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Prof. Dr. Antonio Carta
Università degli Studi di Sassari, Sassari, Italy

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0 Drug Discovery
0 Target validation
0 Structure-based drug design
0 Ligand-Based Drug Design
0 Lead compound design and synthesis

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Mechanism of action of antiviral agents

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Journal article
Published: 04 January 2021 in Viruses
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Enterovirus A71 (EV-A71) infection has emerged as a significant public health concern atthe global level. Epidemic events of EV-A71 have been reported worldwide, and this succession of outbreaks has heightened concern that EV-A71 may become a public health threat. In recent years, widespread A71 enterovirus also occurred in European countries. EV-A71 infection causes hand-foot-mouth disease (HFMD), herpangina, and fever. However, it can sometimes induce a variety of neurological complications, including encephalitis, aseptic meningitis, pulmonary edema, and acute flaccid paralysis. We identified new benzimidazole derivatives and described their in vitro cytotoxicity and broad-spectrum anti-enterovirus activity. Among them, derivative 2b resulted in interesting activity against EV-A71, and therefore it was selected for further investigations. Compound 2b proved to be able to protect cell monolayers from EV-A71-induced cytopathogenicity, with an EC50 of 3 µM. Moreover, Vero-76 cells resulted in being significantly protected from necrosis and apoptosis when treated with 2b at 20 and 80 µM. Compound 2b reduced viral adsorption to Vero-76 cells, and when evaluated in a time-of-addition assay, the derivative had the highest effect when added during the infection period. Moreover, derivative 2b reduced viral penetration into host cells. Besides, 2b did not affect intestinal monolayers permeability, showing no toxic effects. A detailed insight into the efficacy of compound 2b against EV-A71 showed a dose-dependent reduction in the viral titer, also at low concentrations. Mechanism of action investigations suggested that our derivative can inhibit viral endocytosis by reducing viral attachment to and penetration into host cells. Pharmacokinetic and toxicity predictions validated compound 2b as a good candidate for further in vivo assays.

ACS Style

Roberta Ibba; Antonio Carta; Silvia Madeddu; Paola Caria; Gabriele Serreli; Sandra Piras; Simona Sestito; Roberta Loddo; Giuseppina Sanna. Inhibition of Enterovirus A71 by a Novel 2-Phenyl-Benzimidazole Derivative. Viruses 2021, 13, 58 .

AMA Style

Roberta Ibba, Antonio Carta, Silvia Madeddu, Paola Caria, Gabriele Serreli, Sandra Piras, Simona Sestito, Roberta Loddo, Giuseppina Sanna. Inhibition of Enterovirus A71 by a Novel 2-Phenyl-Benzimidazole Derivative. Viruses. 2021; 13 (1):58.

Chicago/Turabian Style

Roberta Ibba; Antonio Carta; Silvia Madeddu; Paola Caria; Gabriele Serreli; Sandra Piras; Simona Sestito; Roberta Loddo; Giuseppina Sanna. 2021. "Inhibition of Enterovirus A71 by a Novel 2-Phenyl-Benzimidazole Derivative." Viruses 13, no. 1: 58.

Journal article
Published: 24 November 2020 in Pharmaceutics
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The role of mycobacterial efflux pumps in drug-resistant tuberculosis has been widely reported. Recently, a new compound, named SS13, has been synthesized, and its activity as a potential efflux inhibitor has been demonstrated. In this work, the chemical–physical properties of the SS13 were investigated; furthermore, a formulative study aimed to develop a formulation suitable for oral administration was performed. SS13 shows nonintrinsic antitubercular activity, but it increases the antitubercular activity of all the tested drugs on several strains. SS13 is insoluble in different simulated gastrointestinal media; thus, its oral absorption could be limited. Solid lipid nanoparticles (SLNs) were, therefore, developed by using two different lipids, Witepsol and/or Gelucire. Nanoparticles, having a particle size (range of 200–450 nm with regards to the formulation composition) suitable for intestinal absorption, are able to load SS13 and to improve its permeation through the intestinal mucosa compared to the pure compound. The cytotoxicity is influenced by the concentration of nanoparticles administered. These promising results support the potential application of these nanocarriers for increasing the oral permeation of SS13 in multidrug-resistant tuberculosis management.

ACS Style

Antonella Obinu; Elena Piera Porcu; Sandra Piras; Roberta Ibba; Antonio Carta; Paola Molicotti; Rossana Migheli; Alessandro Dalpiaz; Luca Ferraro; Giovanna Rassu; Elisabetta Gavini; Paolo Giunchedi. Solid Lipid Nanoparticles as Formulative Strategy to Increase Oral Permeation of a Molecule Active in Multidrug-Resistant Tuberculosis Management. Pharmaceutics 2020, 12, 1132 .

AMA Style

Antonella Obinu, Elena Piera Porcu, Sandra Piras, Roberta Ibba, Antonio Carta, Paola Molicotti, Rossana Migheli, Alessandro Dalpiaz, Luca Ferraro, Giovanna Rassu, Elisabetta Gavini, Paolo Giunchedi. Solid Lipid Nanoparticles as Formulative Strategy to Increase Oral Permeation of a Molecule Active in Multidrug-Resistant Tuberculosis Management. Pharmaceutics. 2020; 12 (12):1132.

Chicago/Turabian Style

Antonella Obinu; Elena Piera Porcu; Sandra Piras; Roberta Ibba; Antonio Carta; Paola Molicotti; Rossana Migheli; Alessandro Dalpiaz; Luca Ferraro; Giovanna Rassu; Elisabetta Gavini; Paolo Giunchedi. 2020. "Solid Lipid Nanoparticles as Formulative Strategy to Increase Oral Permeation of a Molecule Active in Multidrug-Resistant Tuberculosis Management." Pharmaceutics 12, no. 12: 1132.

