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1.
J Nanosci Nanotechnol ; 18(10): 7155-7162, 2018 10 01.
Artigo em Inglês | MEDLINE | ID: mdl-29954552

RESUMO

The Er2O3 nanowires (NWs) were synthesized on Si substrate by using glancing angle deposition technique inside E-beam evaporator. The field-emission gun scanning electron microscopy (FEG-SEM) images showed perpendicular and highly porous Er2O3 NWs with average diameter ∼50 nm and length ∼350 nm. The crystallinity of the Er2O3 NWs improved with annealing but degraded at higher temperature annealing at 900 °C. Transmission electron microscopy (TEM) images show the unsymmetrical NW growth and grain size enhancement with increasing annealing temperature. In addition, two-fold enhanced absorption was observed for as deposited as compared to the annealed samples. A low intense photoluminescence was obtained for the as deposited sample as compared to the annealed samples due to the presence of defects and dangling bonds. The as deposited Er2O3 NW also showed a hydrophobic surface property with a contact angle of as high as 107.4° due to the air trapped in between Er2O3 NWs and oxygen vacancies which turned to hydrophilic surface with contact angle 27° and 25° when annealed at higher temperature of 750 °C and 900 °C respectively.

2.
Lupus ; 24(7): 746-50, 2015 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-25416695

RESUMO

BACKGROUND: Eltrombopag activates the thrombopoietin (TPO) surface receptor on the megakaryocyte, which increases the production of platelets, and rapidly improves circulating platelet numbers in patients with immune thrombocytopenic purpura (ITP). This allows for rapid tapering and/or cessation of corticosteroid therapy. Less is known about the platelet response to this drug in ITP associated with systemic lupus erythematosus (SLE). METHODS: A retrospective review was performed of the clinical course of three consecutive patients, each with SLE-associated ITP who were initially treated with corticosteroids or other immunomodulatory therapy. These patients were treated with eltrombopag at the DMC Center for Bleeding Disorders and Thrombosis. Eltrombopag was administered according the package insert, with an initial dose of 50 mg daily, with weekly, then monthly monitoring of platelet counts and dose adjustments. Some immunomodulatory agents (e.g. hydroxychloroquine) were continued to control non hematologic SLE manifestations. RESULTS: All three patients maintained acceptable platelet counts (>50,000/mm(3) for >3 years) following tapering and cessation of corticosteroids. The drug was well-tolerated and there were no adverse events, and specifically no thrombotic events. CONCLUSION: Eltrombopag is effective as a rapidly acting corticosteroid sparing therapy for patients with ITP associated with SLE. This is important in reducing corticosteroid related side effects and morbidities in treating SLE patients with ITP. Larger studies are needed to ascertain safety and efficacy of eltrombopag in SLE patients with ITP, particularly those with coexisting antiphospholipid antibodies.


Assuntos
Benzoatos/administração & dosagem , Hidrazinas/administração & dosagem , Lúpus Eritematoso Sistêmico/tratamento farmacológico , Púrpura Trombocitopênica Idiopática/tratamento farmacológico , Pirazóis/administração & dosagem , Receptores de Trombopoetina/agonistas , Corticosteroides/uso terapêutico , Adulto , Feminino , Humanos , Lúpus Eritematoso Sistêmico/sangue , Pessoa de Meia-Idade , Púrpura Trombocitopênica Idiopática/sangue , Estudos Retrospectivos , Trombopoetina/metabolismo
3.
Am J Public Health ; 105(5): e74-9, 2015 May.
Artigo em Inglês | MEDLINE | ID: mdl-25790387

RESUMO

OBJECTIVES: We assessed the burden of systemic lupus erythematosus (SLE) among Arab and Chaldean Americans residing in southeast Michigan. METHODS: For those meeting SLE criteria from the Michigan Lupus Epidemiology and Surveillance Registry, we determined Arab or Chaldean ethnicity by links with demographic data from birth certificates and with a database of Arab and Chaldean names. We compared prevalence and incidence of SLE for Arab and Chaldean Americans with estimates for non-Arab and non-Chaldean American Whites and Blacks. RESULTS: We classified 54 individuals with SLE as Arab and Chaldean Americans. The age-adjusted incidence and prevalence estimates for Arab and Chaldean Americans were 7.6 and 62.6 per 100 000, respectively. Arab and Chaldean Americans had a 2.1-fold excess SLE incidence compared with non-Arab and non-Chaldean American Whites. Arab and Chaldean American women had both significantly higher incidence rates (5.0-fold increase) and prevalence estimates (7.4-fold increase) than did Arab and Chaldean American men. CONCLUSIONS: Recognizing that Arab and Chaldean Americans experience different disease burdens from Whites is a first step toward earlier diagnosis and designing targeted interventions. Better methods of assigning ethnicity would improve research in this population.


