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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
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
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
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
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
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
Article in Chinese | WPRIM | ID: wpr-815062


OBJECTIVE@#To explore the effect of compound malt pills (CMP) on polycystic ovarian syndrome (PCOS) rat model induced by letrozole and the underlying mechanisms.
@*METHODS@#To establish a PCOS rat model, 48 female SD rats aged 6 weeks were randomly divided into 6 groups (n=8): A normal group, a model control group, a positive control group, a low-dose CMP group, a middle-dose CMP group, and a high-dose CMP group. Rats were treated for 21 days after the PCOS model was successfully established. Ovarian morphology changes were observed, and the expressions of ERα and ERβ was examined by immunohistochemistry, Western blot and RT-PCR, respectively.
@*RESULTS@#Compared with the normal group, the number of follicular cystic dilatation in the model control group was increased and the granulosa cells were decreased. After the treatment, the number of follicular cystic dilatation was reduced compared with the model control group, but the primordial follicles, corpus luteum and granulosa cells were increased. The expressions of ERα and ERβ in the model control group were significantly decreased (P<0.01), which were increased in the intervention groups (P<0.05 or P<0.01).
@*CONCLUSION@#CMP may play a role in the treatment of PCOS by regulating the expressions of ERα and ERβ.

Animals , Corpus Luteum , Disease Models, Animal , Drugs, Chinese Herbal , Pharmacology , Estrogen Receptor alpha , Metabolism , Estrogen Receptor beta , Metabolism , Female , Granulosa Cells , Letrozole , Nitriles , Ovarian Follicle , Polycystic Ovary Syndrome , Metabolism , Rats , Rats, Sprague-Dawley , Triazoles
Article in English | WPRIM | ID: wpr-633463


INTRODUCTION: GUARD (vildaGliptin clinical Use in reAl woRlD) was  a  multinational,  prospective,  observational  study that assessed the effectiveness,safety  and  tolerability of vildagliptin and vildagliptin+metformin in patients with type 2 diabetes mellitus (T2DM) under real-world conditions across four  geographical  regions  (Asia,  the  Middle  East,  Central  America and Africa). The current paper discusses the results of patients with T2DM enrolled in the Philippines.METHODS: Patients  with  T2DM  who  were  prescribed vildagliptin or vildagliptin+metformin combination therapy were enrolled and followed as per routine clinical practice for 24 ± six weeks. Primary endpoint was the change in HbA1c from  baseline  to  study  end  (week  24±6).  Key  secondary endpoints included proportion of patients reaching target HbA1c ?7.0%, incidence of hypoglycemic events, adverse events (AEs) and serious AEs (SAEs).RESULTS: A total of 1,117 patients were included in the final analysis, 280 on vildagliptin (of these, eight patients received additional oral antidiabetes medications) and 837 on vildagliptin+metformin. At baseline, the mean (±SD) age of the enrolled population was 54.1±11.5 years, BMI 26.3±4.7 kg/m2, HbA1c 8.0±1.2% and T2DM duration 2.3±4.0 years.At  study  end,  significant  mean  (±SE)  reductions  in  HbA1c of -1.2±0.1% (pCONCLUSION: Vildagliptin  and  vildagliptin+metformin significantly  reduced  HbA1c  with  good  weight  control and low incidence of hypoglycemia in patients with T2DM under real-world conditions in Philippines

Humans , Male , Female , Aged , Middle Aged , Adult , Metformin , Vildagliptin , Diabetes Mellitus, Type 2 , Adamantane , Pyrrolidines , Hypoglycemic Agents , Nitriles , Hypoglycemia , Body Weight , Asia , Africa , Central America
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
Rev. Soc. Bras. Med. Trop ; 48(4): 417-421, July-Aug. 2015. tab, ilus
Article in English | LILACS | ID: lil-755968



Despite chemical and physical vector control strategies, persistent infestations of Triatoma sordida have been reported in a large part of Minas Gerais, Brazil, and the cause for this is little investigated. We aimed to characterize the deltamethrin toxicological profile in peridomestic T. sordidapopulations from Triângulo Mineiro area of Minas Gerais.


Susceptibility to deltamethrin was assessed in seventeen peridomestic T. sordida populations. Serial dilutions of deltamethrin in acetone (0.2µL) were topically applied on the first instar nymphs (F1; five days old; fasting weight, 1.2 ± 0.2mg). Dose response results were analyzed using Probit software, and the lethal doses, slope and resistance ratios were determined. Qualitative tests were also performed.


