Potential of natural repellents methylanthranilate and anthraquinone applied on maize seeds and seedlings against house sparrow (Passer domesticus) in captivity / Potencial de repelentes naturais, metilantranilato e antraquinona aplicados em sementes de milho e mudas contra o pardal (Passer domesticus) em cativeiro

Abstract Various bird pests caused severe economic losses to valuable crops and fruit orchards all over the world. Among the birds, house sparrow is also considered to cause heavy plunder, not only to seeds of crops but also seedlings especially in organic farming. In present study two bird repellents, methylanthranilate and anthraquinone tested against house sparrows on maize seeds and seedlings in aviary conditions. Trial group in aviary-I, the treated maize seeds and seedlings with different doses of both bird repellents, control group in aviary-II, untreated seeds and seedlings were provided for three hours in the early morning. In each aviary, two closed circuit cameras were also installed to monitor the behavioral responses against different concentrations of both chemical repellents. Statistical analysis showed that there existed highly significant (P<0.01) variations among the trial and control groups for seeds and seedlings. By comparing both repellents, significant (P<0.05) differences were detected and anthraquinone showed better efficacy when compared to methylanthranilate, but in maize seedlings both repellents equal repellent properties. Non-significant (P>0.05) differences were observed in different grading of both natural chemical repellents for maize seeds while significant (P<0.05) variations were noticed for maize seedlings when provided to sparrows. By videotaped behavior sparrows presented manifest head juddering and feather upsetting activities by consumption of treated seeds and seedlings with higher concentrations of both natural bird repellents.

Resumo Várias pragas de aves causaram graves perdas econômicas para cultivos valiosos e pomares de frutas em todo o mundo. Entre os pássaros, o pardal da casa também é considerado um grande saqueo, não só para as sementes das culturas, mas também para as mudas, especialmente na agricultura orgânica. No presente estudo, dois repelentes de aves, metilantranilato e antraquinona testados contra pardais de casa em sementes de milho e mudas em condições de aviário. O grupo de ensaio em aviary-I, as sementes de milho tratadas e as mudas com diferentes doses de repelentes de aves, grupo de controle em aviary-II, sementes não tratadas e mudas foram fornecidas por três horas no início da manhã. Em cada aviário, duas câmeras de circuito fechado também foram instaladas para monitorar as respostas comportamentais contra diferentes concentrações de ambos os repelentes químicos. A análise estatística mostrou que existiam variações altamente significativas (P<0,01) entre os grupos de teste e controle para sementes e mudas. Ao comparar os dois repelentes, detectaram-se diferenças significativas (P<0,05) e a antraquinona apresentou maior eficácia quando comparada ao metilantranilato, mas em mudas de milho, ambos os repelentes são iguais às propriedades repelentes. As diferenças não significantes (P>0,05) foram observadas em diferentes classificações de repelentes químicos naturais para sementes de milho, enquanto as variações significativas (P<0,05) foram observadas para as mudas de milho quando fornecidas aos pardais. Por um comportamento gravado em video, os pardais apresentaram manifestações de cabeça e vibrações de penas por consumo de sementes tratadas e mudas com maiores concentrações de repelentes de aves naturais.

