Clinical characterization of patients with anal fistula during follow-up of anorectal abscess: a large population-based study.

PURPOSE: Approximately 15-50% of patients with an anorectal abscess will develop an anal fistula, but the true incidence of this entity is currently unknown. The aim of the study was to determine the incidence of anorectal abscess and development of a fistula in a specific population area and to identify potential risk factors associated with demographic, socioeconomic and pre-existing disease (e.g. diabetes and inflammatory bowel disease). METHODS: A longitudinal observational study was designed including a large cohort study in an area with 7,553,650 inhabitants in Spain 1st january 2014 to 31st december 2019. Adults who attended for the first time with an anorectal abscess and had a minimum of 1-year follow-up were included. The diagnosis was made using ICD-10 codes for anorectal abscess and anal fistula. RESULTS: During the study period, we included 27,821 patients with anorectal abscess. There was a predominance of men (70%) and an overall incidence of 596 per million population. The overall incidence of anal fistula developing from abscesses was 20%, with predominance in men, and a lower incidence in the lowest income level. The cumulative incidence of fistula was higher in men and in younger patients (p < 0.0001). On multivariate analysis, patients aged 60-69 years (hazard ratio 2.0) and those with inflammatory bowel disease (hazard ratio 1.8-2.0) had a strong association with fistula development (hazard ratio 2.0). CONCLUSIONS: One in five patients with an anorectal abscess will develop a fistula, with a higher likelihood in men. Fistula formation was strongly associated with inflammatory bowel disease.

Children's visits to the paediatric intensive care unit from the nurses' experience.

BACKGROUND: Family process disruption is one of the main consequences of the hospitalization of a critically ill child in a Paediatric Intensive Care Unit (PICU). Children's visits to PICU may help improve family coping. However, this is not standard practice and nurses' experiences in facilitating children's visits to units where it is encouraged is unknown. AIM: To explore nurses' experience related to promoting the visits of siblings to PICU. METHODS: An interpretative phenomenological study was carried out through in-depth interviews in two PICUs belonging to third level public hospitals in Madrid. Twelve nurses with more than two years of experience in PICU were interviewed. They were all were working in PICU during the study. Furthermore, a PICU psychologist with an experience of four years was interviewed and this was considered shadowed data. Data analysis followed a thematic discourse analysis. RESULTS: Nurses' experience of facilitating children's visits to PICU can be condensed into four themes: emerging demand for visits, progressive preparation, decision-making through common consensus and creating intimate spaces. CONCLUSIONS: The experience of nurses in facilitating visits is mainly in response to the demand of families going through prolonged hospitalisation or end-of-life situations. The role of the nurse is one of accompaniment, recognising the major role of parents in the preparation of children and in developing the visit. Nurses feel insecure and lack resources for emotional support and demand action protocols to guide intervention and decision making.

DHA Selectively Protects SAMP-8-Associated Cognitive Deficits Through Inhibition of JNK.

A potential role of marine n-3 polyunsaturated fatty acids (ω-3 PUFAs) has been suggested in memory, learning, and cognitive processes. Therefore, ω-3 PUFAs might be a promising treatment option, albeit controversial, for Alzheimer's disease (AD). Among the different mechanisms that have been proposed as responsible for the beneficial effects of ω-3 PUFAs, inhibition of JNK stands as a particularly interesting candidate. In the present work, it has been studied whether the administration of two different PUFAs (docosahexaenoic acid (DHA) and eicosapentaenoic acid (EPA)) and a DHA-derived specialized pro-resolving lipid mediator (MaR1) is able to reverse cognitive deficits in the senescence-accelerated mouse prone 8 (SAMP8) mouse model of sporadic AD. The novel object recognition test (NORT) test showed that recognition memory was significantly impaired in SAMP8 mice, as shown by a significantly decreased discrimination index that was reversed by MaR1 and DHA. In the retention phase of the Morris water maze (MWM) task, SAMP8 mice showed memory deficit that only DHA treatment was able to reverse. pJNK levels were significantly increased in the hippocampus of SAMP8 mice compared to SAMR1 mice, and only DHA treatment was able to significantly reverse these increased pJNK levels. Similar results were found when measuring c-Jun, the main JNK substrate. Consequently to the increases in tau phosphorylation after increased pJNK, it was checked that tau phosphorylation (PHF-1) was increased in SAMP mice, and this effect was reversed after DHA treatment. Altogether, DHA could represent a new approach for the treatment of AD through JNK inhibition.

