Pregnant patient with prune belly syndrome: case report.

Prune belly syndrome is a rare congenital disease of unknown etiology that is present in one in every 40 thousand live births, and predominantly affects males, at a ratio of 4:1. In males, it presents with anomalies in the urinary system, absence of abdominal muscles, bilateral cryptorchidism, and infertility. In women, the syndrome has variable presentations, but fertility is preserved. Searching the medical literature, we found only one case of prune belly syndrome in pregnant women. Therefore, the patient in this report is the second case. She was primiparous, 25-years-old, with no abdominal muscles, severe congenital kyphoscoliosis, and pulmonary restriction. Elective cesarean section was performed at 37 weeks of gestation due to maternal risk of uterine rupture by transverse presentation and fetal risk of intrauterine growth restriction. The pre-anesthetic approach defined that general anesthesia might have more risks for the patient due to severe maternal lung disease compared to ultrasound-guided locoregional anesthesia. During prenatal care, there were some maternal complications, such as asthma exacerbations, abdominal pain, and constipation. The newborn was born small for gestational age and this can possibly be explained by maternal restrictive lung capacity. The newborn presented with Apgar score 8/9 and tachypnea, but improved after two hours of life.

Pregnant patient with prune belly syndrome: case report

ABSTRACT Prune belly syndrome is a rare congenital disease of unknown etiology that is present in one in every 40 thousand live births, and predominantly affects males, at a ratio of 4:1. In males, it presents with anomalies in the urinary system, absence of abdominal muscles, bilateral cryptorchidism, and infertility. In women, the syndrome has variable presentations, but fertility is preserved. Searching the medical literature, we found only one case of prune belly syndrome in pregnant women. Therefore, the patient in this report is the second case. She was primiparous, 25-years-old, with no abdominal muscles, severe congenital kyphoscoliosis, and pulmonary restriction. Elective cesarean section was performed at 37 weeks of gestation due to maternal risk of uterine rupture by transverse presentation and fetal risk of intrauterine growth restriction. The pre-anesthetic approach defined that general anesthesia might have more risks for the patient due to severe maternal lung disease compared to ultrasound-guided locoregional anesthesia. During prenatal care, there were some maternal complications, such as asthma exacerbations, abdominal pain, and constipation. The newborn was born small for gestational age and this can possibly be explained by maternal restrictive lung capacity. The newborn presented with Apgar score 8/9 and tachypnea, but improved after two hours of life.

Is Intraoperative Blood Cell Salvage Effective in Hip Surgery?

Objective The present study aims to evaluate the efficacy of blood cell salvage (CS) as a method of reducing allogeneic blood transfusion in patients submitted to transtrochanteric femoral and hip surgeries due to injury. Methods Prospective cohort of 38 patients from a school hospital submitted to hip or trochanteric surgeries and divided into two groups from August 2015 to February 2017. Patients with any malignancy or infectious condition were excluded from the study. Cell savage group (19 patients) received autologous blood using cell saver, whereas control group (19 patients) received just allogeneic blood, if needed. Red blood cell parameters, blood transfusion requirements, and clinical and surgical characteristics, such as age, gender, ASA scale and type of surgery, were compared both preoperatively and postoperatively. Data was processed in SPSS 20.0. Results There were no differences in the clinical parameters studied (age, gender and ASA scale). Red blood cell parameters on the first day postoperative were higher in the cell savage group ( p < 0.05). No significant reduction of intraoperative and postoperative allogeneic blood transfusion requirements was found. Conclusion This study found that CS was not effective in reducing intraoperative and postoperative allogeneic blood transfusion requirements in patients submitted to transtrochanteric femoral and hip surgery.

Is Intraoperative Blood Cell Salvage Effective in Hip Surgery? / A recuperação intraoperatória de células sanguíneas é eficaz em cirurgias de quadril?

