22 results on '"Ciancimino C"'
Search Results
2. Synthesis of pyrazolo[4,3-c][1,2,6]benzothiadiazocine, a new ring system as potential COX inhibitor
- Author
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Onofrio Migliara, Virginia Spanò, Patrizia Diana, Barbara Parrino, Cristina Ciancimino, Spanò, Migliara, O, Spanò, V, Parrino, B, Ciancimino, C, and Diana, P
- Subjects
lcsh:QD241-441 ,chemistry.chemical_compound ,COX Inhibitor ,lcsh:Organic chemistry ,Chemistry ,Stereochemistry ,[1,2,6]Benzothiadiazocine, 1,4-dihydropyrazolo[4,3-c][1,2,6benzothiadiazocin-11(10H)one 5,5-dioxides, pyrazole, COX inhibitors ,Organic Chemistry ,Pyrazole ,Ring (chemistry) ,Settore CHIM/08 - Chimica Farmaceutica - Abstract
Derivatives of the new ring system 1,4-dihydropyrazolo[4,3-c][1,2,6] benzothiadiazocin-11(10H)one 5,5-dioxide were synthesized in five or six steps in 57-66% overall yields and tested as COX inhibitors.
- Published
- 2012
3. 3-[4-(1H-indol-3-yl)-1,3-thiazol-2-yl]-1H-pyrrolo[2,3-b]pyridines, nortopsentin Analogues with antiproliferative activity
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Patrizia Diana, Gloria Di Vita, Girolamo Cirrincione, M. A. Livrea, Anna Carbone, Cristina Ciancimino, Luisa Tesoriere, Paola Barraja, Alessandro Attanzio, Virginia Spanò, Barbara Parrino, Alessandra Montalbano, Parrino, B., Carbone, A., Di Vita, G., Ciancimino, C., Attanzio, A., Spanò, V., Montalbano, A., Barraja, P., Tesoriere, L., Livrea, M., Diana, P., and Cirrincione, G.
- Subjects
Indoles ,Halogenation ,Pyridines ,3-b]pyridines ,Pharmaceutical Science ,Apoptosis ,Antiproliferative activity ,3-[4-(1H-indol-3-yl)-1,3-thiazol-2-yl]-1H-pyrrolo[2,3-b]pyridines ,chemistry.chemical_compound ,Neoplasms ,Drug Discovery ,Imidazole ,Moiety ,indolyl alkaloids ,Pharmacology, Toxicology and Pharmaceutics (miscellaneous) ,lcsh:QH301-705.5 ,Membrane Potential, Mitochondrial ,Molecular Structure ,3-[4-(1H-indol-3-yl)-1 ,3-thiazol-2-yl]-1H-pyrrolo[2 ,Indolyl alkaloids ,Marine alkaloids ,Nortopsentin analogues ,Drug Discovery3003 Pharmaceutical Science ,Imidazoles ,Phosphatidylserine ,Mitochondria ,nortopsentin analogues ,Indolyl alkaloid ,marine alkaloids ,G2 Phase ,Stereochemistry ,Nortopsentin analogue ,Antineoplastic Agents ,Methylation ,Resting Phase, Cell Cycle ,Article ,Alkaloids ,Cell Line, Tumor ,Humans ,Pyrroles ,Thiazole ,Cell Proliferation ,Indole test ,Natural product ,Cell growth ,Settore CHIM/08 - Chimica Farmaceutica ,Thiazoles ,chemistry ,lcsh:Biology (General) ,Cell culture ,Drug Design ,Marine alkaloid ,3-[4-(1H-indol-3-yl)-1,3-thiazol-2-yl]-1H-pyrrolo[2,3-b]pyridine - Abstract
A new series of nortopsentin analogues, in which the imidazole ring of the natural product was replaced by thiazole and the indole unit bound to position 2 of the thiazole ring was substituted by a 7-azaindole moiety, was efficiently synthesized. Two of the new nortopsentin analogues showed good antiproliferative effect against the totality of the NCI full panel of human tumor cell lines (~60) having GI50 values ranging from low micromolar to nanomolar level. The mechanism of the antiproliferative effect of these derivatives, investigated on human hepatoma HepG2 cells, was pro-apoptotic, being associated with externalization of plasma membrane phosphatidylserine and mitochondrial dysfunction. Moreover, the compounds induced a concentration-dependent accumulation of cells in the subG0/G1phase, while confined viable cells in G2/M phase.