Tranilast inhibits myocardial fibrosis in mice with viral myocarditis / 中国当代儿科杂志

<p><b>OBJECTIVE</b>To investigate the effect of tranilast on myocardial fibrosis in mice with viral myocarditis (VMC).</p><p><b>METHODS</b>Male balb/c mice (n=72) were randomly divided into control, VMC and tranilast groups (n=24 each). In the VMC and tranilast groups, the mice were infected with Coxsackie virus B3 (CVB3) to prepare VMC model, while the control group was treated with Eagle's medium. After modeling, the tranilast group was administrated with tranilast [200 mg/(kg.d)] until the day before sampling. On days 7, 14 and 28 after CVB3 or Eagle's medium infection, heart specimens (n=8) were taken and examined after Toluidine blue staining and Nissl staining for counts of mast cells (MC), hematoxylin-eosin staining for myocardial pathological changes, and Masson staining for myocardial fibrosis. The expression of CTGF and type I collagen (Col I) in the myocardial tissue was measured by RT-PCR and Western blot. The correlations of CTGF mRNA expression with MC counts and Col I expression were analyzed.</p><p><b>RESULTS</b>The myocardial pathological changes and collagen volume fraction in the VMC group were significantly higher than in the control group at all three time points (P<0.05). Tranilast treatment significantly decreased the myocardial pathological changes and collagen volume fraction compared with the VMC group (P<0.05). The mRNA and protein expression of CTGF and Col I increased in the VMC group compared with the control group, and the increases were reduced with tranilast treatment (P<0.05). The number of MC was positively correlated to CTGF mRNA expression on the 7th day and 14th day (r=0.439, P=0.049) in the VMC group. There were positive correlations between the mRNA expression of Col I and CTGF on the 7th day and 14th day (r=0.646, P=0.007) and the 28th day (r=0.326, P=0.031).</p><p><b>CONCLUSIONS</b>Tranilast may inhibit the aggregation of MC and down-regulate the expression of CTGF, relieving myocardial fibrosis of mice with VMC.</p>

Tolfenamic Acid Inhibits the Proliferation, Migration, and Invasion of Nasopharyngeal Carcinoma: Involvement of p38-Mediated Down-Regulation of Slug

PURPOSE: Tolfenamic acid (TA), a non-steroidal anti-inflammatory drug, is known to exhibit antitumor effects in various cancers apart from nasopharyngeal cancer (NPC). NPC exhibits high invasiveness, as well as metastatic potential, and patients continue to suffer from residual, recurrent, or metastatic disease even after chemoradiation therapy. Therefore, new treatment strategies are needed for NPC. In this study, we investigated the efficacy and molecular mechanisms of TA in NPC treatment. MATERIALS AND METHODS: TA-induced cell death was detected by cell viability assay in the NPC cell lines, HNE1 and HONE1. Wound healing assay, invasion assay, and Western blot analysis were used to evaluate the antitumor effects of TA in NPC cell lines. RESULTS: Treatment with TA suppressed the migration and invasion of HNE1 and HONE1 cells. Hepatocyte growth factor enhanced the proliferation, migration, and invasion abilities of NPC cells. This enhancement was successfully inhibited by TA treatment. Treatment with TA increased phosphorylation of p38, and the inhibition of p38 with SB203580 reversed the cytotoxic, anti-invasive, and anti-migratory effects of TA treatment in NPC cell lines. Moreover, inhibition of p38 also reversed the decrease in expression of Slug that was induced by TA treatment. CONCLUSION: In conclusion, the activation of p38 plays a role in mediating TA-induced cytotoxicity and inhibition of invasion and migration via down-regulation of Slug.

Preoperative tranilast as adjunctive therapy to primary pterygium surgery with a 1-year follow-up / Terapia auxiliar com o tranilast pré-operatório na cirurgia do pterígio primário com um ano de seguimento

Purpose: To determine the efficacy of tranilast as an adjunctive therapy in conjunctival autograft. Methods: Twenty-nine patients were randomly allocated to the Tranilast Group (n=15) or the Control Group (n=14). The Tranilast Group received a subconjunctival injection of 0.5% tranilast 30 days prior to surgery. Conjunctival autograft was performed in both groups using fibrin sealant and 0.02% subconjunctival mitomycin C at the end of the surgery. After the resection of the pterygium, immunohistochemistry was performed with 100 cells to identify epithelial cells positive for transforming growth factor-β (TGF-β). Subjective symptoms were evaluated using a 5-point scale, and the recurrence rate was assessed. Results: Both groups showed improvements in their symptoms and similar clinical results. Compared with the Control Group, the Tranilast Group failed to show a decreased recurrence rate (p=0.59). However, the number of epithelial cells expressing TGF-β was lower in the Tranilast Group (5 cells; 95% CI: 2.56-13.15; Control Group, 16 cells, 95% CI: 11.53-24.76; p=0.01). Minimal but reversible complications, including glaucoma secondary to corticosteroids and granuloma, occurred during the study. Conclusion: Tranilast was effective in decreasing the number of pterygium epithelial cells expressing TGF-β. .

