Efficacy of application of Equisetum pyramidale Goldm. hydrogel for tissue restoration of induced skin lesions in Wistar rats / Eficácia da aplicação de Equisetum pyramidale Goldm. hidrogel na restauração tecidual em lesões cutâneas induzidas em ratos Wistar

Abstract Medicinal plants, such as E. pyramidale, are alternatives against infections and assist in the healing process of wounds. We evaluated the effects of Hydrogel of E. pyramidale on the healing of cutaneous wounds in animal models by morphological, morphometric and histological analyses, and elucidated major components. The ethanolic extract of E. pyramidale shoots was submitted to phytochemical analysis. For cicatrizing activity assay, Wistar rats were used, and the groups evaluated were hydrogel containing ethanolic extract of E. pyramidale at 2% compared to control groups. The treatment periods were 3, 7 and 21 days, and macroscopic and microscopic analyses were performed. Data were submitted to Analysis of Variance (p <0.05). Phytochemistry and quantification evidenced that flavonoids are main constituents and that they were evidenced by thin layer chromatography (TLC), high efficiency (HPLC) and infrared (IR) methods. In TLC, using flavonoid patterns, we observed pinocembrin. The hydrogel containing ethanolic extract of E. pyramidale at 2% was effective in wound regression. E. pyramidale can be used for the treatment of second intention wounds, and the effective healing may be due to a high flavonoid content.

Resumo As plantas medicinais, como E. pyramidale, são uma alternativa para combater infecções e ajudar o processo de cicatrização de feridas. Avaliar os efeitos do hidrogel de E. pyramidale na cicatrização de feridas cutâneas em modelos animais através de análises morfológicas, morfométricas e histológicas, bem como para elucidar os principais componentes. O extrato etanólico das partes aéreas de E. pyramidale foi submetido a análise fitoquímica. Para o ensaio de atividade cicatrizante, foram utilizados ratos Wistar e os grupos avaliados foram o hidrogel com extrato etanólico de E. pyramidale 2% em comparação com os grupos controle. Os períodos de tratamento foram 3, 7 e 21 dias e as análises macroscópicas e microscópicas foram realizadas e os dados submetidos à Análise de Variância (p <0,05). A fitoquímica e a quantificação indicaram que os flavonóides são os constituintes principais e que mesmos foram evidenciados na cromatografia de camada delgada (CCD), de alta eficiência (HPLC) e por infravermelho (IV). Em CCD, empregando padrões de flavonoides, foi observado a pinocembrina. O hidrogel com extrato etanólico de E. pyramidale 2% foi eficaz na regressão da ferida. E. pyramidale pode ser usado no tratamento de feridas de segunda intenção e a cura efetiva pode ser devido ao alto teor de flavonoides.

Effect of ractopamine and conjugated linoleic acid on performance of late finishing pigs.

The dietary inclusion of feed additives to improve the carcass characteristics of the final product is of great importance for the pork production chain. The aim of our study was to evaluate the effects of the association of ractopamine (RAC) and conjugated linoleic acid (CLA) on the performance traits of finishing pigs during the last 26 days prior to slaughter. In total, 810 commercial hybrid barrows were used. Animals were distributed among treatments according to a randomised block design in a 3 × 3 factorial arrangement, with three RAC levels (0, 5 or 10 ppm) and three CLA levels (0, 0.3 or 0.6%). Pigs fed the diet with 5 ppm RAC had higher average daily feed intake (ADFI) (2.83 kg; P < 0.05) when compared with those fed 10 ppm RAC and the control diet (2.75 and 2.74 kg, respectively). Lower ADFI values (P < 0.01) were observed with the diets containing CLA compared with the control diet with no CLA (2.73 and 2.75 v. 2.85 kg/day, respectively). The average daily weight gain of pigs fed 5 and 10 ppm RAC was +148 and +173 g/dayhigher (P < 0.001), respectively, than those fed the control diet. Dietary RAC levels influenced (P < 0.001) feed conversion ratio (FCR), which was reduced as RAC levels increased, with the pigs fed 10, 5 and 0 ppm RAC presenting FCR values of 2.57, 2.71 and 3.05, respectively. FCR also improved (P < 0.05) with the inclusion of 0.6% CLA relative to the control diet (2.70 v. 2.84, respectively). There was a significant interaction between CLA × RAC levels (P < 0.01) for final BW, loin eye area (LEA) (P < 0.05) and backfat thickness (BT) (P < 0.05). The treatments containing 10 ppm RAC + 0.6% or 0.3% CLA increased LEA and reduced BT. In conclusion, the level of 10 ppm inclusion of RAC increased the overall performance parameters of pigs and therefore improved production efficiency. The combined use of RAC and CLA promoted a lower feed conversion ratio as well as better quantitative carcass traits, as demonstrated by the higher LEA and lower BT. The dietary inclusion of CLA at 0.3% improved feed efficiency, however, without affecting LEA or BT yields.