- Published
- 2015
4. Water-soluble isoindolo[2,1-a]quinoxalin-6-imines: In vitro antiproliferative activity and molecular mechanism(s) of action
- Author
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Claudia Sissi, Paola Barraja, Patrizia Diana, Marzia Pennati, Odra Pinato, Girolamo Cirrincione, Virginia Spanò, Cristina Ciancimino, Manlio Palumbo, Barbara Parrino, Nadia Zaffaroni, Alessandra Montalbano, Péter Mátyus, Marco Folini, Anna Carbone, Giovanni Luca Beretta, Balázs Balogh, Parrino, B., Carbone, A., Ciancimino, C., Spanò, V., Montalbano, A., Barraja, P., Cirrincione, G., Diana, P., Sissi, C., Palumbo, M., Pinato, O., Pennati, M., Beretta, G., Folini, M., Matyus, P., Balogh, B., and Zaffaroni, N.
- Subjects
Stereochemistry ,Strecker amino acid synthesis ,Antineoplastic Agents ,Apoptosis ,Isoindolo[2,1-a]quinoxalin-6-imine ,Topoisomerase I inhibitors ,Topoisomerase-I Inhibitor ,Microtubules ,Tubulin ,Cell Line, Tumor ,Quinoxalines ,Drug Discovery ,Humans ,Cytotoxic T cell ,Cell Proliferation ,Pharmacology ,Topoisomerase I inhibitor ,Chemistry ,Antitubulin agents ,G-quadruplex interaction ,Isoindolo[2 ,1-a]quinoxalin-6-imines ,Drug Discovery3003 Pharmaceutical Science ,Organic Chemistry ,Cell Cycle ,Water ,General Medicine ,Settore CHIM/08 - Chimica Farmaceutica ,In vitro ,Telomere ,Antitubulin agent ,Isoindolo[2,1-a]quinoxalin-6-imines ,DNA Topoisomerases, Type I ,Solubility ,Biochemistry ,Cell culture ,Cancer cell ,Imines ,Drug Screening Assays, Antitumor - Abstract
Water-soluble isoindoloquinoxalin (IIQ) imines and the corresponding acetates were conveniently prepared from the key intermediates 2-(2′-aminophenyl)-2H-isoindole-1-carbonitriles obtained by a Strecker reaction between substituted 1,2-dicarbaldehydes and 1,2-phenylenediamines. Both series were screened by the National Cancer Institute (Bethesda, MD) and showed potent antiproliferative activity against a panel of 60 human tumor cell lines. Several of the novel compounds showed GI50 values at a nanomolar level on the majority of the tested cell lines. Among IIQ derivatives, methoxy substituents at positions 3 and 8 or/and 9 were especially effective in impairing cell cycle progression and inducing apoptosis in cancer cells. These effects were associated to IIQ-mediated impairment of tubulin polymerization at pharmacologically significant concentrations of tested compounds. In addition, impaired DNA topoisomerase I functions and perturbation in telomere architecture were observed in cells exposed to micromolar concentrations of IIQ derivatives. The above results suggest that IIQ derivatives exhibit multi-target cytotoxic activities.
- Published
- 2015
5. Optimization of anti-proliferative activity using a screening approach with a series of bis-heterocyclic G-quadruplex ligands
- Author
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Giulia Vignaroli, Stephan A. Ohnmacht, Mekala Gunaratnam, Stephen Neidle, Cristina Ciancimino, Ohnmacht, SA, Ciancimino, C, Vignaroli, G, Gunaratnam, M, and Neidle, S
- Subjects
Phenotypic screening ,Clinical Biochemistry ,Pharmaceutical Science ,G-quadruplex ,Ligands ,Biochemistry ,chemistry.chemical_compound ,Inhibitory Concentration 50 ,Structure-Activity Relationship ,Heterocyclic Compounds ,Cell Line, Tumor ,Drug Discovery ,Humans ,Molecular Biology ,Gene ,Cell Proliferation ,Organic Chemistry ,Combinatorial chemistry ,Small molecule ,Settore CHIM/08 - Chimica Farmaceutica ,G-Quadruplexes ,chemistry ,Molecular Medicine ,Human genome ,Quadruplex, Anti-proliferative, Phenotypic screening, Telomerase, Oxazoles ,Drug Screening Assays, Antitumor ,Lead compound ,Derivative (chemistry) ,DNA - Abstract
Using a phenotypic screening and SAR optimization approach, a phenyl-bis-oxazole derivative has been identified with anti-proliferative activity, optimized with the use of a panel of cancer cell lines. The lead compound was synthesized by means of a short and effective two-step synthesis using Pd-catalyzed direct arylation. The compound stabilizes several quadruplex DNA sequences including a human telomeric DNA and one from the promoter of the HSP90 gene, although the structure–activity relationships of the series are not obviously related to the quadruplex binding.
