DNA Damage , Dioxoles , Pharmacology , Therapeutic Uses , Doxorubicin , Neoplasm Recurrence, Local , Drug Therapy , Neoplasms, Glandular and Epithelial , Drug Therapy , Ovarian Neoplasms , Drug Therapy , Polyethylene Glycols , Tetrahydroisoquinolines , Pharmacology , Therapeutic Uses , Tumor Microenvironment
11.
Journal of Biomedical Engineering ; (6): 400-404, 2014.
Article in Chinese | WPRIM | ID: wpr-290745

ABSTRACT

This study sought to investigate the in vivo antiviral effect of amantadine (AM) and biphenyl dimethyl dicarboxylate (DDB) on hepatitis B virus (HBV) in HBV replication mice. HBV replication-competent plasmid was transferred into male BALB/c mice by using hydrodynamics-based in vivo transfection procedure to develop HBV replication mouse model. The model mice were matched by body weigh, age and serum levels of hepatitis B e antigen (HBeAg) and were divided into four groups: AM group, DDB group, AM+DDB group and NS group, with the last one as control, and the mice of each group were administered corresponding agent orally twice a day, in a medication course lasting 3 d. On the third day, the mice were sacrificed 4-6 h after the last oral intake. HBV DNA replication intermediates in liver were analyzed by Southern blot hybridization. The serum hepatitis B surface antigen (HBsAg) and HBeAg were detected by enzyme linked immunosorbent assay (ELISA). Compared to the animals in the control group, HBV DNA replication intermediates in liver and HBsAg and HBeAg in serum from the AM and AM plus DDB group of mice decreased, and there was no difference between these two groups of mice. The levels of HBV DNA intermediate from liver and the serum HBsAg and HBeAg between the control and DDB group, however, were not obviously different. In conclusion, the inhibition effect of AM on HBV was detected, but treatment with DDB for 3 days did not influence the viral replication and expression of HBV in the HBV replication mice.


Subject(s)
Animals , Male , Mice , Amantadine , Pharmacology , Antiviral Agents , Pharmacology , DNA Replication , DNA, Viral , Dioxoles , Pharmacology , Disease Models, Animal , Hepatitis B , Virology , Hepatitis B Surface Antigens , Blood , Hepatitis B e Antigens , Blood , Hepatitis B virus , Physiology , Mice, Inbred BALB C , Plasmids , Transfection , Virus Replication
12.
Acta Pharmaceutica Sinica ; (12): 78-82, 2014.
Article in Chinese | WPRIM | ID: wpr-297967

ABSTRACT

High-speed counter-current chromatography (HSCCC) was used to high performance separate and prepare lignans from Schisandrae chinensis fructus. The solvent system is composed of n-hexane-ethyl acetate-methanol-water (9 : 1 : 5 : 5) and n-hexane-ethyl acetate-methanol-water (9 : 1 : 9 : 5), speed is at 900 r.min-1, and flow rate is at 2.0 mL.min-1. Five fractions from Schisandrae chinensis fructus extract were separated and prepared with one HSCCC process. They were identified as schisandrin, gomisin J, schisandrol B, schisantherin A and deoxyschizandrin by electrospray ionization-multiple tandem mass spectrometry (ESI-MSn), respectively. Their contents were obtained in 98.74%, 94.32%, 99.53%, 94.23% and 98.68% by ultra high performance liquid chromatography (UPLC), separately. The rapid and simple method can be applied for the preparation of lignans from Schisandrae chinensis fructus.


Subject(s)
Countercurrent Distribution , Cyclooctanes , Chemistry , Dioxoles , Chemistry , Drugs, Chinese Herbal , Chemistry , Fruit , Chemistry , Lignans , Chemistry , Molecular Structure , Plants, Medicinal , Chemistry , Polycyclic Compounds , Chemistry , Schisandra , Chemistry , Spectrometry, Mass, Electrospray Ionization , Tandem Mass Spectrometry
13.
Acta Pharmaceutica Sinica ; (12): 1442-1445, 2014.
Article in Chinese | WPRIM | ID: wpr-299114

ABSTRACT

To explore novel antifatigue agents targeting with AMPA receptor, 10 compounds were synthesized and their structures were confirmed by 1H NMR, ESI-MS and elemental analysis. 1-BCP was treated as the leading compound. The antifatigue activities were evaluated by weight-loaded forced swimming test, and the AMPA receptor binding affinities were tested with radioligand receptor binding assays. The results unveiled that 5b appeared to possess potent antifatigue activities and high affinity with AMPA receptor, which deserved further studies.


