Individual and social factors associated with active commuting to school in 4-6 years old Spanish children.

To examine the prevalence of active commuting to school (ACS) in 4 to 6 year old children and individual and social factors associated with it. Cross-sectional study including 1,159 children from Cuenca and Ciudad Real (Castilla-La Mancha, Spain). ACS, population area, and socioeconomic status (SES) were self-reported by parents. Body mass index and cardiorespiratory fitness (CRF) were measured using standard procedures. Binary logistic regression models were used to assess the strength of association between the mode of commuting (ACS/no-ACS) and individual (weight status and CRF) and social (population area and SES) factors. Forty-six percent of the children ACS. The probability of ACS was greater in boys and girls from families of low/medium-low SES and in girls who lived in urban areas. ACS was not associated with weight status and CRF. Effective interventions need to be promoted, especially in children from families of high SES and those living in rural areas.

Receptors involved in dexketoprofen analgesia in murine visceral pain.

Various animal models, especially rodents, are used to study pain, due to the difficulty of studying it in humans. Many drugs that produce analgesia have been studied and there is evidence among which NSAIDs deserve to be highlighted. Dexketoprofen (DEX) provides a broad antinociceptive profile in different types of pain; therefore, this study was designed to evaluate the profile of antinociceptive potency in mice. Analgesic activity was evaluated using the acetic acid abdominal constriction test (writhing test), a chemical model of visceral pain. Dose-response curves for i.p. DEX administration (1, 3, 10, 30 and 100 mg/kg), using at least six mice in each of at least five doses, was obtained before and 30 min after pre-treatment with different pharmacological agents. Pretreatment of the mice with opioid receptor antagonists was not effective; however, the serotonin receptor antagonist and nitric oxide synthase inhibitor produce a significant increase in DEX-induced antinociception. The data from the present study shows that DEX produces antinociception in the chemical twisting test of mice, which is explained with difficulty by the simple inhibition of COX. This effect appears to be mediated by other mechanisms in which the contribution of the NO and 5-HT pathways has an important effect on DEXinduced antinociception.

Minimally Invasive Approach for Diagnosing TMJ Osteoarthritis.

This study's objectives were to test correlations among groups of biomarkers that are associated with condylar morphology and to apply artificial intelligence to test shape analysis features in a neural network (NN) to stage condylar morphology in temporomandibular joint osteoarthritis (TMJOA). Seventeen TMJOA patients (39.9 ± 11.7 y) experiencing signs and symptoms of the disease for less than 10 y and 17 age- and sex-matched control subjects (39.4 ± 15.2 y) completed a questionnaire, had a temporomandibular joint clinical exam, had blood and saliva samples drawn, and had high-resolution cone beam computed tomography scans taken. Serum and salivary levels of 17 inflammatory biomarkers were quantified using protein microarrays. A NN was trained with 259 other condyles to detect and classify the stage of TMJOA and then compared to repeated clinical experts' classifications. Levels of the salivary biomarkers MMP-3, VE-cadherin, 6Ckine, and PAI-1 were correlated to each other in TMJOA patients and were significantly correlated with condylar morphological variability on the posterior surface of the condyle. In serum, VE-cadherin and VEGF were correlated with one another and with significant morphological variability on the anterior surface of the condyle, while MMP-3 and CXCL16 presented statistically significant associations with variability on the anterior surface, lateral pole, and superior-posterior surface of the condyle. The range of mouth opening variables were the clinical markers with the most significant associations with morphological variability at the medial and lateral condylar poles. The repeated clinician consensus classification had 97.8% agreement on degree of degeneration within 1 group difference. Predictive analytics of the NN's staging of TMJOA compared to the repeated clinicians' consensus revealed 73.5% and 91.2% accuracy. This study demonstrated significant correlations among variations in protein expression levels, clinical symptoms, and condylar surface morphology. The results suggest that 3-dimensional variability in TMJOA condylar morphology can be comprehensively phenotyped by the NN.

Interleukin-1beta in synergism gabapentin with tramadol in murine model of diabetic neuropathy.