Abstract Objective The present study aims to evaluate the efficacy of blood cell salvage (CS) as a method of reducing allogeneic blood transfusion in patients submitted to transtrochanteric femoral and hip surgeries due to injury. Methods Prospective cohort of 38 patients froma school hospital submitted to hip or trochanteric surgeries and divided into two groups from August 2015 to February 2017. Patients with any malignancy or infectious condition were excluded from the study. Cell savage group (19 patients) received autologous blood using cell saver, whereas control group (19 patients) received just allogeneic blood, if needed. Red blood cell parameters, blood transfusion requirements, and clinical and surgical characteristics, such as age, gender, ASA scale and type of surgery, were compared both preoperatively and postoperatively. Data was processed in SPSS 20.0. Results There were no differences in the clinical parameters studied (age, gender and ASA scale). Red blood cell parameters on the first day postoperative were higher in the cell savage group (p < 0.05). No significant reduction of intraoperative and postoperative allogeneic blood transfusion requirements was found. Conclusion This study found that CS was not effective in reducing intraoperative and postoperative allogeneic blood transfusion requirements in patients submitted to transtrochanteric femoral and hip surgery.

Resumo Objetivo O estudo visa avaliar a eficácia da recuperação intraoperatória de sangue (RIOS) na redução de hemotransfusão alogênica em pacientes submetidos à cirurgia por fratura de fêmur e quadril. Métodos Coorte prospectiva com 38 pacientes submetidos a cirurgia traumatológica para fraturas em quadril e transtrocantéricas de fêmur, divididos em dois grupos em um hospital de ensino de agosto de 2015 a fevereiro de 2017. Pacientes com qualquer enfermidade ou condição infecciosa foram excluídos do presente estudo. O grupo RIOS (19 pacientes) recebeu sangue autólogo com a utilização de Cell Saver, enquanto o grupo controle (19 pacientes) recebeu apenas sangue alogênico, quando necessário.. Grupos comparados em relação ao gênero, idade na cirurgia, escala da Sociedade Americana de Anestesiologistas (ASA) (I, II ou III), uso intraoperatório da RIOS, volume sanguíneo reinfundido pela RIOS, parâmetros hematimétricos pré- e pósoperatórios, volume intra e pós-operatório de sangue alogênico transfundido. Dados processados no software SPSS Statistics for Windows, Versão 20.0 (IBM Corp, Armonk, NY, EUA). Resultados Sem diferenças significativas entre os grupos com as variáveis: idade, gênero e ASA. Percebeu-se que os valores finais de hemoglobina e hematócrito (no 1° dia de pós-operatório) foram mais elevados no grupo que utilizou o dispositivo (p < 0,05). Não houve redução significativa da transfusão alogênica intra e pósoperatória no grupo RIOS em comparação ao controle. Conclusões O presente estudo constatou que a RIOS não foi eficaz em reduzir a transfusão alogênica no intra e pós-operatório de pacientes submetidos à cirurgia de fêmur transtrocantérica e de quadril.

Alpha-lipoic acid in the treatment of psychiatric and neurological disorders: a systematic review.

Despite the existence of many preclinical studies, scientific evidence is lacking on the clinical use of alpha-lipoic acid (ALA) for central nervous system disorders. Therefore, we aimed at revising the literature concerning the use of ALA for the treatment of psychiatric and neurological conditions and to point out what is missing for the introduction of this antioxidant to this purpose. For this systematic review we performed a search using PubMed and SCOPUS databases with the following keywords: "alpha-Lipoic Acid AND central nervous system OR psychiatric disorders OR neurological disorders OR mood disorders OR anxiety OR psychosis OR Alzheimer OR Parkinson OR stroke". The total number of references found after automatically and manually excluding duplicates was 1061. After primary and secondary screening 32 articles were selected. Regarding psychiatric disorders, the studies of ALA in schizophrenia are advanced being ALA administration related to the improvement of schizophrenia symptoms and side effects of antipsychotic medication. In neurological disorders, ALA as a supplement was effective in the prevention of Alzheimer disease progression. For stroke, the use of the supplement ALAnerv® (containing 300 mg ALA) presented important results, since it was observed a reversal of clinical parameters and oxidative imbalance in these patients. For other neurological conditions, such as encephalopathy, multiple sclerosis, traumatic brain injury, mitochondrial disorders and migraine, the results are still preliminary. Overall, there is a need of well-designed clinical trials to enhance the clinical evidences of ALA effects for the treatment of neurological and psychiatric conditions.

