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Relaxamento do corpo cavernoso de coelho induzido pela fraÃÃo alcaloidal F3-5 de Aspidosperma ulei Markgr / Relaxation on of rabbit corpus cavernosum induced by the alkaloidal fraction F3-S from - Aspdidosperma ulei MarkgrFrancisco de Assis Mendes Goes JÃnior 30 May 2007 (has links)
CoordenaÃÃo de AperfeiÃoamento de NÃvel Superior / Erectile dysfunction is a worldwide public health issue and, in spite of advances brougth by the utilization of type-5 phosphodiesterase inhibitors, there is still much interest in new treatment alternatives, especially when derived from natural products. Some investigators observed the pro-erectile effects of an alkaloidal-rich fraction from Aspidosperma ulei Markgr., named F3-5. In this study, it was evaluated the degree of relaxation induced by F3-5 on rabbit corpus cavernosum, as well as possible Pharmacological mechanisms involved, in vitro. Several experimental assays were performed, utilizing the methods of cascade tissue superfusion and isolated tissue bath. WÃth strips ot corpus cavernosum pre-contracted with phenilephrine (5ÂM), dose-response curves of relaxation for F3-5 papaverine and DMSO were produced. were There were also assays fo, evaluation of the effects of L-NAME, 7-NI, 000, propranolol, atropine, sildenafil and F3-5 on the relaxations mediated by sodium litroprusside, acetylcholine, isoproterenol, sildenafil and F3-S. With depolarized preparations of corpus cavernosum, in a calcium-free, potassium-rich (60 mM) medium, the effects of F3-S and DMSO on the contractions induced by the progressive increase in Ca2+ concentration (1 - 300 mM) were observed. F3-5 was capable of inducing complete relaxation of rabbit corpus cavernosum with magnitude similar to that of papaverine for all doses tested, except 3 mg, when Ãt presented a significantly higher relaxation. Superfusions of L-NAME, 7-NI and ODQ did not significantly inhibit the relaxatÃons provoked by F3-5, suggesting that it acts independently of the nitrergià pathway. Propranolol and atropine also did not significantly interfere with relaxations mediated by F3-5 indicating that B-adrenergic or rnuscarinic receptors also might not be involved. F3-5 did not significantly amplify the relaxations promoted by sodium nitroprusside or acetylcholine, as opposed to sildenafil, suggesting that it does not act through inhibition of type-5 ohosphodiesterase. Finally, in cavernous tissue pre-incubated with F3-5, the minimum dose of Ca2+ necessary for muscular contraction was thirty times superior to that utilizedon the tissue without previous treatment, or treated with OMSO. This inhibition of the contractions of corpus cavernosum mediated by Ca2+ suggests, therefore, that F3-S can act through blockade of voltage-dependent calcium channels. / A disfunÃÃo erÃtil à um problema mundial de saÃde pÃblica e, apesar dos avanÃos trazidos pela utilizaÃÃo dos inibidores da fosfodiesterase tipo-5, ainda hà muito interesse em novas alternativas de tratamento, especialmente quando derivadas de produtos naturais. Alguns pesquisadores observaram os efeitos prÃ-erÃteis de uma fraÃÃo rica em alcalÃides de Aspidosperma ulei Markgr., denominada F3-5. Neste estudo, foi avaliado o grau