10 results on '"Vertuani, Silvia"'
Search Results
2. Novel molecular combination deriving from natural aminoacids and polyphenols: Design, synthesis and free-radical scavenging activities
- Author
-
Anna Baldisserotto, Emanuela Scalambra, Stefano Manfredini, Vertuani Silvia, Elisa Durini, and Gemma Malisardi
- Subjects
Antioxidant ,DPPH ,medicine.medical_treatment ,Dopamine ,Context (language use) ,Antioxidants ,chemistry.chemical_compound ,Structure-Activity Relationship ,Picrates ,Drug Discovery ,medicine ,Organic chemistry ,Humans ,Phenols ,Amino Acids ,Pharmacology ,Methionine ,Molecular Structure ,Organic Chemistry ,Biphenyl Compounds ,Polyphenols ,General Medicine ,Phenolic acid ,Free Radical Scavengers ,chemistry ,Polyphenol ,Drug Design ,Indicators and Reagents ,Reactive Oxygen Species ,Cysteine - Abstract
Following the recent output of scientific publications in the matter of synergic activity between different antioxidants, we have undertaken the present study with the aim to synthesize new molecules with radical-scavengers activity based on the conjugation of bioactive portions (i.e. phenols, cysteine, methionine or tyrosine), characterized by different structures and mechanisms of action, to promote the simultaneous quenching of different radical species in the site of the oxidative damage. In this context, derivatives of phenolic acid, aminoacids and dopamine have been also prepared. The newly synthesized compounds were evaluated in vitro applying specific and complementary antioxidant test such as DPPH assay and ORAC test. As emerged from the evaluation, prerequisites for the activity of the synthesized molecules were: i) the maintenance of at least two hydroxylic groups on the aromatic moiety of phenolic portion, ii) the presence of a spacer between the aromatic moiety and the carbonilic group.
- Published
- 2011
3. The use of photochemiluminescence for the measurement of the Integral Antioxidant Capacity of baobab products
- Author
-
Besco, Elena, Braccioli, Elena, Vertuani, Silvia, Ziosi, Paola, Brazzo, F, Bruni, R, Sacchetti, Gianni, and Manfredini, Stefano
- Subjects
antioxidant ,adansonia digitata ,nutraceutical ,cosmeceutical - Published
- 2007
4. Design, synthesis and biological evaluation of novel hydroxy-phenyl-1H-benzimidazoles as radical scavengers and UV-protective agents.
- Author
-
Bino, Alessia, Baldisserotto, Anna, Scalambra, Emanuela, Dissette, Valeria, Vedaldi, Daniela Ester, Salvador, Alessia, Durini, Elisa, Manfredini, Stefano, and Vertuani, Silvia
- Subjects
CHEMICAL synthesis ,BENZIMIDAZOLES ,SOLAR ultraviolet radiation ,SKIN diseases ,THERAPEUTIC use of antioxidants ,DERMIS ,PHYSIOLOGY - Abstract
An ever-increasing incidence of skin neoplastic diseases is registered. Therefore, it is important to protect the skin from the UV radiation that reaches the epidermis and dermis but also to block ROS generated by them. Our attention was attracted in developing new compounds provided with both UV filtering and antioxidant capacities. To this end, 2-phenyl-1H-benzimidazole-5-sulfonic acid (PBSA), a known UV filter, was selected as lead compound for its lack of antioxidant activity, high water solubility and good safety profile. PBSA was sequentially modified introducing hydroxyls on the phenyl ring and also substituting the functional group in position 5 of the benzimidazole ring. At the end of the synthetic study, a new, very potent class of antioxidants has been obtained. Surprisingly some of the developed molecules, while devoid of significant UV-filtering activity was endowed with potent UV-filtering booster capability if associated with known commercial UVB and UVA filters. [ABSTRACT FROM AUTHOR]
