Atividade citotóxica do extrato de Vitis labrusca em culturas de Trichomonas vaginalis / Cytotoxic activity of Vitis labrusca extract in cultures of Trichomonas vaginalis

Objetivos: Avaliar a atividade anti-Trichomonas vaginalis do extrato de folhas de videira (Vitis labrusca) provenientes de cultivo convencional e orgânico.Métodos: Extratos de folhas secas de videira, orgânico e convencional, foram elaborados com extrator Sohxlet. A composição fenólica total dos extratos foi avaliada por Folin-Cicoalteau e Cromatografia Líquida de Alta Eficiência. A atividade antiparasitária dos extratos foi realizada em cultura de T. vaginalis. Os testes foram realizados em três concentrações finais: 5, 10 e 20 mg/mL. Os trofozoítos foram contados em hemocitômetro e sua densidade foi ajustada em meio de cultura Trypticase-Yeast Extract-Maltose (TYM), de forma a se obter a concentração final de 1×105 trofozoítos/mL. Após incubação com os extratos por 24 horas a 37°C, foi feita a contagem dos trofozoítos com motilidade em hemocitômetro. Os controles do veículo foram realizados, adicionando-se água em substituição aos extratos.Resultados: O extrato de folhas convencionais é rico em catequina e os orgânicos, em resveratrol. Os extratos de V. labrusca não apresentaram atividade anti-T. vaginalis nas concentrações de 5 e 10 mg/mL. Entretanto na concentração de 20 mg/L, o extrato de folhas secas convencionais reduziu em 100% e o extrato orgânico em 48% a sobrevivência dos trofozoítos. Os polifenóis catequina, quercetina e rutina estavam em maior concentração no extrato com maior eficácia, os quais podem ser os responsáveis pela ação anti-T. vaginalis do extrato convencional.Conclusões: O extrato de folha de videira pode ser uma alternativa no combate a T. vaginalis. Estudos pré-clínicos e clínicos são necessários para comprovar eficácia e segurança desta intervenção...

AIMS: To evaluate the anti-Trichomonas vaginalis activity of the extract of organic and conventional leaves of Vitis labrusca.METHODS: Organic and conventional grapevine leaf extracts were prepared with extractor Sohxlet. The total phenolic extracts were evaluated by Folin-Cicoalteau and High-Performace Liquid Chromatography. The antiparasitic activity of the extracts was performed on growth of T. vaginalis. Tests were conducted at three final concentrations of 5, 10 and 20 mg/mL. The trophozoites were counted by hemocytometer and their density was adjusted in Trypticase-Yeast Extract-Maltose (TYM) growth environment in order to obtain a final concentration of 1x105 trophozoites/ml. After incubated with the extracts for 24 hours at 37 �C, the count of motile trophozoites was taken by hemocytometer. The vehicle controls were performed by substituting the extract by water.RESULTS: The conventional leaf extract is rich in catechin and the organic in resveratrol. The extracts of V. labrusca showed no anti-T.vaginalis activity at concentrations of 5 and 10 mg/mL. However in the concentration of 20 mg/L conventional grapevine leaf extracts reduced by 100% and the organic extract by 48% the survival of trophozoites. Catechin polyphenols, quercetin and rutin were in higher concentration in the extract with greater efficacy, which may be the responsible for the anti-T. vaginalis action of the conventional extract.CONCLUSIONS: The vine leaf extract may be an alternative to combat T. vaginalis. Pre-clinical and clinical studies are needed to confirm efficacy and safety of this intervention...

Validation of a modified fluorimetric assay for the screening of trichomonacidal drugs