de relaxamento induzido por F3-5 no corpo cavernoso de coelho, bem como possÃveis mecanismos farmacolÃgicos envolvidos, in vitro. Foram realizados diversos ensaios experimentais, utilizando-se os mÃtodos de superfusÃo de tecido em cascata e de banho isolado de tecido. Com tiras de corpo cavernoso prÃ-contraÃdas com fenilefrina (5 μM), foram produzidas curvas de dose-resposta de relaxamento para F3-5, papaverina e DMSO. TambÃm foram realizados ensaios para avaliaÃÃo dos efeitos de L-NAME, 7-NI, ODQ, propranolol, atropina, sildenafil e F3-5 sobre os relaxamentos mediados por nitroprussiato de sÃdio, acetilcolina, isoproterenol, sildenafil e F3-5. Com preparaÃÃes de corpo cavernoso despolarizadas, em um meio livre de cÃlcio e rico em potÃssio (60 mM), os efeitos de F3-5 e DMSO sobre as contraÃÃes induzidas pelo aumento progressivo na concentraÃÃo de Ca2+ (1 â 300 mM) foram observados. F3-5 foi capaz de induzir o relaxamento completo do corpo cavernoso de coelho, com magnitude similar à da papaverina para todas as doses testadas, exceto 3 mg, quando apresentou relaxamento significantemente maior. As superfusÃes de L-NAME, 7-NI e ODQ nÃo inibiram significantemente os relaxamentos provocados por F3-5, sugerindo que este age independentemente da via nitrÃrgica. Propranolol e atropina tambÃm nÃo interferiram significantemente com os relaxamentos mediados por F3-5, indicando que receptores β-adrenÃrgicos ou muscarÃnicos tambÃm nÃo devem estar envolvidos. F3-5 nÃo amplificou significantemente os relaxamentos promovidos por nitroprussiato de sÃdio ou acetilcolina, ao contrÃrio de sildenafil, sugerindo que nÃo age por inibiÃÃo da fosfodiesterase tipo-5. Finalmente, em tecido cavernoso prÃ-incubado com F3-5, a dose mÃnima de Ca2+ necessÃria para contraÃÃo muscular foi trinta vezes superior Ãquela utilizada em tecido sem tratamento prÃvio ou tratado com DMSO. Esta inibiÃÃo das contraÃÃes de corpo cavernoso mediadas pelo Ca2+ sugere, portanto, que F3-5 pode atuar atravÃs do bloqueio de canais de cÃlcio voltagem-dependente.
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Clinical toxicology and genotoxicity evaluation of the phytomedicine Tamaril (Capsule) on healthy vounteers / Estudo de toxicologia clÃnica e genotoxicidade do fitoterÃpico tamaril cÃpsula, em voluntÃrios sadiosMarne Carvalho de Vasconcellos 09 July 2004 (has links)
Conselho Nacional de Desenvolvimento CientÃfico e TecnolÃgico / CoordenaÃÃo de AperfeiÃoamento de Pessoal de NÃvel Superior / Tamaril is a phytomedicine constituded of 5 medicinal plants well known for their laxative proprieties: Cassia fistula (soft extract), Cassia angustifolia (Senna), Coriandrum sativum L. e Glycyrrhiza glabra L. (AlcaÃuz) and Tamarindus indicus L. (soft extract). Every medication to be launched on the market must succeed in a series of research steps, where clinical toxicology evaluation is an important one among them. Genotoxic assessment, which aims on the processes altering DNA integrity, is a relatively recent field in drug development and stands on the interface between toxicology and genetics. This study consisted on the evaluation of clinical safety and genotoxic potential of Tamaril capsules in healthy volunteers. The clinical evaluation consisted of an open