Designed intramolecular blocking of the spin crossover of an Fe(ii) complex.

A ligand derived from 1,3bpp (2-(pyrazol-1-yl)-6-(pyrazol-3-yl)-pyridine) has been prepared to prove that the spin crossover (SCO) of an Fe(ii) complex can be blocked by means of intramolecular interactions not related to the crystal field. Calculations show that the blocking is caused by the energy penalty incurred by the rotation of a phenyl ring, needed to avoid steric hindrance upon SCO.

Towards the tailored design of benzotriazinyl-based organic radicals displaying a spin transition.

The mechanism of the phase transition of 1-phenyl-3-trifluoromethyl-1,4-dihydrobenzo[e][1,2,4]triazin-4-yl (1), the first reported triazinyl radical to present such a feature, is unveiled. In so doing, we identify the key ingredients that are crucial to enable the phase transition in this family of radicals, and how those can be exploited by a rational design of the spin-carrying units.

[Nursing perception of communication with intensive care unit patients family members]. / Percepción de las enfermeras sobre la comunicación con la familia de pacientes ingresados en un servicio de medicina intensiva

INTRODUCTION: Communication is referred as one of the most important needs by the families of intensive care unit patients. AIM OF THE STUDY: To analyze nursing perception of the communication process with the family members of an intensive care unit patient. MATERIALS AND METHODS: Transversal study (December 2012) with a questionnaire Nurse Activities for Communicating with Families (NACF), cross-culturally adapted by Santana Cabrera et al. Participants: intensive care unit nurses from a third level university hospital. Descriptive analysis of variables and inferential statistics with Chi-square and Kruskal-Wallis, statistic program SPSS 17.0; significant P < .05. RESULTS: Complementation was of 80% (132 out of 166 nurses). The average experience was of 9.6 ± 7.95 years. 55.9% sometimes explain to families the treatment and equipment of the patient and a 37% almost always. Nurses talk to the families about the disease and the treatment given to the patient always/almost always in 59% of the cases and sometimes in a 35.38%. 54,6% talk to the family about their feelings sometimes and a 28.46% almost always. A 47.8% notify always/almost always changes on the care plan. 87.9% ensure patient comfort always/almost always. There is no relation between years of experience in ICU and the outcomes of the questionnaire. There is a relation between the different kinds of ICUs and the information given about disease and treatment. DISCUSSION: Nurses tend to inform more about technical aspects than feelings related to the families. Patient comfort is the most referred item regardless of years of experience and the kind of intensive care unit.

[Audit of the bedside monitor alarms in a critical care unit]. / Auditoría de las alarmas del monitor de cabecera en una unidad de cuidados críticos.

AIMS: Quantifying and evaluating the response to the bedside monitor alarms (BMA) by nurses in intensive care unit (ICU). METODOLOGY: Prospective observational study (October 2011-January 2012). Randomized blind audit on alarm management. Alarm programming and alarm limits were related to experience in ICU. We evaluated the response to BMA with the variables: alarm type (relevant/not relevant/alert) and response type. Descriptive analysis of variables for multivariate ANOVA and Chi-square test with SPSS 17.0. RESULTS: 434 audits were analyzed. The programming was: Blood pressure (BP) 88.25%, heart rate (HR) 98.62% O(2) saturation (SO) 96.79%, respiratory rate (FR) 65.75%. The alarms originated were BP 49.73%, 10.75% HR, 39.25% SO, 3.27% FS. The nurse responded to 93.3% of them and 50% were treated before 10 sec. 56.16% of the alarms were not relevant, 25.12% relevant and 18.72% alerting. 41.8% were due to handling. CONCLUSION: The alarms are programmed/attended by the nurse and there is uniformity in programming/selection limits. 25% of BMA carried therapeutic attitude.

