6 results on '"Vertuani, Silvia"'
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2. Design, synthesis and evaluation of benzothiazole derivatives as multifunctional agents.
- Author
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Djuidje EN, Sciabica S, Buzzi R, Dissette V, Balzarini J, Liekens S, Serra E, Andreotti E, Manfredini S, Vertuani S, and Baldisserotto A
- Subjects
- Antifungal Agents pharmacology, Antineoplastic Agents pharmacology, Cell Proliferation drug effects, Drug Evaluation, Preclinical, HEK293 Cells, Humans, Benzothiazoles chemistry, Drug Design
- Abstract
Oxidative stress is the product or aetiology of various multifactorial diseases; on the other hand, the development of multifunctional compounds is a recognized strategy for the control of complex diseases. To this end, a series of benzothiazole derivatives was synthesized and evaluated for their multifunctional effectiveness as antioxidant, sunscreen (filter), antifungal and antiproliferative agents. Compounds were easily synthesized via condensation reaction between 2-aminothiophenols and different benzaldehydes. SAR study, particularly in position 2 and 6 of benzothiazoles, led to the identification of 4g and 4k as very interesting potential compounds for the design of multifunctional drugs. In particular, compound 4g is the best blocker of hERG potassium channels expressed in HEK 293 cells exhibiting 60.32% inhibition with IC
50 = 4.79 μM., Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2020 Elsevier Inc. All rights reserved.)- Published
- 2020
- Full Text
- View/download PDF
3. Synthesis and evaluation of antioxidant and antiproliferative activity of 2-arylbenzimidazoles.
- Author
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Baldisserotto A, Demurtas M, Lampronti I, Tacchini M, Moi D, Balboni G, Pacifico S, Vertuani S, Manfredini S, and Onnis V
- Subjects
- Antineoplastic Agents chemical synthesis, Antineoplastic Agents chemistry, Antioxidants chemical synthesis, Antioxidants chemistry, Benzimidazoles chemical synthesis, Benzimidazoles chemistry, Biphenyl Compounds antagonists & inhibitors, Cell Line, Cell Proliferation drug effects, Dose-Response Relationship, Drug, Drug Screening Assays, Antitumor, Humans, Molecular Structure, Picrates antagonists & inhibitors, Structure-Activity Relationship, Antineoplastic Agents pharmacology, Antioxidants pharmacology, Benzimidazoles pharmacology
- Abstract
Three series of arylbenzimidazole derivatives 3-40, 45 have been simply synthesized and tested for their antioxidant capacity. The 2-arylbenzimidazoles were tested against various radicals by the DPPH, FRAP and ORAC tests and showed different activity profiles. It has been observed that the number and position of the hydroxy groups on the 2-aryl portion and the presence of a diethylamino group or a 2-styryl group are related to a good antioxidant capacity. Furthermore, benzimidazoles showed satisfactory SPF values in vitro compared to the commercial PBSA filter, proving to have a good photoprotective profile. In particular, 2-arylbenzimidazole-5-sulphonic acids 15 and 38, the 2-styryl-benzimidazole 45 showed broad spectrum solar protection against UVA and UVB rays. The antiproliferative effect of the benzimidazoles was tested on human skin melanoma Colo-38 cells. The styrylbenzimidazole 45 exhibited antiproliferative effect at low micromolar concentration against Colo-38 cells and very low antiproliferative activity on normal HaCat keratinocyte cells., (Copyright © 2019 Elsevier Inc. All rights reserved.)
- Published
- 2020
- Full Text
- View/download PDF
4. Indole derivatives as multifunctional drugs: Synthesis and evaluation of antioxidant, photoprotective and antiproliferative activity of indole hydrazones.
- Author
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Demurtas M, Baldisserotto A, Lampronti I, Moi D, Balboni G, Pacifico S, Vertuani S, Manfredini S, and Onnis V
- Subjects
- Antineoplastic Agents chemical synthesis, Antineoplastic Agents chemistry, Cell Line, Tumor, Cell Proliferation drug effects, Drug Screening Assays, Antitumor, Free Radical Scavengers chemical synthesis, Free Radical Scavengers chemistry, Humans, Hydrazones chemical synthesis, Hydrazones chemistry, Indoles chemical synthesis, Indoles chemistry, Molecular Structure, Structure-Activity Relationship, Sunscreening Agents chemical synthesis, Sunscreening Agents chemistry, Antineoplastic Agents pharmacology, Free Radical Scavengers pharmacology, Hydrazones pharmacology, Indoles pharmacology, Sunscreening Agents pharmacology
- Abstract
Two series of indole derivatives 4-17, 20-22 were easily prepared and assayed for their radical-scavenging ability. Arylidene-1H-indole-2-carbohydrazones showed different extent antioxidant activity in DPPH, FRAP and ORAC assays. Good antioxidant activity is related to the number and position of hydroxyl groups on the arylidene moiety as well as to the presence of methoxy or 4-(diethylamino) group. On the contrary low antioxidant activity is showed by the isomeric 1H-indol-2-yl(methylene)-benzohydrazides. Furthermore, hydrazones 4-17 showed photoprotective capacities with satisfactory in vitro SPF as compared to the commercial PBSA sunscreen filter. The indole 16 and 17, showing the best antioxidant and photoprotective profile, were included in different formulation and their topical release was evaluated. Varying the formulation composition, it was possible to optimize skin adsorption and solubility of the active indole in the formulation. The antiproliferative effect of the hydrazones 4-17 was tested on human erythroleukemia K562 and melanoma Colo-38 cells. Hydrazones 11, 16 and 17 showed growth inhibition at sub micromolar concentrations on both cell lines. These results indicate indole hydrazones as potential multifunctional molecules especially in the treatment of neoplastic diseases being the good antioxidant properties of 16 and 17 correlated to their high antiproliferative activity., (Copyright © 2019 Elsevier Inc. All rights reserved.)