study with 25 healthy volunteers of both sexes (13 males and 12 females) who received a daily oral dose of two capsules Tamaril for 28 consecutive days. The volunteers were selected for the study if considered in good health after criterious clinical, physical and laboratorial evaluations. At the end of the 28 study days, blood samples (5 mL) were collected from each volunteer for the genotoxic assessment of Tamaril on peripheral lymphocytes through the comet assay. The mean age of the volunteers was of 30.1 6.9 years and the body mass index was of 24.21Â3.00 Kg/cm2 on the pre-study evaluation and 24.26Â3.05 Kg/cm2 on the post-study. Hematological, hepatic, renal and metabolic functions, as well as sodium and potassium did not show signs of abnormality in any volunteer throughout the weeks of the study. Soften faces, abdominal pain and flatulence were the adverse events regularly observed. Through the comet assay, score 1 DNA damage was most frequently registered on peripheral lymphocytes of volunteers treated with Tamaril (p<0.05). Clinical and genotoxic evaluation of healthy volunteers receiving Tamaril for 28 uninterrupted days did not show signs of toxicity related to the treatment. / O Tamaril à um fitoterÃpico composto de cinco plantas medicinais: Cassia fistula (extrato mole), Cassia angustifolia (Sene), Coriandrum sativum L., Glycyrrhiza glabra L. (AlcaÃuz), e Tamarindus indicus L. (extrato mole); todas com conhecida aÃÃo laxativa. Todo medicamento que vai ser registrado pela AgÃncia Nacional de VigilÃncia SanitÃria (Anvisa), passa por diversas etapas de pesquisa sendo uma delas a toxicologia clÃnica. A genotoxicidade à uma especialidade relativamente recente, e se situa na interface entre a toxicologia e a genÃtica. Esta visa o estudo dos processos que alteram o DNA (Ãcido desoxirribonuclÃico). O objetivo desse estudo foi avaliar a seguranÃa e o potencial genotÃxico da formulaÃÃo de Tamaril cÃpsulas em voluntÃrios saudÃveis. O ensaio clÃnico consistiu de um estudo aberto com 25 voluntÃrios de ambos os sexos, (13 homens e 12 mulheres), que receberam diariamente duas cÃpsulas de Tamaril v.o. por 28 dias ininterruptos. Os voluntÃrios foram incluÃdos no estudo apÃs avaliaÃÃo clÃnica, exames fÃsicos e laboratoriais. Ao final de 28 dias, amostras de sangue (5mL) foram coletadas de cada voluntÃrio, para avaliar o efeito genotÃxico do Tamaril em linfÃcitos perifÃricos humanos atravÃs do teste do cometa. A idade mÃdia dos voluntÃrios foi de 30,1  6,9 anos e o Ãndice de massa corpÃrea foi de 24,21  3,00 Kg/ cm2 no prÃ-estudo e 24,26  3,05 Kg/ cm2 no pÃs-estudo. As funÃÃes hematolÃgica, hepÃtica, renal e metabÃlica, bem como os eletrÃlitos sÃdio e potÃssio foram analisados semanalmente atravÃs dos exames laboratoriais, os quais nÃo evidenciaram sinal de toxicidade, estando todos os resultados dentro da faixa de normalidade. Fezes pastosas, dor abdominal e flatulÃncia foram os eventos adversos mais observados. Pelo teste do cometa, foram observados danos tipo 1 (p<0,05) nos linfÃcitos perifÃricos dos voluntÃrios tratados com TamarilÂ. Os estudos de Toxicologia ClÃnica e genotoxicidade nÃo evidenciaram nenhuma toxicidade nos voluntÃrios tratados com Tamaril por 28 dias ininterruptos 2 cÃpsulas por dia v.o.
