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1.
Anticancer Res ; 39(8): 4095-4100, 2019 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-31366493

RESUMO

BACKGROUND/AIM: Ethacridine is used as a topical antiseptic as well as for second-trimester abortion. Recent studies showed that ethacridine is an inhibitor of poly(ADP-ribose) glycohydrolase (PARG) and an activator of the transcriptional coactivator with PDZ-binding motif (TAZ). This study examined the effects of ethacridine on thyroid cancer cells. MATERIALS AND METHODS: Thyroid cancer cell lines (FTC133 and SW1736) and thyroid follicular epithelial cells (Nthy-ori 3-1) were treated with ethacridine. Viability, clonogenicity, cell-cycle distribution, and apoptosis were evaluated. The expression of thyroid differentiation markers (TTF-1, PAX8, and NIS) was determined by real-time PCR. RESULTS: Ethacridine suppressed cell growth and clonogenic ability of thyroid cancer cells in a time- and dose-dependent manner (p<0.001). No cell-cycle arrest was found, but ethacridine dose-dependently induced apoptosis of thyroid cancer cells (p<0.001). The PAX8 and NIS expressions were significantly increased in SW1736 (3.41-fold and 1.53-fold, respectively) and Nthy-ori 3-1 cells (2.73-fold and 4.12-fold, respectively). CONCLUSION: Ethacridine elicits apoptotic cell death in thyroid cancer cells and promotes differentiation in a subset of thyroid follicular cells.


Assuntos
Apoptose/efeitos dos fármacos , Diferenciação Celular/efeitos dos fármacos , Etacridina/farmacologia , Neoplasias da Glândula Tireoide/tratamento farmacológico , Pontos de Checagem do Ciclo Celular/efeitos dos fármacos , Pontos de Checagem do Ciclo Celular/genética , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Proliferação de Células/genética , Regulação Neoplásica da Expressão Gênica/efeitos dos fármacos , Humanos , Fator de Transcrição PAX8/genética , Simportadores/genética , Neoplasias da Glândula Tireoide/genética , Neoplasias da Glândula Tireoide/patologia , Fator Nuclear 1 de Tireoide/genética
5.
Invest Ophthalmol Vis Sci ; 58(7): 3118-3126, 2017 06 01.
Artigo em Inglês | MEDLINE | ID: mdl-28632878

RESUMO

Purpose: GPR143 regulates melanosome biogenesis and organelle size in pigment cells. The mechanisms underlying receptor function remain unclear. G protein-coupled receptors (GPCRs) are excellent pharmacologic targets; thus, we developed and applied a screening approach to identify potential GPR143 ligands and chemical modulators. Methods: GPR143 interacts with ß-arrestin; we therefore established a ß-arrestin recruitment assay to screen for compounds that modulate activity. Because GPR143 is localized intracellularly, screening with the wild-type receptor would be restricted to agents absorbed by the cell. For the screen we used a mutant receptor, which shows similar basal activity as the wild type but traffics to the plasma membrane. We tested two compound libraries and investigated validated hits for their effects on melanocyte pigmentation. Results: GPR143, which showed high constitutive activity in the ß-arrestin assay, was inhibited by several compounds. The three validated inhibitors (pimozide, niclosamide, and ethacridine lactate) were assessed for impact on melanocytes. Pigmentation and expression of tyrosinase, a key melanogenic enzyme, were reduced by all compounds. Because GPR143 appears to be constitutively active, these compounds may turn off its activity. Conclusions: X-linked ocular albinism type I, characterized by developmental eye defects, results from GPR143 mutations. Identifying pharmacologic agents that modulate GPR143 activity will contribute significantly to our understanding of its function and provide novel tools with which to study GPCRs in melanocytes and retinal pigment epithelium. Pimozide, one of three GPR143 inhibitors identified in this study, maybe be a good lead structure for development of more potent compounds and provide a platform for design of novel therapeutic agents.