- Published
- 2013
6. A Facile Synthesis of Deaza-Analogues of the Bisindole Marine Alkaloid Topsentin
- Author
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Gianfranco Favi, Virginia Spanò, Cristina Ciancimino, Barbara Parrino, Anna Carbone, Orazio A. Attanasi, Carbone, A, Spanò, V, Parrino, B, Ciancimino, C, Attanasi, OA, and Favi, G
- Subjects
Indoles ,Stereochemistry ,Pharmaceutical Science ,Antineoplastic Agents ,Moderate activity ,Article ,Analytical Chemistry ,lcsh:QD241-441 ,Alkaloids ,lcsh:Organic chemistry ,topsentin ,bis-indole alkaloids ,antitumor activity ,ethyl 1-[(tert-butoxycarbonyl)amino]-2-methyl-5-(1-methyl-1H-indol-3-yl)-4-[(1-methyl-1H-indol-3-yl)-carbonyl]-1H-pyrrole-3-carboxylates ,Cell Line, Tumor ,ethyl 1-[(tertbutoxycarbonyl) amino]-2-methyl-5-(1-methyl-1H-indol-3-yl)-4-[(1-methyl-1H-indol-3-yl)- carbonyl]-1H-pyrrole-3-carboxylates ,Drug Discovery ,medicine ,Humans ,Physical and Theoretical Chemistry ,Antitumor activity ,Chemistry ,Alkaloid ,Organic Chemistry ,Imidazoles ,Cancer ,medicine.disease ,Settore CHIM/08 - Chimica Farmaceutica ,In vitro ,Human tumor ,Chemistry (miscellaneous) ,Cell culture ,bis-indole alkaloid ,Molecular Medicine ,Non small cell ,Drug Screening Assays, Antitumor - Abstract
A series of substituted ethyl 1-[(tert-butoxycarbonyl)amino]-2-methyl-5- (1-methyl-1H-indol-3-yl)-4-[(1-methyl-1H-indol-3-yl)carbonyl]-1H-pyrrole-3-carboxylates were prepared in excellent yields (82-98%) by one-pot reactions between β-dicarbonyl compounds 12a-e and 1,2-diaza-1,3-diene (DD) 13. Derivatives 10a,c-e, deazaanalogues of the bis-indole alkaloid topsentin, screened by the National Cancer Institute (Bethesda, MD, USA) in the in vitro one dose primary anticancer assay against a panel of about 60 human tumor cell lines, showed no significant activity, with the exception of compound 9e, which showed moderate activity against the HOP-92 cell line of the non small cell lung cancer sub-panel and the SNB-75 cell line of the CNS sub-panel.
- Published
- 2013
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7. Isoindolo[1,5]benzoxazepines as potential antitumor and/or antiviral agents
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CIANCIMINO, Cristina and Ciancimino, C
- Subjects
Isoindolo[1,5]benzoxazepines, antitumor, antiviral agents ,Settore CHIM/08 - Chimica Farmaceutica - Published
- 2013
8. FUSED PYRROLO[2,3-b]PYRIDINE DERIVATIVES AS TOPOISOMERASE I INHIBITORS
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CIANCIMINO, Cristina and Ciancimino, C
- Subjects
PYRROLO[2,3-b]PYRIDINE, TOPOISOMERASE I INHIBITORS ,Settore CHIM/08 - Chimica Farmaceutica - Published
- 2012
9. Enhancing Corneal Sensitivity in Diabetic Patients Through an Innovative Ophthalmic Solution: In Vivo and Vitro Results.
