Effect of a crude extract of <i>Mandevilla velutina</i> on contractions induced by bradykinin and [des‐Arg<sup>9</sup>]‐bradykinin in isolated vessels of the rabbit

Calixto, João B.; Yunes, Rosendo A.

doi:10.1111/j.1476-5381.1986.tb16269.x

Cited by 25 publications

(11 citation statements)

References 16 publications

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“…As shown previously with the crude extract, in rat uterine muscle and in the isolated vessels of the rabbit (Calixto et al, 1985a;Calixto & Yunes, 1986), the onset of the BK antagonistic activity of these compounds isolated from M. velutina was rapid and was completely reversible following intermittent washing of the preparation for 30-60 min. Fraction 11 (-log g ml-') (Tallarida et al, 1979;Kenakin, 1982 (Calixto & Yunes, 1986), it is possible that these fractions now isolated from this plant, are active against both sub-types of kinin receptor. In addition the crude extract was also effective in antagonizing the endothelial-dependent vasodilatation induced by BK and L-BK in ring preparations of the dog femoral and mesenteric arteries, that had been precontracted with noradrenaline (Calixto et al, 1985b).…”

Section: Antagonistsupporting

confidence: 77%

Section: Introductionmentioning

confidence: 88%

“…The crude extract of this plant was also active in antagonizing BK-and L-BK-induced responses in other smooth muscles such as guinea-pig ileum, rat duodenum and dog mesenteric and femoral arteries (Calixto et al, 1985b). In addition, the crude extract selectively antagonized the contractile effect of BK mediated by both B.-and B2-receptors in rabbit vascular smooth muscles (Calixto & Yunes, 1986 (van Rossum, 1963). Once reproducible curves to a given agonist had been obtained, different concentrations of crude extract (0.5 to 2 mg 1') or the fractions isolated from M. velutina ( Table 1 and were determined by interpolation using regression analysis.…”

Section: Introductionmentioning

confidence: 99%

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Kinin antagonist activity of compounds from Mandevilla velutina in the rat isolated uterus

Calixto¹,

Nicolau²,

Pizzolatti

et al. 1987

British J Pharmacology

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1The effect of four semi-purified compounds obtained from Mandevilla velutina crude extract by silica gel chromatography fractionization were analysed for their inhibitory effects on uterine contractions induced by bradykinin (BK), lysylbradykinin (L-BK), acetylcholine (ACh) and oxytocin, in vitro.2 None of the compounds tested affected uterine tone. Pre-incubation for 20 min with fraction 12 (20 to 80plgmlm'), isolated from M. velutina produced a parallel and concentration-dependent displacement to the right of the concentration-response curves for BK and L-BK (1 to 1000 nM). Schild plots of these data were linear (correlation close to unity), and yielded a nominal pA2 value (as g ml-') of 5.1 and 4.9, respectively, and the values of the slopes were not significantly different from unity. Fraction 11 (10 to 40 ptg ml-') also produced a parallel and concentration-dependent displacement to the right of the BK concentration-response curve. The Schild plot gave a mean pA2 value (g ml-') of 5.4 and a slope not significantly different from unity. 3 Fraction 12 did not influence the uterine contractile responses induced by ACh (0.1 to 100gM) and oxytocin (0.01 to 30 miu ml-') at concentrations less than 80 pg ml-'.4 Fraction 16 (20 to 80 gml-') antagonized the action of BK only at concentrations greater than 40 ggml', whereas fraction 5 (20 to 80 ggml1') was completely inactive against BK-induced responses.5 As observed previously with the crude extract, the onset of the BK antagonistic action of these compounds was rapid and completely reversible following intermittent washing of the preparation for 30-60 min. 6 These results indicate the existence of at least two compounds in the crude extract of Mandevilla velutina that act as competitive and selective kinin antagonists on the isolated uterus of the rat.

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Section: Antagonistsupporting

confidence: 77%

Section: Introductionmentioning

confidence: 88%

Section: Introductionmentioning

confidence: 99%

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Kinin antagonist activity of compounds from Mandevilla velutina in the rat isolated uterus

Calixto¹,

Nicolau²,

Pizzolatti

et al. 1987

British J Pharmacology

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“…In further studies, we demonstrated that the CE of M. velutina also selectively antagonizes the contractile and relaxant responses caused by bradykinin and related kinins in the isolated guinea-pig ileum, rat duodenum and the endothelium-dependent vasodilation response caused by kinins in rings of mesenteric and femoral arteries of the dog [2][3][4]. The CE of M. velutina was also found to be active in antagonizing, in a selective and reversible manner, the contractile response induced by bradykirtin and [Des-Arg9]-bradykinin, mediated by both B 1 and B 2 bradykinin receptors in aorta, mesenteric and jugular vein from rabbits [5]. More recently, we isolated from the CE of M. velutina some nonpeptide pregnane compounds which antagonized in a selective manner the contractile response caused by bradykinin and lysyl-bradykinin in the isolated rat uterus and guinea-pig ileum [4,6,7].…”