Neuropathic pain is a complication of cancer and diabetes mellitus and the most commonly used drugs in the treatment of the diabetic neuropathic pain have only limited efficacy. The aim of this study was to evaluate the role of the biomarker interleukin-1beta (IL-1ß) in the pharmacological interaction of gabapentin with tramadol in a model of diabetic neuropathic pain. CF-1 male mice, pretreated with 200 mg/kg i.p. of streptozocin (STZ), were used and at day 3 and 7 were evaluated by the hot plate test and the spinal cord level of IL-1ß was determined. Antinociceptive interaction of the coadministration i.p. of gabapentin with tramadol, in basic of the fixed the ratio 1:1 of their ED50 values alone, was ascertained by isobolographic analysis. Tramadol was 1.13 times more potent than gabapentin in saline control mice, 1.40 times in STZ mice at 3 days and 1.28 times in STZ at 7 days. The interaction between gabapentin and tramadol was synergic, with an interaction index of 0.30 and 0.22 for mice pretreated with STZ at 3 and 7 days. The combination of gabapentin with tramadol reversed the increased concentration of IL-1ß induced by STZ in diabetic neuropathic mice. These findings could help clarify the mechanism of diabetic neuropathy.

Antinociceptive interaction of gabapentin with minocycline in murine diabetic neuropathy.

OBJECTIVE: Diabetic neuropathy (DN) is the most common complication of diabetes and pain is one of the main symptoms of diabetic neuropathy, however, currently available drugs are often ineffective and complicated by adverse events. The purpose of this research was to evaluate the antinociceptive interaction between gabapentin and minocycline in a mice experimental model of DN by streptozocin (STZ). METHODS: The interaction of gabapentin with minocycline was evaluated by the writhing and hot plate tests at 3 and 7 days after STZ injection or vehicle in male CF1 mice. RESULTS: STZ (150 mg/kg, i.p.) produced a marked increase in plasma glucose levels on day 7 (397.46 ± 29.65 mg/dL) than on day 3 (341.12 ± 35.50 mg/dL) and also developed neuropathic pain measured by algesiometric assays. Gabapentin produced similar antinociceptive activity in both writhing and hot plate tests in mice pretreated with STZ. However, minocycline was more potent in the writhing than in the hot plate test in the same type of mice. The combination of gabapentin with minocycline produced synergistic interaction in both test. CONCLUSION: The combination of gabapentin with minocycline in a 1:1 proportion fulfills all the criteria of multimodal analgesia and this finding suggests that the combination provide a therapeutic alternative that could be used for human neuropathic pain management.

Utility of retrograde ureterocelogram in management of complex ureterocele.