Objetivo: Determinar a eficácia do tranilast, como terapia auxiliar no transplante autólogo de conjuntiva. Métodos: Vinte e nove pacientes foram randomizados em dois grupos: Grupo Tratado (15) e Grupo Controle (14). Trinta dias antes da cirurgia, o Grupo Tratado recebeu uma injeção subconjuntival de tranilast a 0,5%. O transplante autólogo de conjuntiva foi realizado em ambos os grupos, usando-se a cola de fibrina e a mitomicina 0,02% subconjuntival, ao final da cirurgia. Cada paciente foi examinado por 12 meses de acompanhamento. A imuno-histoquímica foi realizada, mediante um total de 100 células, a fim de que se contassem as células epiteliais positivas, para o fator de crescimento transformador beta (TGF-β), após a cirurgia do pterígio. Os sintomas subjetivos foram avaliados usando-se uma escala de cinco pontos, e a taxa de recorrência foi avaliada. Resultados: Os 2 grupos apresentaram melhora dos sintomas e com resultados clínicos similares. Quando comparado com o Grupo Controle, o Grupo Tratado falhou em mostrar uma diminuição da taxa de recorrência (p=0,59). Entretanto o número de células epiteliais expressando o TGF-β foi menor no Grupo Tratado (5 células; 95% CI=2,56-13,15; Grupo Controle, 16 células; 95% CI: 11,53-24,76, p=0,01). Complicações mínimas, mas reversíveis, ocorreram durante o estudo, incluindo glaucoma secundário ao uso de corticoide e granuloma. Conclusão: O tranilast foi efetivo em diminuir o número células epiteliais do pterígio expressando o TGF-β. .

Effect of tranilast on myocardial fibrosis in mice with viral myocarditis / 中国当代儿科杂志

<p><b>OBJECTIVE</b>To study the role of tranilast in the pathogenesis of myocardiac fibrosis in viral myocarditis.</p><p><b>METHODS</b>Seventy-two BALB/C mice were randomly divided into control, model and intervention groups (n=24 each). Mice in the model and intervention groups were infected with Coxsackievirus B3 to induce viral myocarditis. The intervention group was given with tranilast (200 mg/kg) by gavage until sacrifice for sampling, while the other two groups were administered with the same volume of normal saline. Cardiac tissues were obtained from 8 mice on 7, 14 and 28 days after modeling. The mast cell number was observed by toluidine blue staining and thionine staining. The cardiac tissues were stained with hematoxylin and eosin as well as masson trichrome to observe the pathological changes in cardiac tissues. The mRNA and protein expression of osteopontin and transforming growth factor-β1 was measured by RT-PCR and immunohistochemistry respectively.</p><p><b>RESULTS</b>In the model group, the mRNA and protein expression of osteopontin reached the highest level on the 7th day, decreasing from the 14th day, and became to the least on the 28th day; while the expression of TGF-β1 increased from the 7th day, reaching a peak on the 14th day, and decreased slightly on the 28th day. The mRNA and protein expression of TGF-β1 and OPN was lower in the intervention group than the model group (P<0.05), but higher than the control group (P<0.05). The expression of OPN mRNA was positively correlated to the number of mast cells.</p><p><b>CONCLUSIONS</b>Tranilast can reduce myocardial fibrosis by decreasing the number of mast cells, inhibiting the expression of TGF-β1 and OPN.</p>

Tranilast attenuates TGF-beta1-induced epithelial-mesenchymal transition in the NRK-52E cells