Efficacy of application of Equisetum pyramidale Goldm. hydrogel for tissue restoration of induced skin lesions in Wistar rats.

Medicinal plants, such as E. pyramidale, are alternatives against infections and assist in the healing process of wounds. We evaluated the effects of Hydrogel of E. pyramidale on the healing of cutaneous wounds in animal models by morphological, morphometric and histological analyses, and elucidated major components. The ethanolic extract of E. pyramidale shoots was submitted to phytochemical analysis. For cicatrizing activity assay, Wistar rats were used, and the groups evaluated were hydrogel containing ethanolic extract of E. pyramidale at 2% compared to control groups. The treatment periods were 3, 7 and 21 days, and macroscopic and microscopic analyses were performed. Data were submitted to Analysis of Variance (p <0.05). Phytochemistry and quantification evidenced that flavonoids are main constituents and that they were evidenced by thin layer chromatography (TLC), high efficiency (HPLC) and infrared (IR) methods. In TLC, using flavonoid patterns, we observed pinocembrin. The hydrogel containing ethanolic extract of E. pyramidale at 2% was effective in wound regression. E. pyramidale can be used for the treatment of second intention wounds, and the effective healing may be due to a high flavonoid content.

Wound-Healing potential of Sebastiania hispida (Mart) Pax (Euphorbiaceae) ointment compared to low power laser in rats / Potencial cicatrizante da pomada de Sebastiania hispida (Mart) Pax (Euphorbiaceae) comparado ao laser de baixa potência

Abstract Impaired wound healing represents a serious complication in some pathologies and the use of plant extracts has proved to improve tissue repair. The objectives of this study were to evaluate the healing potential of the ointment of Sebastiana hispida compared with Aluminum-Gallium Indium-Phosphide Laser (InGaAlP) in surgically induced wounds in rats and to perform the phytochemical analysis. The phytochemical analysis was performed in the classic way and also by HPLC. A controlled study was developed with 80 rats (200-250 g) in which a linear excision was performed in the dorsal region after shaving, measuring 2 cm × 1 cm (epidermis and dermis) exposing the muscle fascia. The rats were randomly divided into four groups of twenty animals each. The experimental groups (n = 5) were G1 (Saline); G2 (crude methanol plant extract 2% + Carbopol Gel 98%); G3 (crude methanol plant extract 2% + lanolin/vaseline) and G4 (laser). The incision healing processes were monitored during 3, 7, 14 and until 21 days after excision. The histologic parameters evaluated were Collagen fiber types, microscopic examination and neovascularization. There was a significant increase in the deposition of collagen fibers, as evidenced by a better organized epithelial tissue, keratinized and showing greater proliferation of new blood vessels in the inflammatory phase in the group treated with both the extract and laser. The results were correlated to the phenolic derivatives found after qualitative and quantitative analysis. These compounds were considered responsible for the healing process. The topical treatment with S. hispida leaves, in the two different formulations, was more effective than the application of the laser (Ingan ALP) 660 nm in the model used.

Resumo A cicatrização deficiente representa uma complicação grave em algumas patologias e o uso de extratos de plantas tem demonstrado melhora no processo de reparação tecidual. O objetivo deste estudo foi avaliar o potencial cicatrizante da pomada de Sebastiania hispida comparado ao Laser Indio Phosphide-Gallium-Aluminum (InGaAlP) em feridas cutâneas induzidas cirurgicamente em ratos e realizar analise fitoquímica. A análise fitoquímica foi via clássica e por CLAE. O experimento foi desenvolvido com 80 ratos (200-250 g), divididos aleatoriamente em quatro grupos (n = 5): G1 (salina); G2 (extrato bruto metanólico 2% + Carbopol Gel 98%); G3 (extrato bruto metanólico 2% + lanolina/vaselina) e G4 (laser). Após a tricotomia da região dorsal realizou uma excisão linear, medindo 2 cm × 1 cm (epiderme e derme), expondo a fáscia muscular. Em sequência os tratamentos e o monitoramento do processo de cicatrização das feridas cirúrgicas ocorreu nos tempos de: 3, 7, 14 e até 21 dias após a excisão. Os parâmetros histológicos avaliados foram: tipos de fibras colágenas, avaliação morfológica e neovascularização. Houve uma deposição significativa de fibras colágenas, evidenciado por um tecido epitelial mais bem organizado, queratinizado e mostrando uma maior proliferação de novos vasos sanguíneos na fase inflamatória do grupo tratado com o extrato e o laser. A eficiência do processo de cicatrização pode estar relacionada com a presença de compostos fenólicos e derivados detectados na análise qualitativa e quantitativa. A utilização do tratamento tópico com as duas formulações diferentes de S. hispida foram mais eficazes do que a aplicação do Laser (InGaAlP) no modelo utilizado.