INTRODUCTION: Symptomatic pediatric ureterocele has diverse manifestations, making evidence-based management impractical. Thus, detailed visualization of ureterocele anatomy prior to first surgical incision is invaluable. Retrograde ureterocelogram (RUC) is a simple, underutilized radiologic technique that can be performed during cystoscopy. This study sought to determine whether RUC changes surgical management by more accurately depicting the complex ureteral and ureterocele anatomy, compared with renal ultrasound (US) and voiding cystourethrography (VCUG). METHODS: Patients who underwent surgical management of ureterocele from 2003 to 2015 were identified; those who received concomitant fluoroscopic RUC were selected for the case series. Data collected included: demographics, pre-operative evaluation, surgical interventions, and outcomes. The RUC images were individually examined, and the anatomic impression compared with previous renal US and VCUG. Novel RUC findings not previously appreciated by the pre-operative evaluation were noted. The RUC was performed by cystoscopically inserting a needle into the ureterocele and injecting contrast retrograde. If indicated, simultaneous PIC (Positioning the Instillation of Contrast) cystography was performed. RESULTS: Of the 43 patients that underwent surgery for suspected ureterocele, 28 underwent cystoscopy + RUC (10 M: 18 F) at a median age of 4.6 months and median follow-up of 37.0 months. All patients had prior US, 25 had prior VCUG, and 20 had prior radionuclide studies. Ureteroceles were either duplex system (n = 21) or single system (n = 7); 17 were ectopic into the bladder neck or urethra; seven were intravesical; and four were pseudoureteroceles. Fourteen patients underwent concomitant transurethral incision of the ureterocele (TUIU); two were deferred for surgery; and 11 received concomitant definitive surgery (e.g., nephrectomy). The RUC illuminated novel aspects of the anatomy in 20 of the 28 patients. No adverse events occurred. Notably, in nine of the 28 children, significant observations from RUC prompted change to the pre-operative surgical plan. DISCUSSION: Retrograde ureterocelogram clearly revealed ureterocele ectopy, pseudoureterocele, ureterocele disproportion, and unsuspected duplex systems, making it a useful adjunct to standard US and VCUG studies. Retrograde ureterocelogram can also be used to fluoroscopically verify decompression of the ureterocele post incision, document severity of ureteral dilation, and teach residents about the great damage generated by ureterocele variations. Limitations of RUC included increasing radiation dose and overall cost. The study design was limited by its small size, retrospective approach, selection bias, and availability of RUC images. CONCLUSIONS: While not indicated in routine ureterocele management, intraoperative RUC further defined ureterocele anatomy in nearly all cases and yielded changes to the original surgical plan frequently enough to merit greater use in complex patients.

Results of distal hypospadias repair after pediatric urology fellowship training: A comparison of junior surgeons with their mentor.

BACKGROUND: Teaching and learning hypospadias repair is a major component of pediatric urology fellowship training. Educators must transfer skills to fellows, without increasing patient complications. Nevertheless, few studies report results of surgeons during their first years of independent practice. PURPOSE: To review outcomes of distal hypospadias repairs performed during the same 2-year period by consecutive, recently matriculated, surgeons in independent practice, and to compare them to results by their mentor (with >20 years of experience). MATERIALS: Exposure to hypospadias surgery during fellowship was determined from case logs of five consecutive fellows completing training from 2007-2011. TIP was the only technique used to repair distal hypospadias. No fellow operated independently or performed complete repairs under supervision. Instead, the first 3 months were spent assisting their mentor, observing surgical methodology and decision-making. Then, each performed selected portions under direct supervision, including: degloving, penile straightening, developing glans wings, incising and tubularizing the urethral plate, creating a barrier layer, sewing the glansplasty, and skin closure. Overall fellow participation in each case was <50%. In 2011-2012, urethroplasty complications (fistula, glans dehiscence, meatal stenosis, urethral stricture, diverticulum) were recorded for consecutive patients undergoing primary distal repair by these recent graduates in their independent practices. The fellow graduating in 2011 provided 1 year of data. All patients undergoing repair during the study period were included in the analysis, except those lost to follow-up after catheter removal. Composite urethroplasty complications were compared between junior surgeons, and between junior surgeons and their mentor, with Fisher's exact contingency test. RESULTS: Training logs indicated fellow participation ranged from 76-134 hypospadias repairs, including distal, proximal and reoperative surgeries. Post-graduation case volumes ranged from 25-68 by junior surgeons versus 136 by the mentor. With similar mean follow-up, urethroplasty complication rates were statistically the same between the former fellows, and between them versus the mentor, ranging from 5-13%. Nearly all were fistulas or glans dehiscence. Junior surgeons reported they performed TIP as learned during fellowship, with one exception who used 7-0 polydioxanone rather than polyglactin for urethroplasty. DISCUSSION: This is the first study directly comparing hypospadias surgical outcomes by recently graduated fellows in independent practice with those of their mentor. We found junior surgeons achieved similar results for distal TIP hypospadias repair. Although their participation during training largely comprised observation and surgical assistance, with discrete performance of key steps, skills sufficient to duplicate the mentor's results were transferred. These data suggest there should be no learning curve for distal hypospadias after training. This report raises several considerations for surgical educators. First, mentors should review their own results, to be certain that they are correctly performing and teaching procedures. Second, programs need to determine key steps for procedures they teach, and then emphasize their optimal performance. Finally, mentors should expect former fellows to report back their initial results of hypospadias repair to be certain lessons taught were learned. Otherwise, preventable complications resulting from technical errors will be multiplied in the children operated by their trainees as they enter independent practice.