Assuntos
Lúpus Eritematoso Sistêmico/etnologia , Adulto , Árabes , Feminino , Humanos , Incidência , Masculino , Michigan/epidemiologia , Pessoa de Meia-Idade , Prevalência , Vigilância em Saúde Pública , Fatores Socioeconômicos
4.
J Nanosci Nanotechnol ; 14(7): 5390-4, 2014 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-24758037

RESUMO

The Si nanowire (NW) network was fabricated on the Si substrate with the help of glancing angle synthesized Ag NPs assisted etching technique. The horizontal Si NWs network was characterized by field emission gun-scanning electron microscopy which shows the formation of long Si NWs of diameter within the range of 110-180 nm. The TiO2 thin film (TF) was deposited on the Si NWs, which shows -2.5 times enlarged optical absorption than that of bare Si substrate. Ag-TiO2 contacts exhibit Schottky behaviour and higher photoconduction was observed for TiO2-Si NW detector than that of TiO2 TF under illumination. The dark currents of TiO2 TF and TiO2-Si NW devices were exerted to be 0.1 mA/cm2 and 0.2 mA/cm2 at +1 V, which increased to 0.2 mA/cm2 and 1.23 mA/cm2, respectively, under the illumination of 100 W filament bulb. A threefold enhanced photodetection for the Si NW device was observed compared to the TiO2 TF device. The nonlinear rise of photocurrent of 2 x 10(-2) mA/cm2, after 5 min light illumination was observed due to carrier diffusion effect.

5.
Womens Health Rep (New Rochelle) ; 4(1): 328-337, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37476603

RESUMO

Objective: A health disparity exists for African American (AA) women with systemic lupus erythematosus (SLE) who have increased prevalence of human papilloma virus (HPV) infection and cervical neoplasia. We used a self-sampling brush to obtain cervical cells to assess cytology, HPV infection, and vaginal cytokine production in AA women with SLE. Methods: Thirty AA women with SLE ages 18-50 years consented to participate. Clinical information was obtained by review of records and patient interviews, and surveys administered to assess cervical health history, knowledge of HPV, and satisfaction with the self-sampling brush. Vaginal samples were analyzed for cytology, HPV DNA and RNA, and vaginal cytokine RNA. Results: Our cohort (mean 36.9, ±9.4 years) had moderate/severe SLE and were on immunosuppressives. The majority had history of abnormal pap smears (63%) with prevalent risk factors for HPV infection: multiple sex partners (9.5 ± 7), not vaccinated for HPV (83.3%), smoking (26.7%), and not using condoms (73.3%). Most were aware of HPV causing cervical cancer (70%) but were unaware of other HPV-related diseases. Most preferred self-sampling over traditional pap smear (80%). Abnormal cytology was detected in 13.3%. HPV DNA was detected in 70%, with half showing multiple types, and all showing active infection (+RNA). HPV-infected samples demonstrated RNA expression of multiple cytokines with no specific/ consistent pattern. Conclusion: Our high-risk cohort lacked knowledge about HPV-related diseases and were not employing strategies to reduce their risk with vaccination and condoms. This study highlights the need for cervical health education, increased monitoring, and intervention in these high-risk women.

6.
HIV Med ; 13 Suppl 2: 87-157, 2012 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-22830373

RESUMO

The overall purpose of these guidelines is to provide guidance on best clinical practice in the treatment and management of human immunodeficiency virus (HIV)-positive pregnant women in the UK. The scope includes guidance on the use of antiretroviral therapy (ART) both to prevent HIV mother-to-child transmission (MTCT) and for the welfare of the mother herself, guidance on mode of delivery and recommendations in specific patient populations where other factors need to be taken into consideration,such as coinfection with other agents. The guidelines are aimed at clinical professionals directly involved with, and responsible for, the care of pregnant women with HIV infection.