Wound-Healing potential of Sebastiania hispida (Mart.) Pax (Euphorbiaceae) ointment compared to low power laser in rats.

Impaired wound healing represents a serious complication in some pathologies and the use of plant extracts has proved to improve tissue repair. The objectives of this study were to evaluate the healing potential of the ointment of Sebastiana hispida compared with Aluminum-Gallium Indium-Phosphide Laser (InGaAlP) in surgically induced wounds in rats and to perform the phytochemical analysis. The phytochemical analysis was performed in the classic way and also by HPLC. A controlled study was developed with 80 rats (200-250 g) in which a linear excision was performed in the dorsal region after shaving, measuring 2 cm × 1 cm (epidermis and dermis) exposing the muscle fascia. The rats were randomly divided into four groups of twenty animals each. The experimental groups (n = 5) were G1 (Saline); G2 (crude methanol plant extract 2% + Carbopol Gel 98%); G3 (crude methanol plant extract 2% + lanolin/vaseline) and G4 (laser). The incision healing processes were monitored during 3, 7, 14 and until 21 days after excision. The histologic parameters evaluated were Collagen fiber types, microscopic examination and neovascularization. There was a significant increase in the deposition of collagen fibers, as evidenced by a better organized epithelial tissue, keratinized and showing greater proliferation of new blood vessels in the inflammatory phase in the group treated with both the extract and laser. The results were correlated to the phenolic derivatives found after qualitative and quantitative analysis. These compounds were considered responsible for the healing process. The topical treatment with S. hispida leaves, in the two different formulations, was more effective than the application of the laser (Ingan ALP) 660 nm in the model used.

Efficacy of application of Equisetum pyramidale Goldm. hydrogel for tissue restoration of induced skin lesions in Wistar rats

Abstract Medicinal plants, such as E. pyramidale, are alternatives against infections and assist in the healing process of wounds. We evaluated the effects of Hydrogel of E. pyramidale on the healing of cutaneous wounds in animal models by morphological, morphometric and histological analyses, and elucidated major components. The ethanolic extract of E. pyramidale shoots was submitted to phytochemical analysis. For cicatrizing activity assay, Wistar rats were used, and the groups evaluated were hydrogel containing ethanolic extract of E. pyramidale at 2% compared to control groups. The treatment periods were 3, 7 and 21 days, and macroscopic and microscopic analyses were performed. Data were submitted to Analysis of Variance (p 0.05). Phytochemistry and quantification evidenced that flavonoids are main constituents and that they were evidenced by thin layer chromatography (TLC), high efficiency (HPLC) and infrared (IR) methods. In TLC, using flavonoid patterns, we observed pinocembrin. The hydrogel containing ethanolic extract of E. pyramidale at 2% was effective in wound regression. E. pyramidale can be used for the treatment of second intention wounds, and the effective healing may be due to a high flavonoid content.

Resumo As plantas medicinais, como E. pyramidale, são uma alternativa para combater infecções e ajudar o processo de cicatrização de feridas. Avaliar os efeitos do hidrogel de E. pyramidale na cicatrização de feridas cutâneas em modelos animais através de análises morfológicas, morfométricas e histológicas, bem como para elucidar os principais componentes. O extrato etanólico das partes aéreas de E. pyramidale foi submetido a análise fitoquímica. Para o ensaio de atividade cicatrizante, foram utilizados ratos Wistar e os grupos avaliados foram o hidrogel com extrato etanólico de E. pyramidale 2% em comparação com os grupos controle. Os períodos de tratamento foram 3, 7 e 21 dias e as análises macroscópicas e microscópicas foram realizadas e os dados submetidos à Análise de Variância (p 0,05). A fitoquímica e a quantificação indicaram que os flavonóides são os constituintes principais e que mesmos foram evidenciados na cromatografia de camada delgada (CCD), de alta eficiência (HPLC) e por infravermelho (IV). Em CCD, empregando padrões de flavonoides, foi observado a pinocembrina. O hidrogel com extrato etanólico de E. pyramidale 2% foi eficaz na regressão da ferida. E. pyramidale pode ser usado no tratamento de feridas de segunda intenção e a cura efetiva pode ser devido ao alto teor de flavonoides.