Assuntos
Albinismo Ocular/genética , Proteínas do Olho/genética , Doenças Genéticas Ligadas ao Cromossomo X/genética , Glicoproteínas de Membrana/genética , Mutação , RNA/genética , Albinismo Ocular/tratamento farmacológico , Albinismo Ocular/metabolismo , Células Cultivadas , Análise Mutacional de DNA , Etacridina/farmacologia , Éxons , Proteínas do Olho/antagonistas & inibidores , Proteínas do Olho/metabolismo , Doenças Genéticas Ligadas ao Cromossomo X/dietoterapia , Doenças Genéticas Ligadas ao Cromossomo X/metabolismo , Humanos , Ligantes , Glicoproteínas de Membrana/antagonistas & inibidores , Glicoproteínas de Membrana/metabolismo , Niclosamida/farmacologia , Linhagem , Pimozida/farmacologia
6.
Drug Discov Ther ; 11(6): 346-348, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-29332894

RESUMO

A lot of diseases occur on the skin of elderly persons. We report four elderly cases of bullous dermatosis that did not meet various differential diagnoses. Japanese, heart failure, atrophic skin and leg edema probably due to aging, as well as flaccid or tense bullae localized in legs were the common factors to our patients. Such conditions may be increased in coming aging society. Accordingly, it is worth regarding such symptom as the new clinical entity, which may comfort patients with similar condition and attract further attention.


Assuntos
Dermatoses da Perna/diagnóstico , Dermatopatias Vesiculobolhosas/diagnóstico , Fatores Etários , Idoso de 80 Anos ou mais , Anti-Infecciosos Locais/uso terapêutico , Diagnóstico Diferencial , Etacridina/uso terapêutico , Feminino , Insuficiência Cardíaca/complicações , Humanos , Mordeduras e Picadas de Insetos/diagnóstico , Dermatoses da Perna/complicações , Dermatoses da Perna/patologia , Dermatoses da Perna/terapia , Masculino , Penfigoide Bolhoso/diagnóstico , Pênfigo/diagnóstico , Dermatopatias Vesiculobolhosas/complicações , Dermatopatias Vesiculobolhosas/patologia , Dermatopatias Vesiculobolhosas/terapia , Meias de Compressão
7.
Arch Gynecol Obstet ; 295(1): 119-124, 2017 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-27658386

RESUMO

PURPOSE: This study was aimed to evaluate the safety and efficacy of the second-trimester medical abortions using mifepristone and ethacridine lactate in women with placenta previa and/or prior cesarean deliveries. METHODS: The patients who underwent a second-trimester pregnancy termination from January 2009 to December 2015 were retrospectively analyzed. The eligible patients were assigned to four groups based on placentation and cesarean history. The abortion interval (AI), blood loss, hospital stays, incidence of curettage, and transfusion were reviewed. RESULTS: Two women underwent cesarean sections for placenta increta. Finally, 443 patients were enrolled in this study, including 92 with placenta previa, 153 with prior cesarean deliveries, 36 with the both factors, and 236 with normal placentation and no cesarean delivery history. All the included cases had a successful vaginal delivery. There was no significant difference in AI, hospital stay, rate of hemorrhage, and transfusion among the four groups. Patients with prior cesarean section had higher blood loss than the normal group (P = 0.0017), as well as patients with both placenta previa and prior cesarean (P = 0.0018). However, there was no obvious blood loss in patients with placenta previa when compared with normal placetal patients (P = 0.23). No uterine rupture occurred in all patients. CONCLUSIONS: Mifepristone combined with ethacridine lactate is safe and effective for patients with low placentation or/and prior cesarean in the second-trimester pregnancy termination.


Assuntos
Aborto Induzido/métodos , Cesárea/métodos , Etacridina/uso terapêutico , Mifepristona/uso terapêutico , Placenta Prévia/tratamento farmacológico , Adulto , Etacridina/administração & dosagem , Etacridina/farmacologia , Feminino , Humanos , Mifepristona/administração & dosagem , Gravidez , Segundo Trimestre da Gravidez
8.
Thyroid ; 27(2): 292-299, 2017 02.
Artigo em Inglês | MEDLINE | ID: mdl-27829313