We previously reported that tranilast can halt the pathogenesis of chronic cyclosporine nephrotoxicity in rats via the transforming growth factor-beta [TGF-beta] /Smad pathway, an important signaling system involved in epithelialmesenchymal transition [EMT], but the exact underlying cellular mechanisms are not yet clear. Thus, by selecting [0]TGF-beta1-induced normal rat kidney proximal tubular epithelial cells [NRK-52E] as a model, we demonstrated potential modifying effect of tranilast on EMT-induced by TGF-beta1 in vitro. NRK-52E cells were incubated with the blank vehicle [Dulbecco's modified Eagle's medium and F-12 [DMEM/F12] added with 10% fetal bovine serum [FBS]], 10 ng/ml TGF-beta1 alone or together with 100, 200 or 400microM tranilast for 48 h after incubation in medium containing 1% FBS for 24 h. Cell morphological changes were observed to confirm occurrence of EMT. Protein expressions of two typical markers of EMT, E-cadherin and alpha-smooth muscle actin [alpha-SMA], were assessed by western blotting and flow cytometry, respectively. Our results showed that TGF-beta1 induced spindle-like morphological transition, the loss of Ecadherin protein and upregulation of expression of alpha-SMA. However, the TGF-beta1-produced changes in cellular morphology, E-cadherin and alpha-SMA were inversed by tranlilast in concentration-dependent manner. Our findings indicate that tranilast can directly inhibit EMT. Thus, it may be implied that regulation of EMT be the target to prevent renal tubulointerstitial fibrosis.

Outcome of the patients with chronic mesh infection following open inguinal hernia repair / 대한외과학회지

PURPOSE: Hernia repairs are the most common elective abdominal wall procedures performed by general surgeons. The use of a mesh has become the standard for hernia repair surgery. Herein, we discuss a management strategy for chronic mesh infections following open inguinal hernia repair with onlay prosthetic mesh. METHODS: In this study, 15 patients with chronic mesh infections following open inguinal hernia repairs were included. The medical records of these patients were retrospectively reviewed and information regarding presentation, type of previous hernia repair, type of mesh, operative findings and bacteriological examination results were obtained. In all cases, the infected mesh was removed completely and the patients were treated with antibiotic regimens and local wound care. RESULTS: Fifteen mesh removals due to chronic infection were performed between January 2000 and March 2012. The mean interval of hernia repair to mesh removal was 49 months. All patients were followed up for a median period of 62 months (range, 16 to 115 months). In all patients, the infections were resolved successfully and none were persistent or recurrent. However, one patient developed recurrent hernia and one developed nerve injury. CONCLUSION: Chronic mesh infection following hernia repair mandates removal of the infected mesh, which rarely results in hernia recurrence.

Role of Postoperative Radiotherapy for Microscopic Margin Involvement in the Squamous Cell Carcinoma of Esophagus / Journal of the Korean Cancer Association, 대한암학회지

PURPOSE: The objective of this study was to assess the effect of postoperative radiotherapy on the outcome of esophageal cancer with microscopically positive resection margin by comparing the results with those of patients with negative resection margin. MATERIALS AND METHODS: Medical records of 88 patients treated with macroscopic resection followed by postoperative radiotherapy for stage II or III squamous cell carcinoma of the esophagus from June 1984 to March 2008 were reviewed. Twelve patients had received chemotherapy. Patients were classified into two groups based on resection margin status: negative resection margin (group A, n=66) and microscopically positive resection margin (group B, n=22). Median follow-up duration of living patients was 68 months (range, 18 to 115 months). Median total radiation dose of group A and group B was 51.5 Gy (range, 45 to 69 Gy) and 52.1 Gy (range, 45 to 64 Gy), respectively. RESULTS: Median overall survival and disease-free survival were 15 and 10 months, respectively. The five-year overall survival, disease-free survival, and local control rates for group A and group B were 15.9% and 16.4%, 13.5% and 9.1%, and 76.3% and 69.6%, respectively. No statistically significant difference in terms of overall survival, disease-free survival, and local control (p=0.295, p=0.209, and p=0.731, respectively) was observed between group A and group B. Seven patients experienced toxicity of grade 3 or higher. CONCLUSION: A significant portion of patients with margin involvement reached long term survival after addition of postoperative radiotherapy. These results suggest a potential role of postoperative radiotherapy, especially for patients with margin involvement.