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Aspectos morfolÃgicos e morfomÃtricos da cicatrizaÃÃo da anastomose colÃnica, em ratos, sob aÃÃo de enema de aroeira-do-sertÃo a 10% (Myracrodruon urundeuva Fr. All.) / Morphological and morphometric analysis of colonic anastomosis healing, in rats, under action of 10% aroeira-do-sertÃo enema (Myracrodruon urundeuva Fr. All.)Annya Costa AraÃjo de MacÃdo Goes 26 August 2005 (has links)
FundaÃÃo de Amparo à Pesquisa do Estado do Cearà / Os procedimentos cirÃrgicos para tratamento das doenÃas dos cÃlons sÃo comuns
na prÃtica mÃdica. As deiscÃncias de anastomoses colÃnicas podem determinar considerÃveis morbidade e mortalidade. A cicatrizaÃÃo destas anastomoses à um
processo complexo, e vÃrios fatores podem modificar sua evoluÃÃo. Os antiinflamatÃrios tÃm interessado aos pesquisadores, pelo potencial de interferir nas fases de inflamaÃÃo e fibroplasia do processo cicatricial. A aroeira-do-sertÃo (Myracrodruon urundeuva Fr. All.) Ã uma planta usada popularmente como antiinflamatÃrio e promotor da cicatrizaÃÃo, em vÃrias afecÃÃes. Neste estudo, o objetivo foi avaliar a aÃÃo do extrato aquoso da aroeira-do-sertÃo a 10%, sob a forma de enemas, na anastomose colÃnica, em ratos. Foram utilizados 48 ratos da
linhagem Wistar, machos, com peso mÃdio 320 g, distribuÃdos em dois grupos, com 24 animais, cada. Todos os animais foram submetidos à laparotomia, com secÃÃo transversa completa do cÃlon descendente, seguida de anastomose colÃnica. Os ratos do grupo A receberam diariamente, no pÃs-operatÃrio, enemas de veÃculo à base de carboximetilcelulose (CMC), atà a data da eutanÃsia. Os animais do grupo B receberam diariamente, no pÃs-operatÃrio, enemas de extrato aquoso de aroeira-do sertÃo a 10% em veÃculo à base de CMC. Nas datas 3, 7, 14 e 21 do experimento, seis ratos de cada grupo foram submetidos à remoÃÃo de segmento colÃnico, incluindo a anastomose, destinado à apreciaÃÃo histolÃgica e anÃlise qualitativa e quantitativa da resposta celular inflamatÃria e cicatricial. A evoluÃÃo morfolÃgica do processo cicatricial foi significantemente menor no grupo aroeira que no grupo controle, no dia 7 do experimento (ρ < 0,05). Na avaliaÃÃo morfomÃtrica, verificou-se menor migraÃÃo neutrofÃlica, nos dias 7 e 21, e mais angiogÃnese e fibrogÃnese, no dia 14, no grupo aroeira (ρ < 0,05). TambÃm houve menor deposiÃÃo do colÃgeno, nos dias 3, 7 e 14 do experimento, no grupo aroeira (ρ < 0,05). Conclui-se, portanto, que a aroeira à eficaz como antiinflamatÃrio, pois diminui a intensidade da resposta inflamatÃria aguda inicial (dia 7), durante a cicatrizaÃÃo das anastomoses colÃnicas. Contudo, apesar de demonstrar aÃÃo angiogÃnica e fibrogÃnica (dia 14), hà retardo na deposiÃÃo de colÃgeno (dias 3, 7 e 14), no grupo aroeira. Mais tardiamente (dia 21), entretanto, a aroeira nÃo causa alteraÃÃes histolÃgicas no processo cicatricial / The surgical procedures for treatment of colonic diseases are common in medical
practice. Colonic anastomoses dehiscences can determine considerable morbidity
and mortality. The healing of these anastomoses is a complex process, and several factors can modify its evolution. Anti-inflammatories have interested researchers, for the potential to interfere on the phases of inflammation and fibroplasia of the healing process. The aroeira-do-sertÃo (Myracrodruon urundeuva Fr. All.) is a plant popularly used as an anti-inflammatory and promoter of healing, in several affections. In this study, the purpose was to evaluate the action of the 10% aqueous extract of aroeirado- sertÃo, under the form of enemas, on colonic anastomosis, in rats. There were utilized 48 Wistar rats, males, with average weight 320 g, distributed in two groups, with 24 animals, each. All animals were subjected to laparotomy, with complete transverse section of the descending colon, followed