RESUMO

OBJECTIVE: The differentiation program for human thyroid follicular cells (TFCs) relies on the interplay between sequence-specific transcription factors and transcriptional co-regulators. Transcriptional co-activator with PDZ-binding motif (TAZ) is a co-activator that regulates several transcription factors, including PAX8 and NKX2-1, which play a central role in thyroid-specific gene transcription. TAZ and PAX8/NKX2-1 are co-expressed in the nuclei of thyroid cells, and TAZ interacts directly with both PAX8 and NKX2-1, leading to their enhanced transcriptional activity on the thyroglobulin (TG) promoter and additional genes. METHODS: The use of a small molecule, ethacridine, recently identified as a TAZ activator, in the differentiation of thyroid cells from human embryonic stem (hES) cells was studied. First, endodermal cells were derived from hES cells using Activin A, followed by induction of differentiation into thyroid cells directed by ethacridine and thyrotropin (TSH). RESULTS: The expression of TAZ was increased in the Activin A-derived endodermal cells by ethacridine in a dose-dependent manner and followed by increases in PAX8 and NKX2-1 when assessed by both quantitative polymerase chain reaction and immunostaining. Following further differentiation with the combination of ethacridine and TSH, the thyroid-specific genes TG, TPO, TSHR, and NIS were all induced in the differentiated hES cells. When these cells were cultured with extracellular matrix-coated dishes, thyroid follicle formation and abundant TG protein expression were observed. Furthermore, such hES cell-derived thyroid follicles showed a marked TSH-induced and dose-dependent increase in radioiodine uptake and protein-bound iodine accumulation. CONCLUSION: These data show that fully functional human thyroid cells can be derived from hES cells using ethacridine, a TAZ activator, which induces thyroid-specific gene expression and promotes thyroid cell differentiation from the hES cells. These studies again demonstrate the importance of transcriptional regulation in thyroid cell development. This approach also yields functional human thyrocytes, without any gene transfection or complex culture conditions, by directly manipulating the transcriptional machinery without interfering with intermediate signaling events.


Assuntos
Diferenciação Celular/efeitos dos fármacos , Etacridina/farmacologia , Células-Tronco Embrionárias Humanas/efeitos dos fármacos , Peptídeos e Proteínas de Sinalização Intracelular/efeitos dos fármacos , Células Epiteliais da Tireoide/efeitos dos fármacos , Tireotropina/farmacologia , Ativinas/farmacologia , Autoantígenos/efeitos dos fármacos , Autoantígenos/genética , Diferenciação Celular/genética , Células-Tronco Embrionárias Humanas/citologia , Humanos , Peptídeos e Proteínas de Sinalização Intracelular/genética , Iodeto Peroxidase/efeitos dos fármacos , Iodeto Peroxidase/genética , Proteínas de Ligação ao Ferro/efeitos dos fármacos , Proteínas de Ligação ao Ferro/genética , Fator de Transcrição PAX8/efeitos dos fármacos , Fator de Transcrição PAX8/genética , Receptores da Tireotropina/efeitos dos fármacos , Receptores da Tireotropina/genética , Simportadores/efeitos dos fármacos , Simportadores/genética , Tireoglobulina/efeitos dos fármacos , Tireoglobulina/genética , Células Epiteliais da Tireoide/citologia , Fator Nuclear 1 de Tireoide/efeitos dos fármacos , Fator Nuclear 1 de Tireoide/genética , Fatores de Transcrição
9.
Forensic Sci Int ; 268: e18-e22, 2016 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-27789047