[Pain assessment of tracheal suctioning on brain injury patients by pain behavioral indicator scale (ESCID)]. / Valoración del dolor en la aspiración de secreciones traqueales en pacientes con traumatismo craneal mediante la Escala de conductas indicadoras de dolor (ESCID).

OBJECTIVE: To assess pain response on patients with moderate to severe head injury before a common nursing procedure: tracheal suctioning. MATERIAL AND METHOD: An observational longitudinal pilot study with consecutive sampling performed from September to December of 2012. Pain was assessed by a pain behavioral indicator scale 5 minutes before, meanwhile and 15 minutes after tracheal suctioning the days 1, 3 and 6 of their intensive care unit (ICU) stay, as well as a non-painful procedure: rubbing with gauze the forearm of the patient. Pseudo-analgesia and hemodynamic variables were also recorded. Descriptive analysis of the variables, inferential statistics with t-student and Anova with SPSS 17.0; statistical tests were considered significant if the critical level observed was less than 5% (P<.05). RESULTS: Pain was assessed on 27 patients. 82% suffered from severe head trauma and 18% moderate. The average pain value during nursing procedure day 1 was 3, 18±2.6, day 3: 2, 59±2 and day 6: 3, 94±2.3. There was a significant increase in mean pain while performing suctioning during the three days of assessment (P<.05); however no significant differences between the average pain value on the three days of the assessment (P>.05) were shown. Data for the painless procedure were significantly different on day 6 (P<.05) CONCLUSION: During tracheal suctioning in patients with head injury in the first 6 days in the ICU, objective mild-moderate pain according to ESCID scale has been detected.

[Analysis of constipation in severe trauma patients]. / Análisis del estreñimiento en pacientes con traumatismo grave.

OBJECTIVES: To evaluate the incidence and risk factors of constipation in patients with severe trauma (ST). MATERIALS AND METHOD: A retrospective observational study (January-December 2011) of medical records in ST-patients with a minimum stay of 5 days was performed. Descriptive analysis of variables, inferential analysis: Student's T test and Chi-square of SPSS 17.0. Significance level P<.05. RESULTS: A total of 80 patients fulfilled the inclusion criteria, but only 69 could be analyzed. Of these, 84.06% showed constipation (according to its definition by the Work Group for Metabolism and Nutrition SEMICYUC). The most frequent day of first stool was day 7 and 9 after tolerance of enteral nutrition. Statistical significance (S.S.) of constipation was found with stay, days of sedation/relaxation/opiates, and mechanical ventilation. There was no S.S. between early enteral nutrition (EEN) and constipation (P>.05). CONCLUSIONS: There is a very high incidence of constipation in ST patients. ICU stay, days of analgesic sedation, relaxation, and mechanical ventilation are risk factors that influence the occurrence of this problem. Laxatives should be prescribed prophylactically.

[Pain behaviour indicator scale (ESCID) application in severe non-communicative trauma patients receiving mechanical ventilation]. / Aplicación de la Escala de conductas indicadoras de dolor (ESCID) en el paciente con trauma grave no comunicativo y ventilación mecánica.

OBJECTIVE: To assess pain in non-communicative patients with severe trauma undergoing mechanical ventilation prior to, during and after tracheal suctioning, mobilization and wound care. MATERIAL AND METHOD: A prospective and observational study from October to December 2011 was performed. Study variables were ESCID scale and monitoring of vital signs (blood pressure, heart rate, and respiratory rate). Data were gathering 5 minutes before, during and 15 minutes after the 3 procedures. The nursing evolutive report recorded pain assessment, administration and effectiveness of the analgesia. Descriptive analysis of variables included Student's T test/ANOVA for multivariate analysis with SPSS 17.0. RESULTS: A hundred eighty four observations: 46.8% tracheal suctioning, 38.5% mobilization and 14.7% wound care were performed in 29 patients. ESCID score was 0.4±1 before, 3.4±2.7 during and 0.4±1 after for wound care; 0.4±1.1 before, 3.6±2.2 during and 1.1±0.5 for tracheal suctioning; 0.5±1.1 before, 3±2.8 during and 0.2±0.8 after for mobilization. These increased significantly during the performance of the 3 procedures before-during/during-after: P=.000. All the hemodynamic variables were significantly modified during mobilization and tracheal suctioning: before-during/during-after: P=.000, with the exception of the cures that only affected respiratory rate. 27% of the procedures received analgesia: 9% received it before, 15% during and 3.2% after, with more analgesia being required for the wound care (33.3%). The data collected in the nursing report on the evaluation of pain/effectiveness of the analgesia showed 20.66%. CONCLUSION: An increase on the ESCID score was observed while performing the procedures.