Subject(s)
Animals , Benzamides , Chemistry , Pharmacology , Dioxoles , Chemistry , Pharmacology , Fatigue , Piperidines , Chemistry , Pharmacology , Radioligand Assay , Receptors, AMPA , Metabolism , Swimming
14.
China Journal of Chinese Materia Medica ; (24): 1579-1583, 2014.
Article in Chinese | WPRIM | ID: wpr-300226

ABSTRACT

The effect of plant growth regulator forchlorfenuron (CPPU) 1 x 10(-6), 0.67 x 10(-6), 0.5 x 10(-6) on fruit morphology and effective components lignans was studied. Those morphologies were the combination of four basic morphological changes. The result showed, diametre were increased and longitudinal diametre of fruits were inhibited by foliage fertilizers including CPPU. At the same time, 1 000-grain weight and yield showed the varying degrees increase under CPPU. The order of the degree was 0.5 x 10(-6) > 1 x 10(-6) > 0.67 x 10(-6). Six lignans content of Schisandra chinensis of different harvest time and different CPPU processing groups were determined, the results showed that lignans accumulation occurred mainly in periods of premature the half mature fruiting stages. Under the 0.67 x 10(-6) CPPU treatment, schisandrol B, schisandrin B, schisandrin C content of S. chinensis showed different increase.


Subject(s)
Chromatography, High Pressure Liquid , Cyclooctanes , Metabolism , Dioxoles , Metabolism , Dose-Response Relationship, Drug , Fruit , Metabolism , Lignans , Metabolism , Phenylurea Compounds , Pharmacology , Polycyclic Compounds , Metabolism , Pyridines , Pharmacology
15.
Chinese Journal of Industrial Hygiene and Occupational Diseases ; (12): 357-360, 2014.
Article in Chinese | WPRIM | ID: wpr-306300

ABSTRACT

<p><b>OBJECTIVE</b>To investigate the protective effect of sesamin against cadmium chloride (CdCl2)-induced cardiotoxicity in rats.</p><p><b>METHODS</b>Fifty male Wistar rats were randomly assigned to five groups: control group, CdCl2 group, and low-, middle-, and high-dose sesamin groups. The control group was given normal saline. The CdCl2 group and sesamin groups were intraperitoneally injected with CdCl2 (5 mg/kg×2 d), and the low-, middle-, and high-dose sesamin groups were given 20, 40, and 80 mg/kg sesamin, respectively. All treatments lasted for four weeks. ECG was measured by a physiological recorder, and serum myocardial enzyme levels were determined by biochemical assay. The heart was weighed, and heart tissues were used in histopathological examination and determination of malondialdehyde (MDA) level.</p><p><b>RESULTS</b>Compared with the control group, the CdCl2 group showed significantly higher levels of serum CK and CK-MB, an increased heart coefficient, significant ST-segment elevation, and higher level of MDA in myocardial tissue (P < 0.05). Histopathological analysis showed edema of myocardial tissues and cells, myocardial fibers disorder, karyopyknosis, and uneven or deep staining of nuclear chromatin. Different doses of sesamin relieved the myocardial pathological changes induced by CdCl2, and high-dose sesamin was the most effective. The middle- and high-dose sesamin groups showed significantly reduced serum CK and CK-MB levels compared with the CdCl2 group (P < 0.05). The heart coefficient of the high-dose sesamin group (0.19±0.01%) was significantly lower than that of the CdCl2 group (0.21±0.01%) (P < 0.05). Myocardial MDA levels of the three sesamin groups (42.32±4.65, 36.71±5.34, and 33.12±4.62 nmol/mg pro, respectively) were all significantly lower than that of the CdCl2 group (55.87±3.65 nmol/mg pro) (P < 0.05).</p><p><b>CONCLUSION</b>Sesamin can relieve myocardial injury induced by CdCl2, and one possible mechanism is the enhancement of antioxidant capacity of myocardial tissue.</p>


Subject(s)
Animals , Male , Rats , Cadmium Chloride , Toxicity , Creatine Kinase, MB Form , Blood , Dioxoles , Pharmacology , Heart , Lignans , Pharmacology , Malondialdehyde , Metabolism , Myocardium , Metabolism , Pathology , Rats, Wistar
16.
The Korean Journal of Gastroenterology ; : 31-39, 2014.
Article in Korean | WPRIM | ID: wpr-113903