RESUMO

Approximately during the 30th week of pregnancy, a woman gave birth to a still-born child in a hospital. After first citing an extraneous cause for the premature still-birth, the woman later admitted to having self-induced the abortion by injecting the antiseptic Rivanol® (active agent: ethacridine lactate) through her abdominal wall into the amniotic cavity. The investigating authorities ordered an autopsy of the fetus along with additional toxicological investigations. To the naked eye, no obvious cause of death was apparent. The main autopsy findings were four skin defects (puncture/stabbing wounds) on the ball of the fetus's left thumb, with slight bleeding around the punctures and into the underlying fatty tissue, and a yellowish discoloration of the fetus's body surface, especially of the umbilical cord and fingernails. On basis of the results, the child would have been viable. Femoral vein blood and urine from the fetus were analyzed for ethacridine, as were an amniotic fluid sample and maternal blood and urine samples, which had been collected as evidence. The concentration of ethacridine in the amniotic fluid was 16mg/l. In the postmortem fetal blood and urine samples, the concentrations were 0.36mg/l and 0.34mg/l, respectively, while concentrations of 0.091mg/l and 0.42mg/l, respectively, were found in the serum and urine samples from the mother. In many countries, foremost in China, ethacridine lactate, to which both mother and child are exposed, is widely used as safe abortion method. Although the ethacridine concentrations found in blood and urine samples of the mother in our case are consistent with published values, we believe to be the first to report postmortem ethacridine concentrations in a fetus. While exposure to ethacridine is not toxicologically relevant for the mother, it is fatal for the fetus because it causes the placental decidua capsularis to separate from the decidua parietalis or decidua placentalis, respectively. Prostaglandins that are then produced induce labor. In medicolegal contexts, the proof for an abortion through the administration of ethacridine lactate lies in the typical yellow discoloration of the fetus in conjunction with the toxicological demonstration of the substance in fetal body fluids, and if possible also in maternal body fluids.


Assuntos
Aborto Criminoso , Anti-Infecciosos Locais/administração & dosagem , Etacridina/administração & dosagem , Injeções Intraperitoneais , Adulto , Líquido Amniótico/química , Anti-Infecciosos Locais/análise , Etacridina/análise , Feminino , Sangue Fetal/química , Humanos , Masculino , Gravidez
10.
Talanta ; 160: 489-498, 2016 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-27591643

RESUMO

A simple and reliable method for preparing a selective dopamine (DA) sensor based on a molecularly imprinted polymer of ethacridine was proposed. The molecularly imprinted polymer electrode was prepared through electrodepositing polyethacridine-dopamine film on the glassy carbon electrode and then removing DA from the film via chemical induced elution. The molecular imprinted sensor was tested by cyclic voltammetry as well as by differential pulse voltammetry (DPV) to verify the changes in oxidative currents of DA. In optimized DPV conditions the oxidation peak current was well-proportional to the concentration of DA in the range from 2.0×10(-8)M up to 1×10(-6)M. The limit of detection (3σ) of DA was found to be as low as 4.4nM, by the proposed sensor that could be considered a sensitive marker of DA depletion in Parkinson's disease. Good reproducibility with relative standard deviation of 1.4% and long term stability within two weeks were also observed. The modified sensor was validated for the analysis of DA in deproteinized human serum samples using differential pulse voltammetric technique.


Assuntos
Dopamina/análise , Carbono/química , Dopamina/sangue , Dopamina/química , Técnicas Eletroquímicas , Eletrodos , Etacridina/química , Humanos , Limite de Detecção , Impressão Molecular , Polimerização , Polímeros/química
12.
Oncotarget ; 7(3): 2765-79, 2016 Jan 19.
Artigo em Inglês | MEDLINE | ID: mdl-26624983

RESUMO

Targeting Bruton's tyrosine kinase (BTK) with the small molecule BTK inhibitor ibrutinib has significantly improved patient outcomes in several B-cell malignancies, with minimal toxicity. Given the reported expression and constitutive activation of BTK in acute myeloid leukemia (AML) cells, there has been recent interest in investigating the anti-AML activity of ibrutinib. We noted that ibrutinib had limited single-agent toxicity in a panel of AML cell lines and primary AML samples, and therefore sought to identify ibrutinib-sensitizing drugs. Using a high-throughput combination chemical screen, we identified that the poly(ADP-ribose) glycohydrolase (PARG) inhibitor ethacridine lactate synergized with ibrutinib in TEX and OCI-AML2 leukemia cell lines. The combination of ibrutinib and ethacridine induced a synergistic increase in reactive oxygen species that was functionally important to explain the observed cell death. Interestingly, synergistic cytotoxicity of ibrutinib and ethacridine was independent of the inhibitory effect of ibrutinib against BTK, as knockdown of BTK did not sensitize TEX and OCI-AML2 cells to ethacridine treatment. Thus, our findings indicate that ibrutinib may have a BTK-independent role in AML and that PARG inhibitors may have utility as part of a combination therapy for this disease.


