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Braz. j. biol ; 84: e253948, 2024. tab, graf
Article in English | LILACS, VETINDEX | ID: biblio-1355909


Abstract The assessment of the comparative effect of biosal (phytopesticide), deltamethrin, and lambda-cyhalothrin (pyrethroids) were made against two fodder pests, Hermolaus modestus and Hermolaus ocimumi by filter paper impregnation method. The activity of total protein contents, GPT (glutamic-pyruvic transaminase) and GOT (glutamic oxaloacetate transaminase) were affected in Hermolaus modestus and Hermolaus ocimumi against biosal, deltamethrin, and lambda cyhalothrin. The activity of total protein contents in H. modestus was 31.053%, 4.607%, and 24.575%, against biosal, deltamethrin, and lambda-cyhalothrin, respectively. The activity of total protein contents was observed as 24.202%, 15.25%, and 56.036% against deltamethrin, lambda-cyhalothrin, and biosal, respectively in H. ocimumi. The activity of GOT was observed as 98.675% for biosal 33.95% for deltamethrin and 83.619% for lambda-cyhalothrin in H. modestus. The GOT activity was estimated in H. ocimumi as 78.831%, 47.645%, and 71.287% against biosal, deltamethrin, and lambda-cyhalothrin, respectively. The efficacy of GPT enzyme against biosal, deltamethrin, and lambda-cyhalothrin was calculated as 89.26%, 73.07%, and 47.58%, respectively in H. modestus. The H. ocimumi showed GPT activity as 77.58% for biosal, 68.84% for deltamethrin, and 52.67% for lambda-cyhalothrin, respectively.

Resumo A avaliação do efeito comparativo do biosal (fitopesticida), deltametrina e lambda-cialotrina (piretróides) foi feita contra duas pragas forrageiras, Hermolaus modestus e Hermolaus ocimumi, pelo método de impregnação com papel de filtro. A atividade do conteúdo de proteína total, GPT (transaminase glutâmico-pirúvica) e GOT (oxaloacetato transaminase glutâmico) foram afetados em Hermolaus modestus e Hermolaus ocimumi contra biosal, deltametrina e lambda cialotrina. A atividade do conteúdo de proteína total em H. modestus foi 31.053%, 4.607% e 24.575%, contra biosal, deltametrina e lambda-cialotrina, respectivamente. A atividade do conteúdo de proteína total foi observada como 24.202%, 15.25% e 56,036% contra deltametrina, lambda-cialotrina e biosal, respectivamente em H. ocimumi. A atividade do GOT foi observada em 98.675% para o biosal, 33,95% para a deltametrina e 83.619% para a lambda-cialotrina em H. modestus. A atividade do GOT foi estimada em H. ocimumi como 78.831%, 47.645% e 71.287% contra biosal, deltametrina e lambda-cialotrina, respectivamente. A eficácia da enzima GPT contra biosal, deltametrina e lambda-cialotrina foi calculada como 89.26%, 73.07% e 47.58%, respectivamente em H. modestus. A H. ocimumi apresentou atividade GPT de 77.58% para biosal, 68.84% para deltametrina e 52.67% para lambda-cialotrina, respectivamente.

Animals , Pyrethrins , Insecticides , Heteroptera , Alanine Transaminase , Animal Feed , Nitriles
Article in Chinese | WPRIM | ID: wpr-935796


Objective: To establish a method for the determination of butyronitrile and isobutyronitrile in the air of workplace by gas chromatography. Methods: In March 2020, butyronitrile and isobutyronitrile in the air of workplace was collected by silica gel, eluted with methanol, separated and determined by gas chromatogram with flame ionization detector, the characteristics of determination of nitrile and isobutyronitrile by gas chromatography were analyzed. Results: The limit of detection for butyronitrile and isobutyronitrile was 0.33 μg/ml. The linear range of butyronitrile determined by this method was 1.60-1600.00 μg/ml, y=2.295x-3.480, and the coefficient correlation was 0.99998, and the minimum detection concentration was 0.22 mg/m(3) (collected sample volume was 1.50 L) . The within-run precisions were 2.43%-4.12%, the between-run precisions were 1.72%-3.70%, and the desorption rates were 93.26%-98.41%. The linear range of isobutyronitrile determined by this method was 1.52-1520.00 μg/ml, y=2.208x-0.102, and the coefficient correlation was 0.99998, and the minimum detection concentration was 0.22 mg/m(3) (collected sample volume was 1.50 L) . The within-run precisions were 2.52%-3.22%, the between-run precisions were 1.20%-3.82%, and the desorption rates were 96.85%-102.50%. The sealed samples could be stored at least 10 days at room temperature without significant loss. Conclusion: The method has the advantages of good precision, high sensitivity and simple operation. It is suitable for the simultaneous determination of butyronitrile and isobutyronitrile in the air of workplace.

Air Pollutants, Occupational/analysis , Chromatography, Gas/methods , Nitriles , Workplace
Chinese Journal of Hematology ; (12): 323-329, 2022.
Article in Chinese | WPRIM | ID: wpr-935089


Objective: To assess the effect of gene mutations on the efficacy of ruxolitinib for treating myelofibrosis (MF) . Methods: We retrospectively analyzed the clinical data of 56 patients with MF treated with ruxolitinib from July 2017 to December 2020 and applied second-generation sequencing (NGS) technology to detect 127 hematologic tumor-related gene mutations. Additionally, we analyzed the relationship between mutated genes and the efficacy of ruxolitinib. Results: ①Among the 56 patients, there were 36 cases of primary bone marrow fibrosis (PMF) , 9 cases of bone marrow fibrosis (ppv-mf) after polycythemia vera, and 11 cases of bone marrow fibrosis (PET-MF) after primary thrombocytosis (ET) . ②Fifty-six patients with MF taking ruxolitinib underwent NGS, among whom, 50 (89.29%) carried driver mutations, 22 (39.29%) carried ≥3 mutations, and 29 (51.79%) carried high-risk mutations (HMR) . ③ For patients with MF carrying ≥ 3 mutations, ruxolitinib still had a better effect of improving somatic symptoms and shrinking the spleen (P=0.001, P<0.001) , but TTF and PFS were significantly shorter in patients carrying ≥ 3 mutations (P=0.007, P=0.042) . ④For patients carrying ≥ 2 HMR mutations, ruxolitinib was less effective in shrinking the spleen than in those who did not carry HMR (t= 10.471, P=0.034) , and the TTF and PFS were significantly shorter in patients carrying ≥2 HMR mutations (P<0.001, P=0.001) . ⑤Ruxolitinib had poorer effects on spleen reduction, symptom improvement, and stabilization of myelofibrosis in patients carrying additional mutations in ASXL1, EZH2, and SRSF2. Moreover, patients carrying ASXL1 and EZH2 mutations had significantly shorter TTF [ASXL1: 360 (55-1270) d vs 440 (55-1268) d, z=-3.115, P=0.002; EZH2: 327 (55-975) d vs 404 (50-1270) d, z=-3.219, P=0.001], and significantly shorter PFS compared to non-carriers [ASXL1: 457 (50-1331) d vs 574 (55-1437) d, z=-3.219, P=0.001) ; 428 (55-1331) d vs 505 (55-1437) d, z=-2.576, P=0.008]. Conclusion: The type and number of mutations carried by patients with myelofibrosis and HMR impact the efficacy of ruxolitinib.