Journal article
Published: 18 June 2020 in Antibiotics
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The rapid emergence of drug-resistant strains and novel viruses have motivated the search for new anti-infectious agents. In this study, the chemical compositions and cytotoxicity, as well as the antibacterial, antifungal, antitrichomonas, and antiviral activities of essential oils from the leaves, rhizomes, and whole plant of Hornstedtia bella were investigated. The GC/MS analysis showed that β-pinene, E-β-caryophyllene, and α-humulene were found at high concentrations in the essential oils. The essential oils exhibited (i) inhibition against Staphylococcus aureus, methicillin-resistant Staphylococcus aureus, Staphylococcus epidermidis with minimum inhibitory concentrations (MIC) and minimum lethal concentration (MLC) values from 1 to 4% (v/v); (ii) MIC and MLC values from 2 to 16% (v/v) in Candida tropicalis and Candida parapsilosis; (iii) MIC and MLC values from 4 to 16% in Enterococcus faecalis; and (iv) MIC and MLC values from 8 to greater than or equal to 16% (v/v) in the remaining strains, including Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae, Candida albicans, and Candida glabrata. In antitrichomonas activity, the leaves and whole-plant oils of Hornstedtia bella possessed IC50, IC90, and MLC values of 0.008%, 0.016%, and 0.03% (v/v), respectively, whilst those of rhizomes oil had in turn, 0.004%, 0.008%, and 0.016% (v/v).Besides, the leaf oil showed a weak cytotoxicity against Vero 76 and MRC-5; meanwhile, rhizomes and whole-plant oils did not exert any toxic effects on cell monolayers. Finally, these oils were not active against EV-A71.

ACS Style

Matthew Gavino Donadu; Nhan Trong Le; Duc Viet Ho; Tuan Quoc Doan; Anh Tuan Le; Ain Raal; Marianna Usai; Mauro Marchetti; Giuseppina Sanna; Silvia Madeddu; Paola Rappelli; Nicia Diaz; Paola Molicotti; Antonio Carta; Sandra Piras; Donatella Usai; Hoai Thi Nguyen; Piero Cappuccinelli; Stefania Zanetti. Phytochemical Compositions and Biological Activities of Essential Oils from the Leaves, Rhizomes and Whole Plant of Hornstedtia bella Škorničk. Antibiotics 2020, 9, 334 .

AMA Style

Matthew Gavino Donadu, Nhan Trong Le, Duc Viet Ho, Tuan Quoc Doan, Anh Tuan Le, Ain Raal, Marianna Usai, Mauro Marchetti, Giuseppina Sanna, Silvia Madeddu, Paola Rappelli, Nicia Diaz, Paola Molicotti, Antonio Carta, Sandra Piras, Donatella Usai, Hoai Thi Nguyen, Piero Cappuccinelli, Stefania Zanetti. Phytochemical Compositions and Biological Activities of Essential Oils from the Leaves, Rhizomes and Whole Plant of Hornstedtia bella Škorničk. Antibiotics. 2020; 9 (6):334.

Chicago/Turabian Style

Matthew Gavino Donadu; Nhan Trong Le; Duc Viet Ho; Tuan Quoc Doan; Anh Tuan Le; Ain Raal; Marianna Usai; Mauro Marchetti; Giuseppina Sanna; Silvia Madeddu; Paola Rappelli; Nicia Diaz; Paola Molicotti; Antonio Carta; Sandra Piras; Donatella Usai; Hoai Thi Nguyen; Piero Cappuccinelli; Stefania Zanetti. 2020. "Phytochemical Compositions and Biological Activities of Essential Oils from the Leaves, Rhizomes and Whole Plant of Hornstedtia bella Škorničk." Antibiotics 9, no. 6: 334.

Journal article
Published: 24 April 2020 in Antibiotics
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The present study aimed to determine the bioactivities of essential oils extracted from the leaves of Paramignya trimera and Limnocitrus littoralis, including cytotoxicity, antiviral, antibacterial, antimycotic, and antitrichomonas effects. Herein, it was indicated that P. trimera and L. littoralis oils showed no cytotoxicity on normal cells, namely MT-4, BHK-21, MDBK, and Vero-76. P. trimera oil (i) exhibited the strongest inhibition against Staphylococcus aureus with MIC and MLC values of 2% (v/v); (ii) showed MIC and MLC values of 8% (v/v) in Candida parapsilosis; and (iii) in the remaining strains, showed MIC and MLC values greater than or equal to 16% (v/v). On the other hand, L. littoralis oil (i) displayed the strongest inhibition against Candida tropicalis and Candida parapsilosis with 2% (v/v) of MIC and MLC; and (ii) in the remaining strains, possessed MIC and MLC greater than or equal to 16% (v/v). In addition, antitrichomonas activities of the oils were undertaken, showing IC50, IC90, MLC values, respectively, at 0.016%, 0.03%, and 0.06% (v/v) from P. trimera, and 0.03%, 0.06%, 0.12% (v/v) from L. littoralis, after 48 h of incubation. The oils were completely ineffective against ssRNA+ (HIV-1, YFV, BVDV, Sb-1, CV-B4), ssRNA- (RSV, VSV), dsRNA (Reo-1), and dsDNA (HSV-1, VV) viruses. This is the first report describing the cytotoxicity, antiviral, antibacterial, antimycotic, and antitrichomonas activities of the essential oils of P. trimera and L. littoralis.

ACS Style

Nhan Trong Le; Duc Viet Ho; Tuan Quoc Doan; Anh Tuan Le; Ain Raal; Donatella Usai; Giuseppina Sanna; Antonio Carta; Paola Rappelli; Nicia Diaz; Piero Cappuccinelli; Stefania Zanetti; Hoai Thi Nguyen; Matthew Gavino Donadu. Biological Activities of Essential Oils from Leaves of Paramignya trimera (Oliv.) Guillaum and Limnocitrus littoralis (Miq.) Swingle. Antibiotics 2020, 9, 207 .

AMA Style

Nhan Trong Le, Duc Viet Ho, Tuan Quoc Doan, Anh Tuan Le, Ain Raal, Donatella Usai, Giuseppina Sanna, Antonio Carta, Paola Rappelli, Nicia Diaz, Piero Cappuccinelli, Stefania Zanetti, Hoai Thi Nguyen, Matthew Gavino Donadu. Biological Activities of Essential Oils from Leaves of Paramignya trimera (Oliv.) Guillaum and Limnocitrus littoralis (Miq.) Swingle. Antibiotics. 2020; 9 (4):207.

Chicago/Turabian Style

Nhan Trong Le; Duc Viet Ho; Tuan Quoc Doan; Anh Tuan Le; Ain Raal; Donatella Usai; Giuseppina Sanna; Antonio Carta; Paola Rappelli; Nicia Diaz; Piero Cappuccinelli; Stefania Zanetti; Hoai Thi Nguyen; Matthew Gavino Donadu. 2020. "Biological Activities of Essential Oils from Leaves of Paramignya trimera (Oliv.) Guillaum and Limnocitrus littoralis (Miq.) Swingle." Antibiotics 9, no. 4: 207.