Surgical Resection for Lung Metastases from Colorectal Cancer

PURPOSE: The lung is the second most common site of metastasis from colorectal cancer. Of all patients who undergo a curative resection for colorectal cancer, 10% to 15% will develop lung metastasis. As a hepatic resection of colorectal liver metastases results in improved survival, many reports have suggested that a pulmonary resection of a colorectal lung metastasis would also improve survival. The aim of this study was to analyze the postoperative outcomes of and the prognostic factors for a surgical resection of a lung metastasis. METHODS: Between August 1997 and March 2006, 27 patients underwent surgical resections for colorectal lung metastases at Seoul St. Mary's hospital. A retrospective review of patients' characteristics and various tumor factors was performed. RESULTS: The mean interval between colorectal resection and lung metastasis was 24.0 +/- 15.1 months. The overall 3- and 5-year survival rates were 76.5% and 22.2%, respectively. The mean follow-up after pulmonary resection was 39.5 +/- 21.6 months (range, 3.3 to 115 months). Except for the existence of hilar-lymph-node metastasis (P < 0.001), no risk factors that we studied were statistically significant. Two patients had hilar-lymph-node metastasis. They survived for only for 3.3- and 11.6-months, respectively. CONCLUSION: In our study, we found that a pulmonary resection for metastases from colorectal cancer may improve survival in selected patients.

Determination of salylic acid, syringic acid, benzoic acid and anthranilic acid in Radix Isatidis by HPCE / 中国中药杂志

<p><b>OBJECTIVE</b>To develop a simple and rapid capillary electrophoresis (CE) method for the separation and determination of four active organic acids including salicylic acid, syringic acid, benzoic acid, and anthranilic acid in Radix Isatidis.</p><p><b>METHOD</b>The HPCE system consisted of a fused-silica capillary column of 47.3 cm (38.3 cm to the detector) x50 microm i.d. and a mixture ofacetonitrile-borate buffer (15% acetonitrile, 25 mmol L(-1) borate, 15 mmol L(-1) beta-CD, pH 9.10) solution as the operating buffer. The applied voltage was 11.5 kV and the UV detection was set at 220 nm. The effects of the applied voltage, detection wavelength, and the pH of buffer, the concentration of buffer, acetonitrile and beta-CD were investigated.</p><p><b>RESULT</b>The linear calibration rang was 3.0-90 mg L(-1) (r=0.9994) for salylic acid, 4.0-120 mg L(-1) (r=0.9995) for syringic acid, 2.0-60 mg L(-1) (r=0.9998) for benzoic acid and 5.0-100 mg L(-1) (r=0.9992) for anthranilic acid. The recoveries of salylic acid, syringic acid, benzoic acid and anthranilic acid were 95.9%-102.6%, 98.6%-103.4%, 98.7%-104.1%, 96.1%-104.3% respectively. The detection limits of salylic acid, syringic acid, benzoic acid and anthranilic acid were 0.7, 1.1, 1.2 and 1.5 mg L(-1), respectively.</p>

Acute Hyponatremic Encephalopathy after Ingestion of Polyethylene Glycol Solution before Colonoscopy / 대한소화기내시경학회지

Preparation for colonoscopy involves a thorough cleansing of the large bowel. Cleansing is performed using several methods, including ingestion of 4 liters of polyethylene glycol solution. However, these methods can induce hyponatremia by various mechanisms. Severe or rapidly progressing hyponatremia can result in the swelling of the brain, and the symptoms of hyponatremia are mainly neurological. Recently, we encountered a 41-year-old woman who developed acute hyponatremia with encephalopathy after undergoing bowel preparation for colonoscopy. She presented with general weakness, nausea, headache, agitation, delusions, and slurred speech one day after the ingestion of polyethylene glycol solution. Her serum sodium level was very low (110 to 115 mEq/L). Her symptoms pertaining to hyponatremia continued to persist for more than 2 days despite continuous intravenous administration of hypertonic saline for the correction of hyponatremia.