Assuntos
Apoptose/efeitos dos fármacos , Etacridina/farmacologia , Glicosídeo Hidrolases/antagonistas & inibidores , Leucemia Mieloide Aguda/tratamento farmacológico , Inibidores de Proteínas Quinases/farmacologia , Proteínas Tirosina Quinases/genética , Pirazóis/farmacologia , Pirimidinas/farmacologia , Tirosina Quinase da Agamaglobulinemia , Animais , Linhagem Celular Tumoral , Sinergismo Farmacológico , Quimioterapia Combinada , Humanos , Taninos Hidrolisáveis/farmacologia , Células Jurkat , Camundongos , Camundongos SCID , Interferência de RNA , RNA Interferente Pequeno/genética , Espécies Reativas de Oxigênio/metabolismo
13.
J Biochem ; 158(5): 413-23, 2015 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-25979969

RESUMO

Transcriptional co-activator with PSD-95/Dlg-A/ZO-1 (PDZ)-binding motif (TAZ) regulates in cell proliferation and differentiation. In mesenchymal stem cells it promotes osteogenesis and myogenesis, and suppresses adipogenesis. TAZ activators are expected to prevent osteoporosis, obesity and muscle atrophy. TAZ activation induces epithelial-mesenchymal transition, confers stemness to cancer cells and leads to poor clinical prognosis in cancer patients. In this point of view, TAZ inhibitors should contribute to cancer therapy. Thus, TAZ attracts attention as a two-faced drug target. We screened for TAZ modulators by using human lung cancer A549 cells expressing the fluorescent reporter. Through this assay, we obtained TAZ activator candidates. We unexpectedly found that ethacridine, a widely used antiseptic and abortifacient, enhances the interaction of TAZ and protein phosphatases and increases unphosphorylated and nuclear TAZ. Ethacridine inhibits adipogenesis in mesenchymal C3H10T1/2 cells through the activation of TAZ. This finding suggests that ethacridine is a bona fide TAZ activator and supports that our assay is useful to discover TAZ activators.


Assuntos
Adipogenia/efeitos dos fármacos , Fármacos Antiobesidade/farmacologia , Etacridina/farmacologia , Peptídeos e Proteínas de Sinalização Intracelular/agonistas , Células-Tronco Mesenquimais/efeitos dos fármacos , Proteína Fosfatase 1/metabolismo , Proteína Fosfatase 2/metabolismo , Transporte Ativo do Núcleo Celular/efeitos dos fármacos , Proteínas Adaptadoras de Transdução de Sinal/agonistas , Proteínas Adaptadoras de Transdução de Sinal/genética , Proteínas Adaptadoras de Transdução de Sinal/metabolismo , Linhagem Celular Tumoral , Avaliação Pré-Clínica de Medicamentos , Genes Reporter/efeitos dos fármacos , Células HEK293 , Humanos , Peptídeos e Proteínas de Sinalização Intracelular/antagonistas & inibidores , Peptídeos e Proteínas de Sinalização Intracelular/genética , Peptídeos e Proteínas de Sinalização Intracelular/metabolismo , Proteínas Luminescentes/genética , Proteínas Luminescentes/metabolismo , Células-Tronco Mesenquimais/citologia , Células-Tronco Mesenquimais/metabolismo , Fosfoproteínas/agonistas , Fosfoproteínas/genética , Fosfoproteínas/metabolismo , Fosforilação/efeitos dos fármacos , Regiões Promotoras Genéticas/efeitos dos fármacos , Proteína Fosfatase 1/química , Proteína Fosfatase 1/genética , Proteína Fosfatase 2/química , Proteína Fosfatase 2/genética , Processamento de Proteína Pós-Traducional/efeitos dos fármacos , Proteínas Serina-Treonina Quinases/antagonistas & inibidores , Proteínas Serina-Treonina Quinases/genética , Proteínas Serina-Treonina Quinases/metabolismo , Interferência de RNA , Proteínas Recombinantes de Fusão/química , Proteínas Recombinantes de Fusão/metabolismo , Fatores de Transcrição , Proteínas Supressoras de Tumor/antagonistas & inibidores , Proteínas Supressoras de Tumor/genética , Proteínas Supressoras de Tumor/metabolismo
14.
Chin Med J (Engl) ; 128(4): 450-4, 2015 Feb 20.
Artigo em Inglês | MEDLINE | ID: mdl-25673444