- Author
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Scarinci F, De Simone G, Ciancimino C, Caggiano C, Pocobelli G, and Di Masi A
- Abstract
Background/Objectives : Diabetes is a well-recognised factor inducing a plethora of corneal alterations ranging from dry eye to reduced corneal sensibility, epithelial defects, and reduced cicatrisation. This cohort study aimed to assess the efficacy of a novel ophthalmic solution combining cross-linked hyaluronic acid (CHA), chondroitin sulfate (CS), and inositol (INS) in managing diabetes-induced corneal alterations. Specifically, it evaluated the solution's impact on the tear breakup time (TBUT), the ocular surface disease index (OSDI), and corneal sensitivity after three months of treatment. Additionally, the solution's potential to promote wound healing was examined. Methods : Two different populations were retrieved from the database; the first one was composed of 20 diabetic subjects treated for three months with the ophthalmic CAH-CS (OPHTAGON srl, Rome, Italy), while the second group was composed of 20 diabetic subjects who did not want to use any eye lubricant or other treatment. The outcome measures were the TBUT, the OSDI score, and the corneal sensitivity measured using a Cochet-Bonnet aesthesiometer. To investigate the wound-healing properties, in vitro tests were conducted using two cell lines, comparing the results of scratch tests with and without the solution. Results : The results indicate that CHA-CS significantly improved the tear film stability, as evidenced by an increased TBUT and a reduction in dry eye symptoms reflected by lower OSDI scores. Moreover, the solution was associated with an enhanced corneal sensitivity in treated patients. In wound-healing assays, CHA-CS promoted cell motility, suggesting a supportive role in tissue repair compared to untreated cells. Conclusions : Collectively, the results suggest that CHA-CS could serve as an innovative tool for the treatment of diabetic patients with corneal alterations and delayed corneal sensitivity. Clinical trial registration number: Clinical Trial.gov NCT06573606.
- Published
- 2025
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10. Posterior Polar Annular Choroidal Dystrophy: Genetic Insights and Differential Diagnosis in Inherited Retinal Diseases.
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Ruggeri F, Ciancimino C, Guillot A, Fumi D, Tizio FD, Fragiotta S, and Abdolrahimzadeh S
- Abstract
Posterior polar annular choroidal dystrophy (PPACD) is a rare ocular disorder and presents as symmetric degeneration of the retinal pigment epithelium (RPE) and the underlying choriocapillaris, encircling the retinal vascular arcades and optic disc. This condition distinctively preserves the foveal region, optic disc, and the outermost regions of the retina. Despite its distinct clinical presentation, due to the infrequency of its occurrence and the limited number of reported cases, the pathophysiology, and the genetic foundations of PPACD are still largely uncharted. This review aims to bridge this knowledge gap by investigating potential genetic contributors to PPACD, assessing current findings, and identifying genes that warrant further study. Emphasis is also placed on the crucial role of multimodal imaging in diagnosing PPACD, highlighting its importance in understanding disease pathophysiology. By analyzing existing case reports and drawing comparisons with similar retinal disorders, this paper endeavors to delineate the possible genetic correlations in PPACD, providing a foundation for future genetic research and the development of targeted diagnostic strategies.
- Published
- 2024
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11. Multimodal Ophthalmic Imaging in Spinocerebellar Ataxia Type 7.
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Ciancimino C, Di Pippo M, Manco GA, Romano S, Ristori G, Scuderi G, and Abdolrahimzadeh S
- Abstract
The aim of this case series and narrative literature review is to highlight the importance of multimodal imaging in the ophthalmological examination of patients with spinocerebellar ataxia type 7 and provide a summary of the most relevant imaging techniques. Three patients with SCA7 were included in this case series. A literature review revealed twenty-one publications regarding ocular manifestations of SCA7, and the most relevant aspects are summarized. The role of different imaging techniques in the follow-up of SCA7 patients is analyzed, including color vision testing, corneal endothelial topography, color fundus photography (CFP) and autofluorescence, near infrared reflectance imaging, spectral domain optical coherence tomography (SDOCT), visual field examination, and electrophysiological tests. SDOCT provides a rapid and non-invasive imaging evaluation of disease progression over time. Additional examination including NIR imaging can provide further information on photoreceptor alteration and subtle disruption of the RPE, which are not evident with CFP at an early stage. Electrophysiological tests provide essential results on the state of cone and rod dystrophy, which could be paramount in guiding future genetic therapies. Multimodal imaging is a valuable addition to comprehensive ophthalmological examination in the diagnosis and management of patients with SCA7.
- Published
- 2023
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12. An Update on Multimodal Ophthalmological Imaging of Diffuse Choroidal Hemangioma in Sturge-Weber Syndrome.