- Published
- 2019
- Full Text
- View/download PDF
5. Herbal extracts, lichens and biomolecules as natural photo-protection alternatives to synthetic UV filters. A systematic review.
- Author
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Radice M, Manfredini S, Ziosi P, Dissette V, Buso P, Fallacara A, and Vertuani S
- Subjects
- Antioxidants pharmacology, DNA Damage drug effects, Humans, Photochemical Processes, Skin radiation effects, Skin Neoplasms prevention & control, Sunburn prevention & control, Ultraviolet Rays adverse effects, Biological Products pharmacology, Lichens chemistry, Plant Extracts pharmacology, Skin drug effects, Sunscreening Agents pharmacology
- Abstract
Besides the unquestionable positive effects of solar exposure for human health, UV rays have been widely investigated for toxicology aspects related to excessive UVB and UVA doses, which involve sunburns, skin aging, DNA skin damage and tumorigenesis. At present, synthetic and mineral sunscreens are used to protect against these damages but several natural molecules can provide UV protection, including also synergic effect or enhanced photo stability. Although a large number of herbal extracts and plant origin molecules can deserve potential applications, most of the study reported utilizes different method and different strategies of investigation, making thus difficult to understand the real versus claimed potential. This is possibly one of the reasons why, beside the large body of literature there are no officially approved natural commercial sun-filter but a consistent number of commercially available solar products (sunscreen) on the market that contain herbal derivatives. In this review we have evaluated the papers appeared in the last 15years and we have critically collected the most significant data. Several databases, namely Scifinder, Pubmed, Google Scholar, ISI-Web of Science and Scopus, were used as literature sources; excluding patents and symposium or congress papers. Only articles in the English language have been selected. New formulation, new skin delivery systems, skin penetration enhancers and boosters are most likely the next frontier of investigation in order to better understand the role of whole herbal extracts in exerting their photo protective activity., (Copyright © 2016 Elsevier B.V. All rights reserved.)
- Published
- 2016
- Full Text
- View/download PDF
6. Synthesis and biological evaluation of pro-drugs of GW196771, a potent glycine antagonist acting at the NMDA receptor.
- Author
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Angusti A, Durini E, Vertuani S, Dalpiaz A, Ruffo A, Di Fabio R, Donati D, Pentassuglia G, Vitulli G, Barnaby RJ, and Manfredini S
- Subjects
- Animals, Drug Evaluation, Preclinical methods, Glycine therapeutic use, Indenes therapeutic use, Monosaccharides chemistry, Monosaccharides metabolism, Neurodegenerative Diseases drug therapy, Prodrugs metabolism, Pyrrolidines chemistry, Pyrrolidines pharmacology, Pyrrolidines therapeutic use, Rats, Receptors, N-Methyl-D-Aspartate therapeutic use, Glycine antagonists & inhibitors, Glycine pharmacology, Indenes metabolism, Indenes pharmacology, Prodrugs chemical synthesis, Pyrrolidines metabolism, Receptors, N-Methyl-D-Aspartate drug effects
- Abstract
GW196771 is a potent antagonist of the modulatory glycine site of the N-methyl-D-aspartate (NMDA) receptor exhibiting outstanding in vivo profile in different animal models of chronic pain. With the aim to maximize the drug delivery to the target organs a suitable "pro-drug approach" was attempted; in this regards two conjugates of GW196771 with nutrients actively transported into the brain, namely adenosine and glucose, were prepared and investigated. These compounds, were evaluated in vitro in terms of their stability in rat plasma and in vivo on rats. Although an improvement was observed in terms of brain penetration of the esters vs. the parent compound, the amount of the latter did not increase significantly, probably due to some degradation events in the brain, different from the expected ester hydrolysis, resulting in a reduced availability of GW196771.
- Published
- 2005
- Full Text
- View/download PDF
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