Communication
Published: 20 January 2020 in Viruses
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Orthohantaviruses, previously known as hantaviruses (family Hantaviridae, order Bunyavirales), are emerging zoonoses hosted by different rodent and insectivore species. Orthohantaviruses are transmitted by aerosolized excreta (urine, saliva and feces) of their reservoir hosts. When transmitted to humans, they cause hemorrhagic fever with renal syndrome (HFRS) in Asia and Europe and hantavirus (cardio) pulmonary syndrome (HPS) in the Americas. Clinical studies have shown that early treatments of HFRS patients with ribavirin (RBV) improve prognosis. Nevertheless, there is the need for urgent development of specific antiviral drugs. In the search for new RNA virus inhibitors, we recently identified a series of variously substituted 5,6-dichloro-1(2)-phenyl-1(2)H-benzo[d][1,2,3]triazole derivatives active against the human respiratory syncytial virus (HRSV). Interestingly, several 2-phenyl-benzotriazoles resulted in fairly potent inhibitors of the Hantaan virus in a chemiluminescence focus reduction assay (C-FRA) showing an EC50 = 4–5 µM, ten-fold more active than ribavirin. Currently, there are no FDA approved drugs for the treatment of orthohantavirus infections. Antiviral activities and cytotoxicity profiles suggest that 5,6-dichloro-1(2)-phenyl-1(2)H-benzo[d][1,2,3]triazoles could be promising candidates for further investigation as a potential treatment of hantaviral diseases.

ACS Style

Giuseppina Sanna; Sandra Piras; Silvia Madeddu; Bernardetta Busonera; Boris Klempa; Paola Corona; Roberta Ibba; Gabriele Murineddu; Antonio Carta; Roberta Loddo. 5,6-Dichloro-2-Phenyl-Benzotriazoles: New Potent Inhibitors of Orthohantavirus. Viruses 2020, 12, 122 .

AMA Style

Giuseppina Sanna, Sandra Piras, Silvia Madeddu, Bernardetta Busonera, Boris Klempa, Paola Corona, Roberta Ibba, Gabriele Murineddu, Antonio Carta, Roberta Loddo. 5,6-Dichloro-2-Phenyl-Benzotriazoles: New Potent Inhibitors of Orthohantavirus. Viruses. 2020; 12 (1):122.

Chicago/Turabian Style

Giuseppina Sanna; Sandra Piras; Silvia Madeddu; Bernardetta Busonera; Boris Klempa; Paola Corona; Roberta Ibba; Gabriele Murineddu; Antonio Carta; Roberta Loddo. 2020. "5,6-Dichloro-2-Phenyl-Benzotriazoles: New Potent Inhibitors of Orthohantavirus." Viruses 12, no. 1: 122.

Original research article
Published: 16 April 2019 in Frontiers in Chemistry
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Human Respiratory Syncytial Virus (RSV) is the primary cause of bronchopneumonia in infants and children worldwide. Clinical studies have shown that early treatments of RSV patients with ribavirin improve prognosis, even if the use of this drug is limited due to myelosuppression and toxicity effects. Furthermore, effective vaccines to prevent RSV infection are currently unavailable. Thus, the development of highly effective and specific antiviral drugs for pre-exposure prophylaxis and/or treatment of RSV infections is a compelling need. In the quest of new RSV inhibitors, in this work we evaluated the antiviral activity of a series of variously substituted 5,6-dichloro-1-phenyl-1(2)H-benzo[d][1,2,3]triazole derivatives in cell-based assays. Several 1- and 2-phenyl-benzotriazoles resulted fairly potent (μM concentrations) inhibitors of RSV infection in plaque reduction assays, accompanied by low cytotoxicity in human highly dividing T lymphoid-derived cells and primary cell lines. Contextually, no inhibitory effects were observed against other RNA or DNA viruses assayed, suggesting specific activity against RSV. Further results revealed that the lead compound 10d was active during the early phase of the RSV infection cycle. To understand whether 10d interfered with virus attachment to target cells or virus-cell fusion events, inhibitory activity tests against the RSV mutant strain B1 cp-52—expressing only the F envelope glycoprotein—and a plasmid-based reporter assay that quantifies the bioactivity of viral entry were also performed. The overall biological results, in conjunction with in silico modeling studies, supported the conclusion that the RSV fusion process could be the target of this new series of compounds.

ACS Style

Sandra Piras; Giuseppina Sanna; Antonio Carta; Paola Corona; Roberta Ibba; Roberta Loddo; Silvia Madeddu; Paola Caria; Suzana Aulic; Erik Laurini; Maurizio Fermeglia; Sabrina Pricl. Dichloro-Phenyl-Benzotriazoles: A New Selective Class of Human Respiratory Syncytial Virus Entry Inhibitors. Frontiers in Chemistry 2019, 7, 247 .

AMA Style

Sandra Piras, Giuseppina Sanna, Antonio Carta, Paola Corona, Roberta Ibba, Roberta Loddo, Silvia Madeddu, Paola Caria, Suzana Aulic, Erik Laurini, Maurizio Fermeglia, Sabrina Pricl. Dichloro-Phenyl-Benzotriazoles: A New Selective Class of Human Respiratory Syncytial Virus Entry Inhibitors. Frontiers in Chemistry. 2019; 7 ():247.

Chicago/Turabian Style

Sandra Piras; Giuseppina Sanna; Antonio Carta; Paola Corona; Roberta Ibba; Roberta Loddo; Silvia Madeddu; Paola Caria; Suzana Aulic; Erik Laurini; Maurizio Fermeglia; Sabrina Pricl. 2019. "Dichloro-Phenyl-Benzotriazoles: A New Selective Class of Human Respiratory Syncytial Virus Entry Inhibitors." Frontiers in Chemistry 7, no. : 247.

Original research article
Published: 09 April 2019 in Frontiers in Chemistry
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A series of N-((3-phenyl-1-(phenylsulfonyl)-1H-pyrazol-4-yl)methyl)anilines 7a-p and 8a-l, structurally related to previously synthesized and tested (N-(1,3-diphenyl-1H-pyrazol-4-yl)methyl)anilines (1a-v), were designed and synthesized. The new derivatives were evaluated in cell-based assays for their cytotoxicity and antiviral activity against a large panel of RNA and DNA viruses of public health significance. Generally, the tested compounds did not display cytotoxicity toward the cell lines used. The majority of derivatives 7a-p were able to interfered with YFV and RSV replication in the micromolar range showing a marked improvement in potency and selectivity with respect to the reference inhibitors 6-azauridine and ribavirin, respectively. The introduction of a p-methoxy substituent on the phenylsulfonyl group (compounds 8a-l) completely abolished the anti-RSV activity and reduced or eliminated the potency against YFV. On the contrary, several p-methoxy analogs were able to interfere with BVDV replication with a comparable (8b, 8c, 8g, and 8k) or better (8a and 8f) potency than the reference inhibitor, ribavirin. Compound 7e, selected for time of addition experiments on BHK-21 cell cultures infected with YFV, achieved the highest reduction of virus titer when added 2 h post infection and maintained up to 4 h post infection.