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Ciancimino C, Di Pippo M, Rullo D, Ruggeri F, Grassi F, Scuderi G, and Abdolrahimzadeh S
- Abstract
Sturge-Weber syndrome (SWS) is characterized by facial port-wine stains, leptomeningeal hemangiomas, and prominent ocular manifestations such as glaucoma and diffuse choroidal hemangiomas (DCHs). Imaging modalities are critical for diagnosing and longitudinally monitoring DCHs in SWS. Fundus photography is fundamental in assessing both eyes simultaneously, fluorescein angiography and indocyanine green angiography effectively map the retinal and choroidal circulation, and ultrasonography offers essential structural insights into the choroid and retina. NIR imaging reveals subtle retinal pigment changes, often overlooked in standard fundus examination. Enhanced depth imaging spectral domain optical coherence tomography (EDI-SDOCT) and swept-source OCT (SSOCT) improve the visualization of the choroidal-scleral boundary, essential for DCH characterization. The potential of OCT angiography (OCTA) is under exploration, particularly its role in predicting signs of disease progression or worsening, as well as potential new biomarkers such as the choroidal vascularity index (CVI). The present review aims to provide an update on multimodal imaging of DCHs in SWS.
- Published
- 2023
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13. The Choroidal Vascularity Index Versus Optical Coherence Tomography Angiography in the Evaluation of the Choroid with a Focus on Age-Related Macular Degeneration.
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Di Pippo M, Santia C, Rullo D, Ciancimino C, Grassi F, and Abdolrahimzadeh S
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- Humans, Choroid diagnostic imaging, Angiography, Neovascularization, Pathologic, Tomography, Optical Coherence, Macular Degeneration diagnostic imaging
- Abstract
The choroid is the most vascularized structure of the eye and it is fundamental for the trophism of the outer retina. Its proper functioning and homeostasis represent key points in maintaining normal retinal physiology. Choroidal alterations may be implicated in the development and progression of numerous pathologies; therefore, in-depth studies using imaging techniques can be of crucial relevance to understanding the pathophysiology of retinal-choroidal diseases. The advent of spectral-domain optical coherence tomography (SDOCT) has enabled the non-invasive study of the choroid in vivo and the most recent development, optical coherence tomography angiography (OCTA), allows for the high-resolution visualization of the choriocapillaris and the choroid in regard to vascularization. The choroidal vascularity index (CVI) is a new parameter calculated on SDOCT scans and is defined as the ratio of the luminal area to the total choroidal area. In this review, a study of the choroid using OCTA and CVI will be evaluated in depth and the pros and cons of these two methods will be analyzed, with a particular focus on age-related macular degeneration.
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- 2023
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14. Choroidal vascularity index and choroidal thickness: potential biomarkers in retinitis pigmentosa.
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Abdolrahimzadeh S, Di Pippo M, Ciancimino C, Di Staso F, and Lotery AJ
- Subjects
- Humans, Visual Acuity, Choroid pathology, Biomarkers, Tomography, Optical Coherence, Retinitis Pigmentosa diagnosis
- Abstract
Retinitis pigmentosa (RP) is the commonest inherited retinal dystrophy. It is characterized by progressive photoreceptor degeneration and cell death and ongoing neuronal and vascular impairment. In recent years, pathophysiological alterations of the choroid have begun to be appreciated in RP. Thus, representing a potential diagnostic and therapeutic biomarker. In particular, choroidal thickness and the choroidal vascularity index can be used to understand the pathogenesis of disease and evaluate new therapeutic possibilities. Photoreceptor changes seen in eyes with RP are directly correlated to a decrease of choroidal flow, leading to a strong association between relative choroidal ischemia and visual impairment. In this review we analyse the literature on choroidal thickness and choroidal vascularity index in patients with RP and assess whether these markers may reflect progression of disease from an anatomical and functional point of view., (© 2022. The Author(s).)
- Published
- 2023
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15. Near-Infrared Reflectance Imaging in Retinal Diseases Affecting Young Patients.
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Abdolrahimzadeh S, Ciancimino C, Grassi F, Sordi E, Fragiotta S, and Scuderi G
- Abstract
Near-infrared reflectance (NIR) is a noninvasive, contactless, and rapid in vivo imaging technique for visualizing subretinal alterations in the photoreceptor layer, retinal pigment epithelium, and choroid. The present report describes the application of this imaging method in retinal and choroidal pathologies affecting young patients where scarce cooperation, poor fixation, and intense glare sensation can result in a challenging clinical examination. A literature search of the MEDLINE database was performed using the terms "near-infrared reflectance" and "spectral-domain optical coherence tomography." Articles were selected if they described the diagnostic use of NIR in children or young adults. Of 700 publications, 42 manuscripts published between 2005 and 2020 were inherent to children or young adults and were considered in this narrative literature review. The first disease category is the phakomatoses where NIR is essential in visualizing choroidal alterations recognized as cardinal biomarkers in neurofibromatosis type 1, microvascular retinal alterations, and retinal astrocytic hamartomas. Another diagnostic application is the accurate visualization of crystals of various nature, including the glistening crystals that characterize Bietti crystalline dystrophy. Acute macular neuropathy and paracentral acute middle maculopathy represent a further disease category with young adulthood onset where NIR is not only diagnostic but also essential to monitor disease progression. A further interesting clinical application is to facilitate the detection of laser-induced maculopathy where funduscopic examination can be normal or subnormal. In conclusion, NIR imaging has a noninterchangeable role in diagnosing certain retinal diseases, especially in children and young adults where there is scarce collaboration and a lack of evident clinical findings. Moreover, this technique can reveal unique retinal and choroidal biomarkers highly specific to rare conditions., Competing Interests: The authors declare that there are no conflicts of interest., (Copyright © 2021 Solmaz Abdolrahimzadeh et al.)