The deltamethrin susceptibility profile of T. sordida populations revealed resistance ratios ranging from 0.84 to 2.8. The percentage mortality in response to a diagnostic dose was 100.0% in all populations.


From our results, the lack of resistance to insecticides but persistent T. sordida infestations in the Triângulo Mineiro area may be because of: 1) environmental degradation facilitating dispersion of T. sordida , allowing colonization in artificial ecotopes; 2) operational failures; and 3) complexity of the peridomicile in the study area.These variables are being investigated.


Animals , Insecticides , Nitriles , Pyrethrins , Triatoma , Biological Assay , Brazil , Chagas Disease/transmission
Rev. Soc. Bras. Med. Trop ; 48(2): 157-161, mar-apr/2015. tab
Article in English | LILACS | ID: lil-746229


INTRODUCTION: Despite years of efforts towards the elimination of Triatoma infestans in Brazil, residual foci still persist in some areas of the States of Bahia and Rio Grande do Sul. The persistence of these T. infestans populations in the country has two different origins of equal concern: operational failures or insecticide resistance. Thus, the objective of this study was to characterize the susceptibility profile of the residual Brazilian populations of T. infestans to deltamethrin. METHODS: The susceptibility reference lineage was derived from Cipein/Argentina. The populations studied were manually collected using a dislodging agent in peridomiciles in the States of Bahia (Novo Horizonte) and of Rio Grande do Sul (Santa Rosa and Doutor Maurício Cardoso). Serial dilutions of deltamethrin were prepared and applied at the dorsal abdomen of first instar nymphs. The control group received only pure acetone. Mortality was evaluated after 72h. Qualitative tests assessed the mortality of a diagnostic dose of 1xLD99 (2.76ng a.i./nymph) determined for the susceptibility reference lineage. RESULTS: The susceptibility profile characterization of the T. infestans populations revealed an RR50 ranging from 1.73 to 3.26. The mortality percentage in response to a diagnostic dose was 100%. The results obtained in the quantitative and qualitative assays corresponded for all populations. CONCLUSIONS: The results of this study indicate that the persistence of residual foci of T. infestans in Bahia and Rio Grande do Sul is not related to insecticide resistance but may be associated with operational failures. In Rio Grande do Sul, we must consider the possibility of continuous reinfestation by Argentinian individuals, which justifies active and efficient epidemiological surveillance. .

Animals , Insect Vectors , Insecticide Resistance , Nitriles , Pyrethrins , Triatoma , Biological Assay , Brazil , Chagas Disease/transmission
Indian J Exp Biol ; 2015 Mar; 53(3): 143-151
Article in English | IMSEAR | ID: sea-158399


In animals, long-term feeding with peanut (Arachis hypogaea) seed coats causes hypertrophy and hyperplasia of the thyroid gland. However, to date there have been no detailed studies. Here, we explored the thyroidal effects of dietary peanut seed coats (PSC) in rats. The PSC has high levels of pro-goitrogenic substances including phenolic and other cyanogenic constituents. The PSC was mixed with a standard diet and fed to rats for 30 and 60 days, respectively. Animals fed with the PSC-supplemented diet showed a significant increase in urinary excretion of thiocyanate and iodine, thyroid enlargement, and hypertrophy and/or hyperplasia of thyroid follicles. In addition, there was inhibition of thyroid peroxidase (TPO) activity, 5’-deiodinase-I (DIO1) activity, and (Na+-K+)-ATPase activity in the experimental groups of rats as compared to controls. Furthermore, the PSC fed animals exhibited decreased serum circulating total T4 and T3 levels, severe in the group treated for longer duration. These data indicate that PSC could be a novel disruptor of thyroid function, due to synergistic actions of phenolic as well as cyanogenic constituents.

Animal Feed/adverse effects , Animals , Antithyroid Agents/isolation & purification , Antithyroid Agents/toxicity , Arachis/chemistry , Drug Synergism , Glucosides/analysis , Glucosides/pharmacology , Glucosides/toxicity , Hyperplasia , Hypertrophy , Hyperthyroidism/blood , Hyperthyroidism/chemically induced , Iodide Peroxidase/antagonists & inhibitors , Iodine/urine , Male , Nitriles/analysis , Nitriles/pharmacology , Nitriles/toxicity , Ovule/chemistry , Polyphenols/analysis , Polyphenols/pharmacology , Polyphenols/toxicity , Rats , Rats, Wistar , Sodium-Potassium-Exchanging ATPase/antagonists & inhibitors , Thiocyanates/urine , Thyroid Gland/drug effects , Thyroid Gland/enzymology , Thyroid Gland/pathology , Thyroid Hormones/blood
Rev. bras. epidemiol ; 18(1): 234-247, Jan-Mar/2015. tab
Article in Portuguese | LILACS | ID: lil-736431