Neuroprotective evidence of alpha-lipoic acid and desvenlafaxine on memory deficit in a neuroendocrine model of depression.

Cognitive impairment is present in patients with depression. We hypothesized that alpha-lipoic acid (ALA) can reduce cognitive impairment, especially when combined to antidepressants. Female mice received vehicle or corticosterone (CORT) 20 mg/kg, s.c. for 14 days. From the 15th to 21st day, the animals were divided in groups: vehicle, CORT, CORT+desvenlafaxine (DVS) 10 or 20 mg/kg, ALA 100 or 200 mg/kg, DVS10+ALA100, DVS20+ALA100, DVS10+ALA200, or DVS20+ALA200. Tail suspension (TST), social interaction (SIT), novel object recognition (NOR), and Y-maze tests were conducted. Acetylcholinesterase activity (AChE) was measured in the prefrontal cortex (PFC), hippocampus (HC), and striatum (ST). CORT caused depressive-like behavior, impairment in SIT, and cognitive deficits. Alpha-lipoic acid and DVS, alone or combined, reversed CORT effect on TST. In the NOR, ALA200 alone, DVS10+ALA100, or DVS10+ALA200 reversed the deficits in short-term memory, while DVS20 alone or DVS20+ALA200 reversed the deficits in long-term memory. In the Y-maze test, ALA200 alone, DVS20+ALA100, or DVS20+ALA200 reversed the deficits caused by CORT in the working memory. CORT increased AChE in the PFC, HC, and ST. ALA200 alone or DVS20+ALA200 reversed this effect in the PFC, while DVS20 or DVS20+ALA100 reversed this effect in the HC. In the ST, DVS10 or 20, alone or combined, and ALA100 reversed the effects of CORT. These results suggest that DVS+ALA, by reversing CORT-induced memory and social deficits, seems to be a promising therapy for the treatment of depression and reversal of cognitive impairment observed in this disorder.

Advantages of the Alpha-lipoic Acid Association with Chlorpromazine in a Model of Schizophrenia Induced by Ketamine in Rats: Behavioral and Oxidative Stress evidences.

Schizophrenia is a chronic mental disorder reported to compromise about 1% of the world's population. Although its pathophysiological process is not completely elucidated, evidence showing the presence of an oxidative imbalance has been increasingly highlighted in the literature. Thus, the use of antioxidant substances may be of importance for schizophrenia treatment. The objective of this study was to evaluate the behavioral and oxidative alterations by the combination of chlorpromazine (CP) and alpha-lipoic acid (ALA), a potent antioxidant, in the ketamine (KET) model of schizophrenia in rats. Male Wistar rats (200-300 g) were treated for 10 days with saline, CP or ALA alone or in combination with CP previous to KET and the behavioral (open field, Y-maze and PPI tests) and oxidative tests were performed on the last day of treatment. The results showed that KET induced hyperlocomotion, impaired working memory and decreased PPI. CP alone or in combination with ALA prevented KET-induced behavioral effects. In addition, the administration of KET decreased GSH and increased nitrite, lipid peroxidation and myeloperoxidase activity. CP alone or combined with ALA prevented the oxidative alterations induced by KET. In conclusion, the treatment with KET in rats induced behavioral impairments accompanied by hippocampal oxidative alterations, possibly related to NMDA receptors hypofunction. Besides that, CP alone or combined with ALA prevented these effects, showing a beneficial activity as antipsychotic agents.

The anxiolytic-like effect of 6-styryl-2-pyrone in mice involves GABAergic mechanism of action.

