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Biomedical subjects

José Maria Barbosa-Filho

Publications and source records attributed to José Maria Barbosa-Filho.

12 recordsLinked to original sources

Anti-allergic properties of Cissampelos sympodialis and its isolated alkaloid warifteine.

Development of new agents capable of regulating eosinophilic inflammation can uncover novel therapeutic approaches for the treatment of allergic diseases, such as asthma. Here, we evaluated the anti-allergic properties of an extract of the Brazilian Menispermaceae Cissampelos sympodialis, focusing on its effects on allergic eosinophilia. By studying two models of allergic inflammation, an asthma model and the allergic pleurisy in actively sensitized Balb/c mice, we observed that the oral pre-treatment with C. sympodialis reduced pleural eosinophil influx triggered by allergen challenge in a dose-dependent manner. The mechanism involved in C. sympodialis inhibitory effect appeared to be independent of a direct effect on eosinophil locomotory machinery, but depend on a blockage of eotaxin production, a key eosinophil chemoattractant with important roles in allergic reactions. C. sympodialis was also able to affect eosinophil activation, as attested by its ability of inhibiting formation of new cytoplasmic lipid bodies and the secretion of cysteinyl leukotrienes. The alkaloid warifteine isolated from the C. sympodialis extract represents an active component responsible for the anti-eosinophilic effects of the extract, since warifteine was able to reproduce C. sympodialis inhibitory effects on allergic eosinophilia and cysteinyl leukotrienes production. Of interest, C. sympodialis and warifteine post-treatments also effectively inhibited eosinophilic reaction observed after allergic challenge. Therefore, C. sympodialis/warifteine may be a promising anti-allergic therapy, inasmuch as it presents potent anti-eosinophil and anti-leukotrienes activities.

Alkaloids↗

Anxiolytic-like effects of (O-methyl)-N-2,6-dihydroxybenzoyl-tyramine (riparin III) from Aniba riparia (Nees) Mez (Lauraceae) in mice.

This work presents behavioral effects of (O-methyl)-N-2,6-dihydroxybenzoyl-tyramine (riparin III) isolated from the unripe fruit of Aniba riparia (Nees) Mez (Lauraceae) in animal models of open field, rota rod, elevated plus maze and hole board tests in mice. Riparin III (ripIII) was administered orally, in male mice, at single doses of 25 and 50 mg/kg. The results showed that ripIII, at both doses, had no effects on the spontaneous motor activity in the rota rod test nor in the number of squares crossed in the open field test. However, riparin III decreased the number of grooming and rearing. In the plus maze test, ripIII, at both doses increased the following parameters: percentage of entries in the open arms (PEOA), time of permanence in the open arms (TPOA) and percentage of time of permanence in the open arms (PTOA) and at the dose of 50 mg/kg, increased the number of entries in the open arms (NEOA). Similarly, ripIII, at both doses, showed an increase in the number of head dips into the holes of the hole board test. These results show that riparin III presents anxiolytic effects in the plus maze and hole board tests which are not influenced by the locomotor activity in the open field test.

Animals↗

Antianxiety effects of riparin I from Aniba riparia (Nees) Mez (Lauraceae) in mice.

This work presents the behavioral effects of riparin I (methyl ether of N-benzoyl tyramine) from unripe fruit of Aniba riparia (Lauraceae) on the elevated plus maze, open field, rota rod and hole board tests in mice. Riparin I was administered acutely by intraperitoneal (i.p.) and oral routes to male mice at doses of 25 and 50 mg/kg. The results showed that riparin I (25 and 50 mg/kg, i.p. and per os) increased the number of entries and the time of permanence in the open arms in the plus maze test. Similarly, in the hole board test, riparin I in both routes increased the number of head dips. Riparin I with both doses and routes had no effects on spontaneous motor activity in mice or in the rota rod test, but decreased the number of groomings. These results showed that riparin I by both administration routes has effects on the central nervous system with antianxiety effects on the plus maze and hole board tests. The substance is devoid of myorelaxant effects.

Animals↗

Chemical constituents from Tillandsia recurvata.

The CHCl3 extract of Tillandsia recurvata yielded 5,3'-dihydroxy-6,7,8,4'-tetramethoxyflavanone (1), 1,3-di-O-cinnamoyl-glycerol (2) and ethyl ester of caffeic acid. Their structures were elucidated by means of spectroscopic methods such as mass spectroscopy and 1 and 2D-NMR.

Cinnamates↗

Cardiovascular effects induced by reticuline in normotensive rats.