- Published
- 2021
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16. Volume Rendering of Angiographic Optical Coherence Tomography Angiography in Fovea Plana and Normal Foveal Pit.
- Author
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Fragiotta S, Ciancimino C, Perdicchi A, de Paula A, Abdolrahimzadeh S, and Scuderi G
- Abstract
This paper aims to study adaptative vascular arrangements in idiopathic fovea plana with volume-rendered optical coherence tomography angiography (OCTA). A retrospective review of two cases of idiopathic fovea plana (mean age: 26.5 years) and two age-matched controls imaged with OCTA was conducted using spectral-domain OCTA (RTVue XR Avanti, Optovue, Inc., Fremont, CA) equipped with the AngioVue software. Both en face OCTA slabs and OCTA b scans were processed through Fiji software (http://fiji.sc; software version 2.0.0-rc-68/1.52e), and then extracted as image sequences for volume rendering reconstructions using the ImageVis3D volume rendering system (3.1.0 release). Eyes with idiopathic fovea plana demonstrated a regular superficial vascular plexus connecting to a single vascular monolayer representing the deeper vascular plexuses. At this location, several vertical short path connections were demonstrated, in contraposition with normal eyes where short path connections were infrequently observed. Advances in three-dimensional OCTA reconstruction increase the understanding of vascular connections and arrangement in retinal plexuses and possible anatomical variations that cannot be detected with conventional two-dimensional b scans., Competing Interests: The authors declare that the research was conducted in the absence of any commercial or financial relationships that could be construed as a potential conflict of interest., (Copyright © 2021 Fragiotta, Ciancimino, Perdicchi, de Paula, Abdolrahimzadeh and Scuderi.)
- Published
- 2021
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17. An Iconic Case of Pigmentary Glaucoma: Brief Review of the Literature.
- Author
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Di Pippo M, Ciancimino C, Scuderi L, and Perdicchi A
- Abstract
Pigment dispersion syndrome and pigmentary glaucoma are two conditions characterized by pigment dispersion originating from the posterior part of the iris and its accumulation on the trabecular meshwork, corneal endothelium, and anterior surface of the lens. The pigment on the trabecular meshwork can cause chronic inflammation with a secondary reduction of its function and an increase in intraocular pressure. The case presented represents a typical example of pigmentary glaucoma in a myopic patient in which all the signs, symptoms, and complications typical of these pathologies were present. We report and describe an 8-year-long follow-up period with clinical and instrumental examinations., Competing Interests: The authors have no conflicts of interest to declare., (Copyright © 2020 by S. Karger AG, Basel.)
- Published
- 2020
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18. Short-Term Effects of Dark Chocolate on Retinal and Choriocapillaris Perfusion in Young, Healthy Subjects Using Optical Coherence Tomography Angiography.