A fluorimetric microassay that uses a redox dye to determine the viability of the flagellate Trichomonas vaginalis has been optimised to provide a more sensitive method to evaluate potential trichomonacidal compounds. Resazurin has been used in recent years to test drugs against different parasites, including trichomonadid protozoa; however, the reproducibility of these resazurin-based methods in our laboratory has been limited because the flagellate culture medium spontaneously reduces the resazurin. The objective of this work was to refine the fluorimetric microassay method previously developed by other research groups to reduce the fluorescence background generated by the media and increase the sensitivity of the screening assay. The experimental conditions, time of incubation, resazurin concentration and media used in the microtitre plates were adjusted. Different drug sensitivity studies against T. vaginalis were developed using the 5-nitroimidazole reference drugs, new 5-nitroindazolinones and 5-nitroindazole synthetic derivatives. Haemocytometer count results were compared with the resazurin assay using a 10% solution of 3 mM resazurin dissolved in phosphate buffered saline with glucose (1 mg/mL). The fluorimetric assay and the haemocytometer counts resulted in similar percentages of trichomonacidal activity in all the experiments, demonstrating that the fluorimetric microtitre assay has the necessary accuracy for high-throughput screening of new drugs against T. vaginalis.

Preparation and in vitro and in vivo study on tinidazole in situ forming sustained-release injection / 药学学报

This study is to prepare the in situ forming sustained-release injection which can perform sustained release behavior at the periodontal site for 7 days and to evaluate its in vitro and in vivo properties. After preparation of in situ forming sustained-release injection the in situ time was studied. And the surface of the solid injection was characterized by SEM. The rheological curve at 0 degrees C, 25 degrees C, 37 degrees C was determined and the impact of the temperature on the viscosity was examined. The in vitro release behavior was investigated. At last, rabbit periodontitis model was established to study its pharmacokinetics. The injection was stable, hard to stratify and decompose. The in situ forming time was about 6 seconds. It can easily adhere into periodontal pockets. There were lots of holes on the surface of the solid injection for the drug to diffuse. The drug releasing curves could be fit by Korsmeyer-Peppas equation. The drug smoothly released for 7 days at pH 7.4 PBS buffer with a very slight burst release and maintained a certain concentration. In vivo pharmacokinetics results indicated that after administration with the in situ forming injection, achievement of tinidazole (TNZ) concentration in gingival crevicular fluid (GCF) was more comparable and long-lasting than usual solution of TNZ management and relatively constant TNZ levels were attained until 168 h. All these results supported the prospect of tinidazole in situ forming sustained-release injection in clinical applications.

Empiema pleural causado por tricomonas: caso clínico / Pleural empyema caused by trichomonas: case report

Pleural empyema formation is one of the potential complications of lower respiratory tract infections and it is characterized by bacterial organisms seen on gram stain or the aspiration of pus on thoracentesis. Very rarely empyema can be caused by trichomonas species, of which Trichomonas Tenax appears to be the most common cause. In this article we report the case of a 51-year-old man who developed a pleural empyema caused by trichomonas, and review the available literature of this rare infection of unknown incidence and uncertain pathogenetic significance. Our patient was treated with metronidazole, however complete cure was not achieved and pulmonary decortication was necessary for the successful outcome. As far as we know, this is the first case of pleural empyema caused by trichomonas reported in Chile.

La formación de un empiema pleural es una de las potenciales complicaciones de las infecciones de la vía aérea inferior, y se caracteriza por la observación de bacterias en la tinción de Gram, o la aspiración de pus en la toracocentesis. Muy infrecuentemente el empiema puede ser causado por alguna de las especies de tricomonas, de las cuales Trichomonas Tenax parece ser la causa más común. En este artículo, reportamos el caso de un hombre de 51 años que desarrolló un empiema pleural causado por tricomonas, y revisamos la literatura disponible de esta rara infección, de incidencia desconocida, y significancia patogénica incierta. Nuestro paciente fue tratado con metronidazol, observándose sólo una respuesta parcial, necesitándose decorticación pulmonar para una recuperación completa. Hasta donde sabemos, este es el primer caso de empiema pleural causado por tricomonas reportado en Chile.

