Antitumoral photoinduced effects of crude extract, fractions, and naphthoquinones from Sinningia magnifica (Otto & A. Dietr.) Wiehler (Gesneriaceae) in a bioguided study.

Photodynamic therapy (PDT) has been used for various purposes, including as an antitumor resource in a noninvasive therapy with minimal side effects. Sinningia magnifica (Otto & A. Dietr.) Wiehler is a rupicolous plant found in rock crevices in Brazilian tropical forests. Initial studies indicate the presence of phenolic glycosides and anthraquinones in species of the genus Sinningia (Generiaceae family). It is known that anthraquinones are natural photosensitizers with potential PDT applications. This led us to investigate the potential compounds of S. magnifica for use as a natural photosensitizer against the melanoma (SK-MEL-103) and the prostate cancer (PC-3) cell lines in a bioguided study. Our results showed that singlet oxygen production by the 1,3-DPBF photodegradation assay greatly increased in the presence of crude extract and fractions. The biological activity evaluation showed photodynamic action against melanoma cell line SK-MEL-103 and prostate cell line PC-3. These results suggest the presence of potential photosensitizing substances, as demonstrated in this in vitro antitumor PDT study by the naphthoquinones Dunniol and 7-hydroxy-6-methoxy-α-dunnione for the first time. Naphthoquinones, anthraquinones and phenolic compounds were identified in the crude extract by UHPLC-MS/MS analysis, motivating us to continue with the bioguided phytochemical study aiming to discover more photochemically bioactive substances in Gesneriaceae plants.

Reproductive toxicity of the hydroethanolic extract of the flowers of Acmella oleracea and spilanthol in zebrafish: In vivo and in silico evaluation.

Hydroethanolic preparations of Acmella oleracea is used in the north of Brazil as a female aphrodisiac. Thus, the objective of this study was to evaluate the action of the hydroethanolic extract of Acmella oleracea (EHFAo) flowers (21.873 and 44.457 mg/kg) and spilanthol (3 mg/kg) administered orally on reproductive performance and effects on the embryonic development of zebrafish F1 generation. It was observed that in the groups in which males and females received EHFAo and spilanthol, the spawning was interrupted, whereas in the groups in which only the females were treated, spawning occurred during the 21 days. Thus, in the histopathological evaluation of the gonads, it was possible to observe that the percentage of mature cells in the spermatozoa and females was significantly reduced. Only the embryo groups in which parental generation was treated with EHFAo showed lethal and teratogenic effects. On the other hand, the parental groups treated with the spilanthol presented only the lethality. Spilanthol and some metabolites showed good oral availability and important toxicological properties. Thus, it is suggested that the treatment of parental generation of zebrafish with EHFAo and spilanthol caused severe changes in the gonads and on fertility. However, on the embryo, the most striking effects in the development were recorded in the groups in which the parental generation was treated with the EHFAo, while the spilanthol influenced the lethality of the embryos.

Compostos coordenados híbridos de platina no tratamento do câncer / Platinum hybrid coordinated compounds in cancertreatment

O câncer, ou neoplasia, é uma doença caracterizada pela propagação descontrolada de formas anormais das próprias células corporais e corresponde à segunda doença que mais causa mortes no mundo. A história da platina no tratamento do câncer teve início com a descoberta da sua atividade, em 1965, com a aprovação para uso clínico acontecendo apenas após 10 anos. Atualmente, os fármacos com platina estão entre os mais bem sucedidos agentes anticancerígenos, onde se destacam cisplatina (1), carboplatina (2) e oxaliplatina (3). Seus mecanismos de ação são similares: estes fármacos formam adutos com o DNA, impedindo a sua síntese e reparo, levando à morte celular. Contudo, os efeitos adversos desencadeados pelo tratamento e o desenvolvimento de resistência ao medicamento têm limitado suas aplicações. Uma das principais estratégias para a diminuição de tais efeitos consiste em alterar a estrutura destas moléculas, levando à formação de compostos híbridos, que se caracterizam pela presença de pelo menos dois fragmentos funcionais distintos em uma mesma molécula e podem apresentar maior espectro de atividade antitumoral. Dentre as alterações mais comuns encontram-se a modificação da solubilidade, através da inserção de grupos abandonadores mais ou menos hidrofóbicos e a introdução de ligantes com atividade biológica própria. Dessa forma, esta revisão visa verificar os avanços mais recentes na síntese de compostos híbridos de platina, bem como as melhorias na atividade anticâncer dos novos compostos platinados...

