Search results for " Farm"
showing 10 items of 2009 documents
Aminoacidic derivatives as novel CNS-targeted neurotherapeutics
2012
Drug delivery to the CNS is subject to the permeability limitations imposed by the BBB that regulates movements of actives in and out of the brain. During the drug discovery phase a key aspect could be the selection of the compounds properties crucial for brain penetration. Novel CNS-targeted neurotherapeutics should possess the optimal characteristics that allow passive diffusion through the BBB via the transcellular route, or have the structural features necessary to serve as a substrate for one of the endogenous transport systems of the BBB. An attractive and rewarding chemistry-based strategy, employed to increase the CNS transport of poorly penetrating therapeutic agents, is the transi…
4,5,6,9-TETRAHYDROPYRROLO[2',3'-3,4]CYCLOEPTA[1,2-d]ISOSSAZOLE, PROCESS FOR THEIR PRODUCTION AND THEIR USES AS ANTITUMOR AGENTS
2016
The present invention concerns the synthesis of compounds bearing the PYRROLO[2',3'-3,4]CYCLOEPTA[1,2-d]ISOSSAZOLE structure, and their use for the treatment of pathologies having hyperproliferative features included those having neoplastic nature.
LE VARIANTI DEL GENE CYP2C19 NELLA FARMACO-GENOMICA DEL CLOPIDOGREL
2010
Il clopidogrel per espletare la propria funzione di antiaggregante piastrinica necessita l’intervento di diversi citocromi epatici. Le varianti del gene CYP2C19 sembrano influenzarne sensibilmente l’attivazione e pertanto l’azione farmacologica. Sono stati identificati tre alleli principali. L’allele CYP2C19*1 è il wild type e codifica per un enzima costituzionalmente attivo. Gli alleli CYP2C9*2 e CYP2C9*3 codificano invece per forme enzimatiche parzialmente funzionanti e sono responsabili sia in eterozigosi che in omozigosi della variazione di attività farmacologica. La valutazione delle varianti è stata eseguita mediante le metodiche PCR-RFLP e sequenziamento diretto. Abbiamo allestito du…
COUMARINS FROM CACHRYS SICULA L.
2017
One new coumarin, 8-hydroxymethylpsoralen (1), was isolated from the dried leaves of Cachrys sicula L. along with the known coumarins sprengelianin (2) and (RS)-oxypeucedanin (3). The structure of the new compound was elucidated on the basis of NMR and ESI-MS spectral analysis.
Hand-made paper obtained by green procedure of cladode waste of Opuntia ficus indica (L.) Mill. from Sicily
2019
Cellulosic fibres have been obtained by green procedures from the cladodes of Opuntia ficus indica (L.) Mill., constituting a large agro industrial waste in our territory. The materials have been analysed for its relative composition, applying, IR and TG methodologies and it was characterised by the absence of lignin. The fibrous material allowed the manufacture of a handmade paper obtaining an ecological material suitable for packaging purposes. The authors evidenced that the simple protocol based on hot water treatment was able to decrease the amount of hemicellulose in the final material.
PHEA-graft-polymethacrylate supramolecular aggregates for protein oral delivery
2013
Abstract Salmon calcitonin (sCT) is characterized by a poor oral availability. A new copolymer, β-poly(N-2-hydroxyethyl)-graft-{N-2-ethylene[2-poly(methacrylic acid sodium salt)isobutyrate]}- d , l -aspartamide (PHEA-IB-p(MANa + )), was designed for the oral administration of sCT through the formation of supramolecular aggregates (SAs) based on electrostatic interactions. Several sCT/PHEA-IB-p(MANa + ) weight ratios were characterized by turbidimetry, DLS, zeta potential, and microscopy analysis. After the incubation of sCT/PHEA-IB-p(MANa + ) complex with digestive enzymes, 10% (w/w) of loaded sCT was released in the native form. In vitro investigation was carried out to determine the copol…
Composite Hydrogels of Alkyl Functionalized Gellan Gum Derivative and Hydroxyapatite/Tricalcium Phosphate Nanoparticles as Injectable Scaffolds for b…
2021
An alkyl functionalized gellan gum derivative was here used to produce hydrogels containing hydroxyapatite and tricalcium phosphate nanoparticles as injectable nanostructured scaffolds for bone regeneration. The amphiphilic nature of the polysaccharide derivative along with its thermotropic behavior and ionotropic crosslinking features made possible to produce injectable bone mimetic scaffolds that can be used to release viable cells and osteoinductive biomolecules. The influence of different nanoparticles concentration on the rheological and physicochemical properties of the injectable systems was studied. We found that the presence of inorganic nanoparticles reinforces the three-dimension…
Histone deacetylase inhibition modulates deoxyribonucleotide pools and enhances the antitumor effects of the ribonucleotide reductase inhibitor 3’-C-…
2011
Histone deacetylase (HDAC) inhibitors are a new class of epigenetic agents that were reported to enhance the cytotoxic effects of classical anticancer drugs through multiple mechanisms. However, which of the possible drug combinations would be the most effective and clinically useful are to be determined. We treated the HL60 and NB4 promyelocytic leukaemia cells with a combination of the ribonucleotide reductase (RR) inhibitor 3'-C-methyladenosine (3'-Me-Ado) and several hydroxamic acid-derived HDAC inhibitors, including two recently synthesized molecules, MC1864 and MC1879, and the reference compound trichostatin A (TSA). The results showed significant growth inhibitory and apoptotic syner…
Patterns of Innate or Acquired Resistance to Anticancer Drugs: Our Experience to Overcome It
2021
Drug resistance, which is often of a multiple type, can be defined as the ability of cancer cells to obtain resistance to both conventional and novel chemotherapy agents. It remains a major problem to solve in cancer therapy. The mechanisms of resistance are multifactorial, and in our cellular models of acute myeloid leukemia, hepatocellular carcinoma, and triple-negative breast cancer, it involves the NF-κB pathway. In our opinion, multitarget molecules can be considered as privileged compounds capable of attacking and reversing the resistant phenotype. In the phenomena of both innate and acquired drug resistance that we have been studying since 1998 to today and up to 2016 under the guida…
STAT5 and STAT5 Inhibitors in Hematological Malignancies
2019
The JAK-STAT pathway is an important physiologic regulator of different cellular functions including proliferation, apoptosis, differentiation, and immunological responses. Out of six different STAT proteins, STAT5 plays its main role in hematopoiesis and constitutive STAT5 activation seems to be a key event in the pathogenesis of several hematological malignancies. This has led many researchers to develop compounds capable of inhibiting STAT5 activation or interfering with its functions. Several anti-STAT5 molecules have shown potent STAT5 inhibitory activity in vitro. However, compared to the large amount of clinical studies with JAK inhibitors that are currently widely used in the clini…