Assuntos
Fármacos Anti-HIV/uso terapêutico , Infecções por HIV/tratamento farmacológico , Transmissão Vertical de Doenças Infecciosas/prevenção & controle , Adulto , Terapia Antirretroviral de Alta Atividade , Parto Obstétrico/métodos , Feminino , HIV-1 , Humanos , Gravidez , Sociedades Médicas , Reino Unido
7.
J Nanosci Nanotechnol ; 12(8): 6445-8, 2012 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-22962762

RESUMO

TiO2 nanowires (NWs) have been synthesized by glancing angle deposition technique using e-beam evaporator. The average length 490 nm and diameter 80 nm of NWs were examined by field emission-scanning electron microscopy. Transmission electron microscopy emphasized that the NWs were widely dispersed at the top. X-ray diffraction has been carried out on the TiO2 thin film (TF) and NW array. A small blue shift of 0.03 eV was observed in Photoluminescence (PL) main band emission for TiO2 NW as compared to TiO2 TF. The high temperature annealing at 980 degrees C partially removed the oxygen vacancy from the sample, which was investigated by PL and optical absorption measurements.

8.
Hum Vaccin Immunother ; 14(9): 2318-2322, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-29708835

RESUMO

OBJECTIVE: To determine if natural human papillomavirus (HPV) infection would induce an anamnestic response to quadrivalent (qHPV) vaccine in women with Systemic Lupus Erythematosus (SLE). METHODS: Thirty four women (19-50 years) with mild to moderate and minimally active or inactive SLE received standard qHPV vaccine. Neutralizing antibody titers to HPV 6, 11, 16 and18 were evaluated pre- and post- vaccine using HPV competitive Luminex Immunoassay. For each HPV type, logistic regressions were performed to explore the relationship between a positive titer at baseline with their final geometric mean titer and with the rise in titer. Fisher's Exact Test was used to assess the association of at least one positive HPV antibody test at baseline and history of abnormal pap. RESULTS: History of abnormal pap smear/cervical neoplasia occurred in 52.9%. Baseline anti HPV antibody titers: 21% = negative for all 4 HPV types, 79% = positive for ≥1 of the HPV types. Statistical analysis showed: those with a history of abnormal pap smear/cervical neoplasia were likely to have a positive anti-HPV antibody result pre-vaccine to ≥ 1 of the 4 types, p = 0.035 Fisher's Exact Test. In general, HPV exposed women showed higher post vaccine GMTs than HPV unexposed women with higher point estimates. However, when examining the rise in titers using logistic regression, there was no evidence of an anamnestic response. CONCLUSION: Prior HPV infection and cervical neoplasia in SLE are linked with no anamnestic response to HPV vaccine. This supports not checking HPV-antibodies pre-vaccine. Women with SLE should be vaccinated for HPV.


Assuntos
Vacina Quadrivalente Recombinante contra HPV tipos 6, 11, 16, 18/imunologia , Imunidade Humoral , Lúpus Eritematoso Sistêmico/complicações , Infecções por Papillomavirus/prevenção & controle , Neoplasias do Colo do Útero/prevenção & controle , Neoplasias Uterinas/prevenção & controle , Adolescente , Adulto , Anticorpos Neutralizantes/sangue , Anticorpos Antivirais/sangue , Feminino , Vacina Quadrivalente Recombinante contra HPV tipos 6, 11, 16, 18/administração & dosagem , Humanos , Imunoensaio , Memória Imunológica , Pessoa de Meia-Idade , Teste de Papanicolaou , Infecções por Papillomavirus/imunologia , Neoplasias do Colo do Útero/imunologia , Neoplasias Uterinas/imunologia , Adulto Jovem
9.
Vaccine ; 35(20): 2642-2646, 2017 05 09.
Artigo em Inglês | MEDLINE | ID: mdl-28404357