- Author
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Scuderi G, Ciancimino C, D'Apolito F, Maurizi Enrici M, Guglielmelli F, Scuderi L, and Abdolrahimzadeh S
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- Adult, Choroid diagnostic imaging, Female, Fluorescein Angiography, Healthy Volunteers, Humans, Male, Prospective Studies, Retinal Vessels physiology, Tomography, Optical Coherence, Treatment Outcome, Visual Acuity physiology, Chocolate, Choroid physiology, Feeding Behavior physiology, Retinal Vessels diagnostic imaging
- Abstract
(1) Aim: Contrasting results have been published on the effect of dark chocolate on visual function. The aim of this study was to evaluate retinal and choriocapillaris perfusion, using optical coherence tomography angiography (OCT-A), and visual function in healthy subjects following dark chocolate ingestion. (2) Methods: This prospective randomized study was carried out on 18 healthy young subjects at the St. Andrea Hospital, Sapienza, University of Rome. Visual acuity assessment and a complete ophthalmologic examination were carried out at baseline. In session one, each subject was randomized to eat either a 100 g dark chocolate bar or a 100 g white chocolate bar. In session two, the opposite chocolate was given to each participant. OCT-A and best corrected visual acuity (BCVA) were performed before the chocolate was eaten and repeated 1, 2, and 3 h after that. Retinal vessel density and choriocapillaris flow area were assessed. (3) Results: 18 patients with a mean (SD) age of 26.3 (1.5) years were included. No significant differences between dark or white chocolate were found when evaluating foveal density (%), whole density (%), choriocapillaris flow area, and BCVA. (4) Conclusions: Dark chocolate did not result in significant changes in retinal perfusion and choriocapillaris flow area. However, given the results of other studies showing the positive effects of flavonoids on visual function, further studies are warranted using pure chocolate without other components such as caffeine that can potentially affect results. Furthermore, we cannot rule out the possible benefits of higher doses of flavonoids in dietary supplementation over a more extended period and in a larger patient population.
- Published
- 2020
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19. Water-soluble isoindolo[2,1-a]quinoxalin-6-imines: in vitro antiproliferative activity and molecular mechanism(s) of action.
- Author
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Parrino B, Carbone A, Ciancimino C, Spanò V, Montalbano A, Barraja P, Cirrincione G, Diana P, Sissi C, Palumbo M, Pinato O, Pennati M, Beretta G, Folini M, Matyus P, Balogh B, and Zaffaroni N
- Subjects
- Apoptosis drug effects, Cell Cycle drug effects, Cell Line, Tumor, Cell Proliferation drug effects, DNA Topoisomerases, Type I metabolism, Humans, Imines chemistry, Microtubules drug effects, Microtubules metabolism, Quinoxalines chemistry, Solubility, Tubulin metabolism, Water, Antineoplastic Agents chemistry, Antineoplastic Agents pharmacology, Drug Screening Assays, Antitumor methods
- Abstract
Water-soluble isoindoloquinoxalin (IIQ) imines and the corresponding acetates were conveniently prepared from the key intermediates 2-(2'-aminophenyl)-2H-isoindole-1-carbonitriles obtained by a Strecker reaction between substituted 1,2-dicarbaldehydes and 1,2-phenylenediamines. Both series were screened by the National Cancer Institute (Bethesda, MD) and showed potent antiproliferative activity against a panel of 60 human tumor cell lines. Several of the novel compounds showed GI50 values at a nanomolar level on the majority of the tested cell lines. Among IIQ derivatives, methoxy substituents at positions 3 and 8 or/and 9 were especially effective in impairing cell cycle progression and inducing apoptosis in cancer cells. These effects were associated to IIQ-mediated impairment of tubulin polymerization at pharmacologically significant concentrations of tested compounds. In addition, impaired DNA topoisomerase I functions and perturbation in telomere architecture were observed in cells exposed to micromolar concentrations of IIQ derivatives. The above results suggest that IIQ derivatives exhibit multi-target cytotoxic activities., (Copyright © 2015 Elsevier Masson SAS. All rights reserved.)
- Published
- 2015
- Full Text
- View/download PDF
20. 3-[4-(1H-indol-3-yl)-1,3-thiazol-2-yl]-1H-pyrrolo[2,3-b]pyridines, nortopsentin analogues with antiproliferative activity.
- Author
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Parrino B, Carbone A, Di Vita G, Ciancimino C, Attanzio A, Spanò V, Montalbano A, Barraja P, Tesoriere L, Livrea MA, Diana P, and Cirrincione G
- Subjects
- Alkaloids chemical synthesis, Alkaloids chemistry, Alkaloids pharmacology, Antineoplastic Agents chemistry, Antineoplastic Agents pharmacology, Apoptosis drug effects, Cell Line, Tumor, Cell Proliferation drug effects, G2 Phase drug effects, Halogenation, Humans, Imidazoles chemistry, Imidazoles pharmacology, Indoles chemistry, Indoles pharmacology, Membrane Potential, Mitochondrial drug effects, Methylation, Mitochondria drug effects, Mitochondria pathology, Molecular Structure, Neoplasms pathology, Pyridines chemistry, Pyridines pharmacology, Pyrroles chemistry, Pyrroles pharmacology, Resting Phase, Cell Cycle drug effects, Thiazoles chemical synthesis, Thiazoles chemistry, Thiazoles pharmacology, Antineoplastic Agents chemical synthesis, Drug Design, Imidazoles chemical synthesis, Indoles chemical synthesis, Neoplasms drug therapy, Pyridines chemical synthesis, Pyrroles chemical synthesis
- Abstract
A new series of nortopsentin analogues, in which the imidazole ring of the natural product was replaced by thiazole and the indole unit bound to position 2 of the thiazole ring was substituted by a 7-azaindole moiety, was efficiently synthesized. Two of the new nortopsentin analogues showed good antiproliferative effect against the totality of the NCI full panel of human tumor cell lines (~60) having GI50 values ranging from low micromolar to nanomolar level. The mechanism of the antiproliferative effect of these derivatives, investigated on human hepatoma HepG2 cells, was pro-apoptotic, being associated with externalization of plasma membrane phosphatidylserine and mitochondrial dysfunction. Moreover, the compounds induced a concentration-dependent accumulation of cells in the subG0/G1phase, while confined viable cells in G2/M phase.