Antitrichomonal and antioxidant activities of Dorstenia barteri and Dorstenia convexa

Dorstenia barteri and D. convexa extracts and some isolated components of the former were investigated for effectiveness against Trichomonas gallinarum and compared with quercetin and quercitrin. The antioxidant activity of the extracts/compounds was also determined. The minimum lethal concentrations (MLCs) for the extract of D. barteri leaves and twigs at 24 h were found to be 15.625 and 15.625 æg/ml, respectively. However, the MLCs of the leaf and twig extract of D. convexa were 125 and 437.5 æg/ml, respectively. The prenylated and geranylated chalcones were as active as the prenylated flavones, 6-prenylapigenin and the diprenylated derivative 6,8-diprenyleridictyol. The order of the antitrichomonal activity of the compounds at 24 h was: quercetin (0.121 æg/ml) > quercitrin (0.244 æg/ml) > or = bartericin B (0.244 æg/ml) > bartericin A (0.73 æg/ml) > stigmasterol (0.98 æg/ml) > 6,8-diprenyleridictyol = isobavachalcone = dorsmanin F (31.25 æg/ml). D. barteri extracts, quercitrin, and bartericin A, and the prenylated flavonoids had potent antioxidant properties. The twig extract of D. barteri was more potent than the leaf extract. Moderate (EC50 >50 æg/ml) and high (EC50 <50 æg/ml) antioxidant activities were detected in the leaf and twig extracts of D. barteri and the prenylated flavonoids. Prenylated flavonoids and the isolated compounds with antioxidant properties described here may account for the anti-inflammatory action of these extracts. The antitrichomonal and antioxidant activities shown by the extracts and compounds in this study are consistent with the ethnomedicinal and local use of the Dorstenia species studied.

Efficacy and tolerability of a combination of ofloxacin and tinidazole in the management of infectious diabetic foot ulcer.

The management of infectious diabetic foot ulcers is a major concern. Various treatment modalities are used. The efficacy and tolerability of a combination of ofloxacin and tinidazole in diabetic foot ulcer has been assessed in 60 patients in the present trial. The results are promising.

Relative bioavailability of two brands of ornidazole in twelve healthy volunteers.

AIM OF THE STUDY: To determine the bioequivalence of two marketed ornidazole formulations in healthy volunteers. METHODOLOGY: A single dose relative bioavailability of Ornidazole 1.5 g (3 x 500 mg tablets) of test product (Giro, Panacea Biotec Ltd.) and that of standard reference (Dazolic, Sun Pharmaceutical Industries), was investigated in healthy adult males. A total of 12 subjects wee enrolled in the study and investigations consisted of two treatment phases separated by a washout period of seven days. Both treatment phases were of 12 hours durations each. Blood samples were collected at 0, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10 and 12 hours post-administration of assigned drug product. Appropriate fasting restrictions were employed during both the treatment phases. Drug assay was done using HPTLC method. The statistical significance of difference in pharmacokinetic parameters between preparations was tested using ANOVA. RESULTS: The mean peak plasma concentration (Cmax) of 32.67 +/- 4.45 microg/ml was achieved at 1.54 +/- 0.81 hours following administration of test product as against mean Cmax of 31.55 +/- 5.04 microg/ml at 1.79 +/- 0.89 hours for reference standard. The area under time concentration curve (AUC(0-12)) hours was 261.67 +/- 77 microg/ml hours with reference standard and 265.41 +/- 30.82 microg/ml hours for test product. CONCLUSION: There was no statistically significant difference between the two formulations and the two products

Biological variability in clinical isolates of Trichomonas vaginalis

Eighteen clinical isolates of Trichomonas vaginalis were obtained from women who attended health centers of the Goverment of Madrid. A total of 1,848 vaginal specimens recovered during the gynaecological examination were seeded in culture tubes containing liquid Diamond medium. Pathogenicity to mice was determined after intraperitoneal inoculation of mice by quantification of mortality and gross damage to abdominal organs. As could be expected, a broad variability was obtained, being some of the isolates more virulent than the reference strain. Regarding to metronidazole susceptibility, none resistant isolate was found but different degrees of susceptibility were determined

Eradication of Helicobacter pylori with lansoprazole based triple therapy in peptic ulcer disease.

Lansoprazole 30 mg, amoxicillin 1000 mg, and tinidazole 500 mg were given twice daily to 39 peptic ulcer patients (26 duodenal and 13 gastric ulcer, mean age 52.4 +/- 15.01) who had H. pylori infection for two weeks. Additional lansoprazole 30 mg daily was given to duodenal and gastric ulcer patients for another two and six weeks respectively. Follow-up gastroduodenoscope was performed at fourth and eighth week and eighth and twelfth week for all duodenal and gastric ulcer patients, respectively. H. pylori status was evaluated by rapid urease test (CLO test) and histology at first and last endoscope. The ulcers were healed at the last endoscopy in 11 (85%) gastric ulcer patients and 24 (92%) duodenal ulcers patients. H. pylori infection was eradicated in 31 patients (79%). Mild side effects were observed in 15 per cent. In conclusion, 2 week regimen of lansoprazole, amoxicillin, and tinidazole triple therapy resulted in a relatively high healing rate of peptic ulcer (90%) and an acceptable eradication rate of H. pylori infection (79%).