Condylomata, cytological abnormalities and human papillomavirus infection in the anal canal in HIV-infected men.

BACKGROUND: Genital infections with low-risk (LR) and high-risk (HR) human papillomavirus (HPV) genotypes are associated with ano-genital condylomata and anal squamous cell cancer. HPV-related pathologies in HIV-infected men are a serious concern. In this study, the prevalence of anal condylomata and their association with cytological abnormalities and HPV infection in the anal canal in HIV-infected men [men who have sex with men (MSM) and heterosexuals] were estimated. METHODS: This was a cross-sectional study based on the first visits of patients in the Can Ruti HIV-positive Men (CARH·MEN) cohort. Anal condylomata were assessed by clinical and proctological examination. Samples from the anal canal were collected for HPV genotyping and cytological diagnoses. RESULTS: A total of 640 HIV-infected men (473 MSM and 167 heterosexuals) were included in the study. The overall prevalence of anal condylomata was 25% [157 of 640; 95% confidence interval (CI) 21-28%]; in MSM it was 28% and in heterosexuals it was 15% [odds ratio (OR) 2.2; 95% CI 1.4-3.5]. In patients with anal condylomata, HPV infection in the anal canal was more prevalent (92% vs. 67% in those without anal condylomata; OR 8.5; 95% CI 3.2-22). This higher HPV prevalence involved at least two HPV genotypes (OR 4.0; 95% CI 2.2-7.1), mainly HR genotypes (OR 3.3; 95% CI 1.7-6.4). Similarly, the cumulative prevalence of HPV-6 and HPV-11 was higher in patients with anal condylomata (63% vs. 19% in those without anal condylomata). Having anal condylomata was associated with higher prevalences of cytological abnormalities (83% vs. 32% in those without anal condylomata; OR 6.9; 95% CI 3.8-12.7) and high-grade squamous intraepithelial lesions (HSILs) (9% vs. 3% in those without anal condylomata; OR 9.0; 95% CI 2.9-28.4) in the anal canal. CONCLUSIONS: HIV-infected men with anal condylomata were at risk of presenting HSILs and harbouring multiple HR HPV infections in the anal canal. Although MSM presented the highest prevalence of anal condylomata, heterosexual men also had a clinically important prevalence. Our findings emphasize the importance of screening and follow-up for condylomata in the anal canal in HIV-infected men.

Protective roles of quinone reductase and tamoxifen against estrogen-induced mammary tumorigenesis.

We previously reported that antiestrogen-liganded estrogen receptor beta (ERbeta) transcriptionally activates the major detoxifying enzyme quinone reductase (QR) (NAD(P)H:quinone oxidoreductase). Further studies on the functional role of ERbeta-mediated upregulation of antioxidative enzymes indicated protective effects against estrogen-induced oxidative DNA damage (ODD). We now report on in vivo and in vitro studies that show that ERbeta-mediated upregulation of QR are involved in the protection against estrogen-induced mammary tumorigenesis. Using the August Copenhagen Irish (ACI) model of estrogen-induced carcinogenesis, we observed that increased ODD and decreased QR expression occur early in the process of estrogen-induced mammary tumorigenesis. Prevention of ACI mammary gland tumorigenesis by tamoxifen was accompanied by decreased ODD and increased QR levels. These correlative findings were supported by our findings that downregulation of QR levels led to increased levels of estrogen quinone metabolites and enhanced transformation potential of 17beta-estradiol treated MCF10A non-tumorigenic breast epithelial cells. Concurrent expression of ERbeta and treatment with 4-hydroxytamoxifen decreased tumorigenic potential of these MCF10A cells. We conclude that upregulation of QR, through induction by tamoxifen, can inhibit estrogen-induced ODD and mammary cell tumorigenesis, representing a possible novel mechanism of tamoxifen prevention against breast cancer.