ACS Style

Nicoletta Desideri; Rossella Fioravanti; Luca Proietti Monaco; Elena Maria Atzori; Antonio Carta; Ilenia Delogu; Gabriella Collu; Roberta Loddo. Design, Synthesis, Antiviral Evaluation, and SAR Studies of New 1-(Phenylsulfonyl)-1H-Pyrazol−4-yl-Methylaniline Derivatives. Frontiers in Chemistry 2019, 7, 1 .

AMA Style

Nicoletta Desideri, Rossella Fioravanti, Luca Proietti Monaco, Elena Maria Atzori, Antonio Carta, Ilenia Delogu, Gabriella Collu, Roberta Loddo. Design, Synthesis, Antiviral Evaluation, and SAR Studies of New 1-(Phenylsulfonyl)-1H-Pyrazol−4-yl-Methylaniline Derivatives. Frontiers in Chemistry. 2019; 7 ():1.

Chicago/Turabian Style

Nicoletta Desideri; Rossella Fioravanti; Luca Proietti Monaco; Elena Maria Atzori; Antonio Carta; Ilenia Delogu; Gabriella Collu; Roberta Loddo. 2019. "Design, Synthesis, Antiviral Evaluation, and SAR Studies of New 1-(Phenylsulfonyl)-1H-Pyrazol−4-yl-Methylaniline Derivatives." Frontiers in Chemistry 7, no. : 1.

Journal article
Published: 28 February 2019 in The Journal of Infection in Developing Countries
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Introduction: with the continuous emergence of pathogenic resistance to conventional drugs through efflux pumps, increasing efforts are directed toward discovering efflux inhibitory molecules. Methodology: in this study three P-glycoprotein (P13CP, P22CP, P34CP) efflux-inhibitors (EIs), belonging to the series of phenoxymethylquinoxalines capable to restore/potentiate the antiproliferative activity of doxorubicin and vincristine against human tumor cell lines and different antibiotics against clinical isolates, were investigated on 10 clinical strains of Candida and 12 clinical and ATCC strains of Gram positive and Gram-negative bacteria. Results: MFC values of FLC were reduced in all Candida strains by the P22CP and P34CP inhibitors, and in 5/10 fungal strains by the P13CP inhibitor. Conclusion: novel antibiotics with new modes of action are urgently required to suppress the rise of MDR bacteria. An alternative approach would be to identify molecules that can interfere with the process of efflux.

ACS Style

Donatella Usai; Matthew Donadu; Alessandra Bua; Paola Molicotti; Stefania Zanetti; Sandra Piras; Paola Corona; Roberta Ibba; Antonio Carta. Enhancement of antimicrobial activity of pump inhibitors associating drugs. The Journal of Infection in Developing Countries 2019, 13, 162 -164.

AMA Style

Donatella Usai, Matthew Donadu, Alessandra Bua, Paola Molicotti, Stefania Zanetti, Sandra Piras, Paola Corona, Roberta Ibba, Antonio Carta. Enhancement of antimicrobial activity of pump inhibitors associating drugs. The Journal of Infection in Developing Countries. 2019; 13 (2):162-164.

Chicago/Turabian Style

Donatella Usai; Matthew Donadu; Alessandra Bua; Paola Molicotti; Stefania Zanetti; Sandra Piras; Paola Corona; Roberta Ibba; Antonio Carta. 2019. "Enhancement of antimicrobial activity of pump inhibitors associating drugs." The Journal of Infection in Developing Countries 13, no. 2: 162-164.

Journal article
Published: 17 October 2018 in European Journal of Medicinal Chemistry
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A number of new F-triazolequinolones (FTQs) and alkoxy-triazolequinolones (ATQs) were designed, synthesized and evaluated for their activity against Mycobacterium tuberculosis H37Rv. Five out of 21 compounds exhibited interesting minimum inhibitory concentration (MIC) values (6.6–57.9 μM), ATQs generally being more potent than FTQs. Two ATQs, 21a and 30a, were endowed with the best anti-Mtb potency (MIC = 6.9 and 6.6 μM, respectively), and were not cytotoxic in a Vero cell line. Tested for activity against M. tuberculosis DNA gyrase in a DNA supercoiling activity assay, 21a and 30a showed IC50 values (27–28 μM) comparable to that of ciprofloxacin (10.6 μM). 21a was next selected for screening against several Mtb strains obtained from clinical isolates, including multi-drug-resistant (MDR) variants. Importantly, this compound was effective in all cases, with very promising MIC values (4 μM) in the case of some isoniazid/rifampicin-resistant Mtb strains. Finally, computer-based simulations revealed that the binding mode of 21a in the Mtb gyrase cleavage core complexed with DNA and the relevant network of intermolecular interactions are utterly similar to those described for ciprofloxacin, yielding a molecular rationale for the comparable anti-mycobacterial and DNA gyrase inhibition activity of this quinolone.

ACS Style

Antonio Carta; Alessandra Bua; Paola Corona; Sandra Piras; Irene Briguglio; Paola Molicotti; Stefania Zanetti; Erik Laurini; Suzana Aulic; Maurizio Fermeglia; Sabrina Pricl. Design, synthesis and antitubercular activity of 4-alkoxy-triazoloquinolones able to inhibit the M. tuberculosis DNA gyrase. European Journal of Medicinal Chemistry 2018, 161, 399 -415.

AMA Style

Antonio Carta, Alessandra Bua, Paola Corona, Sandra Piras, Irene Briguglio, Paola Molicotti, Stefania Zanetti, Erik Laurini, Suzana Aulic, Maurizio Fermeglia, Sabrina Pricl. Design, synthesis and antitubercular activity of 4-alkoxy-triazoloquinolones able to inhibit the M. tuberculosis DNA gyrase. European Journal of Medicinal Chemistry. 2018; 161 ():399-415.