RESUMO

BACKGROUND: The rate of cesarean delivery has significantly increased in China in the last decade. Women with prior cesarean history tend to have a higher risk of uterine rupture during termination of the pregnancy in mid-trimester than those without such a history. The aim of our study was to evaluate the influences of the potential risk factors on uterine rupture in women with prior cesarean. METHODS: We conducted this retrospective study of women with prior cesarean section, who underwent mid-trimester pregnancy termination between January 2006 and December 2013 in Peking Union Medical College Hospital. The protocol was oral administration of mifepristone and misoprostol for the patients with the gestational ages below 16 weeks or intra-amniotic injection of ethacridine lactate (EL) for those with at least 16 weeks of gestational ages. The thickness of the lower uterine segment (LUS) was measured before the termination of pregnancy. Logistic regression was used to study the risk factors of uterine rupture. RESULTS: The total rate of successful abortion was 93.9% (62/66). Four patients failed in induction, and one of them received curettage, whereas the other three experienced uterine rupture (4.5%). The successful rates of abortion were 85.7% (30/35) for women treated with mifepristone-misoprostol and 86.1% (31/36) for those treated with EL. There was a significant difference in the mean LUS thickness between the uterine rupture group (3.0 ± 2.0 mm) and the nonrupture group (7.0 ± 3.0 mm) (P < 0.05). The LUS thickness of <3 mm was associated with uterine rupture during mid-trimester pregnancy termination in women with prior cesarean (odds ratio, 94.0; 95% confidence interval 4.2-2106.1) after adjusted maternal age, gestational age, interdelivery interval and prior cesarean section. Severe bleeding that required transfusion occurred in one case (1.5%). CONCLUSIONS: Both the mifepristone-misoprostol and the EL regimens were effective and safe for the termination of mid-trimester pregnancy in women with prior cesarean. A thinner LUS is associated with a relatively high risk of uterine rupture.


Assuntos
Aborto Induzido/efeitos adversos , Aborto Induzido/métodos , Cesárea , Etacridina/uso terapêutico , Feminino , Humanos , Mifepristona/uso terapêutico , Misoprostol/uso terapêutico , Gravidez , Trimestres da Gravidez , Estudos Retrospectivos , Ruptura Uterina/etiologia
15.
J Huazhong Univ Sci Technolog Med Sci ; 35(1): 129-134, 2015 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-25673206

RESUMO

Severe liver dysfunction in pregnancy (SLDP) is rare but serious complications with high mortality rate. This study compared the effectiveness and safety of double-balloon catheter versus intra-amniotic injection of ethacridine lactate for the termination of second trimester pregnancy in patients with SLD. A total of 55 patients with indications of labor induction were enrolled and analyzed by retrospective control analysis method. Twenty-three cases adopted Cook double balloon dilation as Cook group, and 32 cases received intra-amniotic injection of ethacridine lactate as EL group. The primary outcome was evaluated by successful abortion rate and the difference in the induction-to-abortion interval. Secondary outcomes included liver function recovery and the frequency of adverse events. Both Cook and EL regimens were effective, with successful abortion rate of 87.0% and 93.8%, respectively (P=0.639). The induction-to-delivery interval was similar between Cook group and EL group (38.1 ± 21.5 vs. 41.3 ± 17.4, P=0.543). The liver disease status was more severe in Cook group than in EL group, but it did not show any significant difference after pregnancy termination between the two groups and the improvement rate also did not show any significant difference. Both treatments were safe and there was no significant difference in bleeding and cervical laceration adverse events between the two groups. Our study firstly compared double-balloon catheter and ethacridine lactate for the induction of labor in women with SLD during second trimester pregnancy.