Predictive factors for successful laparoscopic splenectomy in immune thrombocytopenic purpura: study of clinical and laboratory data.

BACKGROUND: Laparoscopic splenectomy (LS) offers better short-term results than open surgery for the treatment of immune thrombocytopenic purpura (ITP), but long-term follow-up is required to ensure its efficacy. The remission rate after splenectomy ranges from 49 to 86% and the factors that predict a successful response to surgical management have not been clearly defined. The goal of this study was to determine the preoperative factors that predict a successful outcome following LS. METHODS: From February 1993 to December 2003, LS was consecutively performed in a series of 119 nonselected patients diagnosed with ITP (34 men and 85 women; mean age, 41 years), and clinical results were prospectively recorded. Postoperative follow-up was based on clinical records, follow-up data provided by the referring hematologist, and a phone interview with the patient and/or relative. Univariate and multivariate analyses were performed for clinical preoperative variables to identify predictive factors of success following LS. RESULTS: Over a mean period of 33 months, 103 patients (84%) were available for follow-up with a remission rate of 89% (92 patients, 77 with complete remission with platelet count > 150,000). Eleven patients did not respond to surgery (platelet count < 50,000). Mortality during follow-up was 2.5% (two cases not related to hematological pathology and one case without response to splenectomy). Preoperative clinical variables evaluated to identify predictive factors of response to surgery were sex, age, treatment (corticoids alone or associated with Ig or chemotherapy), other immune pathology, duration of disease, and preoperative platelet count. In a subgroup of 52 patients, we also evaluated the type of autoantibodies and corticoid doses required to maintain a platelet count > 50,000. Multivariate analysis showed that none of the variables evaluated could be considered as predictive factors of response to LS due to the high standard error. CONCLUSION: Long-term clinical results show that LS is a safe and effective therapy for ITP. However, a higher number of nonresponders is needed to determine which variables predict response to LS for ITP.

Sulfatase activity in the oyster Crassostrea virginica: its potential interference with sulfotransferase determination.

Two sulfatase isoforms, a soluble one with an optimum pH of 5.0, and a microsomal one with an optimum pH of 7.6, were observed in digestive gland, gonads, mantle and gills of the oyster C. virginica. The highest sulfatase activity was recorded in the digestive gland cytosol and is likely to interfere with the in vitro determination of sulfotransferase activity. Indeed, the sulfatase inhibitor Na(2)SO(3) led to an increase of measured sulfotransferase activity (31+/-9%), suggesting that those sulfatases might be partially responsible for the low sulfotransferase activities found in C. virginica.

The effects of steroidal estrogens in ACI rat mammary carcinogenesis: 17beta-estradiol, 2-hydroxyestradiol, 4-hydroxyestradiol, 16alpha-hydroxyestradiol, and 4-hydroxyestrone.

Several investigators have suggested that certain hydroxylated metabolites of 17beta-estradiol (E2) are the proximate carcinogens that induce mammary carcinomas in estrogen-sensitive rodent models. The studies reported here were designed to examine the carcinogenic potential of different levels of E2 and the effects of genotoxic metabolites of E2 in an in vivo model sensitive to E2-induced mammary cancer. The potential induction of mammary tumors was determined in female ACI rats subcutaneously implanted with cholesterol pellets containing E2 (1, 2, or 3 mg), or 2-hydroxyestradiol (2-OH E2), 4-hydroxyestradiol (4-OH E2), 16alpha-hydroxyestradiol (16alpha-OH E2), or 4-hydoxyestrone (4-OH E1) (equimolar to 2 mg E2). Treatment with 1, 2, or 3 mg E2 resulted in the first appearance of a mammary tumor between 12 and 17 weeks, and a 50% incidence of mammary tumors was observed at 36, 19, and 18 weeks respectively. The final cumulative mammary tumor incidence in rats treated with 1, 2, or 3 mg E2 for 36 weeks was 50%, 73%, and 100% respectively. Treatment of rats with pellets containing 2-OH E2, 4-OH E2, 16alpha-OH E2, or 4-OH E1 did not induce any detectable mammary tumors. The serum levels of E2 in rats treated with a 1 or 3 mg E2 pellet for 12 weeks was increased 2- to 6-fold above control values (approximately 30 pg/ml). Treatment of rats with E2 enhanced the hepatic microsomal metabolism of E2 to E1, but did not influence the 2- or 4-hydroxylation of E2). In summary, we observed a dose-dependent induction of mammary tumors in female ACI rats treated continuously with E2; however, under these conditions 2-OH E2, 4-OH E2, 16alpha-OH E2, and 4-OH E1 were inactive in inducing mammary tumors.

