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Amélia T Henriques

Publications and source records attributed to Amélia T Henriques.

6 recordsLinked to original sources

Role of glutamate and dopamine receptors in the psychopharmacological profile of the indole alkaloid psychollatine.

Psychollatine (1), a new glycoside indole monoterpene alkaloid isolated from Psychotria umbellata, has shown an interesting psychopharmacological profile. This study aimed to investigate the role of NMDA glutamate and dopamine receptors in mediating the properties of 1. Psychollatine (1) was assessed for NMDA-induced seizures, MK-801-induced hyperlocomotion, amphetamine-induced lethality, and apomorphine-induced climbing behavior in mice. Psychollatine (1) (100 mg/kg) and MK-801 (0.3 mg/kg) prevented NMDA-induced seizures (P < 0.01), while 1 (100 mg/kg) attenuated the MK-801-induced hyperlocomotion (P < 0.05). Compound 1 (3 and 10 mg/kg), as well as chlorpromazine (4 mg/kg), prevented amphetamine-induced lethality (P < 0.05). Finally, 1 (10 mg/kg) (P < 0.05), MK-801 (0.2 mg/kg) (P < 0.01), and chlorpromazine (4 mg/kg) (P < 0.01) attenuated apomorphine-induced climbing behavior. The present results strongly support the involvement of NMDA glutamate receptors in the mode of action of psychollatine (1).

Amphetamine↗

Antitumor activity of three benzopyrans isolated from Hypericum polyanthemum.

In the present study we have investigated the in vitro antitumor effects of three benzopyrans, 6-isobutyryl-5,7-dimethoxy-2,2-dimethylbenzopyran (1), 7-hydroxy-6-isobutyryl-5-methoxy-2,2-dimethylbenzopyran (2) and 5-hydroxy-6-isobutyryl-7-methoxy-2,2-dimethylbenzopyran (3) isolated from Hypericum polyanthemum. The three compounds tested demonstrated potent growth inhibitory activity at 40 microg/ml (<25% control growth) in the NCI-H460, HT-29 and U-373MG human cell lines. Determination of cell cycle distribution demonstrated that the antiproliferative effect of the three benzopyrans could be associated to alterations in the cell cycle phase distribution. Treatment with the IC50 of the three compounds induced an arrested in S phase. Only in cells treated with compound 3 did the percentage of sub-G1 population increase up to 9%, suggesting that this compound induced more cell death than the others. Consistent with sub-G1 analysis, appreciable oligonucleosomal DNA fragmentation was only observed in the NCI-H460 cell line treated with compound 3. From these results it can be suggested that despite no differences among the cytotoxicity of the three compounds, it was observed that the mechanism of their antiproliferative effects appears to be different.

Antineoplastic Agents, Phytogenic↗

Benzophenones from Hypericum carinatum.

Two new benzophenones were isolated from the leaves of Hypericum carinatum. Their structures were established on the basis of 2D NMR spectroscopic analyses and mass spectrometry as cariphenone A (6-benzoyl-5,7-dihydroxy-2,2,8-trimethyl-2H-chromene) (1) and cariphenone B (8-benzoyl-5,7-dihydroxy-2,2,6-trimethyl-2H-chromene) (2). Five known compounds, the phloroglucinol derivative uliginosin B (3), 1-eicosanol, sitosterol, stigmasterol, and campesterol, were also characterized. Compounds 1-3 were evaluated for their total antioxidant capacity through a total radical-trapping parameter assay. Only compound 1 showed moderate antioxidant activity, exhibiting inhibition of chemiluminescence similar to that of quercetin at the same concentration.

Antioxidants↗

Psychopharmacological profile of the alkaloid psychollatine as a 5HT2A/C serotonin modulator.

Behavioral effects of psychollatine, a new glycoside indole monoterpene alkaloid isolated from Psychotria umbellata, was investigated in models of anxiety, depression, memory, tremor, and sedation related to 5-HT and/or GABA neurotransmission. The GABA antagonist picrotoxin and the 5-HT2 antagonist ritanserin were used to examine the role of GABA and 5-HT2 receptors in psychollatine-induced effects. In the light/dark and hole-board models of anxiety, diazepam (0.75 mg/kg) and psychollatine (7.5 and 15 mg/kg) showed anxiolytic-like effect at doses that do not increase sleeping time nor alter spontaneous locomotor activity. The anxiolytic effect of psychollatine was prevented by prior administration of ritanserin, but not of picrotoxin, indicating that 5-HT2 but not GABA receptors are implicated. In the forced swimming model of depression, psychollatine (3 and 7.5 mg/kg) effects were comparable to the antidepressants imipramine (15 mg/kg) and fluoxetine (20 mg/kg). Psychollatine suppressed oxotremorine-induced tremors in all doses. In the step-down learning paradigm, diazepam (0.85 mg/kg), MK-801 (0.15 mg/kg), and psychollatine 100 mg/kg impaired the acquisition of learning and memory consolidation, without interfering with retrieval. It is concluded that the effects of psychollatine at the central nervous system involve serotonergic 5HT2(A/C) receptors.

Anti-Anxiety Agents↗

N,beta-D-Glucopyranosyl vincosamide, a light regulated indole alkaloid from the shoots of Psychotria leiocarpa.

From leaves of Psychotria leiocarpa, an indole alkaloid was isolated to which the structure N,beta-D-glucopyranosyl vincosamide (1) was assigned. This represents the first report of an N-glycosylated monoterpenoid indole alkaloid. In field-grown plants highest amounts of 1 were found in the leaves (2.5% of dry wt) and fruit pulp (1.5% dry wt). Lower amounts were found in the stems (0.2% dry wt) and the seeds (0.1% of dry wt), whereas the alkaloid was not detected in the roots. The accumulation of 1 in aseptic seedlings was also restricted to the shoots and increased with plant age and light exposure, independent of the supply of sucrose in the culture medium.

Darkness↗

Isolation and on-line identification of antioxidant compounds from three Baccharis species by HPLC-UV-MS/MS with post-column derivatisation.

The aqueous extracts of aerial parts of Baccharis trimera (Less.) DC., B. crispa Spreng. and B. usterii Heering (Asteraceae) displayed significant radical scavenging activity in a diphenylpicrylhydrazole (DPPH)/TLC assay. In order to rapidly identify the active principles, the crude extracts were analysed by HPLC-UV, and an HPLC-micro-fractionation of the extract of B. usterii was performed. Six quinic acids derivatives (1-6) were isolated from B. usterii by MPLC. The fractions were monitored by DPPH/TLC assay and a series of radical-scavenging quinic acid derivatives could be identified. The comparison of the HPLC profiles of the extracts of B. usterii, B. trimera and B. crispa was performed. In order to obtain complementary on-line structural information for all peaks of interest, HPLC-MS/MS together with HPLC-UV involving post-column addition of UV shift reagents was undertaken on the crude extract. The interpretation of these data permitted the on-line identification of known compounds, some of which are reported for the first time in this plant.

Antioxidants↗