Assuntos
Aborto Induzido , Cateteres , Etacridina/administração & dosagem , Hepatopatias/fisiopatologia , Feminino , Humanos , Gravidez , Segundo Trimestre da Gravidez
16.
Eur J Obstet Gynecol Reprod Biol ; 178: 12-5, 2014 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-24948048

RESUMO

OBJECTIVE: To compare the efficacy of mifepristone and ethacridine lactate with ethacridine lactate alone for second trimester pregnancy termination. STUDY DESIGN: Two hundred and seventy-six healthy women between 16 and 27 weeks of gestation, desiring a termination, were assigned at random into two groups. The study group consisted of 140 women who received an intra-amniotic injection of 100mg ethacridine lactate, followed by oral administration of 50mg mifepristone at 0, 12 and 24h (total dose of mifepristone 150mg). The control group consisted of 136 women who received an intra-amniotic injection of 100mg ethacridine lactate alone. The primary outcome measure was the induction-to-abortion interval. Secondary outcomes included blood loss in 24h, successful abortion rate, retained placental tissue rate, rate of uterine evacuation and cervical laceration. RESULTS: Induction-to-abortion interval, blood loss in 24h, rate of retained placental tissue and uterine evacuation were significantly less in the study group compared with the control group (p<0.001). Termination was successful in 140 of 140 women (100%) in the study group and 133 of 136 women (97.8%) in the control group. All women in the study group delivered within 72h, and three nulliparous women in the control group did not deliver within 72h. The cervical laceration rate was 0 and 1.47% (2/136) in the study group and the control group, respectively. No significant difference in the successful abortion rate (p=0.235) or the cervical laceration rate (p=0.242) was found between the two groups. CONCLUSION: Mifepristone in combination with ethacridine lactate may significantly improve the outcomes of second trimester pregnancy termination compared with ethacridine lactate alone, without increasing complications and side effects apart from nausea.


Assuntos
Abortivos/administração & dosagem , Etacridina/administração & dosagem , Mifepristona/administração & dosagem , Aborto Induzido , Administração Intravaginal , Administração Oral , Adulto , China , Feminino , Humanos , Gravidez , Segundo Trimestre da Gravidez
17.
Int Wound J ; 11(6): 730-4, 2014 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-23445335

RESUMO

Increasing data suggesting that microorganisms in the biofilm form are among the leading agents of persistent infections of chronic wounds require the development of new approaches to treatment. The aim of this article was to compare the efficacy of three commonly used antiseptics using a biofilm-oriented approach. Biofilm-oriented antiseptics test (BOAT), the innovative method, allows to estimate, in a quick and reliable manner, the in vitro activity of working solutions of antiseptics in real contact times against bacteria in the biofilm form and to use the results in the selection of an appropriate antiseptic to treat local infections in the clinical practice.


Assuntos
Anti-Infecciosos Locais/farmacologia , Biofilmes/efeitos dos fármacos , Etacridina/farmacologia , Povidona-Iodo/farmacologia , Pseudomonas aeruginosa/efeitos dos fármacos , Piridinas/farmacologia , Staphylococcus aureus/efeitos dos fármacos , Pseudomonas aeruginosa/fisiologia , Staphylococcus aureus/fisiologia
18.
Artigo em Inglês | MEDLINE | ID: mdl-23841224

RESUMO

Matrix-assisted laser desorption/ionization (MALDI) has been shown to be highly sensitive for analyzing low-mass compounds such as metabolites if the right matrix is used. 9-aminoacridine (9AA) is the most commonly employed matrix for negative mode MALDI-MS in metabolomics. However, matrix interferences and the strongly varying sensitivity for different metabolites make a search for alternative matrices desirable, in order to identify compounds with a different chemical background and/or favoring a different range of analytes. We tested the performance of a series of potential negative mode MALDI matrices with a mix of 29 metabolites containing amino acids, nucleotide phosphates and Krebs cycle intermediates. While ethacridine lactate was found to provide limits of detection (LODs) in the low femtomole range for nucleotide phosphates, amino acids and Krebs cycle intermediates in the low picomole range, 4-amino-2-methylquinoline showed LODs in the picomole range for most metabolites, but is capable of ionizing a broader range of analytes than both 9AA and ethacridine.