OBJETIVO: Estimar a prevalência de dor crônica e sua associação com a situação socioeconômica, demográfica e atividade física no lazer em idosos. MÉTODOS: Este estudo é parte do inquérito epidemiológico e transversal de base populacional e domiciliar EpiFloripa Idoso 2009-2010 realizado com 1.705 idosos (≥ 60 anos), residentes em Florianópolis, Santa Catarina. A partir da resposta afirmativa de dor crônica, foram investigadas as associações com as variáveis obtidas por meio de entrevista estruturada. Realizou-se a estatística descritiva, incluindo cálculos de proporções e intervalos de confiança 95% (IC95%). Na análise bruta e ajustada, empregou-se regressão de Poisson, estimando-se as razões de prevalência, com intervalos de confiança de 95% e valores p ≤ 0,05. RESULTADOS: Dentre os idosos investigados, 29,3% (IC95% 26,5 - 32,2) relataram dor crônica. Na análise ajustada, observou-se que as variáveis sexo feminino, menor escolaridade e pior situação econômica ficaram associadas significativamente com maior prevalência de dor crônica; ser fisicamente ativo no lazer ficou associado significativamente com menor prevalência do desfecho. CONCLUSÕES: Percebe-se que a dor crônica é um agravo que acomete considerável parcela de idosos, havendo desigualdades sociais na sua frequência e sendo beneficamente afetada pela atividade física no lazer. É necessário que políticas públicas de saúde subsidiem programas multidisciplinares de controle da dor incluindo a prática regular de atividade física, voltada especificamente à promoção da saúde do idoso, evitando assim que a dor crônica comprometa a qualidade de vida desta população. .

OBJECTIVE: To estimate the prevalence of chronic pain and its association with socioeconomic and demographic status, and leisure physical activity in the elderly population. METHODS: This study is part of an epidemiological cross-sectional population-based household survey called EpiFloripa Elderly 2009-2010, which was conducted with 1,705 elderly individuals (≥ 60 years) residents of Florianópolis, Santa Catarina. From the positive response to chronic pain, the associations with the variables were investigated through a structured interview. Descriptive statistics were conducted, including ratio calculation and 95% confidence intervals. In crude and adjusted analysis, Poisson regression was utilized, estimating prevalence ratios, with 95% confidence intervals and ≤ 0.05 p-values. RESULTS: Among the subjects, 29.3% (IC95% 26.5 - 32.2) reported chronic pain. Adjusted analysis showed that being female, having less years of schooling, and being in worse economic situation were significantly associated with a higher prevalence of chronic pain. Being physically active during leisure time was significantly associated with lower prevalence of the outcome. CONCLUSIONS: Therefore, it is clear that chronic pain affects a considerable amount of elderly individuals. Social inequalities are a harmful influence in these individuals' quality of life, inasmuch as those inequalities increase the frequency with which chronic pain afflicts them. At the same time, physical activity during leisure time decreases chronic pain frequency. It is fundamental that public health policies subsidize multidisciplinary pain management programs, which should include health targeted physical activity for the elderly, thus preventing the decrease in quality of life that chronic pain brings to this population. .

Animals , Humans , Early Growth Response Protein 1/genetics , Epithelial Cells/drug effects , Mitogen-Activated Protein Kinase 1/metabolism , /metabolism , Sulindac/analogs & derivatives , Apoptosis/drug effects , Blotting, Western , Butadienes/pharmacology , Cell Line , Cell Survival/drug effects , Dose-Response Relationship, Drug , Early Growth Response Protein 1/metabolism , Epithelial Cells/cytology , Epithelial Cells/metabolism , Imidazoles/pharmacology , Intestines/cytology , Intestines/drug effects , Intestines/metabolism , Luciferases/genetics , Luciferases/metabolism , Microscopy, Confocal , Mitogen-Activated Protein Kinase 1/antagonists & inhibitors , /antagonists & inhibitors , Nitriles/pharmacology , Pyridines/pharmacology , Reverse Transcriptase Polymerase Chain Reaction , RNA, Messenger/genetics , RNA, Messenger/metabolism , Signal Transduction/drug effects , Sulindac/pharmacology , Transfection , Up-Regulation/drug effects , ets-Domain Protein Elk-1/genetics , ets-Domain Protein Elk-1/metabolism