Chicago/Turabian Style

Antonio Carta; Alessandra Bua; Paola Corona; Sandra Piras; Irene Briguglio; Paola Molicotti; Stefania Zanetti; Erik Laurini; Suzana Aulic; Maurizio Fermeglia; Sabrina Pricl. 2018. "Design, synthesis and antitubercular activity of 4-alkoxy-triazoloquinolones able to inhibit the M. tuberculosis DNA gyrase." European Journal of Medicinal Chemistry 161, no. : 399-415.

Original paper
Published: 09 June 2018 in Monatshefte für Chemie - Chemical Monthly
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In this study, we designed and synthesized a series of new 5-chlorobenzotriazole derivatives. Compounds were tested for cytotoxicity and antiviral activity in cell-based assays against several positive single-stranded RNA viruses: BVDV, YFV, CVB-5, and Sb-1; two negative single-stranded RNA viruses: RSV and VSV; a double-stranded RNA virus (Reo-1); and two DNA viruses: VV and HSV-1. N-[4-(5-Chloro-2H-benzo[d][1,2,3]triazol-2-yl)phenyl]-3,4,5-trimethoxybenzamide turned out to be the most potent compound against bovine viral diarrhea virus (BVDV). Its activity was shown to be comparable to the activity of the reference drug NM 107 (EC50 3.0 vs. 1.7 μM). It is going to be used as a lead compound for future antiviral drug developments.

ACS Style

Roberta Ibba; Paola Corona; Antonio Carta; Paolo Giunchedi; Roberta Loddo; Giuseppina Sanna; Ilenia Delogu; Sandra Piras. Antiviral activities of 5-chlorobenzotriazole derivatives. Monatshefte für Chemie - Chemical Monthly 2018, 149, 1247 -1256.

AMA Style

Roberta Ibba, Paola Corona, Antonio Carta, Paolo Giunchedi, Roberta Loddo, Giuseppina Sanna, Ilenia Delogu, Sandra Piras. Antiviral activities of 5-chlorobenzotriazole derivatives. Monatshefte für Chemie - Chemical Monthly. 2018; 149 (7):1247-1256.

Chicago/Turabian Style

Roberta Ibba; Paola Corona; Antonio Carta; Paolo Giunchedi; Roberta Loddo; Giuseppina Sanna; Ilenia Delogu; Sandra Piras. 2018. "Antiviral activities of 5-chlorobenzotriazole derivatives." Monatshefte für Chemie - Chemical Monthly 149, no. 7: 1247-1256.

Journal article
Published: 01 December 2017 in European Journal of Medicinal Chemistry
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By the antiviral screening of an in house library of pyrazoline compounds, 4-(3-(4-phenoxyphenyl)-5-phenyl-4,5-dihydro-1H-pyrazol-1-yl)benzenesulfonamide (5a) was identified as a promising hit compound for the development of anti- Yellow Fever Virus (YFV) agents. Structural optimization studies were focused on the development of 5a analogues which retain the potency as YFV inhibitors and show a reduced cytotoxicity. The synthesized 1-3,5-triphenyl-pyrazolines (4a-j, 5a-j, 6a-j) were evaluated in cell based assays for cytotoxicity and antiviral activity against representative viruses of two of the three genera of the Flaviviridae family, i.e.: Pestivirus (BVDV) and Flavivirus (YFV). These compounds were also tested against a large panel of different pathogenic RNA and DNA viruses. Most of the new 1-3,5-triphenyl-pyrazolines (4a-j, 5a-j, 6a-j) exhibited a specific activity against YFV, showing EC50 values in the low micromolar range with almost a 10-fold improvement in potency compared to the reference inhibitor 6-azauridine. However, the selectivity indexes of the unsubstituted (4a-j) and the phenoxy (5a-j) analogues were generally modest due to the pronounced cytotoxicity against BHK-21 cells. Otherwise, the benzyloxy derivatives (6a-j) generally coupled high potency and selectivity. On the basis of both anti-YFV activity and selectivity index, pyrazolines 6a and 6b were chosen for time of addition experiments. The selected pyrazolines and the reference inhibitor 6-azauridine displayed maximal inhibition when added in the pretreatment or during the infection.

ACS Style

Rossella Fioravanti; Nicoletta Desideri; Antonio Carta; Elena Maria Atzori; Ilenia Delogu; Gabriella Collu; Roberta Loddo. Inhibitors of Yellow Fever Virus replication based on 1,3,5-triphenyl-4,5-dihydropyrazole scaffold: Design, synthesis and antiviral evaluation. European Journal of Medicinal Chemistry 2017, 141, 15 -25.

AMA Style

Rossella Fioravanti, Nicoletta Desideri, Antonio Carta, Elena Maria Atzori, Ilenia Delogu, Gabriella Collu, Roberta Loddo. Inhibitors of Yellow Fever Virus replication based on 1,3,5-triphenyl-4,5-dihydropyrazole scaffold: Design, synthesis and antiviral evaluation. European Journal of Medicinal Chemistry. 2017; 141 ():15-25.

Chicago/Turabian Style

Rossella Fioravanti; Nicoletta Desideri; Antonio Carta; Elena Maria Atzori; Ilenia Delogu; Gabriella Collu; Roberta Loddo. 2017. "Inhibitors of Yellow Fever Virus replication based on 1,3,5-triphenyl-4,5-dihydropyrazole scaffold: Design, synthesis and antiviral evaluation." European Journal of Medicinal Chemistry 141, no. : 15-25.

Journal article
Published: 01 December 2017 in European Journal of Medicinal Chemistry
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In this paper we report the synthesis, in vitro anticancer activity, and the experimental/computational characterization of mechanism of action of a new series of E isomers of triazolo[4,5-b/c]pyridin-acrylonitrile derivatives (6c-g, 7d-e, 8d-e, 9c-f, 10d-e, 11d-e). All new compounds are endowed with moderate to interesting antiproliferative activity against 9 different cancer cell lines derived from solid and hematological human tumors. Fluorescence-based assays prove that these molecules interfere with tubulin polymerization. Furthermore, isothermal titration calorimetry (ITC) provides full tubulin/compound binding thermodynamics, thereby ultimately qualifying and quantifying the interactions of these molecular series with the target protein. Lastly, the analysis based on the tight coupling of in vitro and in silico modeling of the interactions between tubulin and the title compounds allows to propose a molecular rationale for their biological activity.