Expression Patterns of KCNJ10 K+ Channel in the Cochlear Lateral Wall After Acoustic Trauma / 대한이비인후과학회지

BACKGROUND AND OBJECTIVES: It is well known that noise exposure leads to the sensory hair cell loss and other neuronal damage in the cochlea. But recently it has been reported that noise exposure could also damage lateral wall of cochlea such as stria vascularis and spiral ligament. K+ is the major cation in endolymph and important to maintain homeostasis within the cochlea. We have investigated the expression patterns of KCNJ10 K+ channel in noise induced cochlear damage. MATERIALS AND METHOD: Twenty adult male guinea pigs (300-350 g) were included in this study. In experimental group (n=16), acoustic trauma was induced by continuous broad band noise for 2 hr to 115 dB SPL and broad band noise for 6 hr to 120 dB SPL with 3 consecutive days. After noise exposure, auditory brainstem response threshold shift and hair cell loss were evaluated. A study for KCNJ10 K+ channel expression was examined by immunohistochemical staining. RESULTS: After noise exposure, auditory brainstem response showed transient threshold shift (TTS) and permanent threshold shift (PTS) in accordance with noise exposure. The expression patterns of CKNJ10 K+ channel were changeable in TTS group. But there were no change of expression patterns in PTS group. CONCLUSION: In the cochlear lateral wall, KCNJ10 K+ channel expressions were affected with noise exposure and these changes might be associated with the regulation of homeostasis in the cochlea lateral wall.

The Effectiveness of Tranilast in the Prevention of Posterior Capsular Opacity

PURPOSE: To evaluate the inhibitory effect of tranilast on the formation of posterior capsular opacity (PCO) after a cataract operation ex vivo and in a rabbit model. METHODS: A human lens epithelial cell line (B3) was treated with 0.005-0.1 mM tranilast. Cytotoxicity assessment and effective dosage determination of tranilast were performed using MTT assays. B3 cell lines were cultured in Eagle's minimal essential medium (EMEM) containing 20% FBS with different concentrationsof tranilast, and morphological differences were observed. To investigate the effect of tranilast on cytokine production in B3 cell lines, cells were treated with 0.01 mM tranilast and expression profiles of cytokines were analyzed by RT-PCR. After performing phacoemulsification and intraocular lens implantation in 10 white rabbits, 0.5% tranilast eye drops were given 4 times per day, and the severity of PCO was evaluated bi-weekly using POCOman for 8 weeks after the operation. RESULTS: Cell death was observed in the 0.05 mM tranilast-treated B3 cell lines, and inhibition of epithelial-mesenchymal transition (EMT) was also observed in the 0.01 mM tranilast-treated B3 cell lines. TGF-beta1/2, IL-18, and CDK7 mRNA expression decreased in the 0.01 mM tranilast-treated B3 cell lines. Significant suppression of PCO formation was observed in rabbits treated with 0.5% tranilast eye drops 5 weeks post operative (p<0.05). CONCLUSIONS: The results from this study show that tranilast suppresses EMT through inhibition of TGF-beta, IL-18,and CDK7 expression. The results suggest that tranilast can be used toprevent PCO formation after cataract surgery.

The Effectiveness of Tranilast in the Prevention of Posterior Capsular Opacity

PURPOSE: To evaluate the inhibitory effect of tranilast on the formation of posterior capsular opacity (PCO) after a cataract operation ex vivo and in a rabbit model. METHODS: A human lens epithelial cell line (B3) was treated with 0.005-0.1 mM tranilast. Cytotoxicity assessment and effective dosage determination of tranilast were performed using MTT assays. B3 cell lines were cultured in Eagle's minimal essential medium (EMEM) containing 20% FBS with different concentrationsof tranilast, and morphological differences were observed. To investigate the effect of tranilast on cytokine production in B3 cell lines, cells were treated with 0.01 mM tranilast and expression profiles of cytokines were analyzed by RT-PCR. After performing phacoemulsification and intraocular lens implantation in 10 white rabbits, 0.5% tranilast eye drops were given 4 times per day, and the severity of PCO was evaluated bi-weekly using POCOman for 8 weeks after the operation. RESULTS: Cell death was observed in the 0.05 mM tranilast-treated B3 cell lines, and inhibition of epithelial-mesenchymal transition (EMT) was also observed in the 0.01 mM tranilast-treated B3 cell lines. TGF-beta1/2, IL-18, and CDK7 mRNA expression decreased in the 0.01 mM tranilast-treated B3 cell lines. Significant suppression of PCO formation was observed in rabbits treated with 0.5% tranilast eye drops 5 weeks post operative (p<0.05). CONCLUSIONS: The results from this study show that tranilast suppresses EMT through inhibition of TGF-beta, IL-18,and CDK7 expression. The results suggest that tranilast can be used toprevent PCO formation after cataract surgery.