Cancer, or neoplasm, is a disease characterized by the uncontrolled propagation of abnormal cells of the body and is the second leading death-causing disease. The history of platinum in cancer treatment goes back to the discovery of its activity in 1965 and its approval for clinical use just 10 years later. Some of the most successful anticancer agents are Pt-based chemotherapeutics, among which cisplatin (1), carboplatin (2), and oxaliplatin (3) stand out. They have similar mechanisms of action: they form adducts with DNA, preventing its synthesis and repair and leading to cell death. However, adverse effects triggered by treatment and the development of resistance to these drugs have limited their application. One of the most important strategies to reduce such effects is to carry out structural modifications of these molecules, leading to hybrid compounds that are characterized by the presence of at least two distinct functional fragments on the same molecule and can exhibit a broader antitumor activity spectrum. Among the most typical modifications are changes to the solubility pattern, created by the insertion of leaving groups with high or low hydrophobicity, and the introduction of biologically active ligands as non-leaving groups. The purpose of these strategies is to obtain compounds capable of reducing systemic toxicity and/or overcoming acquired resistance factors to cisplatin. Therefore, the aim of this review is to discuss the most recent advances in the synthesis of hybrid platinum compounds, as well as improvements in the anticancer activity of Pt-compounds...

Occurrence of Candida orthopsilosis in Brazilian tomato fruits (Lycopersicum esculentum Mill.).

We aimed to isolate and identify yeasts found in the tomato fruit in order to obtain isolates with biotechnological potential, such as in control of fungal diseases that damage postharvest fruits. We identified Candida orthopsilosis strains LT18 and LT24. This is the first report of this yeast on Lycopersicum esculentum fruits in Brazil.

Comparison of two bioelectrical impedance devices and dual-energy X-ray absorptiometry to evaluate body composition in heart failure.

BACKGROUND: The utilisation of bioelectrical impedance analysis (BIA) in heart failure can be affected by many factors and its applicability remains controversial. The present study aimed to verify the adequacy of single-frequency BIA (SF-BIA) and multifrequency BIA (MF-BIA) compared to dual-energy x-ray absorptiometry (DEXA) for evaluating body composition in outpatients with heart failure. METHODS: In this cross-sectional study, 55 patients with stable heart failure and left ventricle ejection fraction ≤45% were evaluated for fat mass percentage, fat mass and fat-free mass by DEXA and compared with the results obtained by SF-BIA (single frequency of 50 kHz) and MF-BIA (frequencies of 20 and 100 kHz). RESULTS: MF-BIA and DEXA gave similar mean values for fat mass percentage, fat mass and fat-free mass, whereas values from SF-BIA were significantly different from DEXA. Both SF-BIA and MF-BIA measures of body composition correlated strongly with DEXA (r > 0.8; P < 0.001), except for fat mass assessed by SF-BIA, which showed a moderate correlation (r = 0.760; P < 0.001). MF-BIA also showed a better agreement with DEXA by Bland-Altman analysis in all measurements. However, both types of equipment showed wide limits of agreement and a significant relationship between variance and bias (Pitmans's test P > 0.05), except MF-BIA for fat-free mass. CONCLUSIONS: Compared with DEXA, MF-BIA showed better accuracy than SF-BIA, although both types of equipment showed wide limits of agreement. The BIA technique should be used with caution, and regression equations might be useful for correcting the observed variations, mainly in extreme values of body composition.

Occurrence of Candida orthopsilosis in Brazilian tomato fruits (Lycopersicum esculentum Mill)

We aimed to isolate and identify yeasts found in the tomato fruit in order to obtain isolates with biotechnological potential, such as in control of fungal diseases that damage postharvest fruits. We identified Candida orthopsilosis strains LT18 and LT24. This is the first report of this yeast on Lycopersicum esculentum fruits in Brazil.

Dietary vitamin K intake and stability of anticoagulation with coumarins: evidence derived from a clinical trial.