ACS Style

Irene Briguglio; Erik Laurini; Maria Antonietta Pirisi; Sandra Piras; Paola Corona; Maurizio Fermeglia; Sabrina Pricl; Antonio Carta. Triazolopyridinyl-acrylonitrile derivatives as antimicrotubule agents: Synthesis, in vitro and in silico characterization of antiproliferative activity, inhibition of tubulin polymerization and binding thermodynamics. European Journal of Medicinal Chemistry 2017, 141, 460 -472.

AMA Style

Irene Briguglio, Erik Laurini, Maria Antonietta Pirisi, Sandra Piras, Paola Corona, Maurizio Fermeglia, Sabrina Pricl, Antonio Carta. Triazolopyridinyl-acrylonitrile derivatives as antimicrotubule agents: Synthesis, in vitro and in silico characterization of antiproliferative activity, inhibition of tubulin polymerization and binding thermodynamics. European Journal of Medicinal Chemistry. 2017; 141 ():460-472.

Chicago/Turabian Style

Irene Briguglio; Erik Laurini; Maria Antonietta Pirisi; Sandra Piras; Paola Corona; Maurizio Fermeglia; Sabrina Pricl; Antonio Carta. 2017. "Triazolopyridinyl-acrylonitrile derivatives as antimicrotubule agents: Synthesis, in vitro and in silico characterization of antiproliferative activity, inhibition of tubulin polymerization and binding thermodynamics." European Journal of Medicinal Chemistry 141, no. : 460-472.

Journal article
Published: 01 July 2016 in European Journal of Medicinal Chemistry
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In this work, we present and discuss a comprehensive set of both newly and previously synthesized compounds belonging to 5 distinct molecular classes of linear aromatic N-polycyclic systems that efficiently inhibits bovine viral diarrhea virus (BVDV) infection. A coupled in silico/in vitro investigation was employed to formulate a molecular rationale explaining the notable affinity of all molecules to BVDV RNA dependent RNA polymerase (RdRp) NS5B. We initially developed a three-dimensional common-feature pharmacophore model according to which two hydrogen bond acceptors and one hydrophobic aromatic feature are shared by all molecular series in binding the viral polymerase. The pharmacophoric information was used to retrieve a putative binding site on the surface of the BVDV RdRp and to guide compound docking within the protein binding site. The affinity of all compounds towards the enzyme was scored via molecular dynamics-based simulations, showing high correlation with in vitro EC50 data. The determination of the interaction spectra of the protein residues involved in inhibitor binding highlighted amino acids R295 and Y674 as the two fundamental H-bond donors, while two hydrophobic cavities HC1 (residues A221, I261, I287, and Y289) and HC2 (residues V216, Y303, V306, K307, P408, and A412) fulfill the third pharmacophoric requirement. Three RdRp (K263, R295 and Y674) residues critical for drug binding were selected and mutagenized, both in silico and in vitro, into alanine, and the affinity of a set of selected compounds towards the mutant RdRp isoforms was determined accordingly. The agreement between predicted and experimental data confirmed the proposed common molecular rationale shared by molecules characterized by different chemical scaffolds in binding to the BVDV RdRp, ultimately yielding compound 6b (EC50 = 0.3 μM; IC50 = 0.48 μM) as a new, potent inhibitor of this Pestivirus.

ACS Style

A. Carta; I. Briguglio; S. Piras; P. Corona; R. Ibba; E. Laurini; M. Fermeglia; S. Pricl; N. Desideri; E.M. Atzori; P. La Colla; G. Collu; I. Delogu; R. Loddo. A combined in silico / in vitro approach unveils common molecular requirements for efficient BVDV RdRp binding of linear aromatic N-polycyclic systems. European Journal of Medicinal Chemistry 2016, 117, 321 -334.

AMA Style

A. Carta, I. Briguglio, S. Piras, P. Corona, R. Ibba, E. Laurini, M. Fermeglia, S. Pricl, N. Desideri, E.M. Atzori, P. La Colla, G. Collu, I. Delogu, R. Loddo. A combined in silico / in vitro approach unveils common molecular requirements for efficient BVDV RdRp binding of linear aromatic N-polycyclic systems. European Journal of Medicinal Chemistry. 2016; 117 ():321-334.

Chicago/Turabian Style

A. Carta; I. Briguglio; S. Piras; P. Corona; R. Ibba; E. Laurini; M. Fermeglia; S. Pricl; N. Desideri; E.M. Atzori; P. La Colla; G. Collu; I. Delogu; R. Loddo. 2016. "A combined in silico / in vitro approach unveils common molecular requirements for efficient BVDV RdRp binding of linear aromatic N-polycyclic systems." European Journal of Medicinal Chemistry 117, no. : 321-334.

Journal article
Published: 01 December 2015 in Colloids and Surfaces B: Biointerfaces
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Propolis shows therapeutic properties ascribed to the presence of some flavonoids, phenolic acids, and their esters; it is a natural multifunctional material, solid at room temperature, and composed mainly of resin and waxes. We therefore used propolis as a lipid material to prepare solid lipid nanoparticles (SLNs); SLNs are proposed bioactive medications for topical intranasal therapy. Suitable formulation parameters were studied and the SLNs obtained by the high shear homogenization method were characterized; a selected formulation was viscosized to increase the residence time. Dimensional, morphological, and solid-state characterizations of the formulated SLNs were performed. In vitro and ex vivo permeation tests of diclofenac sodium, the model drug, and polyphenols were carried out. The propolis amount and surfactant concentration represent the key parameters that affect nanoparticle properties in terms of size, drug and polyphenol content, and physical stability. Size dispersions of about 600 nm and 0.4 PI were obtained, which do not change by increasing the viscosity. Drug is encapsulated in SLNs, as demonstrated by FTIR and DSC analyses. In vitro and ex vivo studies prove that drug and polyphenols do not cross the membranes; therefore, propolis-based SLNs could be used as delivery systems of diclofenac and flavonoids for the local treatment of nasal cavity diseases. Due to propolis composition, the proposed formulation could be used as a bioactive medication in which the carrier can exert a complementary effect with the loaded drug.

ACS Style

Giovanna Rassu; Massimo Cossu; Rita Langasco; Antonio Carta; Roberta Cavalli; Paolo Giunchedi; Elisabetta Gavini. Propolis as lipid bioactive nano-carrier for topical nasal drug delivery. Colloids and Surfaces B: Biointerfaces 2015, 136, 908 -917.