In vitro sensitivity of Trichomonas vaginalis to DNA topoisomerase II inhibitors.

Vaginal trichomoniasis is a highly prevalent sexually transmitted disease caused by a microaerophilic protozoan Trichomonas vaginalis. The disease is one of the most common sexually transmitted disease and can augment the predisposition of individuals to human immunodeficiency virus (HIV) infection. Although the disease can be treated with metronidazole and related 5-nitroimidazole, cases of trichomonal vaginitis which are refractory to standard treatment seems to be increasing. Clearly, new antitrichomonad agents are needed and DNA topoisomerase II may acts as a new target for antitrichomonad agents. In this study, in vitro sensitivity of T. vaginalis to DNA topoisomerase II was investigated. Axenic culture of local strain of T. vaginalis was performed. Both eukaryotic and prokaryotic DNA topoisomerase II inhibitors such as ellipticine, amsacrine and fluoroquinolones were tested for effectiveness against T. vaginalis in vitro compared to metronidazole. T. vaginalis was sensitive to metronidazole under aerobic conditions. Minimal inhibitory concentrations (MICs) of eukaryotic DNA topoisomerase II inhibitors, ellipticine and amsacrine, were 6.4 mM and 64 mM, respectively. The MICs of prokaryotic DNA topoisomerase II or DNA gyrase inhibitors; ciprofloxacin, ofloxacin and norfloxacin were 64, 960 and 1,280 mM, respectively. Based on the results, among DNA topoisomerase II inhibitors ellipticine was the most effective drug against T. vaginalis in vitro whereas fluoroquinolones did not show high antitrichomonad activity.

Aspectos técnicos e vantagens da realizaçäo de estomas por video-laparoscopia / Thecnical aspects and advantages of laparoscopic stoma creation

A derivaçäo do conteúdo fecal pode ser realizada por meio de laparotomia ou de maneira mais simples pela técnica conhecida como "trephine stoma". A laparotomia apresenta as desvantagens de requerer incisäo abdominal maior, resultado em dor, íleo pós-operatório e complicaçöes potenciais como aderências abdominais e infecçäo. Já a técnica de trefinaçäo prevê visualizaçäo insuficiente além de näo permitir exploraçäo da cavidade abdominal. A realizaçäo de operaçöes colorretais por acesso laparoscópico representa um grande avanço e uma alternativa importante à cirurgia convencional. Neste trabalho säo apresentados alguns aspectos técnicos, indicaçöes e as vantagens da confecçäo de estomas intestinais por VL. Os autores concluem que este procedimento é seguro e tecnicamente simples, requerendo equipamento mínimo; além disso, permite reproduzir detalhes técnicos importantes da cirurgia convencional, facilita a inspeçäo da cavidade abdominal, a verificaçäo da orientaçä e vitalidade das alças intestinais, o estadiamento de neoplasias e apresenta todas as vantagens potenciais de um procedimento minimamente invasivo. Por todos os motivos apresentados, o desvio do trânsito intestinal por vídeo-laparoscopia representa o método ideal nas derivaçöes intestinais paliativas e é uma opçäo atraente para aqueles que estäo se iniciando no treinamento em cirurgia laparoscópica colorretal

Itraconazol + Secnidazol* cápsulas vs. óvulos vaginales Acetónido de Fluocinolona 0.05 mg, Nistatina 100,000 U y Metronidazol 500 mg en el tratamiento sintomático de la vaginitis / Itraconazol + Secnidazol* capsules Vs. Acetónido of Fluocinolona 0.05 mg, Nistatina 100,000 U and Metronidazol 500 mg vaginal ovules, en the symptomatic treat of vaginitis