Assuntos
Metabolômica/métodos , Espectrometria de Massas por Ionização e Dessorção a Laser Assistida por Matriz/métodos , Aminacrina/química , Aminoácidos/análise , Aminoácidos/química , Aminoquinolinas/química , Etacridina/química , Limite de Detecção , Nucleotídeos/análise , Nucleotídeos/química , Quinaldinas/química
19.
J Enzyme Inhib Med Chem ; 28(5): 894-9, 2013 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-22803677

RESUMO

Non-denaturing electrophoresis can be used to screen enzymes that self-regulate their activities by using a combination of enzymes and their inhibitors. Furthermore, this technique can be applied to develop enzyme reactors that self-regulate their activities. After separation of proteins from mouse liver cytosol by non-denaturing isoelectric focusing, lactate dehydrogense (LDH) and esterase activities were qualitatively and quantitatively examined using a combination of two-dimensional electrophoresis (2-DE) and non-denaturing stacking gel electrophoresis. Activities of mouse liver-derived LDH and carboxylesterase were reversibly inhibited by oxamate and 6,9-diamino-2-ethoxyacridine (acrinol), respectively, in the stacking gels and recovered when the enzymes migrated towards the separation gels. After separation and immobilization of the enzymes, their activities were inhibited by inhibitors and recovered after inhibitor removal. These results indicate that non-denaturing electrophoresis can be applied to select enzymes that self-regulate their activities and subsequently aid in the development of enzyme reactors that can control the enzyme activities.


Assuntos
Ativadores de Enzimas/metabolismo , Esterases/metabolismo , L-Lactato Desidrogenase/metabolismo , Eletroforese em Gel de Poliacrilamida Nativa , Animais , Citosol/enzimologia , Citosol/metabolismo , Relação Dose-Resposta a Droga , Eletroforese , Ativação Enzimática/efeitos dos fármacos , Inibidores Enzimáticos/química , Inibidores Enzimáticos/farmacologia , Esterases/antagonistas & inibidores , Esterases/isolamento & purificação , Etacridina/química , Etacridina/farmacologia , Focalização Isoelétrica , L-Lactato Desidrogenase/antagonistas & inibidores , L-Lactato Desidrogenase/isolamento & purificação , Fígado/enzimologia , Fígado/metabolismo , Camundongos , Ácido Oxâmico/química , Ácido Oxâmico/farmacologia , Relação Estrutura-Atividade
20.
Contraception ; 85(2): 211-4, 2012 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-22067783

RESUMO

BACKGROUND: We reviewed our experience with adding mifepristone to the protocol for the termination of pregnancy up to 24 weeks of gestation by intra-amniotic ethacridine lactate. STUDY DESIGN: The study consisted of women who presented for the termination of a second-trimester pregnancy between August 2000 and July 2008. RESULTS: Of 1245 women who requested a termination of a second-trimester pregnancy, 744 women underwent the induction of abortion by intra-amniotic ethacridine lactate with mifepristone (mifepristone group), and 501 received intra-amniotic ethacridine lactate alone (control group). The proportion of women who delivered within 24 h was 25.94% in the mifepristone group and 10.18% in the control group (p < .001); the failure rate of abortion was 5.38% in the mifepristone group and 4.99% in the control group (p < .001). There was no significant difference in the complication rate between the two groups. The rate of cervical laceration was 0.54% in the mifepristone group and 0.60% in the control group (p = .9315). The rate of retained placental tissue was 6.99% in the mifepristone group and 6.19% in the control group (p = .1112). Nausea was reported by 34.0% of women in the mifepristone group and none in the control group. CONCLUSION: The addition of mifepristone to ethacridine lactate may shorten the induction-to-abortion time compared with the use of ethacridine lactate alone without increasing the number of complications.


Assuntos
Abortivos Esteroides/administração & dosagem , Aborto Induzido , Anti-Infecciosos Locais/administração & dosagem , Etacridina/administração & dosagem , Mifepristona/administração & dosagem , Adulto , Feminino , Humanos , Gravidez , Segundo Trimestre da Gravidez , Adulto Jovem
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