Humans , Mutation , Nitriles , Primary Myelofibrosis/genetics , Pyrazoles , Pyrimidines , Retrospective Studies , Technology , Transcription Factors/genetics
Article in Chinese | WPRIM | ID: wpr-928706


OBJECTIVE@#To analyze the kinetic characteristics of lymphocyte subsets and myeloid-derived suppressor cell (MDSC) in patients who newly diagnosed intermediate- to high-risk aGVHD and treated with steroids-ruxolitinib as the first line therapy from a single-arm, open clinical trial (NCT04061876).@*METHODS@#We prospectively observed the efficacy of 23 patients having intermediate- to high-risk aGVHD and treated with steroids-ruxolitinib as the first line therapy. The kinetic characteristics of lymphocyte subsets and MDSC were monitored, and then we compared them in steroids-ruxolitinib group (n=23), free-aGVHD group (n=20) and steroids group (n=23).@*RESULTS@#Of the 23 patients, the CR rate was 78.26% (18/23) on day 28 after first-line treatment with steroids-ruxolitinib. On day 28 after treatment, patients had lower level of CD4+CD29+ T cells (P=0.08) than that of pre-treatment, whereas levels of other lymphocyte subsets in this study were higher than that of pre-treatment; CD4+CD29+ T cells in CR patients decreased, compared with refractory aGVHD patients. On day 28 of treatment, CD8+CD28- T cells (P=0.03) significantly increased in patients with aGVHD than that in patients without aGVHD, so did CD8+CD28- T / CD8+CD28+ T cell ratio (P=0.03). Compared with patients without aGVHD, patients with aGVHD had lower level of G-MDSC, especially on day 14 after allo-HSCT (P=0.04). Compared with pre-treatment, M-MDSC was higher in CR patients on day 3 and 7 post-treatment (P3=0.01, P7=0.03), e-MDSC was higher on day 28 post-treatment (P=0.01). Moreover, compared with CR patients, M-MDSC was lower in refractory aGVHD patients on day 3 post-treatment (P=0.01) and e-MDSC was lower on day 28 post-treatment (P=0.01). Compared with steroids group, MDSC in steroids-ruxolitinib group was higher, with the most significant difference in M-MDSC (P3=0.0351; P7=0.0142; P14=0.0369).@*CONCLUSION@#We found that patients newly diagnosed intermediate- to high-risk aGVHD receiving first-line therapy with steroids-ruxolitinib achieved high response rate. Moreover, the novel first-line therapy has a small impact on the immune reconstitution of patients after allo-HSCT. Elevated MDSC might predict a better response in aGVHD patients receiving this novel first-line therapy. M-MDSC responded earlier to steroids-ruxolitinib than e-MDSC, G-MDSC.

Graft vs Host Disease , Hematopoietic Stem Cell Transplantation , Humans , Kinetics , Myeloid-Derived Suppressor Cells , Nitriles , Pyrazoles , Pyrimidines , Retrospective Studies , Steroids
Rev. Soc. Bras. Med. Trop ; 53: e20200680, 2020. tab, graf
Article in English | LILACS, ColecionaSUS, SES-SP | ID: biblio-1143869


Abstract INTRODUCTION: The use of insecticide-impregnated dog collars is a potentially useful tool for the control of visceral leishmaniasis. The objective of the present study was to perform a cost-effectiveness analysis of a program based on insecticide-impregnated collars compared to traditional visceral leishmaniasis control strategies used in Brazil. METHODS: A cost-effectiveness analysis was performed from the perspective of the Unified Health System, using data from the Visceral Leishmaniasis Control Program implemented in the municipality of Montes Claros, Minas Gerais. The direct costs of the three control strategies, which were 1) canine infection screening + sacrifice, 2) residual chemical control of the vector, and 3) insecticide-impregnated dog collars (Scalibor®), were evaluated over the two-year study period. RESULTS: The total cost of the program in the area subjected to the traditional control strategies (strategies 1 and 2; control area) was R$ 1,551,699.80, and in the area subjected to all three control strategies (intervention area), it was R$ 1,898,190.16. The collar program was considered highly cost-effective at preventing canine visceral leishmaniasis (incremental cost-effectiveness ratio of approximately R$ 578 per avoided dog sacrifice). CONCLUSIONS: These results provide support for the decision by the Brazilian Ministry of Health in 2019 to provide insecticide-impregnated collars for the control of canine visceral leishmaniasis in a pilot project.