- Published
- 2017
- Full Text
- View/download PDF
5. Design, synthesis and biological activity of a novel Rutin analogue with improved lipid soluble properties.
- Author
-
Baldisserotto, Anna, Vertuani, Silvia, Bino, Alessia, De Lucia, Daniela, Lampronti, Ilaria, Milani, Roberta, Gambari, Roberto, and Manfredini, Stefano
- Subjects
- *
RUTIN , *BIOACTIVE compounds , *ORGANIC synthesis , *LIPIDS , *FLAVONOIDS , *MOLECULAR weights - Abstract
Recent interest in flavonoids has increased greatly due to their biological and pharmacological activities. Flavonoids, consist of a large group of low molecular weight polyphenolic substances, naturally occurring in fruits, vegetables, tea, and wine, and are an integral part of the human diet. Rutin is a common dietary flavonoid that is widely consumed worldwide from plant-derived beverages and foods as traditional and folk medicine remedy as well. Rutin exhibit important pharmacological activities, including anti-oxidation, anti-inflammation, anti-diabetic, anti-adipogenic, neuroprotective and hormone therapy. Here, we present the synthesis, antimicrobial, antiproliferative and pro-apoptotic effect on human leukemic K562 cells of compound R2 , a new semi-synthetic derivative of Rutin as compared to Rutin itself. The new derivative was also included in finished topical formulations to evaluate a potential application to the dermatology field in view of the antioxidant/antimicrobial/antiinflammatory properties. Stability studies were performed by HPLC; PCL assay and ORAC tests were used to determine the antioxidant activity. R2 presented an antioxidant activity very close to that of the parent Rutin while bearing much better lipophilic character. Regarding antiproliferative effects on the human K562 cell line, R2 was found to be more effective than parent Rutin. Preliminary experiments demonstrated that R2 inhibits NF-kB activity and promotes cellular apoptosis. [ABSTRACT FROM AUTHOR]
- Published
- 2015
- Full Text
- View/download PDF
6. Benzothiazole Derivatives as Multifunctional Antioxidant Agents for Skin Damage: Structure–Activity Relationship of a Scaffold Bearing a Five-Membered Ring System.
- Author
-
Djuidje, Ernestine Nicaise, Barbari, Riccardo, Baldisserotto, Anna, Durini, Elisa, Sciabica, Sabrina, Balzarini, Jan, Liekens, Sandra, Vertuani, Silvia, and Manfredini, Stefano
- Subjects
BENZOTHIAZOLE derivatives ,STRUCTURE-activity relationships ,CANDIDA albicans ,SKIN diseases ,OXIDATIVE stress ,BENZOXAZOLES ,BENZIMIDAZOLES - Abstract
Skin diseases often give multifactorial damages; therefore, the development of multifunctional compounds represents a suitable approach especially against disorders that are induced by oxidative stress. Thus, taking into account the successful results we achieved on benzimidazoles, we have devised a new series of isosteric benzothiazoles and investigated their antioxidant, photoprotective, antifungal and antiproliferative activity. Particular attention has been paid to synergistic antioxidant and photoprotective properties. For compounds 9a and 10a, a multifunctional profile was outlined, supported by an excellent filtering capacity, mainly UVB, which has higher capacities than those of the reference PBSA which is currently in the market as a UV sunscreen filter. The two compounds were also the best in terms of growth inhibition of dermatophytes and Candida albicans, and 10a also showed good antioxidant activity. Furthermore, 9a was also effective on melanoma tumor cells (SK-Mel 5), making these compounds good candidates in the development of new skin protective and preventive agents. [ABSTRACT FROM AUTHOR]
- Published
- 2022
- Full Text
- View/download PDF
7. A New Approach to UV Protection by Direct Surface Functionalization of TiO2 with the Antioxidant Polyphenol Dihydroxyphenyl Benzimidazole Carboxylic Acid.
- Author
-
Battistin, Mattia, Dissette, Valeria, Bonetto, Alessandro, Durini, Elisa, Manfredini, Stefano, Marcomini, Antonio, Casagrande, Elisa, Brunetta, Andrea, Ziosi, Paola, Molesini, Sonia, Gavioli, Riccardo, Nicoli, Francesco, Vertuani, Silvia, and Baldisserotto, Anna
- Subjects
CARBOXYLIC acids ,SKIN cancer ,ULTRAVIOLET radiation ,ANTIOXIDANTS ,RADIATION exposure ,RHEOLOGY (Biology) ,BENZIMIDAZOLES ,FILTERS & filtration - Abstract
Skin cancer is the most common malignant cancer with an incidence of 1 million cases/year. It is well known that exposure to UV radiation from sunlight leads the most frequent risk factors for several skin disorders including skin cancer. Sunscreen filters represent a valid protection against dangerous effects derived from UV radiation, and they can be divided in organic and inorganic UV filters. Adding, at the product formulation, molecules with booster effect, or also substances that can increase the protecting effectiveness via synergic mechanisms, can further enhance their protection activity. Moreover, this approach leads to develop formulations with high SPF (Sun Protection Factor) with a reduced content of UV filters, this is in line with the recent decisions of yet a few countries (Palau, Thailand, Philippines, and Hawaii) to ban some sunscreen filters to preserve marine environments (i.e., reef). In this work, a new class of sunscreen UV filters has been synthesized, by means the combination of physical filter and Oxisol, an antioxidant molecule with booster effect. In this study, the synthesis of new physical multifunctional ingredients is reported, by means the direct surface functionalization of inorganic filters (in particular TiO
2 ) with Oxisol. In this study, the full characterization of these multifunctional ingredients is also reported, in addition to the cytotoxicity tests, the photocatalytic activity and the rheological properties involved on skin application. [ABSTRACT FROM AUTHOR]- Published
- 2020
- Full Text
- View/download PDF
8. Synthesis and Characterization of New Multifunctional Self-Boosted Filters for UV Protection: ZnO Complex with Dihydroxyphenyl Benzimidazole Carboxylic Acid.