AMA Style

Giovanna Rassu, Massimo Cossu, Rita Langasco, Antonio Carta, Roberta Cavalli, Paolo Giunchedi, Elisabetta Gavini. Propolis as lipid bioactive nano-carrier for topical nasal drug delivery. Colloids and Surfaces B: Biointerfaces. 2015; 136 ():908-917.

Chicago/Turabian Style

Giovanna Rassu; Massimo Cossu; Rita Langasco; Antonio Carta; Roberta Cavalli; Paolo Giunchedi; Elisabetta Gavini. 2015. "Propolis as lipid bioactive nano-carrier for topical nasal drug delivery." Colloids and Surfaces B: Biointerfaces 136, no. : 908-917.

Review article
Published: 30 September 2014 in European Journal of Medicinal Chemistry
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Discovered in late 1960, azoles are heterocyclic compounds class which constitute the largest group of available antifungal drugs. Particularly, the imidazole ring is the chemical component that confers activity to azoles. Triazoles are obtained by a slight modification of this ring and similar or improved activities as well as less adverse effects are reported for triazole derivatives. Consequently, it is not surprising that benzimidazole/benzotriazole derivatives have been found to be biologically active. Since benzimidazole has been widely investigated, this review is focused on defining the place of benzotriazole derivatives in biomedical research, highlighting their versatile biological properties, the mode of action and Structure Activity Relationship (SAR) studies for a variety of antimicrobial, antiparasitic, and even antitumor, choleretic, cholesterol-lowering agents.

ACS Style

I. Briguglio; S. Piras; P. Corona; E. Gavini; Maria Nieddu; Gianpiero Boatto; A. Carta. Benzotriazole: An overview on its versatile biological behavior. European Journal of Medicinal Chemistry 2014, 97, 612 -648.

AMA Style

I. Briguglio, S. Piras, P. Corona, E. Gavini, Maria Nieddu, Gianpiero Boatto, A. Carta. Benzotriazole: An overview on its versatile biological behavior. European Journal of Medicinal Chemistry. 2014; 97 ():612-648.

Chicago/Turabian Style

I. Briguglio; S. Piras; P. Corona; E. Gavini; Maria Nieddu; Gianpiero Boatto; A. Carta. 2014. "Benzotriazole: An overview on its versatile biological behavior." European Journal of Medicinal Chemistry 97, no. : 612-648.

Journal article
Published: 01 September 2014 in European Journal of Medicinal Chemistry
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Continuing our program of research concerning the antiviral activity of a wide series of new angular and linear azolo bicyclic and tricyclic derivatives, now we have simplified and modified the 4-chloro-2-(4-nitrophenyl)-3H-imidazo[4,5-g]quinoline 1, which previously resulted the most active derivative, through either the elimination of the central ring or the opening of the imidazole ring, obtaining various imidazopyridines and N-benzylidenequinolinamines respectively. Title compounds were tested in cell-based assays for cytotoxicity and antiviral activity against representatives of two DNA virus families as wells as against representatives of RNA virus families containing single-stranded, either positive-sense (ssRNA+) or negative-sense (ssRNA-), and double-stranded genomes (dsRNA). Some imidazo[4,5-b]pyridines emerged as new derivatives endowed with antiviral activity against Vaccinia Virus (VV) at concentrations ranging from 2 to 16 μM. In particular, compound 2b demonstrate to be about 10 times more potent than Cidofovir, used as reference drug. Similarly, the imidazo[4,5-c]pyridines and N-benzylidenequinolinamines derivatives resulted active against Bovine Viral Diarrhoea virus (BVDV), at concentrations ranging from 1.2 to 28 μM. Above all compounds 1, 3a and 3f showed an EC50 of the same order of magnitude of the reference drug, the 2'-C-methyl-guanosine. Moreover, several N-benzylidenequinolinamines showed an interesting activity against Respiratory Syncytial Virus (RSV) at concentrations between 12 and 26 μM

ACS Style

Roberta Loddo; Irene Briguglio; Paola Corona; Sandra Piras; Mario Loriga; Giuseppe Paglietti; Antonio Carta; Giuseppina Sanna; Gabriele Giliberti; Cristina Ibba; Pamela Farci; Paolo La Colla. Synthesis and antiviral activity of new phenylimidazopyridines and N-benzylidenequinolinamines derived by molecular simplification of phenylimidazo[4,5-g]quinolines. European Journal of Medicinal Chemistry 2014, 84, 8 -16.

AMA Style

Roberta Loddo, Irene Briguglio, Paola Corona, Sandra Piras, Mario Loriga, Giuseppe Paglietti, Antonio Carta, Giuseppina Sanna, Gabriele Giliberti, Cristina Ibba, Pamela Farci, Paolo La Colla. Synthesis and antiviral activity of new phenylimidazopyridines and N-benzylidenequinolinamines derived by molecular simplification of phenylimidazo[4,5-g]quinolines. European Journal of Medicinal Chemistry. 2014; 84 ():8-16.

Chicago/Turabian Style

Roberta Loddo; Irene Briguglio; Paola Corona; Sandra Piras; Mario Loriga; Giuseppe Paglietti; Antonio Carta; Giuseppina Sanna; Gabriele Giliberti; Cristina Ibba; Pamela Farci; Paolo La Colla. 2014. "Synthesis and antiviral activity of new phenylimidazopyridines and N-benzylidenequinolinamines derived by molecular simplification of phenylimidazo[4,5-g]quinolines." European Journal of Medicinal Chemistry 84, no. : 8-16.

Journal article
Published: 01 February 2014 in Carbohydrate Polymers
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Thymol, an effective agent for microbial diseases, has a low aqueous solubility and a strong bitter/irritating taste. These physicochemical characteristics need to be improved to develop pharmaceutical preparations. This study evaluates whether β-cyclodextrin and a copolymer based on dimethylaminoethyl methacrylate (DMAEMA) interact with thymol in order to control powderization, solubilization, and taste-masking properties. The thymol-β-cyclodextrin complex was prepared by co-precipitation and sealed-heating methods. The DMAEMA copolymer was mixed with the complex using a new approach, instead of spray coating, to decrease thymol volatility. In vivo studies were performed. Sealed-heating is a suitable method for including thymol in β-cyclodextrin with a good loading efficiency; thymol volatility control is achieved by mixing the complex with the DMAEMA copolymer. β-Cyclodextrin accelerates the in vivo thymol absorption rate compared with the free drug; the thymol half-life is still long. Therefore, a low number of administrations per day are required. Although bioavailability is unchanged with respect to free thymol, high doses could be administered of a selected formulation without compromising the compliance. Furthermore, thymol that is not absorbed is held along the intestine, where it can useful in the treatment and/or prevention of intestinal bacterial diseases.