Humans , Animals , Dogs , Pyrethrins , Dog Diseases/prevention & control , Insecticides , Leishmaniasis, Visceral/prevention & control , Leishmaniasis, Visceral/veterinary , Brazil , Pilot Projects , Cost-Benefit Analysis , Nitriles
Article in English | WPRIM | ID: wpr-777602


BACKGROUND@#Cervical vestibular evoked myogenic potential (cVEMP) testing is a strong tool that enables objective determination of balance functions in humans. However, it remains unknown whether cVEMP correctly expresses vestibular disorder in mice.@*OBJECTIVE@#In this study, correlations of cVEMP with scores for balance-related behavior tests including rotarod, beam, and air-righting reflex tests were determined in ICR mice with vestibular disorder induced by 3,3'-iminodipropiontrile (IDPN) as a mouse model of vestibular disorder.@*METHODS@#Male ICR mice at 4 weeks of age were orally administered IDPN in saline (28 mmol/kg body weight) once. Rotarod, beam crossing, and air-righting reflex tests were performed before and 3-4 days after oral exposure one time to IDPN to determine balance functions. The saccule and utricles were labeled with fluorescein phalloidin. cVEMP measurements were performed for mice in the control and IDPN groups. Finally, the correlations between the scores of behavior tests and the amplitude or latency of cVEMP were determined with Spearman's rank correlation coefficient. Two-tailed Student's t test and Welch's t test were used to determine a significant difference between the two groups. A difference with p < 0.05 was considered to indicate statistical significance.@*RESULTS@#After oral administration of IDPN at 28 mmol/kg, scores of the rotarod, beam, and air-righting reflex tests in the IDPN group were significantly lower than those in the control group. The numbers of hair cells in the saccule, utricle, and cupula were decreased in the IDPN group. cVEMP in the IDPN group was significantly decreased in amplitude and increased in latency compared to those in the control group. cVEMP amplitude had significant correlations with the numbers of hair cells as well as scores for all of the behavior tests in mice.@*CONCLUSIONS@#This study demonstrated impaired cVEMP and correlations of cVEMP with imbalance determined by behavior tests in a mouse model of vestibular disorder.

Animals , Behavior, Animal , Physiology , Disease Models, Animal , Hair Cells, Vestibular , Pathology , Male , Mice , Mice, Inbred ICR , Nitriles , Postural Balance , Physiology , Saccule and Utricle , Pathology , Sensation Disorders , Vestibular Diseases , Diagnosis , Pathology , Vestibular Evoked Myogenic Potentials , Physiology , Vestibular Function Tests
Int. j. morphol ; 36(1): 345-357, Mar. 2018. tab, graf
Article in English | LILACS | ID: biblio-893233


SUMMARY: An alternative superovulator to replace clomiphene citrate is needed as clomiphene citrate is associated with low pregnancy rates. Anastrozole is an effective superovulator, but it has not been well researched. In order to determine the effectiveness of anastrozole as a superovulator and to compare it with clomiphene citrate in similar situations, this study ascertained the effects of these drugs on the expression of the focal adhesion proteins, vinculin and integrin β5, which are uterine receptivity markers, in the uterine epithelial cells of day 1 and day 6 pregnant Wistar rats. The results show that vinculin and integrin β5 are co-localized at the base of the uterine epithelium at day 1 of pregnancy whereas at day 6, they disassemble from the basal focal adhesions and co-localize and significantly increase their expression apically (p≤0.0001). Moreover, there is a significant difference in the protein expression levels of vinculin and integrin b5 in uterine luminal epithelial cells between untreated (control) and chlomiphene citrate treated rats (p≤0.0001), anastrozole and chlomiphene citrate treated rats at day 6 (p≤0.0001) suggesting the interpretation that anastrozole seems to enhance their expression in order to perhaps assist in the implantation process of the blastocyst. The immunofluorescence experiments agree with the vinculin and integrin β5 gene expression findings in which at day 6 of pregnancy, vinculin and integrin β5 gene expression are significantly upregulated in uterine luminal epithelial cells in the anastrozole treated group relative to the calibrator sample (p≤0.0001). These findings suggest that anastrozole is implantation friendly.

RESUMEN: Es necesario un superovulador alternativo para reemplazar el citrato de clomifeno, debido a que está asociado con bajas tasas de preñez. El anastrozol es un superovulador eficaz, sin embargo es poca su investigación. Con el fin de determinar la efectividad del anastrozol como superovulador y compararlo con citrato de clomifeno en situaciones similares, se determinaron los efectos de estos fármacos sobre la expresión de las proteínas de adhesión focal, vinculina e integrina β5, en marcadores de receptividad uterina en días 1 y 6, en las células epiteliales uterinas de ratas Wistar preñadas. Los resultados muestran que la vinculina y la integrina β5 se co-localizan en la base del epitelio uterino al día 1 de la gravidez mientras que al día 6 se desmontan de las adherencias focales basales, co-localizan y aumentan significativamente su expresión apicalmente (p≤0.0001). Además, existe una diferencia significativa en los niveles de expresión de proteína de vinculina e integrina β5 en células epiteliales luminales uterinas entre ratas no tratadas (control) y tratadas con citrato declomifeno (p≤0.0001), ratas tratadas con anastrozol y citrato declomifeno al día 6 (p≤0,0001) sugiriendo la interpretación de que el anastrozol parece mejorar su expresión con el fin de ayudar en el proceso de implantación del blastocisto. Los experimentos de inmunofluorescencia coinciden con los resultados de la expresión de los genes vinculina e integrina β5 en los cuales al día 6 de la preñez, la vinculina y la integrina β5 están significativamente reguladas en células epiteliales luminales uterinas en el grupo tratado con anastrozol con respecto a la muestra del calibrador (p<0,0001). Estos hallazgos sugieren que el anastrozol es favorable para la implantación.

Animals , Female , Pregnancy , Rats , Integrins/drug effects , Nitriles/pharmacology , Triazoles/pharmacology , Uterus/drug effects , Vinculin/drug effects , Epithelial Cells/drug effects , Focal Adhesions/drug effects , Integrins/genetics , Integrins/physiology , Microscopy, Confocal , Microscopy, Fluorescence , Rats, Wistar , Real-Time Polymerase Chain Reaction , Vinculin/genetics , Vinculin/physiology
Mem. Inst. Oswaldo Cruz ; 113(5): e170377, 2018. tab, graf
Article in English | LILACS | ID: biblio-894922


BACKGROUND There is little information on the effect of using deltamethrin-impregnated dog collars for the control of canine visceral leishmaniasis. OBJECTIVES The objective of this study was to evaluate the effectiveness of the use of 4% deltamethrin-impregnated collars (Scalibor®) in controlling visceral leishmaniasis in Lutzomyia longipalpis by comparing populations in intervention and non-intervention areas. METHODS Phlebotomine flies were captured over 30 months in four neighbourhoods with intense visceral leishmaniasis transmission in Fortaleza and Montes Claros. We calculated the rates of domicile infestation, relative abundance of Lu. longipalpis, and Lu. longipalpis distribution in each site, capture location (intra- and peridomestic locations) and area (intervention and non-intervention areas). FINDINGS In the control area in Fortaleza, the relative abundance of Lu. longipalpis was 415 specimens at each capture site, whereas in the intervention area it was 159.25; in Montes Claros, the relative abundance was 5,660 specimens per capture site in the control area, whereas in the intervention area it was 2,499.4. The use of dog collars was associated with a reduction in captured insects of 15% (p = 0.004) and 60% (p < 0.001) in Montes Claros and Fortaleza, respectively. MAIN CONCLUSIONS We observed a lower vector abundance in the intervention areas, suggesting an effect of the insecticide-impregnated collars.