Long-term outcome after laparoscopic splenectomy related to hematologic diagnosis.

BACKGROUND: Laparoscopic splenectomy (LS) has been demonstrated as an effective and safe treatment for hematological disorders requiring spleen removal, especially in cases of normal-sized spleens. However, although results are promising, long-term outcome data are lacking. We reviewed our clinical experience with LS in a series of 255 cases, with particular attention to the long-term outcome related to the disease process requiring LS. METHODS: From February 1993 to October 2003, LS was attempted in 255 patients (100 males and 155 females with a mean age of 45 +/- 19 years) and clinical information was recorded in a prospective database. Indications for splenectomy included idiopathic thrombocytopenic purpura (ITP) (n = 115), HIV-ITP (n = 9), Evans syndrome (n = 6), autoimmune hemolytic anemia (AIHA) (n = 13), hereditary spherocytosis (HS) (n = 19), hematologic malignancy (n = 66), thrombotic thrombocytopenic purpura (n = 1), and others (n = 26). Long-term postoperative follow-up evaluation was obtained through clinical notes, follow-up visits by the referring hematologist, and by phone interviews both with patients and with the referring hematologist. RESULTS: A total of 186 patients (73%) were available for a mean follow-up of 35 months (range, 1-104). Of the ITP patients, 87 (76%) were followed up, with a remission rate of 89% (complete remission in 75%). A similar remission rate was observed in ITP-HIV; in patients available for follow-up (78%), complete remission was achieved in 83%. In Evans, complete remission was achieved in all patients available for follow-up (67%). Clinical response for hemolytic disease ranged between 70% for AIHA and 100% for HS. In the malignant group, the late mortality rate was 22%. The mortality rate in the miscellaneous group was 5%. No cases of splenectomy-related sepsis occurred during follow-up. CONCLUSIONS: LS offers advantages for all types of splenic diseases requiring surgery. It provides not only good clinical short-term outcome but also satisfactory long-term hematological results.

Mid term analysis of safety and quality of life after the laparoscopic repair of paraesophageal hiatal hernia.

BACKGROUND: Initial experience with the laparoscopic repair of paraesophageal and type III mixed hiatal hernias showed that it is safe and feasible, with excellent immediate and short-term results. However, after a longer follow-up, a recurrence rate of < or =40% has been demonstrated. Data related to the outcome of paraesophageal hernia repair and the recurrence rate are still lacking. Quality-of-life scores may offer a better means of assessing the impact of surgical treatment on the overall health status of patients. Therefore, we performed prospective evaluation of anatomic and/or symptomatic recurrences after paraesophageal or large hiatal hernia repair. In addition, we investigated the correlation between recurrence and the patient's quality of life. METHODS: All patients after who had undergone repair of paraesophageal of mixed hiatal hernia were identified prospectively from a database consisting of all patients who had had laparoscopic operations for gastroesophageal pathology at our hospital between February 1998 and December 2002. The preoperative symptoms were taken from patients' clinical files. In March 2003, all patients with > or =6 months of follow-up had a barium swallow and were examined for radiological and clinical signs of recurrence. Thereafter, the patients' quality of life after surgery was evaluated using three standard questionnaires (Short Form 36 [SF-36], Glasgow Dyspepsia Severity Score [GDSS], and Gastrointestinal Quality of Life Index [GIQLI]. RESULT: During the study period, 46 patients had been operated on. The mean age was 63 years (range, 28-93). Thirty seven of them had a follow-up of > or =6 months. Eight patients (21%) had postoperative gastrointestinal symptoms. Barium swallow was performed in 30 patients (81%) and showed a recurrence in six of them (20%). According to SF-36 and GDSS, the patients' postoperative quality of life reached normal values and did not differ significantly from the standard values for the Spanish population of similar age and with similar comorbidities. Successfully operated patients reached a GIQLI value comparable to the standard population. However, symptomatic patients had significantly lower GIQLI scores than the asymptomatic or the Rx-recurrent group. CONCLUSION: The laparoscopic treatment of large paraesophageal and mixed hiatal hernias is not only feasible and safe but also offers a good quality of life on a midterm basis. However, the anatomic and functional recurrence rate is high. The next step is to identify the subset of patients who are at risk of failure and to establish technical alternatives that would ensure the durability of the repair.