by colonic anastomosis. The rats on group A received daily, post-operative, enemas of carboxymethylcellulose (CMC) based vehicle, until the date of euthanasia. The animals on group B received daily, post-operative, enemas of 10% aqueous extract of aroeira-do-sertÃo in CMC based vehicle. On dates 3, 7, 14 and 21 of the experiment, six rats in each group were subjected to removal of a colonic segment, including the colonic anastomosis, destined to histological appreciation and qualitative and quantitative analysis of inflammatory and healing cell response. The morphological evolution of the healing process was significantly lower on the group aroeira than on the group control, on day 7 of the experiment (ρ < 0,05). On the morphometric evaluation, it was verified less neutrophilic migration, on days 7 and 21, and more angiogenesis and fibrogenesis, on day 14, on the group aroeira (ρ < 0,05). There was also less deposition of collagen, on days 3, 7 and 14 of the experiment, on the group aroeira (ρ < 0,05). It is concluded, therefore, that aroeira is efficient as an anti-inflammatory, because it diminishes the intensity of the initial (day 7) acute inflammatory response, during the healing of colonic anastomoses. However, in spite of showing angiogenic and fibrogenic action (day 14), there is delay on collagen deposition (days 3, 7 and 14), on the group aroeira. Later on (day 21), however, aroeira does not cause histological alterations on the healing process
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Estudo comparativo, randomizado para avaliar a eficÃcia terapÃutica da Mentha crispa e do secnidazol no tratamento da tricomonÃase / Trichomoniasis is a non-viral sexually transmitted disease most common in the world. The current treatment of this disease includes the use of several drugs, including herbal remedies formulated with Mentha crispa have also been used as protozoan The aim of this study was to evaluate the efficacy and safety of herbal medicine containing Mentha crispa in patients with vaginal trichomoniasis. The study was a randomized clinical trial, parallel and opened. It included 60 female volunteers, 35 from Fortaleza - Ceara and 25 from Sinop - Mato Grosso, who had stool examination of vaginal discharge positive for trichomoniasis. Patients were randomly distributed in two treatment groups, the Mentha crispa group and the Secnidazole group. Both groups were composed of 30 volunteers, in which, respectively, 2 tablets of 12 mg of herbal Giamebil and 2 tablets 1000mg Secnidal  were orally administered in single dose. The clinical trial consisted of three steps: pretreatment, treatment and post-treatment. To significance level of 5%, no difference was found between the groups (P = 0.6120), because the proportion of volunteers with no T.vaginalis in the Secnidazole group was 96.67% and the proportion found in the Mentha crispa group was 90.00%. Secondary endpoints for the evaluation of the effectiveness of Mentha crispa in the treatment of trichomoniasis were the improvement of clinical complaints: vaginal discharge, unpleasant odor, genital burning, dysuria, dyspareunia, pelvic pain and itching. It has not been demonstrated statistically significant difference (P = 0 , 4583) between the treatments in the proportion of patients who reported no such complaints. The drugs were considered well tolerated, as no voluntary needed additional pharmacological intervention in order to control or eradicate such discomfort. Therefore, adverse events were assessed as being mild, manifesting itself only once and having spontaneous remission. However, adverse effects were significantly higher (P = 0.0006) in the Secnidazole group (66.67%) than those found in the Mentha crispa group (20.00%). Adverse events reported by volunteers Secnidazole group were nausea (16.67%), the unpleasant odor in