Effect of heat stress and feeding phosphorus levels on pig electron transport chain gene expression.

The purpose of this study was to evaluate the effect of temperature and different levels of available phosphorus (aP) on the expression of nine genes encoding electron transport chain proteins in the Longissimus dorsi (LD) muscle of pigs. Two trials were carried out using 48 high-lean growth pigs from two different growth phases: from 15 to 30 kg (phase 1) and from 30 to 60 kg (phase 2). Pigs from growth phase 1 were fed with three different levels of dietary aP (0.107%, 0.321% or 0.535%) and submitted either to a thermoneutral (24°C and RH at 76%) or to a heat stress (34°C and RH at 70%) environment. Pigs from growth phase 2 were fed with three different levels of dietary aP (0.116%, 0.306% or 0.496%) and submitted either to a thermoneutral (22ºC and RH at 77%) or to a heat stress (32ºC and RH at 73%) environment. Heat stress decreased (P<0.001) average daily feed intake at both growth phases. At 24°C, pigs in phase 1 fed the 0.321% aP diet had greater average daily gain and feed conversion (P<0.05) than those fed the 0.107% or 0.535% while, at 34°C pigs fed the 0.535% aP had the best performance (P<0.05). Pigs from phase 2 fed the 0.306% aP had best performance in both thermal environments. Gene expression profile was analyzed by quantitative real-time polymerase chain reaction. Irrespective of growing phase, the expression of six genes was lower (P<0.05) at high temperature than at thermoneutrality. The lower expression of these genes under high temperatures evidences the effects of heat stress by decreasing oxidative metabolism, through adaptive physiological mechanisms in order to reduce heat production. In pigs from phase 1, six genes were differentially expressed across aP levels (P<0.05) in the thermoneutral and one gene in the heat stress. In pigs from phase 2, two genes were differentially expressed across aP levels (P<0.05) in both thermal environments. These data revealed strong evidence that phosphorus and thermal environments are key factors to regulate oxidative phosphorylation with direct implications on animal performance.

Avaliação da atividade antimicrobiana de Maytenus rigida Mart. (Celastraceae) / Evaluation of the antimicrobial activity of Maytenus rigida Mart. (Celastraceae)

A realização de estudos farmacológicos é fundamental para comprovar a eficácia do uso de plantas medicinais pela população para o tratamento de doenças e descobrir novos fitoterápicos. Esse estudo teve como objetivo avaliar o potencial antimicrobiano do extrato etanólico e fase acetato de etila do bom nome (Maytenus rigida Mart.) sobre Staphylococcus aureus ATCC 25923, 3 amostras de Staphylococcus aureus multirresistentes isoladas de pacientes com infecções nosocomiais, Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 27853 e Salmonella sp. (228-R-Tet, 118-R-Sut e 01-S) isoladas de ambiente aquático, utilizando o método de difusão em agar. Os testes revelaram que o extrato e fase de M. rigida apresentaram atividade antimicrobiana in vitro frente a todas as cepas de S. aureus testadas, apresentando concentração inibitória mínima (MIC) de 400 mg mL-1. Entretanto, estes produtos não apresentaram atividade frente às linhagens de bactérias Gram-negativas testadas, Escherichia coli, Pseudomonas aeruginosa e Salmonella sp.

Ppharmacological studies are essential to prove the effectiveness of using medicinal plants to treat diseases and discover new phytotherapics. This study aimed to evaluate the antimicrobial potential of ethanol and ethyl acetate extracts of "bom-nome" (Maytenus rigida Mart.) against Staphylococcus aureus ATCC 25923, three samples of multiresistant Staphylococcus aureus isolated from patients with nosocomial infections, Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 27853 and Salmonella sp. (228-R-Tet, 118-R-Sut and 01-S) isolated from water environment, using the agar diffusion test. Both extracts showed in vitro antimicrobial activity against all S. aureus strains, presenting 400 mg mL-1 minimum inhibitory concentration (MIC). However, these products did not show activity against strains of the Gram-negative bacteria Escherichia coli, Pseudomonas aeruginosa and Salmonella sp.

Effects of dietary protein level and amino acid supplementation on performance of mixed-parity lactating sows in a tropical humid climate.