The present work aims to investigate the anxiolytic activity of 6-styryl-2-pyrone (STY), obtained from Aniba panurensis, in behavioral tests and amino acids dosage on male Swiss mice. The animals were treated with STY (1, 10 or 20 mg), diazepam (DZP 1 or 2 mg/kg) or imipramine (IMI 30 mg/kg). Some groups were administered with flumazenil, 30 min before administration of the STYor DZP. The behavioral tests performed were open field, rota rod, elevated plus maze (EPM), hole-board (HB) and tail suspension test (TST). After behavioral tests, these animals were sacrificed and had their prefrontal cortex (PFC), hippocampus (HC) and striatum (ST) dissected for assaying amino acids (aspartate- ASP, glutamate- GLU, glycine- GLY, taurine- TAU and Gamma-aminobutyric acid- GABA). In EPM test, STY or DZP increased the number of entries and the time of permanence in the open arms, but these effects were reverted by flumazenil. In the HB test, STY increased the number of head dips however this effect was blocked by flumazenil. The effects of the STY on amino acid concentration in PFC showed increased GLU, GABA and TAU concentrations. In hippocampus, STY increased the concentrations of all amino acids studied. In striatum, STY administration at lowest dose reduced GLU concentrations, while the highest dosage caused the opposite effect. GLI, TAU and GABA concentrations increased with STY administration at highest doses. In conclusion, this study showed that STY presents an anxiolytic-like effect in behavioral tests that probably is related to GABAergic mechanism of action.

The interplay between ventro striatal BDNF levels and the effects of valproic acid on the acquisition of ethanol-induced conditioned place preference in mice.

Alcohol addiction is a chronic, relapsing and progressive brain disease with serious consequences for health. Compulsive use of alcohol is associated with the capacity to change brain structures involved with the reward pathway, such as ventral striatum. Recent evidence suggests a role of chromatin remodeling in the pathophysiology of alcohol dependence and addictive-like behaviors. In addition, neuroadaptive changes mediated by the brain-derived neurotrophic factor (BDNF) seems to be an interesting pharmacological target for alcoholism treatment. In the present study, we evaluated the effects of the deacetylase inhibitor valproic acid (VPA) (300mg/kg) on the conditioned rewarding effects of ethanol using conditioned place preference (CPP) (15% v/v; 2g/kg). Ethanol rewarding effect was investigated using a biased protocol of CPP. BDNF levels were measured in the ventral striatum. Ethanol administration induced CPP. VPA pretreatment did not reduce ethanol-CPP acquisition. VPA pretreatment increased BDNF levels when compared to ethanol induced-CPP. VPA pretreatment increased BDNF levels even in saline conditioned mice. Taken together, our results indicate a modulatory effect of VPA on the BDNF levels in the ventral striatum. Overall, this study brings initial insights into the involvement of neurotrophic mechanisms in the ventral striatum in ethanol-induced addictive-like behavior.

Involvement of monoaminergic systems in anxiolytic and antidepressive activities of the standardized extract of Cocos nucifera L.

Extracts from the husk fiber of Cocos nucifera are used in folk medicine, but their actions on the central nervous system have not been studied. Here, the anxiolytic and antidepressant effects of the standardized hydroalcoholic extract of C. nucifera husk fiber (HECN) were evaluated. Male Swiss mice were treated with HECN (50, 100, or 200 mg/kg) 60 min before experiments involving the plus maze test, hole-board test, tail suspension test, and forced swimming test (FST). HECN was administered orally (p.o.) in acute and repeated-dose treatments. The forced swimming test was performed with dopaminergic and noradrenergic antagonists, as well as a serotonin release inhibitor. Administration of HECN in the FST after intraperitoneal (i.p.) pretreatment of mice with sulpiride (50 mg/kg), prazosin (1 mg/kg), or p-chlorophenylalanine (PCPA, 100 mg/kg) caused the actions of these three agents to be reversed. However, this effect was not observed after pretreating the animals with SCH23390 (15 µg/kg, i.p.) or yohimbine (1 mg/kg, i.p.) The dose chosen for HECN was 100 mg/kg, p.o., which increased the number of entries as well as the permanence in the open arms of the maze after acute and repeated doses. In both the forced swimming and the tail suspension tests, the same dose decreased the time spent immobile but did not disturb locomotor activity in an open-field test. The anxiolytic effect of HECN appears to be related to the GABAergic system, while its antidepressant effect depends upon its interaction with the serotoninergic, noradrenergic (α1 receptors), and dopaminergic (D2 dopamine receptors) systems.