the urine (3.33%) and metallic taste, that was cited by 50% of patients and it showed a statistically significant difference between the treatment groups (P <0.001). The referred events by the volunteers of the Mentha crispa group were: epigastric pain, nausea, vomiting and headache reported by 3.33%, while unpleasant taste was mentioned by 6.67%. No signs of clinical toxicity was observed during treatment. This trial concluded that the herbal medicine containing Mentha crispa showed efficacy and safety when used orally at a dose of 24mg, presenting itself as an alternative therapy safe, effective, accessible and with quality for treatment in patients with trichomoniasis.PacÃfica Pinheiro Cavalcanti 25 January 2010 (has links)
CoordenaÃÃo de AperfeiÃoamento de Pessoal de NÃvel Superior / TricomonÃase à a doenÃa sexualmente transmissÃvel nÃo-viral mais comum no mundo. O tratamento atual dessa patologia compreende o uso de vÃrios fÃrmacos, inclusive fitoterÃpicos formulados com Mentha crispa tambÃm tÃm sido empregados como antiprotozoÃrios. O objetivo desse estudo foi avaliar a eficÃcia terapÃutica e a seguranÃa do fitoterÃpico contendo Mentha crispa (GiamebilÂ) em pacientes com tricomonÃase vaginal. O estudo realizado foi um ensaio clÃnico do tipo randomizado, paralelo e aberto com 60 voluntÃrias do sexo feminino, sendo 35 procedentes de Fortaleza/Cearà e 25 da cidade de Sinop/Mato Grosso, que apresentaram exame parasitolÃgico positivo da secreÃÃo vaginal para tricomonÃase. As pacientes foram distribuÃdas aleatoriamente em dois grupos de tratamento, o grupo Mentha crispa e o grupo Secnidazol, ambos compostos de 30 voluntÃrias, os quais foram administrados por via oral, respectivamente, 2 comprimidos de 12 mg de Giamebil e 2 comprimidos de 1000 mg de SecnidalÂ, em dose Ãnica. O ensaio clÃnico foi constituÃdo de trÃs etapas: prÃ-tratamento, tratamento e pÃs-tratamento. Ao nÃvel de significÃncia de 5%, nÃo se constatou diferenÃa estatÃstica entre os grupos (P=0,6120), pois a proporÃÃo de voluntÃrias com ausÃncia de T.vaginalis no grupo Secnidazol foi de 96,67% e a verificada no grupo Mentha crispa foi de 90,00%. Os desfechos secundÃrios para a avaliaÃÃo da eficÃcia da Mentha crispa no tratamento da tricomonÃase foram a melhora das queixas clÃnicas: corrimento vaginal, odor desagradÃvel, ardor genital, disÃria, dispareunia, prurido e dor pÃlvica. NÃo foi demonstrada diferenÃa estatisticamente significante (P=0,4583) entre os tratamentos em relaÃÃo à proporÃÃo de pacientes que relataram ausÃncia dessas queixas. Os medicamentos foram considerados bem tolerados, pois nenhuma voluntÃria necessitou intervenÃÃo farmacolÃgica adicional no intuito de controlar ou debelar tal desconforto. Portanto, os eventos adversos foram avaliados como sendo de intensidade leve, manifestando-se uma Ãnica vez e com remissÃo espontÃnea. Entretanto, os efeitos adversos foram significativamente maiores (P = 0,0006) no grupo Secnidazol (66,67%) do que os verificados no grupo Mentha crispa (20,00%). Os eventos adversos relatados pelas voluntÃrias do grupo Secnidazol foram: nÃusea (16,67%), odor desagradÃvel na urina (3,33%) e gosto metÃlico, sendo que esse citado por 50% das pacientes evidenciou diferenÃa estatisticamente significante entre os grupos de tratamento (P <0,001). Os eventos referidos pelas voluntÃrias do grupo Mentha crispa foram: epigastralgia, nÃusea, vÃmito e cefalÃia referidos por 3,33%, enquanto gosto desagradÃvel foi mencionado por 6,67%. Nenhum sinal de toxicidade clÃnica foi observado no perÃodo de tratamento. O presente ensaio clÃnico concluiu que o fitoterÃpico contendo Mentha crispa apresentou eficÃcia terapÃutica e seguranÃa quando empregado por via oral na dose Ãnica de 24mg, apresentando-se como uma alternativa terapÃutica segura, eficaz, acessÃvel e de qualidade para o tratatamento de pacientes com