Eighty-six mixed-parity Large White sows were used to determine the effect of diets with reduced CP content or supplemented with essential AA on 28-d lactation performance under humid tropical climatic conditions. This experiment was conducted in Guadeloupe (West French Indies, latitude 16 degrees N, longitude 61 degrees W) between February 2007 and January 2008. Two seasons were distinguished a posteriori from climatic measurement variables continuously recorded in the farrowing room. The average minimum and maximum ambient temperatures and average daily relative humidity for the warm season were 20.5 and 28.2 degrees C, and 93.8%, respectively. The corresponding values for the hot season were 22.7 and 29.4 degrees C, and 93.7%, respectively. The dietary experimental treatments were a normal protein diet (NP), a low protein diet (LP), and a NP diet (NP+) supplemented with essential AA. The NP and LP diets supplied the same levels of standardized digestible Lys (i.e., 0.80 g/MJ of NE), and the NP+ diet supplied 0.95 g/MJ of NE. No interaction between season and diet composition was noted on any response variable evaluated. The ADFI was decreased (P < 0.05) in the hot season (i.e., 3.69 vs. 4.72 kg) and therefore decreased by 500 g per degrees C increase of ambient temperature under high relative humidity conditions. The ADFI tended to be greater with the LP and NP+ diets when compared with the NP treatment (i.e., +10%, P = 0.08). Litter BW gain and mean BW of piglets at weaning were greater (P < 0.05) during the warm season than during the hot season (2.3 vs. 1.8 kg/d and 7.5 vs. 7.1 kg, respectively). Milk production and composition were not affected by dietary treatments but were affected by season (8.1 vs. 6.8 kg/d, for warm and hot seasons, respectively; P < 0.01). The sows fed LP and NP+ diets tended to have decreased backfat thickness losses (3.3 and 3.8 mm, respectively; P > 0.08). In conclusion, the hot season in humid tropical climates, which combines high levels of temperature and humidity, has a pronounced negative impact on performance of lactating sows. Diets with low CP content or supplemented with essential AA can attenuate the effects of hot and humid season by increasing ADFI in lactating sows.

Níveis de cromo orgânico em rações para frangos de corte mantidos sob estresse por calor no período de um a 42 dias de idade / Levels of dietary chromiumin rations for male broilers kept under heat stress from one to 42 days of age

Avaliou-se o efeito da suplementação de cromo sobre o desempenho e o rendimento de cortes de frangos, mantidos em ambiente de alta temperatura, no período de um a 42 dias de idade. Foram utilizados 400 frangos de corte, machos, da linhagem Cobb, em um delineamento experimental inteiramente ao acaso, com cinco tratamentos, 0, 350, 700, 1.050 e 1.400ppb de cromo na ração, oito repetições e 10 aves por repetição. Nos períodos de um a 21 e de um a 42 dias de idade, não houve influência dos tratamentos sobre o ganho de peso, o consumo de ração e a conversão alimentar das aves, mas observou-se que o consumo de cromo aumentou de forma linear. Os tratamentos não influenciaram os pesos absoluto e relativo de nenhum dos cortes, peito, coxa e sobrecoxa, avaliados aos 42 dias de idade. A suplementação de até 1.400ppb de cromo na ração não influenciou o desempenho e o rendimento de cortes nobres de frangos de corte mantidos em estresse por calor, no período de um a 42 dias de idade.

The effect of dietary organic chromium supplementation on the performance and yield of prime cuts of male broilers from one to 42 days of age reared under high environmental temperature was evaluated. Four-hundred Cobb male broilers, averaging 38±0.14g were distributed in a simple sample random design with five treatments (0; 350; 700; 1,050; and 1,400ppb of chromium in ration), eight replicates, and ten birds per replicates. In periods from one to 21 and from one to 42 days of age, the treatments did not influence the weight gain, the food intake, and the feed:gain ratio of the birds. However, the chromium intake increased in a linear way. No effect of both absolute and relative weights of all evaluated cuts (breast, thigh, and drumstick) was observed. The dietary chromium supplementation up to 1,400ppb did not influence the performance and the carcass traits of the male broilers kept under heat stress from one to 42 days of age.

Effects of dietary protein concentration and amino acid supplementation on the feeding behavior of multiparous lactating sows in a tropical humid climate.

