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Plant products provide an alternative and successful source of lead compounds for the pharmaceutical industry. The present study was aimed to evaluate, in cell-based assays, the antiviral properties of essential oils obtained from plants that commonly grow in Sardinia, Italy, against a broad spectrum of RNA/DNA viruses. The essential oils of Helichrisumitalicum (Roth) G. Don ssp. microphyllum (Willd.) Nyman, Laurus nobilis L., Mirtuscommunis L., Pistacia lentiscus L., Salvia officinalis L., Saturejathymbra L., Lavandula angustifolia Mill., Foeniculum vulgare Mill., and Eucalyptus globulus Labill. were extracted by hydrodistillation and analyzed by gas chromatography mass spectrometry (GC–MS). Interestingly, the essential oil of Salvia officinalis showed moderate activity against bovine viral diarrhea virus (BVDV), an enveloped RNA virus belonging to the Flaviviridae family. BVDV is responsible for several clinical manifestations in bovines, including respiratory, gastroenteric, and reproductive diseases, with a significant economic impact. With the aim to individuate the constituent of the Salvia officinalis responsible for the biological activity, we tested the major components of the oil: camphene, β-pinene, limonene, 1,8-cineole, cis-thujone, camphor, (E)-caryophyllene, and α-humulene. Here, we describe α-humulene as an active component that is non-cytotoxic and active against BVDV (EC50 = 36 µM). Its antiviral effects were evaluated using virucidal cytopathic effect inhibition and viral yield reduction assays. This is the first scientific report showing the anti BVDV effects of Salvia officinalis essential oil and α-humulene as the main active component.
Silvia Madeddu; Alessandra Marongiu; Giuseppina Sanna; Carla Zannella; Danilo Falconieri; Silvia Porcedda; Aldo Manzin; Alessandra Piras. Bovine Viral Diarrhea Virus (BVDV): A Preliminary Study on Antiviral Properties of Some Aromatic and Medicinal Plants. Pathogens 2021, 10, 403 .
AMA StyleSilvia Madeddu, Alessandra Marongiu, Giuseppina Sanna, Carla Zannella, Danilo Falconieri, Silvia Porcedda, Aldo Manzin, Alessandra Piras. Bovine Viral Diarrhea Virus (BVDV): A Preliminary Study on Antiviral Properties of Some Aromatic and Medicinal Plants. Pathogens. 2021; 10 (4):403.
Chicago/Turabian StyleSilvia Madeddu; Alessandra Marongiu; Giuseppina Sanna; Carla Zannella; Danilo Falconieri; Silvia Porcedda; Aldo Manzin; Alessandra Piras. 2021. "Bovine Viral Diarrhea Virus (BVDV): A Preliminary Study on Antiviral Properties of Some Aromatic and Medicinal Plants." Pathogens 10, no. 4: 403.
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.
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 StyleRoberta 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 StyleRoberta 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.
Background: Coxsackievirus infections are associated with cases of aseptic meningitis, encephalitis, myocarditis, and some chronic disease. Methods: A series of benzo[d][1,2,3]triazol-1(2)-yl derivatives (here named benzotriazol-1(2)-yl) (4a-i, 5a-h, 6a-e, g, i, j and 7a-f, h-j) were designed, synthesized and in vitro evaluated for cytotoxicity and antiviral activity against two important human enteroviruses (HEVs) members of the Picornaviridae family [Coxsackievirus B 5 (CVB-5) and Poliovirus 1 (Sb-1)]. Results: Compounds 4c (CC50 >100 μM; EC50 = 9 μM), 5g (CC50 >100 μM; EC50 = 8 μM), and 6a (CC50 >100 μM; EC50 = 10 μM) were found active against CVB-5. With the aim of evaluating the selectivity of action of this class of compounds, a wide spectrum of RNA (positive- and negativesense), double-stranded (dsRNA) or DNA viruses were also assayed. For none of them, significant antiviral activity was determined. Conclusion: These results point towards a selective activity against CVB-5, an important human pathogen that causes both acute and chronic diseases in infants, young children, and immunocompromised patients.
Sandra Piras; Paola Corona; Roberta Ibba; Federico Riu; Gabriele Murineddu; Giuseppina Sanna; Silvia Madeddu; Ilenia Delogu; Roberta Loddo; Antonio Carta. Preliminary Anti-Coxsackie Activity of Novel 1-[4-(5,6-dimethyl(H)- 1H(2H)-benzotriazol-1(2)-yl)phenyl]-3-alkyl(aryl)ureas. Medicinal Chemistry 2020, 16, 677 -688.