Changes in hemodynamic parameters and regional myocardial perfusion measured by thermal diffusion probe from the infusion of norepinephrine during displacement of porcine beating heart / 대한마취과학회지

BACKGROUND: This study was done to evaluate the sole effect of norepinephrine on the regional myocardial perfusion during displacement of the porcine beating heart using thermal diffusion method. METHODS: Thermal diffusion probe was inserted into the anterior myocardial wall during 20 procedures in 10 male pigs (30-35 kg). The measurements of regional myocardial perfusion and hemodynamic parameters were performed after complete instrumentation (baseline), after displacement of the beating heart anteriorly, and 5 and 15 minutes after norepinephrine infusion, titrated to restore baseline mean arterial pressure (MAP). RESULTS: Norepinephrine infusion reversed the decrease in MAP and myocardial perfusion, caused by displacement of the beating heart (62 +/- 3% to 115 +/- 4% of baseline, P < 0.01; 41 +/- 5% to 125 +/- 4% of baseline, P < 0.05, respectively). CONCLUSIONS: Restoration of MAP with norepinephrine infusion without any preload augmentation reversed deterioration in regional myocardial perfusion during displacement of the porcine beating heart.

Antagonistic effects of tranilast on proliferation and collagen synthesis induced by TGF-beta2 in cultured human trabecular meshwork cells / 华中科技大学学报（医学）（英德文版）

Whether tranilast had antagonistic effect on proliferation inhibition and collagen synthesis promotion induced by TGF-beta2 in cultured human trabecular meshwork cells was investigated. Suspension of 1 x 10(4) cultured human trabecular meshwork cells of 3-5 passage was distributed in each well of a 96-well disk and divided into control group and experimental group. After 24 h, 0 microg/ml (control), 12.5 microg/ml, 25 microg/ml, 50 microg/ml tranilast with 3.2 ng/ml TGF-beta2 were added into the incubation medium. Another 24 h later, proliferation and collagen synthesis in cultured human trabecular meshwork cells were examined respectively by using tetrazolium-based semiautomated colormetric (MTT) assay and 3H-proline incorporation with liquid scintillation technique. The results showed absorbance (A) values of the experimental groups were 0.9036 +/- 0.3017, 1.1361 +/-0.1352, 1.2457 +/- 0.1524 according to the different concentrations of tranilast, and 0.8956 +/-0.1903 of the control group. In comparison with the control group, 25 microg/ml (q'= 3.23, P< 0.05), 50 microg/ml (q'=4.70, P<0.01) tranilast significantly antagonized the decrease of the A values induced by TGF-beta2 in the cultured human trabecular meshwork cells. In comparison with the control group [817.37+/-124.21 cpm/10(4) cells], 12.5 microg/ml (620.33+/-80.46 cpm/10(4) cells, q'= 4.26, P<0.05), 25 microg/ml (594.58+/-88.13 cpm/10(4) cells, q'=4.81, P<0.01), 50 microg/ml (418.64+/-67.90 cpm/10(4) cells, q'=8.62, P<0.01) tranilast significantly inhibited the incorporation of 3H-proline into the cultured human trabecular meshwork cells promoted by TGF-beta2 in a dose-dependent manner. It was concluded that tranilast had the antagonistic effect on the proliferation inhibition and collagen synthesis promotion induced by TGF-alpha2 in the cultured human trabecular meshwork cells.