ACS Style

Maria Nieddu; Giovanna Rassu; Gianpiero Boatto; Paolo Bosi; Paolo Trevisi; Paolo Giunchedi; Antonio Carta; Elisabetta Gavini. Improvement of thymol properties by complexation with cyclodextrins: In vitro and in vivo studies. Carbohydrate Polymers 2014, 102, 393 -399.

AMA Style

Maria Nieddu, Giovanna Rassu, Gianpiero Boatto, Paolo Bosi, Paolo Trevisi, Paolo Giunchedi, Antonio Carta, Elisabetta Gavini. Improvement of thymol properties by complexation with cyclodextrins: In vitro and in vivo studies. Carbohydrate Polymers. 2014; 102 ():393-399.

Chicago/Turabian Style

Maria Nieddu; Giovanna Rassu; Gianpiero Boatto; Paolo Bosi; Paolo Trevisi; Paolo Giunchedi; Antonio Carta; Elisabetta Gavini. 2014. "Improvement of thymol properties by complexation with cyclodextrins: In vitro and in vivo studies." Carbohydrate Polymers 102, no. : 393-399.

Journal article
Published: 22 July 2013 in Chirality
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An easy-to-prepare chiral CE method for the enantiomeric separation of 13 new amphetamine-like designer drugs, using CDs as chiral selectors, was developed. Sulfated-β-CD was found to be the best chiral selector among the three used (sulfated-β-CD, caroboxymethyl-β-CD, dimethyl-β-CD). The separation of the analytes was achieved in a fused-silica gel capillary at 20 °C using an applied voltage of +25 kV. The optimized background electrolyte consisted of 63.5 mM H3 PO4 and 46.9 mM NaOH in water. Several electrophoretic parameters such as CD type, CD concentration (1 - 40 mg/mL), buffer pH (2.6, 3.6, 5.0, 6.0), length of the capillary (70 - 40 cm total length), amount of the organic solvent (methanol and acetonitrile) were investigated and optimized.

ACS Style

Lucia Burrai; Maria Nieddu; Maria Antonietta Pirisi; Antonio Carta; Irene Briguglio; Gianpiero Boatto. Enantiomeric Separation of 13 New Amphetamine-Like Designer Drugs by Capillary Electrophoresis, Using Modified--Cyclodextrins. Chirality 2013, 25, 617 -621.

AMA Style

Lucia Burrai, Maria Nieddu, Maria Antonietta Pirisi, Antonio Carta, Irene Briguglio, Gianpiero Boatto. Enantiomeric Separation of 13 New Amphetamine-Like Designer Drugs by Capillary Electrophoresis, Using Modified--Cyclodextrins. Chirality. 2013; 25 (10):617-621.

Chicago/Turabian Style

Lucia Burrai; Maria Nieddu; Maria Antonietta Pirisi; Antonio Carta; Irene Briguglio; Gianpiero Boatto. 2013. "Enantiomeric Separation of 13 New Amphetamine-Like Designer Drugs by Capillary Electrophoresis, Using Modified--Cyclodextrins." Chirality 25, no. 10: 617-621.

Evaluation study
Published: 01 January 2013 in Carbohydrate Polymers
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Two water in oil emulsions composed by eudermic ingredients as glycerin, cocoa butter, almond oil and a variety of lipids, were enriched respectively with milk thistle dry extract (MT) or with a binary complex composed by MT and hydroxypropyl-β-cyclodextrin (HP) (1:4 w/w) correspondent to 1% (w/w) in sylimarine in order to obtain two different emulsions designed for the skin delivery and determine influence of hydroxypropyl-β-cyclodextrin on the extract delivery and permeation. Uv-vis spectrophotometric analyses demonstrated that phytocomplex formation influences the finding of MT after the complexation process and the in vitro antioxidant activity. Further in vitro and ex vivo experiments demonstrated that the penetration capability of MT from formulations is strictly influenced by the phytocomplex able to control MT permeation; moreover phytocomplex increases flavonoids stability during the in vitro tests. Additionally, in vivo studies showed that the penetration into the stratum corneum of the active ingredients is effectively achieved by the phytocomplex formation, in fact about 80% of MT is absorbed by the skin along 1h despite the 30% of MT not complexed absorbed during the same period.

ACS Style

Gianpiera Spada; Elisabetta Gavini; Massimo Cossu; Giovanna Rassu; Antonio Carta; Paolo Giunchedi. Evaluation of the effect of hydroxypropyl-β-cyclodextrin on topical administration of milk thistle extract. Carbohydrate Polymers 2013, 92, 40 -47.

AMA Style

Gianpiera Spada, Elisabetta Gavini, Massimo Cossu, Giovanna Rassu, Antonio Carta, Paolo Giunchedi. Evaluation of the effect of hydroxypropyl-β-cyclodextrin on topical administration of milk thistle extract. Carbohydrate Polymers. 2013; 92 (1):40-47.

Chicago/Turabian Style

Gianpiera Spada; Elisabetta Gavini; Massimo Cossu; Giovanna Rassu; Antonio Carta; Paolo Giunchedi. 2013. "Evaluation of the effect of hydroxypropyl-β-cyclodextrin on topical administration of milk thistle extract." Carbohydrate Polymers 92, no. 1: 40-47.

Journal article
Published: 01 November 2012 in Anti-Infective Agents
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ACS Style

Irene Briguglio; Sandra Piras; Paola Corona; Maria Pirisi; Daniela Jabes; Antonio Carta. SAR and Anti-Mycobacterial Activity of Quinolones and Triazoloquinolones: An Update. Anti-Infective Agents 2012, 11, 75 -89.

AMA Style

Irene Briguglio, Sandra Piras, Paola Corona, Maria Pirisi, Daniela Jabes, Antonio Carta. SAR and Anti-Mycobacterial Activity of Quinolones and Triazoloquinolones: An Update. Anti-Infective Agents. 2012; 11 (1):75-89.

Chicago/Turabian Style

Irene Briguglio; Sandra Piras; Paola Corona; Maria Pirisi; Daniela Jabes; Antonio Carta. 2012. "SAR and Anti-Mycobacterial Activity of Quinolones and Triazoloquinolones: An Update." Anti-Infective Agents 11, no. 1: 75-89.