AMA StyleSandra Piras, Paola Corona, Roberta Ibba, Federico Riu, Gabriele Murineddu, Giuseppina Sanna, Silvia Madeddu, Ilenia Delogu, Roberta Loddo, Antonio Carta. Preliminary Anti-Coxsackie Activity of Novel 1-[4-(5,6-dimethyl(H)- 1H(2H)-benzotriazol-1(2)-yl)phenyl]-3-alkyl(aryl)ureas. Medicinal Chemistry. 2020; 16 (5):677-688.
Chicago/Turabian StyleSandra Piras; Paola Corona; Roberta Ibba; Federico Riu; Gabriele Murineddu; Giuseppina Sanna; Silvia Madeddu; Ilenia Delogu; Roberta Loddo; Antonio Carta. 2020. "Preliminary Anti-Coxsackie Activity of Novel 1-[4-(5,6-dimethyl(H)- 1H(2H)-benzotriazol-1(2)-yl)phenyl]-3-alkyl(aryl)ureas." Medicinal Chemistry 16, no. 5: 677-688.
Historically, natural products have been the most successful source of inspiration for the development of new drugs. Members of the Thymelaeaceae family have been of interest owing to their excellent medicinal value. Given the successful history of natural product-based drug discovery, extracts from the aerial parts of Thymelaea hirsuta were evaluated for their potential anti-human immunodeficiency virus type 1 (HIV-1) activity. Ethyl acetate extracts from leaves (71B) and branches (72B) of Thymelaea hirsuta showed potent and selective activity against HIV-1 wt (EC50 = 0.8 µg/mL) at non-cytotoxic concentrations (CC50 > 100 µg/mL). They proved to be active against HIV-1 variants carrying clinically relevant NNRTI and NRTI mutations at low concentration (0.3–4 µg/mL range) and against the M-tropic strain HIV-1 BaL. The 72B extract, chosen as a lead, was not able to inhibit the RT and protease enzymatic functions. Furthermore, it was not virucidal, since exposure of HIV to high concentration did not affect virus infectivity. The pre-clinical safety profile of this extract showed no adverse effect on the growth of Lactobacilli, and non-toxic concentration of the extract did not influence the Caco-2 epithelial cells monolayer integrity. Additionally, extract 72B prevented syncytia formation at low concentration (0.4 µg/mL). The potent inhibitory effect on the syncytia formation in co-cultures showed that 72B inhibits an early event in the replication cycle of HIV. All of these findings prompt us to carry on new studies on Thymelaea hirsuta extracts.
Giuseppina Sanna; Silvia Madeddu; Giuseppe Murgia; Gabriele Serreli; Michela Begala; Pierluigi Caboni; Alessandra Incani; Gianluigi Franci; Marilena Galdiero; Gabriele Giliberti. Potent and Selective Activity against Human Immunodeficiency Virus 1 (HIV-1) of Thymelaea hirsuta Extracts. Viruses 2020, 12, 664 .
AMA StyleGiuseppina Sanna, Silvia Madeddu, Giuseppe Murgia, Gabriele Serreli, Michela Begala, Pierluigi Caboni, Alessandra Incani, Gianluigi Franci, Marilena Galdiero, Gabriele Giliberti. Potent and Selective Activity against Human Immunodeficiency Virus 1 (HIV-1) of Thymelaea hirsuta Extracts. Viruses. 2020; 12 (6):664.
Chicago/Turabian StyleGiuseppina Sanna; Silvia Madeddu; Giuseppe Murgia; Gabriele Serreli; Michela Begala; Pierluigi Caboni; Alessandra Incani; Gianluigi Franci; Marilena Galdiero; Gabriele Giliberti. 2020. "Potent and Selective Activity against Human Immunodeficiency Virus 1 (HIV-1) of Thymelaea hirsuta Extracts." Viruses 12, no. 6: 664.
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.
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 StyleMatthew 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 StyleMatthew 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.