BACKGROUND: Dietary vitamin K intake has been considered a major factor that influences stability of oral anticoagulation (OA) with coumarins. Few studies have evaluated the relationship between amounts of dietary vitamin K intake and stability of anticoagulation. OBJECTIVE: To assess whether high dietary vitamin K intake is associated to stability of International Normalized Ratio (INR) of the prothrombin time. METHODS: We performed a sub-analysis of a randomized clinical trial involving outpatients from the anticoagulation clinic of a university hospital. INR and vitamin K intake were prospectively collected at baseline, 15, 30, 60 and 90 days after randomization. Patients were considered with a stable anticoagulation when their INR coefficient of variation was less than 10%. Dietary vitamin K intake was assessed by a food frequency questionnair and a score of intake was derived. RESULTS: We studied 132 patients on chronic OA (57 ± 13 years; 55% males); 23 patients (17%) were achieved stable anticoagulation. Stable and unstable patients had no significant differences in baseline characteristics. The dietary vitamin K score over the entire follow-up for stable patients was significantly lower than that for unstable patients (p = 0.012). DISCUSSION: Our findings suggest that INR stability could be achieved with relatively low amounts of dietary vitamin K.

Insulin resistance, body fat percentage, and lipid abnormalities as risk factors for cardiovascular diseases in renal transplant recipients: a 1-year analysis.

The aim of this study was to evaluate changes in body mass index (BMI), body fat percentage (BF%), insulin resistance, and lipid profile in 32 patients during the first year after renal transplantation by anthropometric measures. The homeostasis model assessment index (HOMA) was calculated for insulin resistance estimation. Anthropometric measures and biochemical markers were evaluated at the time of transplantation (T(0)), and prospectively at 3 (T(3)), 6 (T(6)), 9 (T(9)), and 12 (T(12)) months posttransplantation. The HOMA index decreased significantly at 3 months after transplantation (T(3)) (2.4 +/- 1.5 vs 1.5 +/- 1.1; P < .01); however, an increment was observed at T(6) and T(9) (1.8 +/- 0.8 and 2 +/- 1.5, respectively), remaining stable at T(12) (2 +/- 1.7). BMI and BF% increased significantly over 12 months (23.3 +/- 2.7 vs 24.4 +/- 2.7 kg/m(2); P = .001 and 23.7 +/- 7.8 vs 25.6 +/- 7.7 %; P = .002). Total cholesterol, low-density lipoprotein cholesterol and triglyceride levels showed significant increases starting at T(3). In conclusion, insulin resistance decreased transitorily post-renal transplantation. BMI, BF%, and lipid profile showed unfavorable changes during the first year post-renal transplantation.

Leptin serum levels in the first year post-renal transplantation.

The aim of the present study was to evaluate the serum levels of leptin in the first year post-renal transplantation. Thirty-two patients and 19 healthy individuals were included. Serum leptin and biochemical markers were evaluated prospectively starting at transplant time (t(0)), and then every 3 months up to 1 year posttransplantation. The mean serum levels of leptin were higher in the pretransplant (t(0)) evaluation as compared with a control group of healthy volunteers (11.9 [9.2-25.2] and 7.7 [5.2-9.9] ng/mL, respectively; P < .0001). Leptinemia decreased significantly in the first 3 months after the renal transplantation (t(3)) (11.9 [9.2-25.2] to 7.1 [4.14-12.5] ng/mL; P < .0001) increased at t(6) to 10.6 (5.6-14.6) ng/mL and remained stable at t(9) (9.0 [5.2-18.3] ng/mL) and t(12) (9.3 [4.9-16.4] ng/mL). No correlation was found between leptin and renal function at any time during the study. In conclusion, during the first posttransplant year the serum leptin levels decreased significantly in relation to pretransplant period.

[Cardiac attacks in patients with acute Chagas disease in a family micro-outbreak, in Abaetetuba, Brazilian Amazon]. / Acometimento cardíaco em pacientes com doença de Chagas aguda em microepidemia familiar, em Abaetetuba, na Amazônia Brasileira.

The authors describe the main clinical findings relative to cardiac involvement, in patients with acute Chagas' disease (CD) in yet another familial micro-epidemic episode of CD in Amazon region. Thirteen patients were studied with acute Chagas' disease, resident in the city of Abaetetuba in Pará state; they were submitted to clinical and heart evaluation, with electrocardiograph and echocardiograph exams. Ventricular extrasystole occurred in 38.5% of the cases. Right bundle branch block and 1st and 2nd degree atrioventricular block were found in 30.8% of the patients. Attention is called to two findings in the Doppler echocardiography: pericardiac involvement and an image suggestive of aneurismatic formation in two patients. The findings reveal acute heart disease, with evidence of cardiomyopathy and alterations in the conduction system of the heart, bearing similarity with the description of the disease in endemic areas.