Samanea tubulosa Benth. (Fabaceae): Antinociceptive effect on acute pain in mice: K+ATP channel and opioid activity.

Samanea tubulosa Benth. it has been widely used in traditional medicine to treat inflammatory processes. The present study aimed to investigate the antinociceptive effect and mechanism of action of the fractions obtained from the Samanea tubulosa pods in mice. The antinociceptive activity was evaluated in formalin, capsaicin and glutamate tests and the. The possible mechanisms of action involved in the antinociceptive effect of the hexane and ethyl acetate fraction in the opioid system, also the the K + ATP channels and the L-arigine pathways of nitric oxide were evaluated. The chemical characterization analysis revealed in the hexane fraction the presence of triterpenes such as lupenone and lupeol. In the glutamate test, the hexane and ethyl acetate fractions showed antinociceptive activity at the dose of 12.5 and 25 mg kg-1. The antinociception produced by the hexane and ethyl acetate fractions was significantly reversed by naloxone, indicating that the fractions act through the opioid pathway. Antinociceptive response of the ethyl acetate fraction was blocked by glibenclamide, indicating that this fraction acts via the K + ATP channels activation. It is concluded that the fractions under study exert antinociceptive activity possibly related to the opioid route and through K+ ATP channels activation.

High Trypanosoma spp. diversity is maintained by bats and triatomines in Espírito Santo state, Brazil.

The aim of this study was to reevaluate the ecology of an area in the Atlantic Forest, southeast Brazil, where Chagas disease (CD) has been found to occur. In a previous study, immediately after the occurrence of a CD case, we did not observe any sylvatic small mammals or dogs with Trypanosoma cruzi cruzi infections, but Triatoma vitticeps presented high T. c. cruzi infection rates. In this study, we investigated bats together with non-volant mammals, dogs, and triatomines to explore other possible T. c. cruzi reservoirs/hosts in the area. Seventy-three non-volant mammals and 186 bats were captured at three sites within the Guarapari municipality, Espírito Santo state. Rio da Prata and Amarelos sites exhibited greater richness in terms of non-volant mammals and bats species, respectively. The marsupial Metachirus nudicaudatus, the rodent Trinomys paratus, and the bats Artibeus lituratus and Carollia perspicillata were the most frequently captured species. As determined by positive hemocultures, only two non-volant mammals were found to be infected by Trypanosoma species: Monodelphis americana, which was infected by T. cascavelli, T. dionisii and Trypanosoma sp., and Callithrix geoffroyi, which was infected by T. minasense. Bats presented T. c. cruzi TcI and TcIII/V, T. c. marinkellei, T. dionisii, T. rangeli B and D, and Trypanosoma sp. infections. Seven dogs were infected with T. cruzi based only on serological exams. The triatomines T. vitticeps and Panstrongylus geniculatus were found to be infected by trypanosomes via microscopy. According to molecular characterization, T. vitticeps specimens were infected with T. c. cruzi TcI, TcII, TcIII/V, and TcIV, T. c. marinkellei and T. dionisii. We observed high trypanosome diversity in a small and fragmented region of the Atlantic Forest. This diversity was primarily maintained by bats and T. vitticeps. Our findings show that the host specificity of the Trypanosoma genus should be thoroughly reviewed. In addition, our data show that CD cases can occur without an enzootic cycle near residential areas.

Pneumoretroperitoneum, pneumomediastinum and subcutaneous emphysema after endoscopic submucosal dissection of a rectal lateral spreading tumor / Pneumorretroperitônio, pneumomediastino e enfisema subcutâneo após dissecção endoscópica da submucosa de lesão retal de crescimento lateral

Introduction: Endoscopic submucosal dissection (ESD) is an already established procedure in the treatment of gastric and esophageal cancer in its early stages. Colorectal lesions, initially approached by endoscopic mucosal resection en bloc or in fragments, are the current focus for submucosal approach, especially for superficial lateral spreading tumor of 20 mm-diameter. The experience of Japanese centers, which are reference in therapeutic endoscopy, demonstrates reduction in the rate of disease recurrence with this approach and, according to specific histopathological criteria, may avoid colectomy in some cases of malignant neoplasia. Case report: The patient was 50-year-old female. She underwent endoscopic submucosal dissection of a rectal lateral spreading tumor measuring 50 mm, located 8 cm from the anal margin. The procedure was performed without major complications, with just two points for muscle layer detachment, without gross perforation and closed with metal clips. However, the patient developed air leakage to the peritoneum, retroperitoneum, mediastinum and subcutaneous tissue, being only treated with clinical procedures and without additional intervention. Conclusion: It is vital to know and be able to apply the technique of ESD, in addition to addressing its complications, since despite the numerous benefits compared to surgery, ESD can result in serious outcomes. (AU)