RESUMO

OBJECTIVE: This study evaluated the safety and immunogenicity of qHPV vaccine in SLE. METHODS: Subjects: 34 women ages 19-50years (yrs.) with mild to moderate SLE & minimally active or inactive SLE received qHPV vaccine at the standard dosing schedule. EXCLUSION CRITERIA: active SLE disease (SELENA-SLEDAI>2), history of severe SLE disease, deep venous thrombosis, on >400mg/day of hydroxychloroquine, on >15mg/day of prednisone, or active infections. Patients were monitored for adverse events (AE), SLE flare, generation of thrombogenic antibodies and thrombosis. Antibody (Ab) levels to HPV 6, 11, 16 & 18 were measured by HPV competitive Luminex Immunoassay and Geometric Mean Titers (GMTs) were calculated for each HPV type. Seroconversion was assessed for those seronegative at baseline. RESULTS: The women in the study: African-American (79%), mean age=38.1years, mean age at diagnosis of SLE=28.6years, 35.3% had a history of smoking, 91% had 4 or more sexual partners, 50% had a history of sexually transmitted diseases, and 27.3% used condoms on a regular basis. Vaccine site reactions (VSRs) occurred in 62%, all mild. Ninety-seven percent experienced at least 1 non vaccine adverse event (nvAE) with a total of 493 nvAEs in 33 patients, of which 90% were mild and none were related to vaccine or SLE. There were 9 serious AEs, none were related to vaccine or SLE, all resolved. No patient experienced an SLE flare, thrombosis, or generation of thrombogenic antibodies. Seroconversion rate was 100% with mean GMTs comparable to Gardasil® package insert data. CONCLUSION: In this SLE vaccine study, qHPV vaccine was generally safe, well tolerated, and highly immunogenic. This clinical trial is registered on Clinical Trials.gov under number, NCT01741012 and was conducted under the FDA IND BB14113.


Assuntos
Vacina Quadrivalente Recombinante contra HPV tipos 6, 11, 16, 18/efeitos adversos , Vacina Quadrivalente Recombinante contra HPV tipos 6, 11, 16, 18/imunologia , Lúpus Eritematoso Sistêmico/complicações , Infecções por Papillomavirus/prevenção & controle , Adolescente , Adulto , Anticorpos Antivirais/sangue , Efeitos Colaterais e Reações Adversas Relacionados a Medicamentos/epidemiologia , Efeitos Colaterais e Reações Adversas Relacionados a Medicamentos/patologia , Feminino , Vacina Quadrivalente Recombinante contra HPV tipos 6, 11, 16, 18/administração & dosagem , Humanos , Pessoa de Meia-Idade , Resultado do Tratamento , Adulto Jovem
10.
Int J STD AIDS ; 17(6): 375-7, 2006 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-16734957

RESUMO

Recent increases in demand on our service have posed challenges to the viability of our walk-in sexually transmitted infection services in Leicester. Areas identified as hot spots were patient waiting times, result provision and staff stress levels. To improve patient and staff satisfaction, new technologies to facilitate communication with patients were explored and then implemented in April 2003. A summary of the data analysed for the period April 2003-June 2004 is presented, including survey of the users and non-users of this facility.


Assuntos
Instituições de Assistência Ambulatorial , Telefone Celular , Doenças Urogenitais Femininas/prevenção & controle , Doenças Urogenitais Masculinas , Infecções Sexualmente Transmissíveis/diagnóstico , Adolescente , Adulto , Confidencialidade , Doenças Urogenitais Femininas/diagnóstico , Pesquisas sobre Atenção à Saúde , Humanos , Satisfação do Paciente , Relações Médico-Paciente , Infecções Sexualmente Transmissíveis/prevenção & controle , Reino Unido
11.
Nat Prod Res ; 20(3): 235-9, 2006 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-16401553

RESUMO

The crude extract, its different fractions and the major pure compound from the active fraction of the powdered fruits of Piper longum were studied for the antifertility effect in female rats. The crude extract and its hexane fraction exhibited 100 and 86% efficacy respectively (days 1-7 post-coitum (p.c.) schedule). On the other hand, 1-butanol soluble, 1-butanol insoluble and chloroform fractions were inactive.


Assuntos
Abortivos , Piper , Plantas Medicinais , Animais , Feminino , Ratos , Ratos Sprague-Dawley
12.
Am J Obstet Gynecol ; 193(4): 1444-55, 2005 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-16202739

