781 research outputs found
Antiprotozoal activity of novel diaryliminophenazines
No full textRecently, we synthesized a set of novel iminofenazines bearing a bicyclic basic head linked through an alkyl chain to the imino nitrogen in position 3 on the phenazine nucleus (Fig.1).
Most of these compounds inhibited the growth of different species of Leishmania promastigotes as well as of chloroquine sensitive (CQ-S) and chloroquine resistant (CQ-R) strains of P. falciparum with IC50 in the submicromolar range. Unfortunately, these compounds exhibited also a significant toxicity against the human endothelial cell line HMEC-1 with IC50 in the low micromolar range and with a consequent low selectivity index.
Figure1.Structures of the previously synthesized compounds.
To continue the studies on the antiprotozoal potentialities of this class of compounds and with the aim to improve their activity and selectivity on protozoa, we have now synthesized novel compounds characterized by the replacement of the aniline moiety in pos. 2 of the phenazine nucleus with an aminopyridine, and/or by a quaternarization of the basic nitrogen in the side chain with a methyl group (Fig.2).
Figure 2. Structures of the new compounds synthesized.
The in vitro activity of the new compounds on Leishmania promastigotes and on CQ-S and CQ-R strains of P. falciparum, as well as on the HMEC-1 cell line will be presented and discussed.
References
[1] A. Barteselli, M. Gavazzi, N. Basilico, S. Parapini, D. Taramelli, A. Sparatore. Clofazimine analogs with antileishmanial and antimalarial activities. XXII National Meeting on Medicinal Chemistry, Roma 2013
Photography as Criticism: Gabriele Basilico and the Project of a “Small Utopia”
No full textThe camera has been used as a tool of architectural representation since the mid-19th century. But can photography be rightly considered a form of criticism? Affirmative answers are suggested by the works of several architects who have embraced this medium to explore the built environment and reflect upon its material and social conditions. Indeed, the writer and photographer Eric de Maré went as far as pronouncing that the photographer was possibly the best architectural critic. In the late-20th century, a key role was played by Gabriele Basilico, who set out to depict the mutation of urban landscapes under the effects of deindustrialisation. Working for magazines as well as for public institutions, the late Italian photographer developed an analytical method that allowed him to probe the complexity of cities as human habitats. The paper revisits Basilico’s early work and discusses its relevance to architectural criticism. It argues, with reference to a series of photographic journeys that span from the 1970s to the 1990s, that his landscape vision was integral to a wider rethinking of the built environment. Driven by a relentless pursuit of harmony, Basilico sought out an intimate relation with places while eschewing the eulogistic rhetoric that dominated in the architectural press. His contemplative images contain the seeds of what he called a “small utopia”: a personal quest nourished by critical dialogues with writers, journalists and architects
Linaria officinarum, Basilico, Sisaro
No full text1. Nome scientifico: Linaria vulgaris Miller
(Scrophulariaceae)
Nome attuale: Linaiola
2. Nome scientifico: Ocimum basilicum L.
(Lamiaceae, Labiatae)
Nome attuale: Basilico
3. Nome scientifico: Sium sisarum L.
(Apiaceae, Umbelliferae)
Nome attuale: Sisaro, Sedanin
Results on geoneutrinos at Borexino
No full textThe latest and more complete geo-neutrinos Borexino results, are briefly presented and discussed. Borexino is a liquid scintillator detector located at the Gran Sasso National Laboratory in Italy, whose primary purpose is the real-time spectroscopy of low energy solar neutrinos. It is the only experiment so far to have provided an evidence of geo-neutrinos existence beyond a 5σ significance level. The geo-neutrinos measurement and analysis, along with implications from the geological point of view, are shortly discussed
Antiplasmodial triterpenoids from the fruits of neem, Azadirachta indica.
No full textJ Nat Prod. 2010 Aug 27;73(8):1448-52.
Antiplasmodial triterpenoids from the fruits of neem, Azadirachta indica.
Chianese G, Yerbanga SR, Lucantoni L, Habluetzel A, Basilico N, Taramelli D, Fattorusso E, Taglialatela-Scafati O.