Electroencephalographic study of chlorpromazine alone or combined with alpha-lipoic acid in a model of schizophrenia induced by ketamine in rats.

Schizophrenia is characterized by behavioral symptoms, brain function impairments and electroencephalographic (EEG) changes. Dysregulation of immune responses and oxidative imbalance underpins this mental disorder. The present study aimed to investigate the effects of the typical antipsychotic chlorpromazine (CP) alone or combined with the natural antioxidant alpha-lipoic acid (ALA) on changes in the hippocampal average spectral power induced by ketamine (KET). Three days after stereotactic implantation of electrodes, male Wistar rats were divided into groups treated for 10 days with saline (control) or KET (10 mg/kg, IP). CP (1 or 5 mg/kg, IP) alone or combined with ALA (100 mg/kg, P.O.) was administered 30 min before KET or saline. Hippocampal EEG recordings were taken on the 1st, 5th and 10th days of treatment immediately after the last drug administration. KET significantly increased average spectral power of delta and gamma-high bands on the 5th and 10th days of treatment when compared to control. Gamma low-band significantly increased on the 1st, 5th and 10th days when compared to control group. This effect of KET was prevented by CP alone or combined with ALA. Indeed, the combination of ALA 100 + CP1 potentiated the inhibitory effects of CP1 on gamma low-band oscillations. In conclusion, our results showed that KET presents excitatory and time-dependent effects on hippocampal EEG bands activity. KET excitatory effects on EEG were prevented by CP alone and in some situations potentiated by its combination with ALA.

Complicações da sífilis congênita: uma revisão de literatura / Complications of congenital syphilis: a review of the literature

A sífilis congênita ocorre após infecção transplacentária, através do agente Treponema pallidum. As consequências da ausência do tratamento do recém-nascido podem acarretar sequelas irreversíveis, como surdez, cegueira e retardo mental. O estudo teve como objetivo realizar uma revisão bibliográfica atualizada sobre as complicações da sífilis congênita. Trata-se de estudo descritivo e bibliográfico. A coleta de dados foi realizada através de levantamento bibliográfico nas bases de dados LILACS, MEDLINE e SciELO, no período de março a junho de 2012, usando os descritores: sífilis congênita, complicações, recém-nascido e enfermagem. A seleção dos artigos foi realizada através da leitura do resumo relacionado com sífilis congênita, sífilis congênita e complicação, sífilis congênita e tratamento, sífilis. Resultados mostram que a contaminação do feto se dá devido à falha no pré-natal.

Behavioral and neurochemical effects of alpha-lipoic Acid in the model of Parkinson's disease induced by unilateral stereotaxic injection of 6-ohda in rat.

This study aimed to investigate behavioral and neurochemical effects of α -lipoic acid (100 mg/kg or 200 mg/kg) alone or associated with L-DOPA using an animal model of Parkinson's disease induced by stereotaxic injection of 6-hydroxydopamine (6-OHDA) in rat striatum. Motor behavior was assessed by monitoring body rotations induced by apomorphine, open field test and cylinder test. Oxidative stress was accessed by determination of lipid peroxidation using the TBARS method, concentration of nitrite and evaluation of catalase activity. α -Lipoic acid decreased body rotations induced by apomorphine, as well as caused an improvement in motor performance by increasing locomotor activity in the open field test and use of contralateral paw (in the opposite side of the lesion produced by 6-OHDA) at cylinder test. α -lipoic acid showed antioxidant effects, decreasing lipid peroxidation and nitrite levels and interacting with antioxidant system by decreasing of endogenous catalase activity. Therefore, α -lipoic acid prevented the damage induced by 6-OHDA or by chronic use of L-DOPA in dopaminergic neurons, suggesting that α -lipoic could be a new therapeutic target for Parkinson's disease prevention and treatment.