Forty-seven mixed-parity Large White sows were used to determine the effect of diets with reduced CP content or supplemented with essential AA on 28-d lactation feeding behavior under humid tropical climatic conditions. The study was conducted at the INRA experimental facilities in Guadeloupe, French West Indies (latitude 16 degrees N, longitude 61 degrees W) between February 2007 and January 2008. Two seasons were distinguished a posteriori from climatic measurements continuously recorded in the open-front farrowing room. The average ambient temperature and average daily relative humidity for the warm season were 23.6 degrees C and 93.8%, respectively. The corresponding values for the hot season were 26.1 degrees C and 93.7%. The dietary experimental treatments were a normal protein diet (17.3%), a low protein diet (14.1%), and a normal protein diet supplemented with essential AA (17.6%). No interaction between season and diet composition was found for all criteria. Average daily feed intake was less (P < 0.01) during the hot season (4,559 +/- 161 vs. 5,713 +/- 204 kg/d). Meal size was reduced during the hot season (542 +/- 37 vs. 757 +/- 47 g/meal; P < 0.01). Daily ingestion time (45.5 +/- 3.2 vs. 55.8 +/- 4.0 min/d; P < 0.05) was less in the hot season. Meal size was reduced during the hot season at night (P < 0.01). In both seasons, daily feed intake, feed ingestion, and rate of feed intake were less (P < 0.01) during the nocturnal period than during the diurnal period. The number of meals per day was not affected (P > 0.10) by season or diet composition. Daily feed intake was greater for the sows fed the low protein diet when compared with normal protein treatments (P < 0.05). Duration of standing was not affected by diet or season (P > 0.05), and averaged 126 +/- 35 min/d. This study confirms that feeding behavior variables of the lactating sow are affected by seasonal pavariations of the tropical climate. Irrespective of season, the reduction of CP content improved feed consumption under tropical conditions.

Negative inotropic and chronotropic effects on the guinea pig atrium of extracts obtained from Averrhoa carambola L. leaves.

It has been reported that star fruit can lead to a fatal outcome in uremic patients. The intoxication syndrome consists of hiccups, mental confusion, dizziness, and vomiting. On the other hand, folk medicine uses teas and infusions of carambola leaves to treat headache, vomiting, cough, insomnia, and diabetes. This motivated us to determine if Averrhoa carambola can act on the contractility and automaticity of the guinea pig heart. We measured the atrial isometric force in stimulated left atria and determined the chronotropic changes in spontaneously beating right atria. The carambola leaf extracts (1.5 mg/ml) abolished the contractile force in a concentration-dependent manner. Among the crude, methanolic, ethanolic, aqueous, and acetic extracts, the aqueous one was the most potent (EC50 = 520 +/- 94 microg/ml; flavonoids and tannins are the main constituents; Na+ and K+ contents in 1.0 mg/ml of aqueous extract were 0.12 +/- 0.016 and 1.19 +/- 0.15 mM, respectively). The aqueous extract abolished the positive Bowditch staircase phenomenon and reduced the inotropic response to CaCl2 (0.17-8.22 mM), events that are dependent on the cellular Ca2+ inward current. The adrenergic, muscarinic or opioid membrane receptors do not seem to participate in the mechanism of action of the cardioactive substance(s). In spontaneously beating atria, the aqueous extract promoted a negative chronotropic effect that was antagonized by 0.1 microM isoproterenol bitartrate. With this agonist, the EC50 of the aqueous extract increased from 133 +/- 58 to 650 +/- 100 microg/ml. These data regarding the effect of A. carambola on guinea pig atrial contractility and automaticity indicate an L-type Ca2+ channel blockade.

Negative inotropic and chronotropic effects on the guinea pig atrium of extracts obtained from Averrhoa carambola L. leaves

It has been reported that star fruit can lead to a fatal outcome in uremic patients. The intoxication syndrome consists of hiccups, mental confusion, dizziness, and vomiting. On the other hand, folk medicine uses teas and infusions of carambola leaves to treat headache, vomiting, cough, insomnia, and diabetes. This motivated us to determine if Averrhoa carambola can act on the contractility and automaticity of the guinea pig heart. We measured the atrial isometric force in stimulated left atria and determined the chronotropic changes in spontaneously beating right atria. The carambola leaf extracts (1.5 mg/ml) abolished the contractile force in a concentration-dependent manner. Among the crude, methanolic, ethanolic, aqueous, and acetic extracts, the aqueous one was the most potent (EC50 = 520 ± 94 æg/ml; flavonoids and tannins are the main constituents; Na+ and K+ contents in 1.0 mg/ml of aqueous extract were 0.12 ± 0.016 and 1.19 ± 0.15 mM, respectively). The aqueous extract abolished the positive Bowditch staircase phenomenon and reduced the inotropic response to CaCl2 (0.17-8.22 mM), events that are dependent on the cellular Ca2+ inward current. The adrenergic, muscarinic or opioid membrane receptors do not seem to participate in the mechanism of action of the cardioactive substance(s). In spontaneously beating atria, the aqueous extract promoted a negative chronotropic effect that was antagonized by 0.1 æM isoproterenol bitartrate. With this agonist, the EC50 of the aqueous extract increased from 133 ± 58 to 650 ± 100 æg/ml. These data regarding the effect of A. carambola on guinea pig atrial contractility and automaticity indicate an L-type Ca2+ channel blockade.