Animals , Dogs , Psychodidae , Leishmaniasis, Visceral , Insect Control/instrumentation , Insect Vectors/drug effects , Nitriles/administration & dosage
Biomédica (Bogotá) ; 37(supl.2): 50-58, jul.-set. 2017. tab, graf
Article in English | LILACS | ID: biblio-888524


ABSTRACT Introduction: The alkaloid girgensohnine has been used as a natural model in the synthesis of new alkaloid-like alpha-aminonitriles with insecticidal effect against disease vectors. Objective: To evaluate the biocide activity of girgensohnine analogues and essential oils of Cymbopogon flexuosus, Citrus sinensis and Eucalyptus citriodora in stage I and stage V Rhodnius prolixus nymphs. Materials and methods: We used a topical application model in tergites and sternites, as well as exposure to treated surfaces with different exploratory doses of each of the molecules and essential oils to determine the lethal doses (LD50 and LD95). Results: Analogue 3 showed the highest insecticidal activity with 83.3±16.7% of mortality when applied on tergites, 38.9±4.8% on sternites and 16.7±0% on treated surfaces in stage I nymphs at 72 hours (h) and 500 mg.L-1. In stage V nymphs, the compounds induced mortality only in sternums (11.1±9.6% for analogue 6 and 5.5±4.7% for analogues 3 and 7 at 72 h and 1500 mg.L-1). The lethal doses for molecule 3 on tergites in stage I nymphs were LD50 225.60 mg.L-1 and LD95 955.90 mg.L-1. The insecticidal effect of essential oils was observed only in stage I nymphs, with 11.1±4.8% for C. flexuosus when applied in sternites, while using exposure to surfaces treated it was 5.6±4.8% for C. sinensis applied on tergites and 8.3±0% on sternites at 72 h and 1000 mg.L-1. Conclusion: Synthetic girgensohnine analogues, and C. flexuosus and C. sinensis essential oils showed insecticidal activity in R. prolixus. Analogue 3 showed the greatest insecticidal activity among all molecules and oils evaluated under our laboratory conditions.

RESUMEN Introducción. El alcaloide natural girgensohnina se ha usado como modelo en la síntesis de nuevos análogos de alcaloidales alfa-aminonitrílicos con efecto insecticida en vectores de enfermedades. Objetivo. Evaluar la actividad biocida de análogos de girgensohnina y de aceites esenciales de las plantas Cymbopogon flexuosus, Citrus sinensis y Eucalyptus citriodora en ninfas de estadios I y V de Rhodnius prolixus. Materiales y métodos. Se empleó la aplicación tópica en terguitos, esternitos y superficies tratadas con diferentes dosis exploratorias de cada una de las moléculas y aceites esenciales para determinar las dosis letales (LD50 y LD95). Resultados. El análogo 3 tuvo la mayor actividad insecticida, con una mortalidad de 83,3±16,7% en los terguitos, de 38,9±4,8 % en los esternitos y de 16,7±0 % a las 72 horas en ninfas de estadioI expuestas a superficies tratadas y 500 mg.L-1. En las ninfas de estadio V solo se presentó mortalidad en los esternitos (11,1±9,6 % con el análogo 6 y 5,5±4,7 % con los análogos 3 y 7 a las 72 h y 1.500 mg.L-1). Las dosis letales para la molécula 3 en los terguitos de ninfas de estadio I fueron las siguientes: DL50, 225,60 mg.L-1 y DL95, 955,90 mg.L-1. En cuanto a los aceites esenciales, el efecto insecticida solo se presentó con C. flexuosus (11,1±4,8%) en los esternitos de ninfas de estadio I expuestas a superficies tratadas; con C. sinensis (5,6±4,8%) en los terguitos y en los esternitos (8,3±0%) a las 72 horas y 1.000 mg.L-1. Conclusión. Los análogos sintéticos del alcaloide girgensohnina y los aceites esenciales de C. flexuosus y C. sinensis exhibieron actividad insecticida en R. prolixus. El análogo 3 exhibió la mayor actividad insecticida de todas las moléculas evaluadas bajo las condiciones de laboratorio.

Animals , Pyrrolidines/pharmacology , Rhodnius , Oils, Volatile/pharmacology , Insecticides , Nitriles/pharmacology , Pyrrolidines/administration & dosage , Pyrrolidines/chemical synthesis , Rhodnius/growth & development , Plant Oils/pharmacology , Oils, Volatile/administration & dosage , Molecular Structure , Administration, Topical , Cymbopogon/chemistry , Citrus sinensis/chemistry , Eucalyptus/chemistry , Hydrophobic and Hydrophilic Interactions , Eucalyptus Oil/pharmacology , Insecticides/administration & dosage , Insecticides/chemical synthesis , Lethal Dose 50 , Nitriles/administration & dosage , Nitriles/chemical synthesis , Nymph
Biomédica (Bogotá) ; 37(supl.2): 180-186, jul.-set. 2017. tab, graf
Article in Spanish | LILACS | ID: biblio-888536