Section: Introductionmentioning

confidence: 98%

Inhibition of rat paw oedema and pleurisy by the extract fromMandevilla velutina

et al. 1991

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This study reports the oral anti-inflammatory profile of the crude extract (CE) of Mandevilla velutina, a plant which has been previously demonstrated to selectively antagonize bradykinin response of the isolated tissues on rat paw oedema and pleurisy caused by different phlogistic agents. The CE (50 to 200 mg/kg), given 60 min before, inhibited in a dose-dependent manner bradykinin (BK) and cellulose sulphate-induced paw oedema, maximal inhibition of 59% and 65%, respectively. In the same range dose the CE also significantly antagonized pleural exudate and cell infiltration caused by these substances, maximal inhibition of 34% and 46%, respectively. In addition, the CE (100 and 200 mg/kg) also inhibited paw oedema induced by serotonin, PAF-acether and zymosan, maximal inhibition of 55%, 38% and 46%, respectively, but enhanced histamine oedema. However, the CE revealed only partial or no inhibition in pleural exudate caused by these agents. The CE (100 and 200 mg/kg) also inhibited in a dose and time-dependent manner carrageenan-induced paw oedema with a maximal inhibition of 44%, but only partially affected carrageenan-induced pleural exudate. The CE also partially inhibited dextran oedema, but even at a higher dose (400 mg/kg) it failed to interfere with Bothrops Jaracaca-induced paw oedema. The CE inhibited BK and to a lesser extent cellulose sulphate-induced cell migration, but failed to interfere with the differential leukocyte migration in the pleural cavity. These findings provide evidence that the CE from M. velutina, besides antagonizing kinin action, exhibit an oral anti-oedematogenic activity against a variety of phologistic agents, but it was more effective in inhibiting those models where kinins are more involved.

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“…The selective antagonism of M. velutina crude extract against bradykinin and its derivatives has been studied by various authors (Calixto et al, 1985;Calixto and Yunes, 1986;Calixto et al, 1987;Calixto and Yunes, 1990) and some active compounds in the extracts have been chemically characterized. The pregnane glycoside compounds isolated from M. velutina have been shown to be effective in antagonizing bradykinin (BK) responses in a variety of preparations and also exhibit potent and long-lasting analgesic, anti-inflammatory and anti-oedematogenic activities against a variety of inflammatory and fever-inducing phlogistic agents but was more effective in inhibiting processes involving kinins Henriques et al, 1991;Maraschin et al, 2000).…”

Section: Introductionmentioning

confidence: 99%

Antigenotoxic effects of Mandevilla velutina (Gentianales, Apocynaceae) crude extract on cyclophosphamide-induced micronuclei in Swiss mice and urethane-induced somatic mutation and recombination in Drosophila melanogaster

Silva

Sousa

Gräf³

et al. 2008

Genet. Mol. Biol.

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A Mandevilla velutina crude extract was investigated using the mouse micronucleus test (MNT) and the Drosophila melanogaster somatic mutation and recombination test (SMART) using standard (ST) and high bioactivation (HB) crosses. The MNT used 10 mg, 20 mg or 40 mg per 100 g of body weight (bw) of extract with and without 0.2 mg per 100 g bw peritoneal cyclophosphamide. There was no genotoxicity in the negative control or extract only groups and, compared to the cyclophosphamide control, there was a significant reduction in micronucleated polychromatic erythrocytes in all the groups given extract plus cyclophosphamide. For SMART larvae were fed 5 or 10 mg mL -1 of extract for seven days with and without 0.89 mg mL -1 of urethane given on day seven. The ST and HB flies showed no significant differences in spots between the negative control and the extract only groups. The number of urethane-induced spots was reduced by the highest concentration of extract for the ST flies and by both concentrations of extract for the HB flies. The results suggest that M. velutina extract is not genotoxic but is antigenotoxic.

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Effect of a crude extract of Mandevilla velutina on contractions induced by bradykinin and [des‐Arg⁹]‐bradykinin in isolated vessels of the rabbit

Cited by 25 publications

References 16 publications

Kinin antagonist activity of compounds from Mandevilla velutina in the rat isolated uterus

Kinin antagonist activity of compounds from Mandevilla velutina in the rat isolated uterus

Inhibition of rat paw oedema and pleurisy by the extract fromMandevilla velutina

Antigenotoxic effects of Mandevilla velutina (Gentianales, Apocynaceae) crude extract on cyclophosphamide-induced micronuclei in Swiss mice and urethane-induced somatic mutation and recombination in Drosophila melanogaster

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Effect of a crude extract of Mandevilla velutina on contractions induced by bradykinin and [des‐Arg9]‐bradykinin in isolated vessels of the rabbit

Cited by 25 publications

References 16 publications

Kinin antagonist activity of compounds from Mandevilla velutina in the rat isolated uterus

Kinin antagonist activity of compounds from Mandevilla velutina in the rat isolated uterus

Inhibition of rat paw oedema and pleurisy by the extract fromMandevilla velutina

Antigenotoxic effects of Mandevilla velutina (Gentianales, Apocynaceae) crude extract on cyclophosphamide-induced micronuclei in Swiss mice and urethane-induced somatic mutation and recombination in Drosophila melanogaster

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Effect of a crude extract of Mandevilla velutina on contractions induced by bradykinin and [des‐Arg⁹]‐bradykinin in isolated vessels of the rabbit