ABSTRACT

BACKGROUND/AIMS: Chronic hepatocellular damage is closely associated with hepatic fibrosis and fatal complication in most liver diseases. The aim of this study is to compare the efficacy and safety of biphenyl dimethyl dicarboxylate (DDB) and ursodeoxycholic acid (UDCA) in patients with abnormal ALT. METHODS: One-hundred thirty-five patients with elevated ALT were randomized to receive either 750 mg/day of DDB or 300 mg/day of UDCA for 24 weeks in 4 referral hospitals. Ninety-three (69%) patients had non-alcoholic steatohepatitits, 27 (20%) had alcoholic hepatitis, and 15 (11%) had chronic hepatitis. The primary end point was the rate of ALT normalization at week 24. The secondary endpoints were changes in AST, liver stiffness, and the incidence of adverse events. RESULTS: A total of 101 patients completed 24 weeks of therapy. ALT normalization at week 24 was observed in 44 (80.0%) patients in DDB group and 16 (34.8%) in UDCA group (p<0.001). Higher mean reduction of ALT levels from baseline to 24 weeks was seen in DDB group compared with UDCA group (-70.0% vs. -35.9%, p<0.001). Normalization of AST level (p=0.53) and change in the liver stiffness (p=0.703) were not significantly different between the two groups. Severe adverse drug reaction occurred in 1 patient in DDB group but the subject continued therapy during the study period. CONCLUSIONS: DDB was not inferior to UDCA for normalizing ALT level. Furthermore it was safe and well tolerated by patients with abnormal ALT.


Subject(s)
Adolescent , Adult , Aged , Female , Humans , Male , Middle Aged , Young Adult , Alanine Transaminase/blood , Cholagogues and Choleretics/therapeutic use , Dioxoles/therapeutic use , Double-Blind Method , Drug Administration Schedule , Follow-Up Studies , Hepatitis, Alcoholic/drug therapy , Hepatitis, Chronic/drug therapy , Non-alcoholic Fatty Liver Disease/drug therapy , Tertiary Care Centers , Treatment Outcome , Ursodeoxycholic Acid/therapeutic use
17.
Chinese Medical Journal ; (24): 3340-3343, 2013.
Article in English | WPRIM | ID: wpr-354484

ABSTRACT

<p><b>BACKGROUND</b>It has been reported that there is a significant difference in the local tissue concentration of transforming growth factor (TGF)-β1 between chronic rhinosinusitis without nasal polyps (CRSsNP) and chronic rhinosinusitis without nasal polyps (CRSwNP) patients. TGF-β has been reported to play an important role in regulating epithelial cell repair in lower airway remodeling and may be a critical factor involved in the remodeling process of chronic rhinosinusitis (CRS).</p><p><b>METHODS</b>Ethmoidal mucosal samples collected from CRS and healthy control patients were analyzed for TGF-β1, TGF-β receptor I, TGF-β receptor II, Smad3, phospho-Smad3, Smad7, and Smad anchor for receptor activation by Western blotting analysis. The proliferation of sinonasal epithelial cells at baseline and after TGF-β1 and/or EGF stimulation was evaluated by the MTT assay.</p><p><b>RESULTS</b>In CRSsNP, TGF-β1, TGF-β receptor I, TGF-β receptor II, and Smad3 protein levels were significantly higher than controls. In CRSwNP, TGF-β1, Smad3, and pSmad3 protein levels were significantly lower than controls. Smad7 protein was significantly higher in CRS than controls. In vitro experiments demonstrated that the baseline proliferation levels of sinonasal epithelial cells were lower in CRS than controls.</p><p><b>CONCLUSIONS</b>CRSwNP is characterized by a lower level of TGF-signaling compared with the control. In CRSsNP, although the upstream signaling of TGF-β was enhanced, the high Smad7 protein expression may restrain the downstream signaling components (e.g., pSmad3) and the TGF-β antiproliferative effect on sinonasal epithelium. The difference in the local tissue concentration of TGF-β1 between CRSsNP and CRSwNP patients did not result in significant differences in epithelial proliferation.</p>


Subject(s)
Adult , Aged , Female , Humans , Male , Middle Aged , Young Adult , Benzamides , Pharmacology , Cells, Cultured , Dioxoles , Pharmacology , Intracellular Signaling Peptides and Proteins , Metabolism , Protein Serine-Threonine Kinases , Metabolism , Receptors, Transforming Growth Factor beta , Metabolism , Serine Endopeptidases , Metabolism , Signal Transduction , Sinusitis , Metabolism , Smad3 Protein , Metabolism , Smad7 Protein , Metabolism , Transforming Growth Factor beta , Metabolism , Transforming Growth Factor beta1 , Metabolism
18.
Acta Pharmaceutica Sinica ; (12): 58-65, 2012.
Article in Chinese | WPRIM | ID: wpr-323080

ABSTRACT

This study is to observe anti-lipotoxic effect of sesamin on renovascular hypertensive rats fed with a high-fat, high-sucrose diet. Thirty-four complex model rats were induced by two-kidney, one-clip method and on high-fat and refined-carbohydrate diet for thirteen weeks. From the fifth week, intragastric administration of sesamin (120, 60 and 30 mg x kg(-1) x d(-1)) lasted for eight weeks. Blood pressure (BP), blood fat (BF), blood glucose (BG), free fatty acids (FFA), insulin (Ins), tumor necrosis factor (TNF)-alpha and interleukin (IL)-6 were determined. Pathological changes of pancreas, perirenal fat and liver were semiquantitatively analyzed. In sesamin (120 and 60 mg x kg(-1) x d(-1)) group, it was found that there were decrease of levels of BP, BF, BG, TNF-alpha, IL-6 and FFA, improvement of insulin resistance and glucose tolerance, alleviation of body weight, humid weight of fat, liver and pancreas and their organ index, and reduction of islet cell hyperplasia and amount of lipid droplet vacuoles in lipocyte and hepatocyte. It is implied that sesamin had anti-lipotoxic effect and its mechanism may be closely associated with the amelioration of insulin resistance via reducing lipidoses in hepatocyte and inflammatory adipokines such as TNF-alpha and IL-6.