RESUMO

OBJECTIVE: The purpose of this study was to evaluate pregnancy outcomes before and after diagnosis of lupus. STUDY DESIGN: Successive selection criterion applied to 148 lupus and 78,905 non-lupus pregnancies, generated 3 groups: lupus group, 84 pregnancies (not-yet-diagnosed group, 15 women; already-diagnosed group, 69 women), and control group, 51,000 pregnancies. Three-way analysis of variance and the chi-squared test were used for analyses. RESULTS: Stillbirth outcome was increased in the lupus group compared with the control group (odds ratio, 4.84 [95% CI, 1.72,11.08]); the not-yet-diagnosed group (odds ratio, 9.89 [95% CI, 1.09,42.63]), and the already-diagnosed group (odds ratio, 3.85 [95% CI, 1.02,10.31]). Considering >1 pregnancy per patient would have overestimated the stillbirth rate. Stillbirth risk was increased significantly in severe maternal disease that was marked by central nervous system involvement. The already-diagnosed group had more hypertensive complications (P = .001 and .0001). Both lupus groups showed a significantly greater proportion of preterm births (P = .03), growth restriction (P = .019), and infants in the very low birth weight category (P = .021) compared with the control group. CONCLUSION: Poor fetal outcomes are seen in pregnancies that are complicated by lupus, even before clinical appearance of disease, which supports a predisease state.


Assuntos
Lúpus Eritematoso Sistêmico/diagnóstico , Resultado da Gravidez , Adulto , Feminino , Humanos , Recém-Nascido , Recém-Nascido Prematuro , Gravidez , Natimorto , Fatores de Tempo
13.
J Nanosci Nanotechnol ; 15(5): 3951-5, 2015 May.
Artigo em Inglês | MEDLINE | ID: mdl-26505030

RESUMO

Glancing angle deposited TiO2 nanowires (NWs) were doped with nitrogen (N) using plasma-enhanced chemical vapour deposition technique, under the treatment of N2/Ar plasma. A red shift (- 0.51 eV) in the main band transition and oxygen defect related transition (-2.1 eV) was observed for the N doped TiO2 nanowires. The interstitial nitrogen introduces mid-gap levels N (2P) above the O (2P) in the TiO2 forbidden gap. The photoluminescence measurement revealed a small red shift of -7 nm of anatase band gap from N doped TiO2 nanowires due to radiative recombination of carriers from conduction band to the N (2P) trap state. The low frequency Raman peaks at 304 cm(-1) (acoustical phonons with LA mode), 618 cm(-1) (optical phonons with LO modes) and the high frequency peak at 832 cm(-1) was observed from Ti-O-N due to the partial replacement of oxygen molecules by nitrogen into TiO2, during the doping process.

14.
Transplantation ; 50(4): 597-8, 1990 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-2219282

RESUMO

Cyclosporine and rifampicin were used simultaneously in 6 renal transplant patients with tuberculosis. The total daily dose of cyclosporine had to be increased 3-5 fold, with the frequency of administration increased from twice to thrice daily. With this regimen, satisfactory cyclosporine levels were attained and there was no adverse affect on graft function.


Assuntos
Ciclosporinas/administração & dosagem , Transplante de Rim , Rifampina/administração & dosagem , Tuberculose Pulmonar/tratamento farmacológico , Adulto , Ciclosporinas/sangue , Ciclosporinas/uso terapêutico , Esquema de Medicação , Interações Medicamentosas , Feminino , Humanos , Masculino , Rifampina/uso terapêutico
15.
Eur J Endocrinol ; 141(4): 426-30, 1999 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-10526259

RESUMO

CDRI-85/287 is an anti-estrogen and interferes with decidualization in the rat uterus. In this study, uterine estrogen receptor (ER) and progesterone receptor (PR) levels were determined during the inhibition of decidualization. The effect of 85/287 on uterine ornithine decarboxylate (ODC) activity (a marker enzyme for decidualization) was also studied, using immature ovariectomized rats divided into four different groups: control, 2.5mg/kg 85/287 only; 1 microg estradiol only; and 85/287 + estradiol. Pseudopregnant rats were administered 85/287 (2.5mg/kg p.o.) on day 3 post-coitum. Deciduoma was induced in one of the uterine horns on day 4 and animals were autopsied 18h post-traumatization. Both ERs and PRs showed an increase in traumatized horns compared with non-traumatized. In the 85/287-treated uterus, there was a reduction in cytosolic ERs in both traumatized horns. However, nuclear ER and PR levels increased in both horns under the influence of 85/287. Similarly, in a tamoxifen (0.03mg/kg)-treated group a decline was noticed in cytosolic ER with a mild increase in nuclear PR. Total ER content, expressed per 100 microg DNA, showed a decline in 85/287- or tamoxifen-treated rats. However, no significant alterations were observed in total PR levels in non-traumatized horns. In an immature rat model, 85/287 caused a significant (>50%) reduction in estradiol-induced ODC activity. These findings suggest that the decidualization inhibitory activity of 85/287 may be attributed to inhibition of certain timed biochemical events and genomic/non-genomic actions of estrogens in the rat uterus.