Introdução: A dissecção endoscópica da submucosa (ESD) já é procedimento consagrado no tratamento do câncer gástrico e esofagiano em suas fases precoces. As lesões colorre-tais, inicialmente abordadas por mucossectomia, em bloco ou em fragmentos, são o foco atual para a abordagem submucosa, principalmente para os tumores de crescimento lateral superficial a partir de 20 mm de diâmetro. A experiência de centros japoneses, referências em endoscopia terapêutica, demonstram redução no índice de recidiva da doença com esta abordagem e, segundo critérios histopatológicos específicos, podem evitar uma colectomia em alguns casos de neoplasia maligna. Relato de caso: Trata-se de paciente de 50 anos, submetida à dissecção endoscópica da submucosa de lesão de crescimento lateral, com 50 mm, localizada no reto, a 8 cm da margem anal. O procedimento foi realizado sem maiores intercorrências, com apenas dois pontos de afastamento da muscular, sem perfuração grosseira, fechados com clipe. Entretanto, a paciente evoluiu com escape aéreo para peritônio, retroperitônio, mediastino e subcútis, sendo tratada sem intervenção adicional, apenas com manejo clínico. Conclusão: É de fundamental importância conhecer e saber aplicar a técnica da ESD, além de abordar suas complicações, uma vez que, mesmo repleta de benefícios em relação à cirurgia, ela pode apresentar desfechos graves. (AU)

In vitro antioxidant and cytotoxic activity of some synthetic riparin-derived compounds.

This study aimed to study the in vitro antioxidant activity and cytotoxicity on tumor cells lines of six synthetic substances derived from riparins. All the substances showed antioxidant activity and riparins C, D, E, F presented cell growth inhibition rates greater than 70%, suggesting that these molecules have antitumor properties. These substances also caused greater than 80% releases of cytoplasmic lactate dehydrogenase enzyme (LDH). Although the antioxidant and antitumor properties presented herein require further assessment, the outcomes indicate that these novel riparins are promising biologically active compounds.

Safe multidisciplinary approach in deeply infiltrating endometriosis (DIE): is it feasible?

OBJECTIVE: Evaluate the type and incidence of postoperative complications after surgery for deep infiltrative endometriosis at Biocor Hospital. METHODS: Our observational study involved a multidisciplinary surgical team that performed laparoscopy on 154 patients suffering from pelvic pain. Surgical complications occurring up to the 30th postoperative day were recorded. RESULTS: Mean age patient age was 34.1 years. Infertility was present in 69 (45%) although 31% had not attempted to get pregnant. Dysmenorrhea was the most frequent symptom (79.3%) followed by chronic pelvic pain (59.7%) and deep dyspareunia (48,7%). Most cases required extensive surgery as the majority (n=117; 76.9%) were classified as severe endometriosis (ASRM grade IV). The most frequent surgical procedures were: 136 adhesiolysis, 100 intestinal surgeries (85 retosigmoidectomies), 92 peritonal lesion excision, 39 vaginal resections, 19 myomectomies, 21 hysterectomies and 5 partial bladder resections. Postoperative complications were recorded in 14 (9.59%) patients: 8 (5.48%) major complications and 6 (4.11%) minor. Major complications included blood transfusion (n=2) retosigmoid anastomosis dehiscence (1), rectovaginal fistula (n=1), urinary fistula (n=1), deep vein thrombosis (n=1), lower limb compartment syndrome with motor deficit (n=1) and one intestinal obstruction (n=1). Minor complications were abdominal wall infection (n=3), peripheral neuropathy (n=3), bladder atony (n=1) and bladder perforation (n=1). No deaths were observed. All major complication cases underwent retosigmoidectomy associated with vaginal resection (n=6), uterosacral ligament excision (n=5) or hysterectomy (n=3). CONCLUSION: The surgical treatment of DIE is complex and subject to complications. The surgical expertise of a multidisciplinary team plays a vital role in this setting.

Phytochemical profile and qualification of biological activity of an isolated fraction of Bellis perennis.