Inotropic effect of Citrus sinensis (L.) Osbeck leaf extracts on the guinea pig atrium.

The objective of the present investigation was to determine the contractile effect of crude and acetone leaf extracts of Citrus sinensis (L.) Osb. on mammalian myocardium. Crude leaf extracts have been used in folk medicine to treat neurological disorders. Some flavonoids isolated from this plant presented a positive inotropic effect on myocardium. This motivated us to test the extracts on the atria of guinea pigs of both sexes (300-500 g) and surprisingly we observed inotropic depression instead of an increase in force. The maximum effect of the crude extract was 79.4 +/- 8.1% of the control force amplitude (N = 5 hearts, 10 trials, 27 +/- 0.1 degrees C, stimulus: 2 Hz, 400 V, 0.5 ms). The EC50 for crude, ethanol, acetic, aqueous, and acetone extracts was 300, 300, 600, 1000, and 140 microg/ml, respectively, with a Hill constant of 1.8, 2.0, 2.5, 2.0, and 1.4, respectively. Blockade of cholinergic, beta-adrenergic, or opioid membrane receptors with 1.5 microM atropine sulfate, 1 microM propranolol, and 10 microM naloxone, respectively, did not change the effect of the crude extract. The acetone extract abolished the Bowditch positive staircase phenomenon (N = 5 hearts, 10 trials, 27 +/- 0.1 degrees C), suggesting a possible reduction of the calcium inward current, and also promoted the so-called Woodworth phenomenon. The effect was concentration-dependent and indicated the existence of another inhibitory contractile mechanism such as the simultaneous activation of some of the membrane potassium channels reducing the myocardial action potential duration and further decreasing the cellular calcium entry.

Inotropic effect of Citrus sinensis ( L. ) Osbeck leaf extracts on the guinea pig atrium

The objective of the present investigation was to determine the contractile effect of crude and acetone leaf extracts of Citrus sinensis (L.) Osb. on mammalian myocardium. Crude leaf extracts have been used in folk medicine to treat neurological disorders. Some flavonoids isolated from this plant presented a positive inotropic effect on myocardium. This motivated us to test the extracts on the atria of guinea pigs of both sexes (300-500 g) and surprisingly we observed inotropic depression instead of an increase in force. The maximum effect of the crude extract was 79.4 ± 8.1 percent of the control force amplitude (N = 5 hearts, 10 trials, 27 ± 0.1°C, stimulus: 2 Hz, 400 V, 0.5 ms). The EC50 for crude, ethanol, acetic, aqueous, and acetone extracts was 300, 300, 600, 1000, and 140 æg/ml, respectively, with a Hill constant of 1.8, 2.0, 2.5, 2.0, and 1.4, respectively. Blockade of cholinergic, beta-adrenergic, or opioid membrane receptors with 1.5 æM atropine sulfate, 1 æM propranolol, and 10 æM naloxone, respectively, did not change the effect of the crude extract. The acetone extract abolished the Bowditch positive staircase phenomenon (N = 5 hearts, 10 trials, 27 ± 0.1°C), suggesting a possible reduction of the calcium inward current, and also promoted the so-called Woodworth phenomenon. The effect was concentration-dependent and indicated the existence of another inhibitory contractile mechanism such as the simultaneous activation of some of the membrane potassium channels reducing the myocardial action potential duration and further decreasing the cellular calcium entry.

Central antinociceptive effect of a hydroalcoholic extract of Dioclea grandiflora seeds in rodents.

The acute treatment of rats and mice with a hydroalcoholic extract from the seeds of Dioclea grandiflora (EHDg) at doses of 250 and 500 mg/kg, by intraperitoneal or oral administration, produced a significant antinociceptive effect in the tail flick and hot plate tests, an effect which was inhibited by naloxone. EHDg given to mice daily for 30 days at a dose of 500 mg/kg, did not cause any observable toxic effect nor any alteration in the pattern of antinociceptive response by the tail immersion test during the course of this treatment. These results suggest that EHDg has a central antinociceptive action devoid of tolerance effect typical of opioid drugs.

Intracellular calcium mobilization as a target for the spasmolytic action of scopoletin.

