[Chemical and pharmacological research on derivatives of 1H-naphtho-(2,1-b)pyran. II. Synthesis of 1-oxo-2-dialkylaminomethyl-3-dialkylamino-1H-naphtho(2,1-b)pyran].
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Animals↗
Biomedical subjects
M Mazzei
Publications and source records attributed to M Mazzei.
The paper electrophoretic study of ion pair formation. 3. Ion pair formation with quaternary ammonium ions.
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Chemical Phenomena↗
Inhibition of neutrophil O(2)(-) production by unsymmetrical methylene derivatives of benzopyrans: their use as potential antiinflammatory agents.
Some unsymmetrical derivatives of benzopyrans 9 were synthesized and tested to verify their PKC inhibitory activity. For this purpose, the Mannich bases of 7-hydroxycoumarins 6 were treated with 2-(dialkylamino)benzopyran-4-ones or 3-(dialkylamino)naphtho[2,1-b]pyran-1-ones 8 in the presence of acetic or propionic anhydride, yielding compounds 9. Human neutrophils stimulated with either PMA and f-MLF were used as the cellular model. The efficiency of the compounds 9 was established on their capacity to reduce the O(2)(-) production by activated human neutrophils. Compounds 9d and 9f, bearing an acetoxy group in position 7 of the chromone moiety, seem to counteract the neutrophil activation efficiently.
Anti-Inflammatory Agents↗
Histological and immunohistochemical study of the bronchial stump with flap coverage in an animal model.
OBJECTIVE: The purpose of our study was to evaluate the healing process of the bronchial stump after pneumonectomy reinforced with different pedicled flaps in an animal model. The specimens were analyzed by means of histology and immunohistochemistry. MATERIALS AND METHODS: We have considered 45 New Zealand White male rabbits that underwent a left pneumonectomy under general anesthesia. Nine animals had no bronchial coverage and represented the controls. The other 36 rabbits were divided into three groups of 12 and had bronchial coverage with either diaphragmatic, intercostal or pericardial flaps. The histological examinations were performed on the animals sacrificed 7, 14 and 30 days after surgery. Immunohistochemical analyses were done on the specimens on postoperative day 7 and 14. On postoperative day 7, the specimens were examined for expression of proliferating cell nuclear antibody (PCNA) expression. On postoperative day 14, neoangiogenesis was measured by CD31 expression. The measurements of antibody expression were done with a computer-assisted morphometric count and analyzed with the t test. RESULTS: On postoperative day 14, standard histology showed more evident neoangiogenesis in the bronchial stump specimens covered with intercostal and diaphragmatic flaps compared to pericardial flaps and controls. The immunohistochemical evaluation of PCNA by morphometric computer-assisted analysis did not show any statistically significant differences among the groups. The CD31 morphometric count revealed a higher and statistically significant antibody expression in muscular flaps compared to pericardial flaps and controls. CONCLUSIONS: Our study showed that bronchial coverage with a pedicled muscular flaps promotes the production of new vessels and gives the possibilities to optimize the healing process of a bronchial stump after pneumonectomy.
Animals↗
Unsymmetrical methylene derivatives of indoles as antiproliferative agents.
Indole-3-carbinol is a natural product which has been shown to reduce the incidence of spontaneous and carcinogen-induced mammary tumours in animals. Eighteen unsymmetrical methylene derivatives of indoles were prepared by reaction of Mannich bases of 7-hydroxycoumarins with substituted indoles in acetic or propionic anhydride. The synthesised molecules were tested in vitro against the MCF7 and MDA-MB-231 breast cancer cell lines by MTT and cell count assays. Results from 16 tested compounds showed that 60% of them exerted some effects against the MDA-MB-231 compared to about 30% towards the MCF7. Among all, the 3-(7'-acetoxy-4-methylcoumarin-8'-yl)methyl-2-methylindole resulted the most effective in both cell lines, compared to indole-3-carbinol. In conclusion, these preliminary results report that some of these compounds might be promising potential antiproliferative agents.
Adenocarcinoma↗
Methyleugenol and eugenol variation in Ocimum basilicum cv. Genovese gigante grown in greenhouse and in vitro.
The variation of the two main aromatic compounds in Ocimum basilicum cv Genovese Gigante grown in greenhouse and "in vitro" was analyzed. The content of methyleugenol and eugenol was correlated to the plants' height rather than to the plants' age and the growth site. Particularly, methyleugenol was prevalent in plants up to 6.5 cm, as plants grew it was replaced by eugenol that was dominant in taller plants. Analysis of basil 20 cm in height showed that methyleugenol is prevalently localized in the low part while eugenol is prevalent in the upper part of the plant. Moreover, a chronic and acute toxicity of methyleugenol was evidentiated in an assay using chicken embryos.
Eugenol↗
Toxicological studies of photosensitizer agents and photodegradable polyolefins.
The authors report the results of a series of toxicological tests conducted on plastic materials (polyethylene) activated with tetraphenylbutadiene (TPB) an additive recently proposed as a sensitizer capable of photodegrading plastic materials. The toxic effects of polyethylene, TPB, and TPB's degradation products were investigated in rabbits, mice and rats. The studies revealed these products to possess a very low toxicity.
Animals↗
[Report on an experimental study with a new psychopharmacological agent: AF 1161 (trazodone)].
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Antidepressive Agents↗
[Clinical and electroencephalographic correlations in a group of children with cerebral paralysis].
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Adolescent↗
HPLC separation of toxic fraction components extracted from planktonic and benthic Cnidaria.
HPLC separation of crude extract components derived from nematocysts and extranematocystic tissues of macroplanktonic jellyfish Aequorea aequorea and Rhizostoma pulmo and benthic sea-anemones Actinia equina and Anemonia sulcata was carried out by different columns. A satisfactory peak separation was obtained analyzing the toxin of Rhizostoma pulmo by cationic and C18 columns. Low molecular weight fragments were separated by C18 column and U.V. monitored varying pH values and obtaining the displacement of significant peaks. Clear differences between chromatographic plots concerning planktonic and benthic species was evidenced by anionic column; this result can point out a clear ecological analogy between species living in the same environment and a similar toxin biosynthesis, due to selective actions related to both the environment and the phylogenetic relationships; these organisms could have developed similar mechanisms useful to tackle the environment.
Animals↗
Anti-PKC activity of some 3-(dialkylamino)-1H-naphtho [2,1-B] pyran-1-ones.
Some 3-(dialkylamino)-1H-naphtho [2,1-b] pyran-1-ones were tested to evaluate their ability to inhibit Protein Kinase C (PKC) activation. The model consisted in the detection of the superoxide anion in activated neutrophils. Naphthopyrans carrying 3-(diethylamino), 3-(1-piperidinyl) and 3-[bis(2-methoxyethyl)amino] groups emerged as the most active ones. Introduction of alkoxy groups in position 8 and 9 and of bromo substituent in position 8 on the naphthalene moiety was associated with an increase in anti-PKC activity. No activity was found when an electron withdrawing group was placed in position 2 of the 3-(dialkylamino)-1H-naphtho [2,1-b] pyran-1-ones.
Enzyme Inhibitors↗