tricomonÃase. / Trichomoniasis is a non-viral sexually transmitted disease most common in the world. The current treatment of this disease includes the use of several drugs, including herbal remedies formulated with Mentha crispa have also been used as protozoan The aim of this study was to evaluate the efficacy and safety of herbal medicine containing Mentha crispa in patients with vaginal trichomoniasis. The study was a randomized clinical trial, parallel and opened. It included 60 female volunteers, 35 from Fortaleza - Ceara and 25 from Sinop - Mato Grosso, who had stool examination of vaginal discharge positive for trichomoniasis. Patients were randomly distributed in two treatment groups, the Mentha crispa group and the Secnidazole group. Both groups were composed of 30 volunteers, in which, respectively, 2 tablets of 12 mg of herbal Giamebil and 2 tablets 1000mg Secnidal  were orally administered in single dose. The clinical trial consisted of three steps: pretreatment, treatment and post-treatment. To significance level of 5%, no difference was found between the groups (P = 0.6120), because the proportion of volunteers with no T.vaginalis in the Secnidazole group was 96.67% and the proportion found in the Mentha crispa group was 90.00%. Secondary endpoints for the evaluation of the effectiveness of Mentha crispa in the treatment of trichomoniasis were the improvement of clinical complaints: vaginal discharge, unpleasant odor, genital burning, dysuria, dyspareunia, pelvic pain and itching. It has not been demonstrated statistically significant difference (P = 0 , 4583) between the treatments in the proportion of patients who reported no such complaints. The drugs were considered well tolerated, as no voluntary needed additional pharmacological intervention in order to control or eradicate such discomfort. Therefore, adverse events were assessed as being mild, manifesting itself only once and having spontaneous remission. However, adverse effects were significantly higher (P = 0.0006) in the Secnidazole group (66.67%) than those found in the Mentha crispa group (20.00%). Adverse events reported by volunteers Secnidazole group were nausea (16.67%), the unpleasant odor in the urine (3.33%) and metallic taste, that was cited by 50% of patients and it showed a statistically significant difference between the treatment groups (P <0.001). The referred events by the volunteers of the Mentha crispa group were: epigastric pain, nausea, vomiting and headache reported by 3.33%, while unpleasant taste was mentioned by 6.67%. No signs of clinical toxicity was observed during treatment. This trial concluded that the herbal medicine containing Mentha crispa showed efficacy and safety when used orally at a dose of 24mg, presenting itself as an alternative therapy safe, effective, accessible and with quality for treatment in patients with trichomoniasis.
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AvaliaÃÃo da atividade antiinflamatÃria e antioxidante das cÃpsulas do extrato seco e da afrormosina, isoflavonÃide, obtidos de Amburana cearensis A C Smith. / Evaluation of anti-inflammatory and antioxidant activity of capsules of dried extract and afrormosin, isoflavonoid, obtained from Amburana cearensis AC Smith.Amanda de AraÃjo Lopes 29 November 2010 (has links)