Resumen Introducción. El uso de mosquiteros tratados con insecticida en fórmulas de larga duración ha demostrado resultados prometedores en el control de Aedes aegypti. Objetivo. Evaluar la eficacia de mosquiteros impregnados con deltametrina en una fórmula de larga duración para el control de A. aegypti en Girardot, Colombia, después de tres lavados. Materiales y métodos. Se hicieron bioensayos de eficacia de los mosquiteros contra A. aegypti silvestres después de utilizar los siguientes tres productos de lavado, siguiendo la metodología de la Organización Mundial de la Salud: detergente en polvo, detergente en polvo y blanqueador, y jabón de barra, todos utilizados hasta en 20 lavados. Resultados. El tipo de producto de lavado y el número de lavados afectaron significativamente la eficacia de los mosquiteros impregnados con deltametrina. El lavado con jabón de barra presentó el mayor efecto, pues en tan solo seis lavados la mortalidad bajó a 50 % (25/50), en contraste con 66 % (33/50 de mortalidad después del lavado con detergente en polvo y de 84 % (42/50) después del lavado con detergente y blanqueador. En cuanto al número de lavados, el jabón en barra también causó una mayor reducción de la eficacia: a 68 % con solo tres lavados. Conclusión. La eficacia de los mosquiteros impregnados con deltametrina de larga duración en el control de A. aegypti varió con el tipo de producto de lavado y el número de lavados, siendo el jabón en barra el que redujo su eficacia en mayor medida. Se requieren nuevos estudios para establecer la disminución en la concentración del insecticida entre lavados.

Abstract Introduction: The use of long lasting insecticidal materials has shown promising results in the control of Aedes aegypti. Objective: To evaluate the efficacy of long-lasting insecticidal nets (PermaNet®) for Aedes aegypti control after three washing treatments in the city of Girardot, Colombia. Materials and methods: Standard bioassays were conducted with the nets following the World Health Organization protocols using wild A. aegypti after three washing treatments: (1) Detergent powder, (2)detergent powder and bleach, and (3) bar soap, until completing 20 washes. Results: The type and number of wash treatments had a significant effect on net efficacy. Greater effects in the insecticide bioavailability were seen for the bar soap treatment. After six washes, mortality decreased by 50% (25/50), vs 66% (33/50) for the detergent powder and 84% (42/50) for the detergent powder and bleach treatments. Regarding the number of washes, the bar soap treatment reduced the efficacy to 68% after only three washes. Conclusion: The effectiveness of long-lasting insecticidal nets (PermaNet 2.0) for A. aegypti control varied in relation to the treatment and number of washes. The bar soap treatment resulted in the greatest reduction of mortality. Further studies on insecticidal reductions are needed under local conditions.

Animals , Female , Pyrethrins , Mosquito Control/instrumentation , Aedes , Insecticide-Treated Bednets , Mosquito Vectors , Insecticides , Laundering , Nitriles , Powders , Pyrethrins/analysis , Pyrethrins/chemistry , Soaps/pharmacology , Solubility , Colombia , Detergents/pharmacology , Bleaching Agents/pharmacology , Insecticides/analysis , Insecticides/chemistry , Nitriles/analysis , Nitriles/chemistry
Arch. endocrinol. metab. (Online) ; 61(4): 391-397, July-Aug. 2017. tab, graf
Article in English | LILACS | ID: biblio-887576


ABSTRACT Aromatase is a cytochrome P450 enzyme (CYP19A1 isoform) able to catalyze the conversion of androgens to estrogens. The aromatase gene mutations highlighted the action of estrogen as one of the main regulators of bone maturation and closure of bone plate. The use of aromatase inhibitors (AI) in boys with short stature has showed its capability to improve the predicted final height. Anastrozole (ANZ) and letrozole (LTZ) are nonsteroidal inhibitors able to bind reversibly to the heme group of cytochrome P450. In this review, we describe the pharmacokinetic profile of both drugs, discussing possible drug interactions between ANZ and LTZ with other drugs. AIs are triazolic compounds that can induce or suppress cytochrome P450 enzymes, interfering with metabolism of other compounds. Hydroxilation, N-dealkylation and glucoronidation are involved in the metabolism of AIs. Drug interactions can occur with azole antifungals, such as ketoconazole, by inhibiting CYP3A4 and by reducing the clearance of AIs. Antiepileptic drugs (lamotrigine, phenobarbital, and phenytoin) also inhibit aromatase. Concomitant use of phenobarbital or valproate has a synergistic effect on aromatase inhibition. Therefore, it is important to understand the pharmacokinetics of AIs, recognizing and avoiding possible drug interactions and offering a safer prescription profile of this class of aromatase inhibitors. Arch Endocrinol Metab. 2017;61(3):391-7.

Humans , Male , Female , Triazoles/pharmacokinetics , Body Height/drug effects , Aromatase Inhibitors/pharmacokinetics , Nitriles/pharmacokinetics , Cytochrome P-450 Enzyme System/metabolism , Aromatase Inhibitors/therapeutic use , Drug Interactions , Letrozole , Anastrozole
Rev. Assoc. Med. Bras. (1992) ; 63(4): 371-378, Apr. 2017. graf
Article in English | LILACS | ID: biblio-842545


Summary Aromatase inhibitors have emerged as an alternative endocrine therapy for the treatment of hormone sensitive breast cancer in postmenopausal women. The use of third-generation inhibitors represented by exemestane, letrozol and anastrozole is currently indicated. Anastrozole is a nonsteroidal compound and a potent selective inhibitor of the aromatase enzyme. Although a few studies have shown that its pharmacodynamic and pharmacokinetic properties may be affected by interindividual variability, this drug has been recently used in all configurations of breast cancer treatment. In metastatic disease, it is currently considered the first-line treatment for postmenopausal women with estrogen receptor-positive breast tumors. Anastrozole has shown promising results in the adjuvant treatment of early-stage breast cancer in postmenopausal women. It has also achieved interesting results in the chemoprevention of the disease. Therefore, due to the importance of anastrozole both for endocrine treatment and chemoprevention of hormone-sensitive breast cancer in postmenopausal women, we proposed the current literature review in the SciELO and PubMed database of articles published in the last 10 years.