Assuntos
Benzopiranos/farmacologia , Decídua/efeitos dos fármacos , Antagonistas de Estrogênios/farmacologia , Ornitina Descarboxilase/efeitos dos fármacos , Piperidinas/farmacologia , Receptores de Esteroides/efeitos dos fármacos , Útero/efeitos dos fármacos , Animais , Feminino , Ratos , Ratos Sprague-Dawley , Receptores de Estrogênio/efeitos dos fármacos , Receptores de Progesterona/efeitos dos fármacos , Útero/enzimologia
16.
Fertil Steril ; 27(5): 566-76, 1976 May.
Artigo em Inglês | MEDLINE | ID: mdl-1278458

RESUMO

The effect of flutamide (Sch 13521; 4'-nitro-3'-trifluoromethylisobutyranilide), a nonsteroidal antiandrogen, on male rat genital organs was studied. Administered at a dose of 25 mg/kg body weight daily for 30 days, flutamide caused a significant increase in the weight of the testis but had no effect on spermatogenesis and Leydig cell morphology. The secretory activity of the epididymis, as evidenced by the level of glycerylphosphoryl-choline and sialic acid, either remained unaffected or was stimulated. There was a significant decrease in seminal vesicle and ventral prostate weight and in the fructose content of the coagulating gland. The anti-androgen at the dose used did not affect the fertility of the rats. The significance of these findings is viewed in relation to the hypothesis of a differential threshold requirement of androgen for the epididymis and the accessory sex glands. The potentiality of antiandrogens as extragonadal antifertility agents in the male is discussed.


Assuntos
Anilidas/farmacologia , Epididimo/efeitos dos fármacos , Flutamida/farmacologia , Animais , Epididimo/fisiologia , Epididimo/ultraestrutura , Masculino , Tamanho do Órgão , Ratos , Testículo/anatomia & histologia
17.
Contraception ; 42(1): 121-38, 1990 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-2387152

RESUMO

The effect of Anandron, a nonsteroidal antiandrogen, on the reproductive system and fertility of adult male rats was studied. Administered at a daily oral dose of 5 mg and 10 mg (per rat) for 30 days, it caused a significant increase in the plasma testosterone levels. Spermatogenic arrest in about 20 to 50% of the tubules in 9 out of 16 rats and stimulation of Leydig cells was observed in rats treated with the higher dose. Although a reduction occurred in accessory sex organ (epididymis, seminal vesicles, SV; ventral prostate, VP; dorsal prostate, DP and coagulating gland, CG) weight, no parallel reduction was evident in the secretory indices of the epididymis (glycerylphosphorylcholine and sialic acid), VP (alkaline phosphatase) and CG (fructose). However, there was a reduction in the total content per organ of these constituents. Females mated with treated males showed postimplantation loss indicating an adverse effect of Anandron during spermiogenesis. The results suggest that the peripheral antiandrogenic potency of Anandron in intact animals is insufficient to completely neutralize the elevated levels of androgens. A microdose (1 microgram) of estradiol efficiently neutralized the central stimulatory effect of Anadron and potentiated its antiandrogenic action. The potential use of such a combination for 'Fertility Regulation' in male is discussed.


Assuntos
Antagonistas de Androgênios/farmacologia , Fertilidade/efeitos dos fármacos , Imidazóis/farmacologia , Imidazolidinas , Sistema Urogenital/efeitos dos fármacos , Fosfatase Alcalina/metabolismo , Animais , Peso Corporal/efeitos dos fármacos , Relação Dose-Resposta a Droga , Epididimo/efeitos dos fármacos , Estradiol/farmacologia , Flutamida/farmacologia , Frutose/metabolismo , Glicerilfosforilcolina/metabolismo , Células Intersticiais do Testículo/efeitos dos fármacos , Masculino , Ácido N-Acetilneuramínico , Tamanho do Órgão/efeitos dos fármacos , Fosfolipídeos/análise , Próstata/efeitos dos fármacos , Proteínas/análise , Ratos , Ratos Endogâmicos , Glândulas Seminais/efeitos dos fármacos , Ácidos Siálicos/metabolismo , Espermatogênese/efeitos dos fármacos , Testículo/citologia , Testículo/efeitos dos fármacos , Testosterona/sangue
18.
Contraception ; 42(6): 655-66, 1990 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-2083488