- Published
- 2015
- Full Text
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21. Optimization of anti-proliferative activity using a screening approach with a series of bis-heterocyclic G-quadruplex ligands.
- Author
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Ohnmacht SA, Ciancimino C, Vignaroli G, Gunaratnam M, and Neidle S
- Subjects
- Cell Line, Tumor, Cell Proliferation drug effects, Drug Screening Assays, Antitumor, Heterocyclic Compounds chemistry, Heterocyclic Compounds pharmacology, Humans, Inhibitory Concentration 50, Ligands, Structure-Activity Relationship, G-Quadruplexes, Heterocyclic Compounds chemical synthesis
- Abstract
Using a phenotypic screening and SAR optimization approach, a phenyl-bis-oxazole derivative has been identified with anti-proliferative activity, optimized with the use of a panel of cancer cell lines. The lead compound was synthesized by means of a short and effective two-step synthesis using Pd-catalyzed direct arylation. The compound stabilizes several quadruplex DNA sequences including a human telomeric DNA and one from the promoter of the HSP90 gene, although the structure-activity relationships of the series are not obviously related to the quadruplex binding., (Copyright © 2013 Elsevier Ltd. All rights reserved.)
- Published
- 2013
- Full Text
- View/download PDF
22. A step backward: the 'Rough' facial nerve grading system.
- Author
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Alicandri-Ciufelli M, Piccinini A, Grammatica A, Salafia F, Ciancimino C, Cunsolo E, Pingani L, Rigatelli M, Genovese E, Monzani D, Gioacchini FM, Marchioni D, and Presutti L
- Subjects
- Blinking physiology, Eye Movements physiology, Eyelids physiopathology, Facial Asymmetry classification, Facial Asymmetry physiopathology, Facial Expression, Facial Muscles physiopathology, Facial Paralysis physiopathology, Female, Humans, Male, Middle Aged, Muscle Weakness classification, Observer Variation, Reproducibility of Results, Smiling physiology, Facial Paralysis classification
- Abstract
Objectives: Several modalities currently exist to rate the degree of facial function clinically but even though it has significant limitations, the most widely used scale is the House-Brackmann grading system (HBGS). A simplified scale is introduced here, the 'Rough' Grading System (RGS - Grade I: normal movement; Grade II: slight paralysis; Grade III: frank paralysis with eye closure; Grade IV: frank paralysis without eye closure; Grade V: almost complete paralysis with only slight movements; Grade VI: total paralysis). The aim of the present study was to verify the interrater reliability and the interscale validity of this simplified grading system., Study Design: Scale validation study based on a prospective cohort., Methods: Fifty patients with facial palsy, consecutively referred to our department were filmed while performing some codified facial movements. Then two independent groups (one rating using the HBGS, the other rating using the RGS) assigned a grade after reviewing the videos. The time required for the rating was also noted., Results: The HBGS showed a mean value of interrater agreement of 0.46 while the RGS showed a mean value of 0.59. The concurrent validity between HBGS and RGS ranged from 0.86 to 0.90 (p < 0.001 for every comparison). There was no statistically significant difference between HBGS and RGS in the mean time taken for rating (p = 0.15)., Conclusions: The RGS reached an adequate level of interrater reliability, higher than the HBGS. The correlation between the two scales is high and the times required for rating are similar. The present results may justify the use of the RGS in routine clinical practice., Level of Evidence: N/A., (Copyright © 2012 European Association for Cranio-Maxillo-Facial Surgery. Published by Elsevier Ltd. All rights reserved.)
- Published
- 2013
- Full Text
- View/download PDF
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