Dexamethasone decreases migraine recurrence observed after treatment with a triptan combined with a nonsteroidal anti-inflammatory drug

BACKGROUND AND OBJECTIVES: Triptans are effective drugs for the acute treatment of migraine. However, 30-40 percent of the patients commonly present recurrence before 24 hours therefore requiring another dose. Nonsteroidal anti-inflammatory drugs (NSAID) such as tolfenamic acid and naproxen sodium combined with sumatriptan have demonstrated efficacy in reducing recurrence observed with the single use of this drug. Steroids also have been suggested to treat refractory migraine and status migranosus. The aim of this study was to evaluate whether patients presenting frequent recurrence with the combination triptan plus NSAID, would decrease it with the association of dexamethasone. METHOD: Twenty three patients, 17 women and 6 men with migraine according to IHS criteria were prospectively studied. All patients presented frequent recurrence ( > or = 60 percent, mean recurrence rate 74,8 percent) with the single use of sumatritpan 100mg or zolmitriptan 2,5mg or rizatriptan 10mg in at least 5 consecutive attacks, and didn't present a reduction of the recurrence rate superior than 20 percent with the combination of tolfenamic acid 200mg or rofecoxib 25mg in at least 5 other consecutive attacks (mean recurrence rate 60 percent). The patients had to treat 6 consecutive moderate or severe migraine attacks with their usual combination plus 4mg of dexamathasone with a maximum of twice a week, and fill out a diary reporting headache parameters. RESULTS: Twenty patients, 16 women and 4 men completed the study. Of those who completed the study, 11 took rizatriptan plus rofecoxib, 4 rizatriptan plus tolfenamic acid, 3 zolmitriptan plus rofecoxib, 1 zolmitriptan plus tolfenamic acid and 1 patient took sumatriptan plus tolfenamic acid, having the 20 patients taken as a third medication, a single tablet of 4mg of dexamethasone. All patients took oral formulations and none presented vomiting after that. Among all 20 patients, one female and one male patient presented recurrence in 3 out of the 6 attacks (50 percent) while the remaining 18 patients revealed recurrence in 1 or 2 treated attacks (mean 23,4 percent) (p<0,001). CONCLUSION: We concluded that the judicious use of oral dexamethasone might be useful for a limited population of migraine patients still presenting recurrence with the combination of a triptan and a NSAID. Case-control studies and studies with a randomized double-blind design are necessary to confirm these observations

Synthesis and behaviour of a static benzoxazinone derivative towards nitrogen and sulphur nucleophieles

4 [H]-3,l-BENZOXAZIN-4-one derivatives bear saturated aliphatic substituents at position-2, [so called dynamic benzoxazinones], e.g., CH[3][1] C[3]H[7] [iso] [2], CH[2]COCH[3][3], CH2CN[4], C[3]H[7][n] and CH[2]CH[2]COOH[5] are among the more recent heterocyclic compounds. The electronically unsaturated character of these rings made difficult the synthesis of satisfactorily stable rings. New organic substituents with special properties in steric and in an electronic manner-helped to solve this problem. In the last two decades, our contribution to the solution of this problem includes the use of bulk substituents involving strong conjugation power [which so called static benzoxazinones[6-12]. In continuation of our recent article [1,3], on the behaviour of a static benzoxazinone derivative towards nitrogen and carbon nucleophiles, another derivative namely 2-[2-[4-bromohydroxyimmobenzyl] phenyl]-4[H]-3,l-benzoxazin-4-one [3] was obtained via the interaction of 1 - [4-bromophenyl] -4[H] -3,2 -benzoxazin-4-one [2] with anthranilic acid in boiling n-butanol in which hetero-ring opening takes place followed by cyclisation

new route for the synthesis of some quinazoline derivatives

S-methyl monothiomalonanilide hydroiodide 1 is a versatile compound for synthesizing the aimed quinazoline derivatives. Thus, compound 1 reacted with either anthranilic acid or ethyl anthranilate hydrochloride to yield 2. Also, polysubstituted pyranylquinazolinone was obtained by the reaction of quinazolin derivative 6 with p-chloro- alpha-cyano-cinnamonitrile 9. Chemical and spectroscopic evidences for the structures of the newly synthesized compounds were described