Antidepressant effect of aminophylline after ethanol exposure.

This work investigated the association of acute ethanol and aminophylline administration on behavioral models of depression and prefrontal monoamine levels (i.e. norepinephrine and dopamine) in mice. The animals received a single dose of ethanol (2 g/kg) or aminophylline (5 or 10 mg/kg) alone or in association. Thirty minutes after the last drug administration, the animals were assessed in behavioral models by the forced swimming and tail suspension tests. After these tests, the animals were sacrificed and the prefrontal cortices dissected to measure monoamine content. Results showed that ethanol presented depression-like activity in the forced swimming and tail suspension tests. These effects were reversed by the association with aminophylline in all tests. Norepinephrine and dopamine levels decreased, while an increase in the dopamine metabolite, (4-hydroxy-3-methoxyphenyl)acetic acid (DOPAC), after ethanol administration was observed. On the contrary, the association of ethanol and aminophylline increased the norepinephrine and dopamine content, while it decreased DOPAC when compared to the ethanol group, confirming the alterations observed in the behavioral tests. These data reinforce the involvement of the adenosinergic system on ethanol effects, highlighting the importance of the norepinephrine and dopamine pathways in the prefrontal cortex to the effects of ethanol.

Aminophylline (a theophylline-ethylenediamine complex) blocks ethanol behavioral effects in mice.

Aminophylline is a complex of theophylline-ethylenediamine, where theophylline is the main component. Theophylline is a methyxanthine and besides inhibiting phosphodiesterase enzymes, it is also a nonselective adenosine antagonist. Several reports suggested the involvement of the brain adenosinergic system in the ethanol-induced motor incoordination. Thus, the objective of this work was to study the effects of the interaction of ethanol with aminophylline as assessed by behavioral tests in mice. Eight groups of male Swiss mice were used. The animals were treated with either distilled water (control) or ethanol (E; 2, 4, and 6 g/kg, orally) for 5 days, or with distilled water for 4 days, and on the fifth day with aminophylline (A; 5 and 10 mg/kg, intraperitoneally). In the association groups (association protocols), the animals were treated with ethanol (E; 6 g/kg, orally) for 4 days, and on the fifth day received aminophylline (A; 10 mg/kg, intraperitoneally), 30 min after the last ethanol administration (first protocol, E/A). In the second association protocol (A/E), ethanol was administered for 4 days, and on the fifth day the animals received aminophylline (A; 10 mg/kg, intraperitoneally), followed again by ethanol (E; 6 g/kg, orally) administration, 30 min later. E (6 g/kg) evoked a central nervous system depressor effect, by decreasing both the locomotor activity and rearing in the open field test, and A (5 and 10 mg/kg) showed opposite effects. However, the E/A or A/E associations blocked the ethanol effect. In the rota rod test, ethanol presented a muscular relaxant effect, which was decreased in both association protocols. In the tail suspension test, while the E/A association decreased immobility, A/E association increased it, as compared with controls. In conclusion, the effects of ethanol were inhibited by its association with aminophylline, suggesting that ethanol acts on the adenosine neurotransmission.

Central action of Araucaria angustifolia seed lectin in mice.

Possible central nervous system effects of the gymnosperm lectin from Araucaria angustifolia seeds were studied in seizure and open field tests. Male Swiss mice were administered saline (control), lectin (0.1, 1, and 10 mg/kg), flumazenil (1 mg/kg), or diazepam (1 mg/kg) intraperitoneally. Lectin at the highest dose increased time to death in the pentylenetetrazole- and strychnine-induced seizure models as compared with control, but not in the pilocarpine model. In the open field test, lectin reduced locomotor activity at all doses tested, as did diazepam, when compared with control. These locomotor effects were reversed by flumazenil pretreatment. In conclusion, A. angustifolia lectin had a protective effect in the pentylenetetrazole- and strychnine-induced seizure models, suggestive of activity in the GABAergic and glycinergic systems, respectively, and also caused a reduction in animal movements, which was reversed by flumazenil, pointing to a depressant action mediated by a GABAergic mechanism.