Resumo Os inibidores de aromatase têm emergido como uma endocrinoterapia alternativa para o tratamento de câncer de mama sensível a hormônios em mulheres pós-menopáusicas. A utilização de inibidores de terceira geração, representados por exemestano, letrozol e anastrozol, é atualmente indicada. Anastrozol é um composto não esteroide e um inibidor potente e seletivo da enzima aromatase. Embora alguns estudos tenham demonstrado que as suas propriedades farmacodinâmicas e farmacocinéticas podem ser afetadas pela variabilidade interindividual, esse fármaco tem sido recentemente utilizado em todas as configurações de tratamento do câncer de mama. Na doença metastática, é atualmente considerado o tratamento de primeira linha em mulheres pós-menopáusicas com tumores de mama e receptor de estrogênio positivo. O anastrozol tem mostrado resultados promissores no tratamento adjuvante do câncer de mama em estágio inicial em mulheres na pós-menopausa. Ele também conseguiu resultados interessantes na quimioprevenção da doença. Portanto, em virtude da importância do anastrozol tanto no tratamento endócrino quanto na quimioprevenção do câncer de mama hormoniossensível em mulheres na pós-menopausa, propusemos a atual revisão da literatura na base de dados SciELO e PubMed de artigos publicados nos últimos 10 anos.

Humans , Female , Triazoles/therapeutic use , Breast Neoplasms/prevention & control , Breast Neoplasms/drug therapy , Chemoprevention/methods , Aromatase Inhibitors/therapeutic use , Nitriles/therapeutic use , Tamoxifen/therapeutic use , Tamoxifen/pharmacokinetics , Triazoles/pharmacokinetics , Reproducibility of Results , Treatment Outcome , Chemotherapy, Adjuvant , Postmenopause , Antineoplastic Agents, Hormonal/therapeutic use , Antineoplastic Agents, Hormonal/pharmacokinetics , Aromatase Inhibitors/pharmacokinetics , Anastrozole , Nitriles/pharmacokinetics
Rev. bras. ginecol. obstet ; 39(1): 14-20, Jan. 2017. tab, graf
Article in English | LILACS | ID: biblio-843905


ABSTRACT Objective: Obesity is associated with an increased risk for breast cancer. Recent studies have shown that aromatase inhibitors may be less effective in women with a high body mass index (BMI). The aim of this study was to establish the relationship between the BMI and plasma estrone and estradiol levels in postmenopausal women with hormone receptor-positive breast cancer using anastrozole. Methods: In this cohort study, the patients were divided into three groups according to BMI (normal weight, overweight and obese) to compare and correlate plasma hormone levels before starting anastrozole hormone therapy and three months after treatment. Plasma hormone levels were compared for age and use of chemotherapy. Results: A statistically significant reduction in estrone and estradiol levels was observed between baseline and three months after starting the anastrozole treatment (p < 0.05). There was no statistically significant difference in plasma estrone and estradiol levels among the BMI groups (p > 0.05), but a significant reduction in plasma estrone levels was observed after three-months' treatment relative to baseline in all groups, as well as a reduction in estradiol in the obese group (p < 0.05). The use of chemotherapy and age > 65 years had no influence on plasma steroid levels. Conclusion: Changes in estrone and estradiol levels in the studied groups were not associated with BMI, chemotherapy or age.

RESUMO Objetivo: A obesidade está associada com risco aumentado de câncer de mama. Estudos recentes têm mostrado que os inibidores de aromatase podem ser menos eficazes em mulheres com alto índice de massa corporal (IMC). O objetivo deste estudo foi estabelecer a relação entre o IMC e os níveis plasmáticos de estrona e estradiol em mulheres no período pós-menopausa com câncer de mama receptor hormonal positivo, em tratamento com anastrozol. Métodos: Este estudo de coorte acompanhou três grupos de pacientes de acordo com o seu IMC (peso normal, sobrepeso e obesidade), a fim de comparar e correlacionar as dosagens dos hormônios estrona e estradiol antes e após três meses do uso do anastrozol. Os níveis plasmáticos dos hormônios foram também relacionados à idade do paciente e ao uso da quimioterapia. Resultados: Redução estatisticamente significativa de estrona e estradiol foi observada entre os níveis basais e três meses após o início do tratamento com anastrozol (p < 0,05). Não houve diferença estatisticamente significativa entre os níveis plasmáticos de estrona e estradiol em relação ao IMC (p > 0,05), mas houve redução significativa entre os níveis plasmáticos basais de estrona após o tratamento em todos os grupos, e redução de estradiol no grupo de pacientes obesas (p < 0,05). A condução da quimioterapia e da idade acima de 65 anos não interfere com os níveis plasmáticos de esteroides. Conclusão: Os níveis plasmáticos de estrona e estradiol nos grupos estudados não foram alterados em termos de IMC, quimioterapia e idade.

Humans , Female , Middle Aged , Antineoplastic Agents, Hormonal/therapeutic use , Aromatase Inhibitors/therapeutic use , Body Mass Index , Breast Neoplasms/blood , Breast Neoplasms/drug therapy , Estradiol/blood , Estrone/blood , Nitriles/therapeutic use , Triazoles/therapeutic use , Cohort Studies
Rev. Inst. Med. Trop. Säo Paulo ; 59: e18, 2017. tab, graf
Article in English | LILACS | ID: biblio-842766


ABSTRACT The aim of the present study was to examine the resistance of PermaNet® 2.0 bed nets against repeated washing and environmental factors by using bioassay tests. After 5, 15 and 21 washings with detergents and by using bioassay tests, the resistance of 40 PermaNet® 2.0 bed nets was compared with that of 40 bed nets conventionally treated with one K-O tablet. To examine the long-term resistance, 31 PermaNet® 2.0 bed nets were also distributed among villagers, and were re-collected to perform bioassay tests after 1, 2 and 5 years. In the first phase of this study, the insecticidal effect of the conventionally-treated nets significantly decreased due to repeated washings (P < 0.001); however, it was not significant regarding PermaNet® 2.0 bed nets (P = 0.92 in continuous exposure and P = 0.12 in mortality tests). In the long-term phase of this study, the time required for knockdown of PermaNet® 2.0 increased over the first 2 years and then decreased. In addition, the mortality rate decreased over the first 2 years and then increased. In conclusion, it seems that the technique used by the manufacturer for impregnation of PermaNet® 2.0 bed nets has an acceptable efficiency in comparison with conventional techniques.