RESUMO

The first site of attachment of the trophoblast to the uterus in rodents is on the antimesometrial side and the inner cell mass is oriented mesometrially. The present study was performed with a view to study if comparable changes occur on both the mesometrial and antimesometrial side during early pregnancy in the rat using the scanning electron microscope. The results showed three types of ectoplasmic projections: namely, (i) a smooth surface and a narrow base; (ii) many folds and pits; and (iii) a ruffled surface and broad base, seen in clusters and located at intervals on the antimesometrial side only. The results suggest that these projections with ruffled surfaces may play a role in adhesion of the blastocyst and localisation of implantation sites in the rat.


Assuntos
Prenhez/fisiologia , Útero/citologia , Animais , Desenvolvimento Embrionário/fisiologia , Epitélio/ultraestrutura , Feminino , Humanos , Microscopia Eletrônica de Varredura , Gravidez , Ratos , Ratos Endogâmicos
19.
Contraception ; 49(6): 609-16, 1994 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-8070266

RESUMO

In an endeavour to develop potent anti-implantation agents, a new antiestrogen, CDRI 85/287 (2-(4-2-piperidinoethoxy)phenyl-3-phenyl(2H)benzo(b)pyran), virtually devoid of agonistic activity, was identified. The present study deals with anti-implantation and estrogen agonistic-antagonistic activities of four structural analogues of 85/287. Results show that none of the compounds induced vaginal cornification, even at doses as high as 2.5 mg/kg. Compounds having p-hydroxyphenyl group at position-3 or hydroxy group at position-7 showed better estrogen receptor affinity (6.6 and 25.3% E2) as well as antiestogenic activity. When 3-p-hydroxyphenyl was replaced by 3-p-methoxyphenyl, a marked reduction in the receptor affinity was observed. However, this compound was relatively more potent as an anti-implantation agent, possibly due to its conversion to hydroxylated metabolite in vivo. The provision of aminoethoxy side chain at para-position and a shift in the piperidinoethoxy side chain from position-4 to position-2 in these molecules resulted in a decrease in estrogenicity and increase in antagonistic property. Results are discussed with regard to molecular configuration, relative binding affinity of these compounds to their biological profile.


Assuntos
Benzopiranos/química , Benzopiranos/farmacologia , Implantação do Embrião/efeitos dos fármacos , Antagonistas de Estrogênios/farmacologia , Piperidinas/química , Animais , Benzopiranos/metabolismo , Estradiol/metabolismo , Feminino , Estrutura Molecular , Piperidinas/metabolismo , Piperidinas/farmacologia , Ratos , Ratos Sprague-Dawley , Receptores de Estrogênio/metabolismo , Relação Estrutura-Atividade , Vagina/efeitos dos fármacos , Vagina/fisiologia
20.
Contraception ; 44(4): 461-72, 1991 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-1824558

RESUMO

Compound CDRI-85/287: 2-[4-(2-N-piperidinoethoxy) phenyl]-3-phenyl (2H) benzo (b) pyran has been identified as a potent antiimplantation agent in rat. A single oral dose (2.5 mg/kg body weight) of the compound administered on days 1, 2 or 3 of pregnancy or multiple dosing (0.05 mg/kg daily) on days 5-7 postcoitum effectively prevented pregnancy. When administered on days 5-7 postcoitum, it failed to interrupt pregnancy even at 20 mg/kg dose. The compound is a potent antiestrogen, with very weak uterotrophic activity; it does not induce vaginal cornification in immature ovariectomised rat. Also, it is devoid of progestational, antiprogestational, androgenic, antiandrogenic and antigonadotrophic activities. The results suggest that the compound exerts its antiimplantation acivity in rat by virtue of its antiestrogenic activity [corrected].


Assuntos
Benzopiranos/farmacologia , Implantação do Embrião/efeitos dos fármacos , Antagonistas de Estrogênios/farmacologia , Piperidinas/farmacologia , Animais , Benzopiranos/normas , Anticoncepcionais Pós-Coito/farmacologia , Anticoncepcionais Pós-Coito/normas , Relação Dose-Resposta a Droga , Antagonistas de Estrogênios/normas , Feminino , Piperidinas/normas , Gravidez , Coelhos , Ratos , Ratos Endogâmicos
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