Pharmacological study of Stachytarpheta cayennensis Vahl in rodents.

Freeze-dried aqueous extracts (AEs, 0.1-1g/kg body wt., p.o.) obtained from entire or selected parts of Stachytarpheta cayennensis were tested for their effects on gastric secretion, gastric motility, inflammation and pain in rodents, with the purpose of validating the plant's ethnomedical uses. The AE-Total, AE-Flowers and AE-Leaves but not AE-Stems inhibited the gastric acid secretion in pylorus-ligated rats with varying potency. Purification of AEs yielded the semipurifed fractions EtFs rich in iridoids. All the EtFs with exception of EtF-Stems inhibited gastric acid secretion of pylorus ligated mice. While AE-Total stimulated the intestinal transit of mice by 43%, AE-Leaves delayed it by 38%. These effects on intestinal transit were not observed when the EtFs were tested. Only AE-Leaves and AE-Flowers altered the gastric emptying of semisolids, increasing it by 45% and 69%, respectively. These results indicate that the compounds related to inhibition of gastric acid secretion and gastrointestinal motility are different. The AE-Total reduced abdominal writhing induced by acetic acid potently (ED50 value = 700 mg/kg, p. o.) without altering the writhes induced by acetylcholine. Attempts to identify the mechanism of analgesia were unsuccessful since the AE-Total did not show analgesic effects when tested in different models of pain such as formalin and capsaicin or the tail-flick test. Pretreatment of animals with AE-Total did not show antiinflammatory activity in any of the acute (paw edema induced by carrageenin, dextran or histamine, pleurisy induced by carrageenin and capsaicin-induced mouse ear edema) or chronic (air pouch) models used. No toxic signs were observed after administration of the different extracts up to 2 g/kg body wt., p.o. Collectively, the results confirmed folk information indicating presence of analgesic, mild laxative and potent inhibition of gastric secretion activities in the aqueous extracts of S. cayennensis. The results do not, however confirm the folk use of the plant as an antiinflammatory medicine.

Inhibition of rat liver sulfotransferases SULT1A1 and SULT2A1 and glucuronosyltransferase by dietary flavonoids.

1. Dietary flavonoids including kaempferol, quercetin, genistein and daidzein were tested for their ability to alter the conjugation of oestradiol (E(2)) via rat liver sulfotransferases and glucuronosyltransferase. 2. All four flavonoids inhibited the sulfonation of E(2) via phenol sulfotransferase, SULT1A1 with IC(50)s ranging from 0.29 to 4.61 micro M. Sulfonation of dehydroisoandrosterone (DHEA) via hydroxysteroid sulfotransferase, SULT2A1, was inhibited by higher amounts of the flavonoids (IC(50)s ranging from 34 to 116 micro M). 3. All flavonoids inhibited the formation of E(2)-beta-glucuronides (at carbon atoms 3 and 17) with IC(50)s ranging from 43 to 260 micro M. Glucuronidation of 4-methylumbelliferone (4-MU) was inhibited by high amounts of the flavonoids (IC(50)s ranging from 860 to 1550 micro M). 4. Hydrolysis of sulfonated oestrogens via arylsulfatase-c (ARSC) or 4-methylumbelliferone beta-glucuronidate (MUG) were not inhibited by the flavonoids. 5. It is concluded that SULT1A1 but not SULT2A1 or glucuronosyltransferase is highly sensitive to inhibition by dietary flavonoids. The potency of the inhibition for SULT1A1 (quercetin > kaempferol > genistein > daidzein) suggests a dependency on the number and position of hydroxyl radicals in the flavonoid molecule.