Animals , Insecticide-Treated Bednets , Insecticides , Malaria/prevention & control , Mosquito Control/methods , Nitriles , Pyrethrins , Biological Assay , Evaluation Studies as Topic , Laundering , Time Factors
Journal of Integrative Medicine ; (12): 95-101, 2017.
Article in English | WPRIM | ID: wpr-346271


<p><b>BACKGROUND</b>Polycystic ovary syndrome (PCOS) is an endocrine disease that affects gynecological health. Treatment of PCOS remains a big challenge for clinicians.</p><p><b>OBJECTIVE</b>This meta-analysis was developed to compare the efficacy of co-treatment with traditional Chinese medicine (TCM) and letrozole against letrozole monotherapy in the treatment of PCOS.</p><p><b>SEARCH STRATEGY</b>Randomized controlled trials (RCTs) were electronically retrieved from PubMed, Cochrane Library, China Biomedical Literature Database, China National Knowledge Infrastructure and Wanfang Data; related papers that were not available electronically were manually checked. All papers were assessed according to the Cochrane Handbook for Systematic Reviews of Interventions and the valid data were analyzed using Revman software (The Cochrane Collaboration, Copenhagen, Denmark).</p><p><b>INCLUSION CRITERIA</b>We included RCTs that compared co-treatment with TCM and letrozole against letrozole monotherapy in women with PCOS, which was defined by anovulation, biochemical or clinical hyperandrogenemia and polycystic ovaries. We included trials from all sources.</p><p><b>DATA EXTRACTION AND ANALYSIS</b>Two independent reviewers extracted data, and evaluated study quality according to the Cochrane Handbook for Systematic Reviews of Interventions criteria for RCT, including issues of patient randomization, blinding and bias.</p><p><b>RESULTS</b>Eight RCTs, involving a total of 537 patients, were included in the present study. The meta-analysis showed that the cycle ovulation rate, the pregnancy rate and the total effective rate of symptom treatment were higher in treatments combining TCM with letrozole, compared with letrozole monotherapy. Although the rate of luteinizing hormone (LH)/follicle-stimulating hormone (FSH) and the body mass index of the group receiving combined therapy were lower than in letrozole monotherapy, no statistical difference was found in the LH and FSH level between the two groups.</p><p><b>CONCLUSION</b>Available evidence showed that co-treatment with TCM and letrozole was more effective than letrozole monotherapy in the treatment of PCOS.</p>

Female , Follicle Stimulating Hormone , Blood , Humans , Luteinizing Hormone , Blood , Medicine, Chinese Traditional , Nitriles , Therapeutic Uses , Polycystic Ovary Syndrome , Blood , Therapeutics , Publication Bias , Randomized Controlled Trials as Topic , Triazoles , Therapeutic Uses
National Journal of Andrology ; (12): 922-927, 2017.
Article in Chinese | WPRIM | ID: wpr-812855


Objective@#To investigate the clinical effects of integrated traditional Chinese and Western medicine in the treatment of castration-resistant prostate cancer (CRPC).@*METHODS@#A total of 54 CRPC patients were randomly divided into a control and a trial group, all treated by endocrine therapy (oral Bicalutamide at 50 mg per d plus subcutaneous injection of Goserelin at 3.6 mg once every 4 wk) and chemotherapy (intravenous injection of Docetaxel at 75 mg/m2 once every 3 wk plus oral Prednisone at 5 mg bid), while the latter group by Fuyang Huayu Prescription (a Traditional Chinese Medicine [TCM] prescription for tonifying yang and dispersing blood stasis) in addition, for a course of 24 weeks. Comparisons were made between the two groups of patients in the level of serum prostate-specific antigen (PSA), Karnofsky physical condition scores, function assessment of cancer therapy-prostate (FACT-P) scores, and TCM symptoms scores before and after 12 or 24 weeks of treatment.@*RESULTS@#Compared with the baseline, the serum PSA level was significantly decreased after 12 weeks of treatment both in the control ([25.9 ± 39.3] vs [20.0 ± 21.1] μg/L, P 0.05). At 24 weeks, however, the PSA levels in the control and trial groups were slightly increased to (23.1 ± 28.4) and (19.6 ± 23.5) μg/L, respectively, with no statistically significant differences in between (P >0.05). Karnofsky, FACT-P and TCM symptoms scores were all markedly improved in the trial group after 12 weeks of treatment (P 0.05).@*CONCLUSIONS@#TCM Fuyang Huayu Prescription combined with endocrine therapy and chemotherapy is effective for CRPC.

Anilides , Antineoplastic Agents, Hormonal , Therapeutic Uses , Antineoplastic Combined Chemotherapy Protocols , Therapeutic Uses , Docetaxel , Drug Administration Schedule , Goserelin , Humans , Male , Nitriles , Prednisone , Prostate-Specific Antigen , Blood , Prostatic Neoplasms, Castration-Resistant , Blood , Drug Therapy , Taxoids , Tosyl Compounds , Treatment Outcome
Rev. méd. Chile ; 144(10): 1356-1359, oct. 2016. ilus
Article in Spanish | LILACS | ID: biblio-845452


Maximum androgen blockade is the standard endocrine treatment for advanced prostate cancer. Interstitial lung disease in different degrees of severity, with low mortality and excellent response to treatment may appear with its use. We report a 77 years old patient with advanced prostate cancer who developed severe and progressive respiratory failure associated to bilateral pulmonary infiltrates, attributed to the direct effect of maximum androgen blockade. Despite the therapeutic efforts, the patient died. Lung pathology revealed Usual Interstitial Pneumonia.