Objetivo: Evaluar la eficacia del tratamiento oral en las vaginitis y la vaginosis con intraconazol y secnidazol, comparándolo con el tratamiento tópico con óvulos vaginales de acetónido de fluocinolona, nistatina 100 000 U. y metronidazol 500 mg. Diseño: Estudios comparativos, longitudinal, prospectivo y abierto Lugar: Servicio de Reproducción Humana. Centro Médico Nacional "20 de Noviembre" I.S.S.S.T.E. Material y métodos: Fueron incluidas 40 pacientes del sexo femenino que asistieron a la consulta externa del Servicio de Reproducción humana con diagnóstico de vaginitis y vaginosis, se dividieron al azar en dos grupos. Grupo 1 (20 pacientes) que recibieron tratamiento oral con Itraconazol y secnidazol y el grupo 2 (20 pacientes) que recibieron tratamiento tópico con fluocinolona, nistatina y metronidazol. Se citaron a las pacientes a los 7 y 14 días después de iniciado el tratamiento valorando la intensidad de la sintomatología clínica y la eficacia del tratamiento. Resultados: Las características poblacionales de ambos grupos no mostraron diferencias. La leucorrea fue el síntoma más importante en ambos grupos el cual fue de intensidad moderada severa, y mostró una diferencia en la evaluación post-tratamiento estadísticamente significativa a favor de las pacientes tratadas con itraconazol y secnidazol. En cuanto al ardor, prurito, dispareunia y disuria no mostraron diferencias en la evaluación post-tratamiento, sin embargo la mejoría fue estadísticamente significativa entre el día 1 y 7 de tratamiento en favor del grupo tratado con Itraconazol y Secnidazol. conclusión. El tratamiento con Itraconazol y Secnidazol ofrece mejoría en menor tiempo y la comodidad que ofrece en cuanto a la facilidad de administración lo hacen un medicamento adecuado para el tratamiento de la vaginitis y la vaginosis o ambas

Profilaxia das complicaçöes pós-operatórias no tratamento cirúrgico das doenças do intestino grosso: I - Infecçäo / Prophylaxy of the postoperative complications in the surgical treatment of the large bowel diseases: I - Infection

A infecçäo pós-cirúrgica continua sendo causa de altos índices de morbimortalidade entre os pacientes operados de doenças do intestino grosso. Os avanços nos cuidados intensivos, a anestesia moderna, as drogas de uso para a profilaxia do tromboembolismo e de complicaçöes cardiorrespiratórias e as conquistas materiais que trouxeram progressos técnicos, de certa forma, permitiram a soluçäo de problemas cirúrgicos mais complexos numa populaçäo mais idosa e de mais alto risco, com reduçäo da mortalidade precoce mas com a chance de aumento da morbidade, em geral, devido às complicaçöes infecciosas. Nesse campo houve relevantes conquistas, principalmente após as publicaçöes de Burke, enriquecidas pela descoberta de grande e diversificado número de novos e potentes antimicrobianos. Apesar disso e das novas modalidades de preparo intestinal mecânico, o índice de complicaçöes infecciosas na prática cirúrgica colorretal permanece invariável, nos últimos anos, indicando que essas duas modalidades de prevençäo atingiram o seu máximo. Se nós pretendermos diminuir ainda mais as complicaçöes sépticas decorrentes das operaçöes cirúrgicas sobre o intestino grosso devemos redirecionar nossas pesquisas para outros fatores que näo os antibióticos ou os métodos de limpeza mecânica dos cólons. Atualmente, vários estudos têm sido endereçados para a resposta imune retardada e a sisceptibilidade a infecçäo. A competência técnica do cirurgiäo tem sido, novamente, valorizada; número de operaçöes a que o paciente é submetido, número de procedimentos cirúrgicos numa mesma operaçäo, duraçäo do ato operatório, tempo de internaçäo pré-operatória, idade do paciente, seu estado nutricional, doenças associadas de repercussäo sistemica; doenças como o diabetes, a insuficiência renal, o alcoolismo crônico, o câncer, as doenças imunossupressoras ou a imunossupressäo terapêutica etc., têm recebido ênfase como fatores de risco para a infecçäo pós-operatória