- Author
-
Battistin, Mattia, Durini, Elisa, Dissette, Valeria, Bonetto, Alessandro, Marcomini, Antonio, Casagrande, Elisa, Brunetta, Andrea, Ziosi, Paola, Molesini, Sonia, Gavioli, Riccardo, Nicoli, Francesco, Manfredini, Stefano, Vertuani, Silvia, Baldisserotto, Anna, and Bencini, Andrea
- Subjects
CARBOXYLIC acids ,ZINC oxide synthesis ,FILTERS & filtration ,BENZIMIDAZOLES ,SKIN cancer ,PHOTOREDUCTION ,CANCER prevention - Abstract
The incidence of skin cancer is increasing both because of climate change and the increase in pollution than people's incorrect habits of sun exposure. In these regards, sunscreen and photoprotection are essential tools in consenting the benefits induced by safe solar light exposition and skin cancer prevention. In this work, a new class of sunscreen filter was synthesized by chemical combination of a physical filter (ZnO) and Oxisol (dihydroxyphenyl benzimidazole carboxylic acid), an antioxidant molecule with booster effect. In this work, a new class of filters with new properties was achieved by direct functionalization of particles surface. A full characterization of this multifunctional ingredient (ZnO–Ox) was conducted: Compared with the simple mixture, the new filter acts as a multifunctional molecule showing a higher Sun Protection Factor (SPF), a better cytotoxic profile (MTT and NRU assay), and anti-acne activity. A strong reduction of photocatalytic activity of ZnO was observed, also improving the safety profile. [ABSTRACT FROM AUTHOR]
- Published
- 2019
- Full Text
- View/download PDF
9. Antioxidant and antimicrobial extracts obtained from agricultural by-products: Strategies for a sustainable recovery and future perspectives.
- Author
-
Guerrini, Alessandra, Burlini, Ilaria, Lorenzo, Belen Huerta, Grandini, Alessandro, Vertuani, Silvia, Tacchini, Massimo, and Sacchetti, Gianni
- Abstract
Durum wheat and rice brans are by-products deriving from the milling industry and source of important phytochemicals, mostly phenolics in bound form. The objectives of this work were to evaluate the most effective method for the extraction of phenolic acids from these by-products with antioxidant and antimicrobial activity and to standardize the obtained extracts to encourage their commercialization in health field. Free phenolics were extracted with ultrasound-assisted extraction (UAE) and bound phenolics with alkaline hydrolysis (AH) and ultrasound-assisted alkaline hydrolysis (UAAH). Extracts were analyzed with HPTLC (high-performance thin-layer chromatography) and RPHPLC-DAD-ESIMS (reversed-phase high-performance liquid chromatography-diode array detector-electrospray ionization mass spectrometry); the content of trans-ferulic acid, p-coumaric acid, total phenolics were also quantified. The antioxidant activity was investigated using DPPH and ABTS methods. The antimicrobial activity was evaluated against Staphylococcus aureus and Staphylococcus epidermidis strains. Results obtained using UAAH showed the most interesting data, suggesting this method as the most effective to obtain active extracts from the by-products. Durum wheat, extracted with UAAH, exhibited the highest content of trans-ferulic acid (406.14 ± 0.65 ji,g FA/mg extract), total phenolics (610.58 ± 57.60 mg GAE/g dried extract) and good antioxidant and antimicrobial activities and it has been selected to formulate oil-in-water cosmetic products. [ABSTRACT FROM AUTHOR]
- Published
- 2020
- Full Text
- View/download PDF
10. Design, synthesis and evaluation of benzothiazole derivatives as multifunctional agents.
- Author
-
Djuidje, Ernestine Nicaise, Sciabica, Sabrina, Buzzi, Raissa, Dissette, Valeria, Balzarini, Jan, Liekens, Sandra, Serra, Elena, Andreotti, Elisa, Manfredini, Stefano, Vertuani, Silvia, and Baldisserotto, Anna
- Subjects
- *
BENZOTHIAZOLE derivatives , *POTASSIUM antagonists , *ANTIFUNGAL agents , *CONDENSATION reactions , *DRUG design - Abstract
• Multifunctional compounds are smart strategy for the treatment of multifactorial diseases. • Benzothiazole derivatives were evaluated for their UV-filtering, antioxidant, antifungal and antiproliferative activities. • Compounds 4g and 4k were potential multifunctional compounds. 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. [ABSTRACT FROM AUTHOR]
- Published
- 2020
- Full Text
- View/download PDF
Catalog
Discovery Service for Jio Institute Digital Library
For full access to our library's resources, please sign in.