Humans , Male , Aged , Lung Diseases, Interstitial/chemically induced , Androgen Antagonists/adverse effects , Antinematodal Agents/adverse effects , Prostatic Neoplasms/drug therapy , Tosyl Compounds/adverse effects , Biopsy , Adenocarcinoma/drug therapy , Tomography, X-Ray Computed , Lung Diseases, Interstitial/pathology , Fatal Outcome , Disease Progression , Anilides/adverse effects , Nitriles/adverse effects
Acta cir. bras ; 31(4): 286-293, Apr. 2016. tab, graf
Article in English | LILACS | ID: lil-781334


PURPOSE: To evaluate the effects of letrozole (Ltz) in carcinogen+estrogen-induced endometrial hyperplasia. METHODS: BALB/c female mice were divided into four groups of 12 animals each receiving an intrauterine dose of N-ethyl-N-nitrosourea (ENU) and weekly subcutaneous injections of estradiol hexaidrobenzoate (EHB), except for group I(control). The groups were divided in I (control), II (ENU+EHB), III (ENU+EHB+MPA) and IV (ENU+EHB+Ltz). Group III also received intramuscular injections of MPA (medroxy progesterone acetate) every four weeks, while group IV received oral doses of Ltz daily. At the end of 16 weeks, the animals were sacrificed, and blood samples were collected for the measurement of serum estradiol and progesterone levels. Uterine histological sections were made to evaluate the presence of endometrial proliferative lesions. Differences between groups were evaluated with student's t test, ANOVA and chi-square test. RESULTS: Groups ENU+EHB, ENU+EHB+MPA and ENU+EHB+Ltz showed varying degrees of endometrial hyperplasia. The incidence of hyperplasia in groups ENU+EHB and ENU+EHB+Ltz was higher and more severe than in group ENU+EHB+MPA. Control group showed lower levels of serum estradiol than the other groups. CONCLUSION: There was no evidence that letrozole could act as an antiestrogenic drug in the development of endometrial proliferative lesions.

Animals , Female , Triazoles/pharmacology , Aromatase Inhibitors/pharmacology , Endometrial Hyperplasia/drug therapy , Carcinogenesis/drug effects , Nitriles/pharmacology , Progesterone/blood , Time Factors , Triazoles/therapeutic use , Adenocarcinoma/etiology , Adenocarcinoma/drug therapy , Reproducibility of Results , Treatment Outcome , Endometrial Neoplasms/etiology , Endometrial Neoplasms/drug therapy , Medroxyprogesterone Acetate/pharmacology , Antineoplastic Agents, Hormonal/pharmacology , Aromatase Inhibitors/therapeutic use , Endometrial Hyperplasia/chemically induced , Endometrial Hyperplasia/pathology , Endometrium/drug effects , Endometrium/pathology , Estradiol/blood , Ethylnitrosourea , Carcinogenesis/pathology , Mice, Inbred BALB C , Nitriles/therapeutic use
Journal of the Egyptian Society of Parasitology. 2016; 46 (1): 131-134
in English | IMEMR | ID: emr-180168


The extensive use of insecticides in public health and agriculture sectors is the main reason for development of resistance in fleas associated in domestic rodents. The present work was planned to investigate the insecticidal efficacy of Lambda-cyhalothrin, Chlorpyrifos and Fenitrothion against rat flea [Xenopsylla cheopis] infesting rodent species in Giza Governorate, Egypt. The lethal concentration LC[50] and Lc[90] of population percent were obtained from the established regression log concentrate-response lines. Data indicated that the values of lethal concentration [LC[50]] were 0.293, 1.725 and 2.328% for Lambda-cyhalothrin, chlorpyrifos and Fenitrothion, respectively. The values of lethal concentration [Lc[90]] were 0.467, 2.839 and 5.197% for Lambda-cyhalothrin, chlorpyrifos and Fenitrothion, respectively

Animals , Flea Infestations , Insecticides , Rodent Diseases , Rats , Fenitrothion , Chlorpyrifos , Nitriles , Pyrethrins
Chinese Journal of Stomatology ; (12): 154-159, 2016.
Article in Chinese | WPRIM | ID: wpr-259425


<p><b>OBJECTIVE</b>To investigate the effect of extracellular signal-regulated kinase (ERK) signaling pathway on the endothelial differentiation of periodontal ligament stem cells (PDLSC).</p><p><b>METHODS</b>Human PDLSC was cultured in the medium with vascular endothelial growth factor (VEGF) and basic fibroblast growth factor (b-FGF) to induce endothelial differentiation. Endothelial inducing cells was incubated with U0126, a specific p-ERK1/2 inhibitor. PDLSC from one person were randomly divided into four groups: control group, endothelial induced group, endothelial induced+DMSO group and endothelial induced+U0126 group. The protein expression of the p-EKR1/2 was analyzed by Western blotting at 0, 1, 3, 6 and 12 hours during endonthelial induction. The mRNA expressions of CD31, VE-cadherin, and VEGF were detected by quantitative real-time reverse transcriptase polymerase chain reaction (qRT-PCR) after a 7-day induction. The proportion of CD31(+) to VE-cadherin(+) cells was identified by flow cytometry, and the ability of capillary-like tubes formation was detected by Matrigel assay after a 14-day induction. The measurement data were statistically analyzed.</p><p><b>RESULTS</b>Phosphorylated ERK1/2 protein level in PDLSC was increased to 1.24±0.12 and 1.03±0.24 at 1 h and 3 h respectively, during the endothelial induction (P<0.01). The mRNA expressions of CD31 and VEGF in induced+U0126 group were decreased to 0.09±0.18 and 0.49±0.17, which were both significantly different with those in induced group (P<0.05). The proportion of CD31(+) to VE-cadherin(+) cells of induced+U0126 group were decreased to 5.22±0.85 and 3.56±0.87, which were both significantly different with those in induced group (P<0.05). In Matrigel assay, the branching points, tube number and tube length were decreased to 7.0±2.7, 33.5±6.4, and (15 951.0±758.1) pixels, which were all significantly different with those in induced group (P<0.05).</p><p><b>CONCLUSIONS</b>The endothelial differentiation of PDLSC is positively regulated by ERK signaling pathway. Inhibition of ERK1/2 phosphorylation could suppress endothelial differentiation of PDLSC.</p>

Antigens, CD , Genetics , Metabolism , Butadienes , Pharmacology , Cadherins , Genetics , Metabolism , Cell Differentiation , Endothelial Cells , Cell Biology , Physiology , Enzyme Inhibitors , Pharmacology , Extracellular Signal-Regulated MAP Kinases , Physiology , Fibroblast Growth Factor 2 , Pharmacology , Humans , Mitogen-Activated Protein Kinase 3 , Metabolism , Nitriles , Pharmacology , Periodontal Ligament , Cell Biology , Metabolism , Phosphorylation , Platelet Endothelial Cell Adhesion Molecule-1 , Genetics , Metabolism , RNA, Messenger , Metabolism , Random Allocation , Signal Transduction , Stem Cells , Cell Biology , Physiology , Time Factors , Vascular Endothelial Growth Factor A , Genetics , Metabolism , Pharmacology