The coumarin scopoletin was isolated in a pure form from the roots of Brunfelsia hopeana Benth. (Solanaceae). In isolated rat aortic rings, scopoletin (26-520 microM) inhibited to approximately the same extent the contractions induced by a variety of substances, including phenylephrine, potassium chloride, serotonin and PGF(2) (alpha). The effect of the coumarin on phenylephrine-induced contractions was not affected by endothelium removal or NO-synthase blockade by L-NAME (100 microM). Scopoletin (78 - 590 microM) antagonized in a concentration-dependent manner (IC(50) = 300 +/- 20 microM, n = 5), transient contractions in Ca(2+)-free media induced by noradrenaline, but not those induced by caffeine. Also, scopoletin did not interfere with the refilling of noradrenaline-sensitive intracellular calcium stores. It is suggested that the non-specific spasmolytic action of scopoletin can be attributed, at least in part, to its ability to inhibit the intracellular calcium mobilization from the noradrenaline-sensitive stores.

[Intensive phototherapy treatment for severe haemolytic disease of the newborn] / Fototerapia intensiva no tratamento de caso grave de doença hemolítica do recém-nascido.

OBJECTIVE: To discuss the use of alternative treatment methods in hemolytic disease of newborn to replace common early exchange transfusion. METHODS: Case report of newborn with intensive Rh incompatibility treated with intensive phototherapy, plus phenobarbital instead of traditional early exchange transfusion.RESULTS: The neonatés cord blood showed 9.2 mg/dL of total bilirubin and 39% hematocrit. He was medicated with phenobarbital and intensive phototherapy at once. There was a rapid growing hyperbilirubinemia followed by stabilization for almost 60 hours with little changes, but without levels that justified an exchange transfusion. He became progressively anemic and needed a concentrate transfusion. When he was five days old, he was discharged and returned to follow-up at the 7th week of life when his bone marrow was beginning to recover from anemia.CONCLUSIONS: This case demonstrates that pharmacologic agents and intensive phototherapy can be as useful as advantageous in severe hemolytic disease of newborn. We should always try to use them before adopting more aggressive therapies.

The monoterpene alkaloid cantleyine from Strychnos trinervis root and its spasmolytic properties.

Cantleyine, a monoterpene alkaloid isolated from the root bark of Strychnos trinervis, was submitted to a broad spectrum pharmacological screening, in which the principal effect observed was a nonspecific relaxation of isolated smooth muscles. Cantleyine relaxed (IC50 2.1 x 10(-4) M) the guinea-pig trachea, pre-contracted by carbachol and antagonized in a nonspecific manner; carbachol (IC50 2.1 x 10(-4) M) and histamine (IC50 1.4 x 10(-4) M) induced contractions in the guinea-pig ileum; and phenylephrine (IC50 3.8 x 10(-4) M) responses in the rat aorta. Cantleyine antagonized (pD'2, 3.82) cumulative concentration response curves to histamine in the ileum in a noncompetitive, reversible (slope, 4.84) and concentration dependent manner. The tonic contractions induced by histamine and KCl were also inhibited in a concentration-dependent and reversible manner (IC50 7.2 x 10(-5) and 1.8 x 10(-4) M, respectively), suggesting that cantleyine should be acting on voltage-dependent Ca2+ channels. This hypothesis was confirmed by the observation that cantleyine inhibited (pD'2, 3.35), in a concentration dependent manner, the CaCl2 induced contraction in depolarizing medium. These results suggest that cantleyine produces nonspecific spasmolytic effects in smooth muscle and that in guinea-pig ileum this effect is, in part, due to the inhibition of Ca+2 influx through voltage-dependent Ca2+ channels.

Spasmolytic actions of the new indole alkaloid Trinervine from Strychnos trinervis root.

Trinervine, a new tertiary indole alkaloid of sarpagine like skeleton with a hemiketal function, isolated from the root bark of Strychnos trinervis was submitted to a broad spectrum pharmacological screening, when the principal effect observed was a nonspecific relaxation of isolated smooth muscles. The spasmolytic actions were confirmed on cumulative concentration-response curves using carbachol and histamine induced contractions of the guinea-pig ileum and 5-hydroxytryptamine (5-HT) and arachidonic acid contractions in the rat fundic strip. The respective pD'2 values (mean ± SE) were 4.04 ± 0.12 and 4.25 ± 0.16, in the guinea-pig ileum and 3.54 ± 0.15 and 3.96 ± 0.16 in the rat fundic strips but trinervine was found inactive against PGE2 induced contractions at concentrations up to 10(-4)M. The values of slopes of the regression lines differed significantly from the unity in all cases and as the maximum effect of the agonists were suppressed, these preliminary results suggest that trinervine produce spasmolytic effects on isolated gastrointestinal smooth muscles through noncompetitive antagonism process.