CoordenaÃÃo de AperfeiÃoamento de Pessoal de NÃvel Superior / A casca do caule de Amburana cearensis A C Smith, conhecida popularmente como cumaru, à utilizada para o tratamento de doenÃas respiratÃrias como bronquite e asma. Estudos farmacolÃgicos anteriores mostraram as atividades antiinflamatÃria, antioxidante e antinociceptiva do extrato e molÃculas isoladas do cumaru: incluindo cumarina (CM) e amburosÃdeo A (AMB). Diante do exposto, o objetivo do presente estudo foi realizar uma avaliaÃÃo preliminar da citotoxicidade, e investigar o potencial antiinflamatÃrio e antioxidante da cÃpsula do extrato seco de A. cearensis (CESAC) e da Afrormosina (AFM), com determinaÃÃo do possÃvel mecanismo de aÃÃo. Para tanto, as cÃpsulas foram produzidas a partir do extrato seco (spray-dryer) padronizado pelo teor de AMB e CM por CLAE. A citotoxicidade foi investigada em neutrÃfilo humano (2,5 x 106 cÃlulas/mL) atravÃs dos testes de exclusÃo ao corante azul de tripan, LDH, MTT e avaliaÃÃo do padrÃo de morte celular pelo corante laranja de acridina/brometo de etÃdio. A AFM (10, 50 e 100 Âg/mL) nÃo mostrou citotoxicidade, enquanto que a CESAC (10, 100 e 200 Âg/mL) aumentou o nÃmero de cÃlulas em apoptose e necrose. A CESAC (100-400 mg/kg, v.o.) inibiu o edema de pata em camundongos, o acÃmulo de cÃlulas e os nÃveis de TBARS-MDA no peritÃnio, induzidos por carragenina. No lavado broncoalveolar de ratos desafiados com ovalbumina, a CESAC reduziu o acÃmulo de cÃlulas, bem como a produÃÃo de TBARS-MDA e nitrito/nitrato, alÃm de restabelecer os nÃveis de GSH. Tanto a CESAC (5, 10, 25, 50, 100 e 200 Âg/mL), quanto AFM (3; 6; 12,5; 25; 50 e 100 Âg/mL) reduziram a ativaÃÃo de neutrÃfilos humano induzida por fMLP (em atà 65 % e 66 %, respectivamente) ou PMA (em atà 72 % e 86 %, respectivamente). AlÃm disso, estes inibiram em atà 70 % aproximadamente a atividade de mieloperoxidase, porÃm apenas a CESAC inibiu a atividade da elastase (6-88 % inibiÃÃo). A adiÃÃo de CESAC ou AFM à suspensÃo de neutrÃfilos reduziu tambÃm os nÃveis de TNFα. O CESAC e a AFM mostraram atividade inibitÃria do metabolismo oxidativo de neutrÃfilos mensurado atravÃs de ensaios de quimioluminescÃncia dependente de luminol (QL lum) e lucigenina (QL luc). / The stem bark of Amburana cearensis AC Smith, popularly known as cumaru, is used to treat respiratory diseases like bronchitis and asthma. Previous pharmacological studies showed the anti-inflammatory, antinociceptive and antioxidant, and / or muscle relaxant activities of the the extract and isolated molecules from cumaru, including coumarin (CM) and amburoside A (AMB). Given the above, the objective of this study was to conduct a preliminary assessment of cytotoxicity, and investigate the anti-inflammatory and antioxidant potential of the capsule of the dryed extract from A. cearensis (CESAC) and afrormosin (AFM) to determine the possible mechanism of action. For this, the capsules were produced from the dried extract (spray-dryer), standardized by the content of CM and AMB by HPLC. Cytotoxicity was investigated in human neutrophil (2.5 x 106 cells / mL) through the tests of the exclusion dye trypan blue, LDH, MTT and evaluation of the pattern of cell death by acridine orange / ethidium bromide. AFM (10, 50 and 100 Âg / mL) showed no cytotoxicity, while CESAC (10, 100 and 200 Âg / mL) increased the number of apoptotic and necrotic cells. The CESAC (100-400 mg / kg, po) inhibited the paw edema in mice, the accumulation of cells and MDA-TBARS levels in the peritoneum induced by carrageenan. In bronchoalveolar lavage of mice challenged with ovalbumin, the CESAC reduced the accumulation of cells, as well as production of TBARS, MDA and nitrite / nitrate, and restore the levels of GSH. Both CESAC (5, 10, 25, 50, 100 and 200 Âg / mL), and AFM (3, 6, 12.5, 25, 50 and 100 Âg / mL) reduced the activation of human neutrophils induced by fMLP ( up to 65% and 66%, respectively) or PMA (up to 72% and 86%, respectively). Moreover, they inhibited by 70% about the activity of myeloperoxidase, but only CESAC inhibited elastase activity (6-88% inhibition). The addition of AFM or CESAC in suspension of neutrophils also reduced the levels of TNFα. The CESAC and AFM showed the inhibitory activity of neutrophil oxidative metabolism measured by tests of luminol- (CL lum) and lucigenin-dependent (CL luc) chemoluminescence.
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