This study describes the isolation and identification of apigenin-7-O-ghicopyranoside, a flavonoid isolated from the flowers of Bellis perennis L., Asteraceae, an species with a broad spectrum of biological activities. The in vitro antioxidant activity and the inhibition of the enzyme acetylcholinesterase were evaluated. The flavonoid showed strong in vitro antioxidant potential, because of the capacity of removal of hydroxyl radicals and nitric oxide, and also prevented the formation of thiobarbituric acid-reactive substances. These parameters were inhibited at the highest concentration of ApG at rates of 77.7%, 72% and 73.4%, respectively, in addition to inhibiting acetylcholinesterase, suggesting potential use in the treatment of neurodegenerative diseases.

Systemic and reproductive toxicity induced by Parkia platycephala ethanolic extract in female Wistar rats

The present study was conducted to evaluate the toxicity of the ethanolic extract of leaves of Parkia platycephala Benth., Fabaceae, on systemic and reproductive parameters. In toxicity on the estrous cycle, four groups of not-pregnant Wistar rats received distilled water and the doses 250, 500 and 1000 mg.kg-1 of plant extract for thirty days, at the end of which they were examined as to the frequency of their phases. The systemic toxicity was assessed through the consumption of water and food and by measuring body mass. After the extract was administered, serum AST, ALT, ALP, bilirubin (total, direct and indirect), urea and creatinine were dosed. The evaluation of the organs (brain, heart, hypophysis, adrenal glands, liver, spleen, uterus and ovaries) in their macroscopic aspects, relative and absolute masses and histological structure showed that the plant extract induced a decrease of water and food consumption and of body mass. It caused an increase in the luteal phase and a decrease in the follicular phase of the estrous cycle and rose serum alkaline phosphatase levels.The data exhibit systemic and reproductive toxicity induced by plant extract in female Wistar rats.

Phytochemical Profile and Qualification of Biological Activity of an Isolated Fraction of Bellis perennis

This study describes the isolation and identification of apigenin-7-O-ghicopyranoside, a flavonoid isolated from the flowers of Bellis perennis L., Asteraceae, an species with a broad spectrum of biological activities. The in vitro antioxidant activity and the inhibition of the enzyme acetylcholinesterase were evaluated. The flavonoid showed strong in vitro antioxidant potential, because of the capacity of removal of hydroxyl radicals and nitric oxide, and also prevented the formation of thiobarbituric acid-reactive substances. These parameters were inhibited at the highest concentration of ApG at rates of 77.7%, 72% and 73.4%, respectively, in addition to inhibiting acetylcholinesterase, suggesting potential use in the treatment of neurodegenerative diseases.

Novel furfurylidene N-acylhydrazones derived from natural safrole: discovery of LASSBio-1215, a new potent antiplatelet prototype.

We describe herein the discovery of (E)-N-methyl-N'-((5-nitrofuran-2-yl)methylene)benzo[d]( 1 , 3 ) dioxole-5-carbohydrazide (9e), named LASSBio-1215, as a novel antiplatelet agent belonging to the N-methyl-N-acylhydrazone class, which exert their antiaggregating actions on human and rabbit platelets induced by different agonists, through cyclooxygenase-1 (COX-1) or thromboxane synthase inhibition. This compound was elected after screening of a series of functionalized furyl N-acylhydrazone derivatives, synthesized from natural safrole 10. In vitro assays showed that compound 9e presents platelet-aggregating activity in rabbit platelet-rich plasma (PRP) induced by arachidonic acid (IC(50) = 0.7 µM) and collagen (IC(50) = 4.5 µM). Moreover, LASSBio-1215 also inhibited almost completely the second wave of adenosine diphosphate-induced platelet aggregation in human PRP, and this effect was correlated with their ability to block the production of pro-aggregating autacoid thromboxane A(2).

New class of potent antinociceptive and antiplatelet 10H-phenothiazine-1-acylhydrazone derivatives.

In this work, we reported the synthesis and evaluation of the analgesic, antiinflammatory, and antiplatelet properties of new phenothiazine-attached acylhydrazone derivatives (6), designed exploring the molecular hybridization approach between antipsychotic chlorpromazine (4) and other heterocyclic derivatives (3) and (5) developed at LASSBio. Target compounds were synthesized in very good yields exploiting diphenylamine (7) as starting material, through regioselective functionalization of the C-1 position of 10H-phenothiazine ring. The evaluation of platelet antiaggregating profile lead us to identify a new potent prototype of antiplatelet derivative, that is (6a) (IC(50)=2.3 microM), which acts in arachidonic acid pathway probably by inhibition of platelet COX-1 enzyme. Additionally, the change of para-substituent group of acylhydrazone framework permitted us to identify hydrophilic carboxylate derivative (6g) and hydrophobic bromo derivative (6b) as two new leads of analgesics more active than dipyrone used as standard and with selective peripheral or central mechanism of action.