Search results for "010404 medicinal & biomolecular chemistry"
showing 10 items of 373 documents
Minkowski-Lorentz Spaces Applications: Resolution of Apollonius and Dupin Problems
2019
International audience
Dual Cherenkov Radiation-Induced Near-Infrared Luminescence Imaging and Photodynamic Therapy toward Tumor Resection
2020
International audience; Cherenkov radiation (CR), the blue light seen in nuclear reactors, is emitted by some radiopharmaceuticals. This study showed that (1) a portion of CR could be transferred in the region of the optical spectrum, where biological tissues are most transparent: as a result, upon radiance amplification in the near-infrared window, the detection of light could occur twice deeper in tissues than during classical Cherenkov luminescence imaging and (2) Cherenkov-photodynamic therapy (CR-PDT) on cells could be achieved under conditions mimicking unlimited depth using the CR-embarked light source, which is unlike standard PDT, where light penetration depth is limited in biologi…
New amide and dioxopiperazine derivatives from leaves of Breynia nivosa
2017
The first chemical investigation of leaves of Breynia nivosa from Nigeria resulted in the isolation of two new amide derivatives breynivosamides A and B (1 and 2) and two new dioxopiperazine derivatives breynivosines A and B (4 and 5) together with seven known compounds (3, 6-11). The structures of the new compounds were elucidated by 1D, 2D NMR and HRESIMS data as well as by comparison with the literature. All isolated compounds were tested for the cytotoxic and antimicrobial activities. Only cristatin A (6) showed cytotoxicity against the L5178Y mouse lymphoma cell line with an IC50 value of 13.9μM while breynivosamide A (1) exhibited moderate antimicrobial activity against Mycobacterium …
Structural Optimization of a Pyridinylimidazole Scaffold: Shifting the Selectivity from p38α Mitogen-Activated Protein Kinase to c-Jun N-Terminal Kin…
2018
Starting from known p38α mitogen-activated protein kinase (MAPK) inhibitors, a series of inhibitors of the c-Jun N-terminal kinase (JNK) 3 was obtained. Altering the substitution pattern of the pyridinylimidazole scaffold proved to be effective in shifting the inhibitory activity from the original target p38α MAPK to the closely related JNK3. In particular, a significant improvement for JNK3 selectivity could be achieved by addressing the hydrophobic region I with a small methyl group. Furthermore, additional structural modifications permitted to explore structure–activity relationships. The most potent inhibitor 4-(4-methyl-2-(methylthio)-1H-imidazol-5-yl)-N-(4-morpholinophenyl)pyridin-2-a…
Phytochemical analysis ofAchillea ligusticaAll. from Lipari Island (Aeolian Islands)
2016
A complete chemical investigation of Achillea ligustica All. growing at Lipari (Aeolian Island, Sicily) has been carried out. Seventeen metabolites have been isolated and characterised from dichloromethane and methanol extracts of flowers and aerial parts, and GC/MS analyses of petroleum ether extracts was carried out, revealing a composition in sesquiterpenoids similar to those reported for populations from Greece, Sicily and Algeria, showing the presence of (3RS,6RS)-2,6-dimethyl-1,7-octadiene-3,6-diol (1), 2,6-dimethyl-octa-3(E),7-diene-2,6-diol (2), iso-seco-tanapartholide (3) from DCM fraction. In addition from the methanolic extract of the aerial parts, peculiar flavonoid glucuronides…
Sesquiterpenoids from the Endophytic Fungus Rhinocladiella similis
2019
Ten new sesquiterpenoid derivatives, rhinomilisins A-J (1-10), along with six known analogues (11-16), were isolated from the mangrove-derived endophytic fungus Rhinocladiella similis. The structures of the new compounds were elucidated by their NMR and MS data, while the absolute configuration of 3 and 6 was determined by X-ray crystallographic analysis and Mosher's method, respectively. All isolated compounds (1-16) were evaluated for their cytotoxicity against the mouse lymphoma cell line L5178Y, and compounds 1, 7, and 15 showed moderate activity with IC50 values of 5.0, 8.7, and 24.4 μM, respectively.
A new depsidone derivative from mangrove sediment derived fungus
2018
A new depsidone derivative botryorhodine I (1), along with eight known compounds (2-9) were obtained from solid rice cultures of the fungal strain, Lasiodiplodia theobromae M4.2-2 isolated from a mangrove sediment sample. The structures of the isolated compounds were elucidated on the basis of 1 D and 2 D NMR analysis as well as by HRESIMS. All compounds were evaluated for their cytotoxic potential against the mouse lymphoma cell line L5178Y as well as for their antibacterial activities against a panel of Gram-positive and Gram-negative bacterial strains. Compound 3 revealed potent cytotoxic activity with an IC50 of 7.3 µM whereas compound 7 showed selective anti-bacterial activity against …
The wild taxa utilized as vegetables in Sicily (Italy): a traditional component of the Mediterranean diet
2018
Background: Wild vegetables in the Mediterranean Basin are still often consumed as a part of the diet and, in particular, there is a great tradition regarding their use in Sicily.In this study, an ethnobotanical field investigation was carried out to (a) identify the wild native taxa traditionally gathered and consumed as vegetables in Sicily, comparing the collected ethnobotanical data with those of other countries that have nominated the Mediterranean diet for inclusion in the UNESCO Representative List of the Intangible Cultural Heritage of Humanity and (b) highlight new culinary uses of these plants.Methods: Interviews were carried out in 187 towns and villages in Sicily between 2005 an…
LATE-ONSET OCULAR HYPERTENSION AFTER VITRECTOMY: A Multicenter Study of 6,048 Eyes
2018
Purpose: To determine the incidence and risk factors for late-onset ocular hypertension (LOH) after vitrectomy. Methods: From the electronic medical records of consecutive patients who underwent primary vitrectomy, from January 2010 to December 2015, at 5 tertiary vitreoretinal centers in Italy, patient demographics, systemic, ophthalmic, operative, and postoperative data were drawn. Main outcome measure was the presence of LOH, defined as intraocular pressure >21 mmHg detected more than 2 months after vitrectomy on at least 2 consecutive visits. Results: Among 6,048 patients, LOH was found in 294 (4.9%) vitrectomized eyes and in 87 (1.4%) fellow eyes, (chi square; P < 0.001). Multiva…
Multifunctional Carrier Based on Halloysite/Laponite Hybrid Hydrogel for Kartogenin Delivery
2018
[Image: see text] A novel carrier system based on halloysite nanotubes (HNT), for the potential intraarticular delivery of kartogenin (KGN) by means laponite (Lap) hydrogel (HNT/KGN/Lap), is developed. The drug was first loaded into HNT, and the hybrid composite obtained was used as filler for laponite hydrogel. Both the filler and the hydrogel were thoroughly investigated by several techniques and the hydrogel morphology was imaged by transmission electron microscopy. Furthermore, the gelating ability of laponite in the presence of the filler and the rheological properties of the hybrid hydrogel were also investigated. The kinetic release of kartogenin from HNT and HNT/Lap hybrid hydrogel …