Abstract
Eight known and two new triterpenoid derivatives, neemfruitins A (9) and B (10), have been isolated from the fruits of neem, Azadirachta indica, a traditional antimalarial plant used by Asian and African populations. In vitro antiplasmodial tests evidenced a significant activity of the known gedunin and azadirone and the new neemfruitin A and provided useful information about the structure-antimalarial activity relationships in the limonoid class
Standardization of the physicochemical parameters to assess in vitro the β-hematin inhibitory activity of antimalarial drugs
No full textIntraerythrocytic plasmodia form hemozoin as a detoxification product of hemoglobin-derived heme. An identical substance. β-hematin (BH), can be obtained in vitro from hematin at acidic pH. Quinoline-antimalarials inhibit BH formation. Standardization of test conditions is essential for studying the interaction of compounds with this process and screening potential inhibitors. A spectrophotometric microassay of heme polymerization inhibitory activity (HPIA) (Basilico et al., Journal of Antimicrobial Chemotherapy 42, 55-60. 1998) previously reported was used to investigate the effect of pH and salt concentration on BH formation. The yield of BH formation decreased with pH. Moreover, under conditions used in the above HPIA assay (18 h, 37°C, pH = 2.7), several salts including chloride and phosphate inhibited the process. Aminoquinoline drugs formulated as salts (chloroquine-phosphate, primaquine-diphosphate), but not chloroquine-base, also inhibited the reaction. Interference by salts was highest at low pH and decreased at higher pH (pH 4). Here, we describe different assay conditions that eliminate these problems (BHIA, β-hematin inhibitory activity). By replacing hematin with hemin as the porphyrin and NaOH solution with DMSO as solvent, the formation of BH was independent of pH up to pH 5.1. No interference by salts was observed over the pH range 2.7-5.1. Dose-dependent inhibition of BH formation was obtained with chloroquine-base, chloroquine-phosphate, and chloroquine-sulfate at pH 5.1. Primaquine was not inhibitory. The final product, characterized by solubility in DMSO, consists of pure BH by FT-IR spectroscopy. The BHIA assay (hemin in DMSO, acetate buffer pH 5 ± 0.1. 18 h at 37°C) is designed to screen for those molecules forming π-π interactions with hematin and thus inhibiting β-hematin formation
INDAGINE SULLA GESTIONE ODORI NEGLI IMPIANTI DI TRATTAMENTO DELLE ACQUE REFLUE NELLE PROVINCE DI VARESE E COMO
No full textPresentazione fatta in occasione del Convegno: "LA GESTIONE DEGLI ODORI NEGLI IMPIANTI DI TRATTAMENTO ACQUE E RIFIUTI LIQUIDI", organizzato da Seam Engineering S.r.l., in data 25 ottobre 2013, presso il Parco Scientifico Tecnologico ComoNExT. Il Convegno è stato occasione di incontro con esperti del settore e sono stati presentati i risultati di un'indagine sull'impatto odorigeno e sugli accorgimenti gestionali per ridurlo condotta presso un campione rappresentativo di impianti di depurazione ricadenti nel territorio delle Province di Varese e di Como
Evaluating the Efficiency of Frontier-based Exploration Strategies
No full textExploration and mapping are fundamental prerequisites for autonomous robots operating in initially unknown environments. In this paper, we evaluate simple yet efficient frontier-based exploration strategies. Furthermore, we discuss improvements to the classic frontier-based exploration strategy by Yamauchi et al. that further shorten the resulting exploration paths and present results from a comparative evaluation with a reference exploration strategy taken from the literature
Ruolo dell’analgesia preventive e anticipate in chirurgia toracica
No full textBackground: la possibiltà di controllare il dolore nel periodo postoperatorio gioca sicuramente un ruolo di primaria importanza nell'alleviare la sofferenza del paziente, durante gli effetti dannosi, abbreviare la degenza opsedaliera e i costi di assistenza. A causa della sua particolare intensità, il dolore di tipo nocicettivo e neuropatico provocato dall'incisione toracotomica rappresenta una delle situazioni a maggior impatto per lo sviluppo di complicanze postoperatorie, ed il suo controloo può rappresentare più che per le altre classi di intervento una significativa opportunità nell'influenzare l'outcome del paziente.
Scopo di questo studio randomizzato e in doppio cieco è quello di analizzare gli effetti del blocco intercostale e dell'uso degli antagonisti e dei recettori N-metil-D-aspartato (NMDA) per valutare l'efficacia dell'analgesia preventiva e dell'analgesia anticipata in chirurgia toracica.
Materiali e metodi: sono stati arruolati 53 pazienti consecutivi sottoposti a toracotomia posterolaterale presoo la nostra Unità Operativa. Sono stati randomizzati in 4 gruppi in base al diverso schema di analgesia usato. I soggetti del gruppo A ricevevano il blocco dei nervi intercostali con bupivacaina da T2 a T10 e assumevano destrometorfano per os preoperatoriamente. I soggetti del gruppo B, blocco intercostale e placebo preoperatoriamente. I soggetti del gruppo C blocco intercostale al termine della procedura chirurgica e destrometorfano preoperatoriamente. I soggetti del gruppo D infine, blocco intercostale al termine della procedura chirurgica e placebo preoperatoriamente. Per tutti i pazienti sono stati rilevati i livelli di dolore utilizzando una scala analogica visiva ed il consumo di farmaci antidolorifici nei tre mesi successivi l'intervento chirurgico.
Risultati: sono stati inclusi nello studio 28 maschi e 25 femmine. I 4 gruppi sono risultati confrontabili rispetto all'età, procedura chirurgica e funzionalità respiratoria preoparatoria. Nelle prime ore dopo l'intervento chirurgico, i livelli di dolore più bassi si sono registrati nei pazienti del gruppo Ce D. I livelli di dolore e consumi di antidolorifici si sono mantenuti più bassi durante i giorni successivi fino alla dimissione nei soggetti dei gruppi A e B, presentandosi più alti in aprticolare nel gruppo D. Nessun vanatggio è risultato nell'uso del destrometorfano sia pre che post operatoriamente.
Conclusioni: il blocco intercostale con bupivacaina sembra ridurre l'intensità del dolore postoperatorio el'incidenza della sindrome nevralgica posttoracotomica
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