[Noscapine and acute pancreatitis: effects of different doses of noscapine on serum amylase level in experimental acute pancreatitis in rats]

Noscapine has been recently known as an antagonist of Bradykinin, and in this study its effect on the animal model of acute pancreatitis has been evaluated. 49 male Wistar rats have been evaluated in five experimental and four control groups. Common bile duct has been ligated by means of surgery to induce acute pancreatitis in rats. The resulted inflammation of the pancreas and the effect of Noscapine on it have been documented by measuring serum amylase levels. Amylase was measured in experimental groups after surgery and injection of Noscapine. Amylase was also measured in control groups while they did not undergo similar procedures. Results: The only meaningful effect of Noscapine values on the level of serum amylase was an unexpected increase in the 0.5 mg/kg dose; and in other doses [1, 2, 5, 10 mg/kg] the changes in the level of serum amylase were not meaningful. Noscapine has affected the inflammation of acute pancreatitis via probable mediation of Bradykinin, but the inflammation was not favorably reduced, probably because of short lifetime of Noscapine

Enzima inativadora de bradicinina liberada de fígado preservado ex-vivo / Bradykinin-inactivating enzyme is released from the ex-vivo stored liver

Objetivo - Ofígado inativa quantidades consideráveis de bradicinina; a principal enzima hepática cinino-inativadora (BIE, bradykinin inativating endopeptidase) hidrolisa especificamente a ligaçao Phe-Ser do nonapeptídio e foi caracterizada como sendo a oligoendopeptidase EC 3.4. 24.15. No transplante ortotópico de fígado existe correlaçao entre aumento da concentraçao de aminoácidos no líquido de preservaçao (conseqUência de proteólise) e falência do enxerto. O objetivo deste trabalho é verificar se ocorre liberaçao da BIE de fígados preservados ex-vivo no líquido Braun-Collins ou em soluçao de Krebs-Henseleit bicarbonato (Krebs). Método. Fígado de ratos Wistar (180-220g) foram exsangüinados e a pós remoçao foram preservados em líquido Braun Collins ou em soluçao Krebs, a 4 graus Celsius. Foram retiradas alíquotas do líquido de preservaçao nos tempos 0, 4, 8 e 24 horas, para dosagem de ALT, AST, DHL e BIE. A atividade fluorimétrica da BIE foi ensaiada com o substrato Abz-RPPGFSPFRQ-EDDnp (análogo sintético da bradicinina) e sua presença confirmada por immunoblotting, revelado com anticorpo específico anti-EC 3.4.24.15. Resultados. A liberaçao de ALT, AST, DHL e BIE é significativa no período 8-24 hs. Nas alíquotas de 24 hs, em relaçao ao tempo zero, a concentraçao das quatro enzimas aumentou, respectivamente, no líquido Braun Collins, 8, 7, 19 e 10 vezes e, na soluçao de Krebs, 21, 17, 27 e 21 vezes; a relaçao ALT/DHL foi sempre inferior a um. Conclusao. Ocorre liberaçao de BIE durante a preservaçao ex-vivo do fígado, o que poderá servir como indicaçao da condiçao de preservaçao do enxerto; diminuiçao da capacidade cinino-inativadora do fígado poderá afetar sua reatividade vascular.

Effects of calcium and EDTA on rat skin capillary permeability and on its response to histamine, serotonin and bradykinin

Para estudiar los efectos del calcio y el EDTA sobre la permeabilidad vascular y su respuesta a mediadores de la inflamación se utilizó el método de la extravasación del azul de Evans. El Ca2+ provocó una disminución concentración-dependeniente de la permeabilidad capilar. El EDTA en concentraciones 0.2 mM o mayores tuvo el efecto opuesto. La extravasación provocada por la inyección intradérmica de histamina 100 microng/ml, serotoninas 5 microng/ml y bradiquinina 5 microng/ml, fue menor cuando se innyectó en el mismo sitio Ca2+ 8mM y mayor en presencia de EDTA e mM. Los efectos del EDTA fueron inhibidos por el calcio. Estos resultados sugieren que, en la piel de la rata, el calcio disminuye la permeabilidad capilar y su respuesta a histamina, serotonina y bradiquinina

Demonstration of anti-bradykinin compounds in callus cultures of Mandevilla velutina

Calluses from stems and leaves of Mandevilla velutina were grown in culture for 30,45 and 60 days. Thin-layer chromatography of ethyl acetate extracts of calluses from stems of M. velutina revealed the presence of 6 compounds. Two of them had RF values identical to those of the anti-bradykinin (BK) compounds MV8609 and MV8610 previously isolated from the natural plant. The ethyl acetate extract (20 to 80 microng/ml) from stem callus culture antagonized in a concentration-dependent and reversible manner contractions caused by BK (0.1-100 nM) in the isolated rat uterus. The extracts obtained from calluses cultured for 30,45 and 60 days were about 79-, 63-and 31-fold more potent, respectively, in antagonizing BK than the crude extract obtained from the rhizome of the plant

Blockade of the bradykinin-evoked diphasic response of isolated rat duodenum by the crude extract of and compounds obtained from Mandevilla velutina

The influence of an aqueous/ethanolic extract of M. velutina (CE) and of two compound (MV 8608 and MV 8612) purified from the plant on BK-, Ad- and K+ -induced responses of the rat duodenum was analyzed in vitro. In preparations precontracted with Ca2+, the CE (1 and 2 mg/ml) markedly inhibited BK -induced relaxation in a dose-dependent manner but was less effective against Ad-induced relaxation. The CE (0.5 mg/ml) also antagonized BK -induced relaxation and contraction of strips bathed in normal medium. The two compounds from M. velutina (10 and 20 microng/ml) also promoted a dose-dependent blockade of both responses to BK, only slightly depressing the response to K+

Anti-spasmogenic effect of cyproheptadine on guinea-pig ileum.

Antagonistic activity of cyproheptadine against common spasmogens, like acetylcholine, histamine, serotonin, bradykinin and angiotensin, was studied on isolated guinea-pig ileum. Cyproheptadine produced a reversible antagonism of non-competitive type and was most effective against serotonin. It was less potent against histamine, bradykinin and angiotensin and least potent against acetylcholine.