Evaluation of TSH Levels in the Program of Congenital Hypothyroidism Newborn Screening in a Pilot Study of Preterm Newborns in Bogotá, Colombia

Abstract Introduction: Preterm infants (<37 weeks of gestation) have low levels of thyroid hormones due to multiple factors. Objective: To evaluate levels of thyroid-stimulation hormone (TSH) in the program congenital hypothyroidism (CH) newborn screening in a sample of preterm infants in the city of Bogotá, Colombia. Methods: The Secretaría de Salud Distrital screening protocol for CH (blood sample is collected from the umbilical cord in all the newborns) remeasured the serum TSH and heel TSH when preterm infants completed 37 weeks of gestation. Results: A total of 59 preterm neonates were rescreened, of which 2 neonates had elevated levels of TSH and 1 neonate had transient hypothyroxinemia. The Kolmogorov-Smirnov 2-sample/bilateral statistical test was used to compare the neonatal TSH levels of preterm and full-term newborns, which do not follow the same distribution. Conclusion: In our pilot study, 2 of the rescreened infants presented high levels of TSH and 1 had transient hyperthyrotropinemia, suggesting the need for rescreening of preterm infants. Additionally, a larger study should be performed to determine the screening cutoff values for preterm newborns.

[Hip fracture, antiplatelet drugs treatment and postoperative complications]. / Fractura de cadera, antiagregantes plaquetarios y complicaciones postoperatorias.

OBJECTIVES: To assess the incidence of postoperative complications, blood transfusions and survival at one month, in the old patients operated for hip fracture undergoing chronic treatment with antiplatelet drugs. MATERIAL AND METHODS: Two hundred twenty three patients operated for hip fracture were studied retrospectively, separated into 3 groups: patients who received acetylsalicylic acid (group I), patients who were given 100mg/day of acetylsalicylic acid or 300mg/day of triflusal (group II) and patients receiving>100mg/day of acetylsalicylic acid, or>300mg/day of triflusal or thienopyridines (group III). Surgery was delayed for 4 days in patients in group III. Demographic, biological, clinical and treatment characteristics, postoperative complications and survival at one month were recorded. RESULTS: Patients in group III were older and sustain worse general health status. Patients with a higher transfusion requirement were those of group II (73.8%) (P=0.192), who also showed a higher percentage of anaemia on admission. Severe cardiovascular complications were experienced by 5.4% of group III patients, 4.8% of group II patients and 2.1% of group I patients. Patients from group III presented a significant amount of respiratory complications (P=0.007). CONCLUSIONS: Our results suggest that delaying surgery for 4 days in patients treated with clopidogrel can be associated to an increase in postoperative respiratory complications and severe adverse cardiovascular events, without increasing the tranfusional index, hospital stay, mortality, and without complications related to neuraxial anaesthesia.

Incidence of hepatic artery variations in liver transplantation: does it really influence short- and long-term results?