Subject(s)
Animals , Male , Rats , Adipocytes , Anticholesteremic Agents , Pharmacology , Antihypertensive Agents , Pharmacology , Blood Glucose , Metabolism , Blood Pressure , Body Weight , Cholesterol , Blood , Diet, High-Fat , Dioxoles , Pharmacology , Dose-Response Relationship, Drug , Fatty Acids, Nonesterified , Blood , Glucose Tolerance Test , Hypertension, Renovascular , Blood , Pathology , Insulin , Blood , Insulin Resistance , Interleukin-6 , Blood , Islets of Langerhans , Pathology , Lignans , Pharmacology , Liver , Pathology , Pancreas , Pathology , Rats, Sprague-Dawley , Sucrose , Triglycerides , Blood , Tumor Necrosis Factor-alpha , Blood
19.
Journal of the Korean Association of Pediatric Surgeons ; : 12-17, 2012.
Article in Korean | WPRIM | ID: wpr-150787

ABSTRACT

The purpose of this study is to analyse clinical impact of specific MRI findings in liver in patients of long-term survivors after Kasai portoenterostomy (KPE). Twenty-eight patients who were underwent KPE were followed up more than 5 years. Macro-regenerative nodule (MRN) and beaded-duct dilatation (BDD) were considered as important findings in liver MRI. The association between these findings in MRI and clinical indicator, serum bilirubin level and history of cholangitis were evaluated. Sixteen patients (57.1%) were shown MRN in liver MRI. There were 14 patients(50%) whose MRI showed BDD. Serum total and direct bilirubin were 3.6mg/dL and 1.8mg/dL respectively in positive MRN group whereas 1.4mg/dL and 0.7mg/dL in negative MRN group (p 0.427). Serum total and direct bilirubin level were 4.2mg/dL and 2.1mg/dL in patients with BDD negative group compare to 1.1mg/dL and 0.5mg/dL in BDD positive group (p 0.281). The odds ratio to have cholangitis in the patient with MRN was 2.3 and 0.53 in patient with BDD in their MRI findings. MRN in liver MRI may suggest high bilirubin level and more chance to have cholangitis, but the findings of BDD may related to low bilirubin level and less change to have cholangitis.


Subject(s)
Humans , Biliary Atresia , Bilirubin , Cholangitis , Dilatation , Dioxoles , Liver , Odds Ratio , Survivors
20.
Journal of Korean Medical Science ; : 572-575, 2012.
Article in English | WPRIM | ID: wpr-119890

ABSTRACT

Sauchinone has been known to have anti-inflammatory and antioxidant effects. We determined whether sauchinone is beneficial in regional myocardial ischemia/reperfusion (I/R) injury. Rats were subjected to 20 min occlusion of the left anterior descending coronary artery, followed by 2 hr reperfusion. Sauchinone (10 mg/kg) was administered intraperitoneally 30 min before the onset of ischemia. The infarct size was measured 2 hr after resuming the perfusion. The expression of cell death kinases (p38 and JNK) and reperfusion injury salvage kinases (phosphatidylinositol-3-OH kinases-Akt, extra-cellular signal-regulated kinases [ERK1/2])/glycogen synthase kinase (GSK)-3beta was determined 5 min after resuming the perfusion. Sauchinone significantly reduced the infarct size (29.0% +/- 5.3% in the sauchinone group vs 44.4% +/- 6.1% in the control, P < 0.05). Accordingly, the phosphorylation of JNK and p38 was significantly attenuated, while that of ERK1/2, Akt and GSK-3beta was not affected. It is suggested that sauchinone protects against regional myocardial I/R injury through inhibition of phosphorylation of p38 and JNK death signaling pathways.


Subject(s)
Animals , Rats , Benzopyrans/pharmacology , Dioxoles/pharmacology , Glycogen Synthase Kinase 3/metabolism , JNK Mitogen-Activated Protein Kinases/metabolism , Mitogen-Activated Protein Kinase 1/metabolism , Mitogen-Activated Protein Kinase 3/metabolism , Myocardial Reperfusion Injury/metabolism , Phosphorylation , Protective Agents/pharmacology , Signal Transduction/drug effects , p38 Mitogen-Activated Protein Kinases/metabolism
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