The cardiovascular effects of reticuline, isolated in a pure form from the stem of Ocotea duckei Vattimo, were studied in rats by using a combined in vivo and in vitro approach. In normotensive rats, reticuline (5, 10 and 20 mg/kg, i. v., randomly) injections produced an intense hypotension. This hypotensive response was attenuated after either, L-NAME (20 mg/kg, i. v.), a nitric oxide (NO) synthase inhibitor, or atropine (2 mg/kg, i. v.), a muscarinic receptor antagonist. In isolated rat aortic rings with intact endothelium, reticuline (3 x 10 ( - 6), 3 x 10 ( - 5), 3 x 10 ( - 4), 9 x 10 ( - 4) and 1.5 x 10 ( - 3) M) inhibited in a concentration-dependent manner the contractions induced by phenylephrine (1 microM), KCl (80 mM) and KCl (30 mM), [IC (50) = (0.4 +/- 0.1, 2.4 +/- 0.4 and 3 +/- 0.4) x 10 ( - 4) M, respectively). The effect of reticuline on phenylephrine-induced contractions was attenuated by removal of the vascular endothelium [IC (50) = (2.5 +/- 0.7) x 10 ( - 4) M]. Similar results were obtained after pretreatment of the rings with L-NAME 100 microM [IC (50) = (1.3 +/- 0.1) x 10 ( - 4) M], L-NAME 300 microM [IC (50) = (3 +/- 0.3) x 10 ( - 4) M] or atropine 1 microM [IC (50) = (1.2 +/- 0.2) x 10 ( - 4) M]. On the other hand, the effect of reticuline on phenylephrine-induced contractions was not affected by indomethacin 1 microM [IC (50) = (0.7 +/- 0.3) x 10 ( - 4) M]. Reticuline (3 x 10 ( - 6), 3 x 10 ( - 5), 3 x 10 ( - 4), 9 x 10 ( - 4) and 1.5 x 10 ( - 3) M) antagonized CaCl (2)-induced contractions, and also inhibited the intracellular calcium dependent transient contractions induced by norepinephrine (1 microM), but not those induced by caffeine (20 mM). These results suggest that the hypotensive effect of reticuline is probably due to a peripheral vasodilation in consequence of: 1) muscarinic stimulation and NOS activation in the vascular endothelium, 2) voltage-dependent Ca (2+) channel blockade and/or 3) inhibition of Ca (2+) release from norepinephrine-sensitive intracellular stores.

Alkaloids↗

Bowdichine, a new diaza-adamantane alkaloid from Bowdichia virgilioides.

A novel alkaloid named bowdichine (1), only the third with a diaza-adamantane skeleton containing an unusual N-acetyl enamine moiety, and the known alkaloids acosmine (2), ormosanine (3) and podopetaline (4) have been isolated from the stem bark of Bowdichia virgilioides. The structures were elucidated on the basis of spectral data, mainly 1D and 2D NMR of the diaza-adamantane alkaloids 1 and 2.

Adamantane↗

Warifteine and milonine, alkaloids isolated from Cissampelos sympodialis Eichl: cytotoxicity on rat hepatocyte culture and in V79 cells.

Two alkaloids were isolated from the leaves of Cissampelos sympodialis; a bisbenzylisoquinoline compound named warifteine and a novel 8,14-dihydromorphinandienone alkaloid named milonine. The cytotoxic effects of these alkaloids were assayed in cultured hepatocytes and V79 fibroblasts. Three independent endpoint assays for cytotoxicity in vitro were used: the nucleic acid content (NAC), tetrazolium reduction (MTT) and neutral red uptake (NRU). Milonine was less toxic than warifteine in both cell cultures. The IC50 values determined in the three different viability assays were around 100 and 400 microM after milonine treatment of V79 cells or hepatocytes. IC50 values ranging from 10 to 35 microM were obtained for warifteine in the viability tests evaluated in V79 cells and hepatocytes. Due to the similar cytotoxic effects detected on V79 cells and hepatocytes, probably warifteine and milonine induced toxic effects independent to the cytochrome P450. This hypothesis was corroborated by the results where Cimetidine (1.0 mM), a traditional cytochrome P450 inhibitor, did not protect the cells from the toxic action of warifteine or milonine. In conclusion, these alkaloids merit further investigations as potential novel pharmacological agents although milonine was less toxic than warifteine in the cells models investigated.

Alkaloids↗

Evaluation of the mutagenic potential of yangambin and of the hydroalcoholic extract of Ocotea duckei by the Ames test.

Ocotea duckei Vattimo is a plant popularly known as "louro-de-cheiro" found in the northeast of Brazil. Traditional medicinal uses of this plant are not known, but recent pharmacological studies with the isolated major constituent yangambin have shown various qualities: platelet activating factor (PAF) antagonist, protective effects against cardiovascular collapse and anaphylactic shock, anti-allergic properties, analgesic activity, and depressant effect in the central nervous system. In this work, the Ames test was used to evaluate the mutagenic potential of the hydroalcoholic extract of O. duckei leaves and of yangambin. Using TA97a, TA98, TA100, TA102 and TA1535 strains of Salmonella typhimurium, positive results were obtained only with the hydroalcoholic extract, with or without metabolic activation. Yangambin was not mutagenic, which is of interest due to its pharmacological properties.

Alcohols↗

Nb-benzoyltryptamine derivatives with relaxant activity in guinea-pig ileum.

A series of derivatives analogous to Nb-benzoyltryptamine were synthesized by the Schotten-Bauman procedure. The products obtained were: Nb-4-methoxy-benzoyltryptamine, Nb-2,4-dimethoxy-benzoyltryptamine, Nb-3,4-dimethoxy-benzoyltryptamine, Nb-3,4-methylenedioxy-benzoyltryptamine and Nb-3,4,5-trimethoxy-benzoyltryptamine. They were characterized through the usual spectrometric methods (UV, IR, 1H and 13C NMR) and showed non-selective relaxant activity in guinea-pig ileum pre-contracted with acetylcholine, histamine and KCl.

Acetylcholine↗