BACKGROUND: Some variations of hepatic artery, which show 30% incidence, must be taken into account to avoid damage to the liver transplant during harvesting, we analyzed the incidence of variations and their influence on postoperative results. PATIENTS AND METHODS: We performed a retrospective study of 325 liver transplantation between 2001 and December 2011. RESULTS: Variations in the hepatic artery were detected in 91 transplantations (32%) including 29 donors (8.9%), 57 recipients (17.5%), and 5 both (1.5%). The main variation among donors was a right hepatic artery originating from the mesenteric artery (38.2%), and a left hepatic artery from the left gastric artery (35.3%). Recipients showed the same distribution: RHA-UMA (right hepatic artery from upper mesenteric artery) (38.7%) and LHA-LGA (left hepatic artery from left gastric artery) (12.9%). 48.5% of donor hepatic variations did not need bench reconstruction, but all RHA-UMA required it mainly due to the donor gastroduodenal artery (7; 58%) We did not observe significant difference in cold or warm ischemia time, surgical time, red blood cell requirement, postoperative mortality, or overall survival when there was or was not an arterial anomaly. But arterial complications were more frequent in cases where there were recipient anomalies or both versus without anomalies or with donor anomalies (20%, 7,8%, 0%, 5,6%; P = .06). Donor RHA-UMA was associated with worse overall survival (69, 2%; P = .07) and longer cold ischemia time and red blood requirement. Bench reconstruction held to longer cold ischemia time and blood cell requirements (P = .01) and shorter overall survival (82.4%). RHA-UMA was associated (P = .08) with worse actuarial survival and a needed for bench reconstruction (P = .01). CONCLUSION: One must be careful during liver harvest to detect hepatic artery variations to avoid damage. Hepatic artery anomalies do not influence liver transplant results except for the presence of an RHA from the UMA with a need for bench reconstruction.

Antinociception induced by atorvastatin in different pain models.

Atorvastatin is a statin that inhibits the 3-hydroxy-methyl-glutaryl coenzyme A (HMG-CoA) reductase. Several landmark clinical trials have demonstrated the beneficial effects of statin therapy for primary and secondary prevention of cardiovascular disease. It is assumed that the beneficial effects of statin therapy are entirely due to cholesterol reduction. Statins have an additional activity (pleiotropic effect) that has been associated to their anti-inflammatory effects. The aim of the present study was to assess the antinociceptive activity of atorvastatin in five animal pain models. The daily administration of 3-100mg/kg of atorvastatin by oral gavage induced a significant dose-dependent antinociception in the writhing, tail-flick, orofacial formalin and formalin hind paw tests. However, this antinociceptive activity of atorvastatin was detectable only at high concentrations in the hot plate assay. The data obtained in the present study demonstrates the effect of atorvastatin to reduce nociception and inflammation in different animal pain models.

Eight years experience with liver transplantation in Rio Hortega hospital.

OBJECTIVES: We sought to evaluate our transplant series in light of the parameters outlined in the quality criteria established by the Spanish Hepatic Transplant Society (Sociedad Española de Trasplante Hepático [SETH]). METHODS: We retrospectively analyzed 240 hepatic transplantations performed in 223 patients from November 2001 to December 2009. RESULTS: Among the series, 57% were in Child class C, 50% had cirrhosis without hepatocellular carcinoma, and 32% had this neoplasm. The most common cause for the illness was alcohol, followed by a virus, namely hepatitis C virus in 76% of cases. The average waiting list time was 45.14 days. The total graft ischemia averaged 460 minutes (range, 265-937). The 4.1% (n = 10), incidence of an urgent retransplantation was mainly due to primary graft failure or arterial thrombosis. During the perioperative period the mortality rate was 2.5% (n = 6) and the 1-month mortality rate was 6.6% (n = 16). The raw survival rates at 1, 3, and 5 years after the operation are 85%, 78%, and 72%, respectively. CONCLUSION: Our perioperative as well as the long-term results fall within the quality standards established by SETH.

Incidence, management, and results of vascular complications after liver transplantation.

INTRODUCTION: Vascular complications show an 8%-15% incidence after liver transplantation and represent an important cause of mortality. An aggressive policy is necessary for an early diagnosis and treatment. PATIENTS AND METHODS: From 2001 to 2009, we performed 240 liver transplantations in 232 patients. We employed Doppler ultrasonography on days 1 and 4 as well as before hospital discharge and always try a radiological approach. RESULTS: The incidence of vascular complications was 7.2% (n = 18) including arterial (n = 12, 4.8%) of early thrombosis (n = 4), late thrombosis (n = 4), and stenosis (n = 4) or portal (n = 3; 1.2%) of thrombosis (n = 2) or stenosis (n = 1); or caval complications (n = 3, 1.2%). Radiologic therapy was effective in 1 patient with arterial stenosis, in the 3 patients with portal complications, and in 2 patients with caval complications. All patients with early thrombosis and 2/4 with late thrombosis required retransplantation. Surgical treatment was effective in 1 patient with late thrombosis, 3 with stenosis, and 2 with caval complications. The overall mortality rate was 16.6%; 2 patients with arterial complications and 1 with a caval complications. CONCLUSION: Vascular complications, mainly artery complications, represent serious problem after liver transplantation, which often requires retransplantation. With an aggressive policy of diagnosis and treatment, we can decrease the mortality rate from these adverse events.