Coumarin effects on amino acid levels in mice prefrontal cortex and hippocampus.

Coumarin is a compound known to be present in a wide variety of plants, microorganisms and animal species. Most of its effects were studied in organs and systems other than the central nervous system. The present work evaluated the effect of coumarin administration on the levels of gamma-aminobutyric acid (GABA), glutamate (GLU), glycine (GLY) and taurine (TAU) in the prefrontal cortex and hippocampus of mice. Male Swiss mice were treated with distilled water (controls), coumarin (20 or 40 mg/kg, i.p.) or diazepam (1 mg/kg, i.p.). Results showed that in the prefrontal cortex, coumarin at the lowest dose increased the levels of GLU and TAU, while GABA increased with both doses studied and GLY had its levels increased only at the dose of 40 mg/kg. Diazepam (DZP) increased the levels of GABA and TAU and decreased the levels of GLU and GLY in this area. In the hippocampus, only glutamate had its levels decreased after coumarin treatment, while diazepam increased the levels of GABA and TAU and decreased the levels of GLU in this brain region. We concluded that coumarin stimulates the release of endogenous amino acids, increasing the levels of inhibitory and excitatory amino acids in the prefrontal cortex, and decreasing glutamate levels in the hippocampus. Together, these results are of interest, considering that some neurodegenerative diseases and seizures are related to the imbalance of the amino acid levels in the CNS suggesting a perspective of a therapeutic use of coumarins in these disorders.

Efeitos farmacológicos do telocinobufagin, um bufadienolídeo oriundo das glândulas parotóides do Bufo paracnemis: estudo comparativo com o anestésico local bupivacaína / Pharmacological effects of telocinobufagin a bufadienolídeo arising from parotóides glands of Bufo paracnemis: a comparative study with the local anesthetic bupivacaine

Foram avaliados os efeitos do bufadienolídeo telocinobufagin (TCB), obtido das glândulas parotóides do Bufo paracnemis por cromatografia líquida de alta eficiência, comparando-os com os do anestésico local bupivacaína (BUPI). TCB (10-8 a 6x10-4 M) inibiu, de modo concentração-dependente, as contrações induzidas por estimulação por campo elétrico (ECE) em íleo isolado de cobaio, cujo valor foi 0,9+-0,9 % da resposta controle, na concentração de 6x10-4 M. Da mesma foram, TCB, (10-6 a 10-4) inibiu, as contrações induzidas pela ACh. BUPI (10-7 - 10-3 M) inibiu, de modo concentração-dependente, tanto as contrações induzidas por ECE quanto as induzidas por ACh. Em nervo ciático isolado de rato, a amplitude pico-a-pico (APP) do potencial de ação composto (PAC) caiu para 64,9+-7,2 e 12,9+-4,4 % do controle, após 15 e 30 min com 1 mM TCB, respectivamente, retornando para 83,2+-17,5 % lavando-se o nervo com Locke por 45 min. Nas mesmas condições, a velocidade de condução (VC) do PAC caiu para 15,0+-15,0 % do controle, após 30 min; sendo recuperada para 78,7%+-7,2% % após 45 min da retirada do TCB. BUPI (1mM) diminuiu tanto a APP do PAC para 46,7+-14,4 % e 11,8+-6,5 % do controle, após 15 e 30 min, respectivamente, quanto a VC para 17,4+-11,2 % do controle, após 30 min; após 45 min da lavagem reverteu parcialmente a APP e a VC para 29,7+-8,3 e 44,8+-14,5 % da obtida no controle, respectivamente. Em átrio isolado de rato, TCB (10-6 a 10-4 M) não alterou o inotropismo espontâneo, o que foi reduzido pela BUPI (10-4 M). Portanto, TCB possui propriedades anestésicas locais reversíveis semelhantes a BUPI, sem apresentar, no entanto, sinais de toxicidade cardíaca in vitro, abrindo perspectivas para busca de novas moléculas com ação anestésica local com potencial interesse terapêutico...