Interaction between dexibuprofen and dexketoprofen in the orofacial formalin test in mice.

Animal models are used to research the mechanisms of pain and to mimic human pain. The purpose of this study was to determine the degree of interaction between dexketoprofen and dexibuprofen, by isobolographic analysis using the formalin orofacial assay in mice. This assay presents two-phase time course: an early short-lasting, phase I, starting immediately after the formalin injection producing a tonic acute pain, leaving a 15 min quiescent period, followed by a prolonged, phase II, after the formalin and representing inflammatory pain. Administration of dexketoprofen or dexibuprofen produced a dose-dependent antinociception, with different potency, either during phases I or II. The co-administration of dexketoprofen and dexibuprofen produced synergism in phase I and II. In conclusion, both dexketoprofen and dexibuprofen are able to induce antinociception in the orofacial formalin assay. Their co-administration produced a synergism, which could be related to the different degree of COX inhibition and other mechanisms of analgesics.

Synergism between COX-3 inhibitors in two animal models of pain.

OBJECTIVE AND DESIGN: The antinociception induced by the intraperitoneal coadministration in mice of combinations of metamizol and paracetamol was evaluated in the tail flick test and orofacial formalin test. METHODS: The antinociception of each drugs alone and the interaction of the combinations was evaluated by isobolographic analysis in the tail-flick and in the formalin orofacial assay of mice. RESULTS: Mice pretreated with the drugs demonstrated that the antinociception of metamizol and paracetamol is dose-dependent. The potency range on the antinocifensive responses for metamizol or paracetamol was as follows: orofacial (Phase II) > orofacial (Phase I) > tail flick. In addition, the coadministration of metamizol with paracetamol induced a strong synergistic antinociception in the algesiometer assays. Both drugs showed effectiveness in inflammatory pain. CONCLUSION: These actions can be related to the differential selectivity of the drugs for inhibition of COX isoforms and also to the several additional antinociception mechanisms and pathways initiated by the analgesic drugs on pain transmission. Since the efficacy of the combination of metamizol with paracetamol has been demonstrated in the present study, this association could have a potential beneficial effect on the pharmacological treatment of clinical pain.

Effects of tramadol and dexketoprofen on analgesia and gastrointestinal transit in mice.

The purpose of the present study was to evaluate the nature of the antinociceptive interaction among dexketoprofen (DEX), a mixed inhibitor of the cyclo-oxygenases, and tramadol (TRAM), a weak opioid with monoaminergic activity that inhibits norepinephrine and serotonin re-uptake. We assessed antinociception in the acetic acid writhing test, the tail flick and the formalin (FT) tests, and gastrointestinal transit (GIT) after the administration of a charcoal meal. The analysis of the interaction was carried out using isobolograms and interaction indexes or the fixed-dose method GIT. The administration of DEX or TRAM individually induced dose-dependent antinociception in all the algesiometric tests. In the three tests, TRAM was between 5.2 (FT, phase I) and 35 times (FT, Phase II) more potent than DEX. When testing combinations at different potency ratios (1 : 1, 1 : 3, 3 : 1), we could demonstrate synergy in all algesiometric tests, only when drugs were combined in a 1 : 1 proportion. Interestingly, the proportion of the drugs in the combination could change the type of interaction from synergy to antagonism. On the inhibition of GIT, a dose-related inhibition was established for TRAM, but not for DEX. Using a fixed-dose protocol, we could demonstrate antagonism between DEX and TRAM on the inhibition of GIT. The results of the present study suggest that a combination of DEX and TRAM in a 1 : 1 proportion could be adequate to use in future clinical trials in humans.

Synergism between NSAIDs in the orofacial formalin test in mice.

Opioids and non-steroidal anti-inflammatory drugs (NSAIDs) are used to relieve acute and chronic pain. The purpose of this study was to determine the degree of interaction between dexketoprofen and NSAID examples of COXs inhibitors using the isobolographic analysis in the formalin orofacial test in mice. The drugs, i.p., induced a dose-dependent antinociception with different potencies in both test phases. Combinations of dexketoprofen with naproxen, nimesulide, ibuprofen or paracetamol on the basis of the fixed ratio (1:1) of their ED(50)'s values alone demonstrated synergism in both phases. This is important since the orofacial pain is a test not currently used in mice; the drugs are all analgesic for humans and phase II is representative of inflammatory pain. The synergism was: COX-3>COX-2>COX-1 inhibitors, this is particularly interesting since the inhibitor of COX-3, paracetamol, displayed a robust anti-inflammatory activity in an assay of acute and inflammatory pain that mimics inflammatory pain in humans. In conclusion, the synergism of the dexketoprofen/NSAID combinations may improve this type of therapeutic profile, since with low doses of the components, side effects are not likely to occur, and they may be used in long-term treatments.

Estradiol inhibits the estrone sulfatase activity in normal and cancerous human breast tissues.

It is well accepted that estradiol (E2) plays an important role in the genesis and evolution of breast cancer. Quantitative evaluation indicates that in human breast tumor, estrone sulfate (E1S) 'via sulfatase' is a much more likely precursor for E2 than is androstenedione 'via aromatase'. In previous studies, it was demonstrated that in isolated MCF-7 and T-47D breast cancer cell lines, estradiol can block estrone sulfatase activity. In the present study, the effect of E2 was explored using total normal and cancerous breast tissues. This study was carried out with post-menopausal patients with breast cancer. None of the patients had a history of endocrine, metabolic or hepatic diseases or had received treatment in the previous 2 months. Each patient received local anaesthetic (lidocaine 1%) and two regions of the mammary tissue were selected: (A) the tumoral tissue and (B) the distant zone (glandular tissue) which was considered as normal. Samples were placed in liquid nitrogen and stored at -80 degrees C until enzyme activity analysis. Breast cancer histotypes were ductal and post-menopausal stages were T2. Homogenates of tumoral or normal breast tissues (45-75 mg) were incubated in 20 mM Tris-HCl, pH 7.2 with physiological concentrations of [3H]-E1S (5 x 10(-9)M) alone or in the presence of E2 (5 x 10(-5) to 5 x 10(-7) M) during 30 min or 3 h. E1S, E1 and E2 were characterized by thin layer chromatography and quantified using the corresponding standard. The sulfatase activity is significantly more intense with the breast cancer tissue than normal tissue, since the concentration of E1 was 3.20 +/- 0.15 and 0.42 +/- 0.07 pmol/mg protein, respectively after 30 min incubation. The values were 27.8 +/- 1.8 and 3.5 +/- 0.21 pmol/mg protein, respectively after 3 h incubation. Estradiol at the concentration of 5 x 10(-7) M inhibits this conversion by 33% and 31% in cancerous and normal breast tissues, respectively and by 53% and 88% at the concentration of 5 x 10(-5) M after 30 min incubation. The values were 24% and 18% for 5 x 10(-7) M and 49% and 42% for 5 x 10(-5) M, respectively after 3h incubation. It was observed that [3H]-E1S is only converted to [3H]-E1 and not to [3H]-E2 in normal or cancerous breast tissues, which suggests a low or no 17beta-hydroxysteroid dehydrogenase (17beta-HSD) Type 1 reductive activity in these experimental conditions. In conclusion, estradiol is a strong anti-sulfatase agent in cancerous and normal breast tissues. This data can open attractive perspectives in clinical trials using this hormone.