The present study aimed to determine the antimicrobial activity and chemical composition of leaves-extracted essential oil of Leoheo domatiophorus Chaowasku, D.T. Ngo and H.T. Le (L. domatiophorus), including antibacterial, antimycotic, antitrichomonas and antiviral effects. The essential oil was obtained using hydrodistillation, with an average yield of 0.34 ± 0.01% (v/w, dry leaves). There were 52 constituents as identified by GC/MS with available authentic standards, representing 96.74% of the entire leaves oil. The essential oil was comprised of three main components, namely viridiflorene (16.47%), (-)-δ-cadinene (15.58%) and γ-muurolene (8.00%). The oil showed good antimicrobial activities against several species: Gram-positive strains: Staphylococcus aureus (two strains) and Enterococcus faecalis, with Minimum Inhibitory Concentration (MIC) and Minimum Lethal Concentration (MLC) values from 0.25 to 1% (v/v); Gram-negative strains such as Escherichia coli (two strains), Pseudomonas aeruginosa (two strains) and Klebsiella pneumoniae, with MIC and MLC values between 2% and 8% (v/v); and finally Candida species, having MIC and MLC between 0.12 and 4% (v/v).Antitrichomonas activity of the oil was also undertaken, showing IC50, IC90 and MLC values of 0.008%, 0.016% and 0.03% (v/v), respectively, after 48h of incubation. The essential oil resultedin being completely ineffective against tested viruses, ssRNA+ (HIV-1, YFV, BVDV, Sb-1, CV-B4), ssRNA- (hRSVA2, VSV), dsRNA (Reo-1), and dsDNA (HSV-1, VV) viruses with EC50 values over 100 µg/mL. This is the first, yet comprehensive, scientific report about the chemical composition and pharmacological properties of the essential oil in L. domatiophorus.
Nhan Trong Le; Duc Viet Ho; Tuan Quoc Doan; Anh Tuan Le; Ain Raal; Donatella Usai; Silvia Madeddu; Mauro Marchetti; Marianna Usai; Paola Rappelli; Nicia Diaz; Stefania Zanetti; Hoai Thi Nguyen; Piero Cappuccinelli; Matthew Gavino Donadu. In Vitro Antimicrobial Activity of Essential Oil Extracted from Leaves of Leoheo domatiophorus Chaowasku, D.T. Ngo and H.T. Le in Vietnam. Plants 2020, 9, 453 .
AMA StyleNhan Trong Le, Duc Viet Ho, Tuan Quoc Doan, Anh Tuan Le, Ain Raal, Donatella Usai, Silvia Madeddu, Mauro Marchetti, Marianna Usai, Paola Rappelli, Nicia Diaz, Stefania Zanetti, Hoai Thi Nguyen, Piero Cappuccinelli, Matthew Gavino Donadu. In Vitro Antimicrobial Activity of Essential Oil Extracted from Leaves of Leoheo domatiophorus Chaowasku, D.T. Ngo and H.T. Le in Vietnam. Plants. 2020; 9 (4):453.
Chicago/Turabian StyleNhan Trong Le; Duc Viet Ho; Tuan Quoc Doan; Anh Tuan Le; Ain Raal; Donatella Usai; Silvia Madeddu; Mauro Marchetti; Marianna Usai; Paola Rappelli; Nicia Diaz; Stefania Zanetti; Hoai Thi Nguyen; Piero Cappuccinelli; Matthew Gavino Donadu. 2020. "In Vitro Antimicrobial Activity of Essential Oil Extracted from Leaves of Leoheo domatiophorus Chaowasku, D.T. Ngo and H.T. Le in Vietnam." Plants 9, no. 4: 453.
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.
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 StyleGiuseppina 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 StyleGiuseppina 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.
A series of 2-(1H-indol-3-yl)ethylthiourea derivatives were prepared by condensation of 2-(1H-indol-3-yl)ethanamine with appropriate aryl/alkylisothiocyanates in anhydrous media. The structures of the newly synthesized compounds were confirmed by spectroscopic analysis and the molecular structures of 8 and 28 were confirmed by X-ray crystallography. All obtained compounds were tested for antimicrobial activity against Gram-positive cocci, Gram-negative rods and for antifungal activity. Microbiological evaluation was carried out over 20 standard strains and 30 hospital strains. Compound 6 showed significant inhibition against Gram-positive cocci and had inhibitory effect on the S. aureus topoisomerase IV decatenation activity and S. aureus DNA gyrase supercoiling activity. Compounds were tested for cytotoxicity and antiviral activity against a large panel of DNA and RNA viruses, including HIV-1 and other several important human pathogens. Interestingly, derivative 8 showed potent activity against HIV-1 wild type and variants bearing clinically relevant mutations. Newly synthesized tryptamine derivatives showed also a wide spectrum activity, proving to be active against positive- and negative-sense RNA viruses.
Giuseppina Sanna; Silvia Madeddu; Gabriele Giliberti; Sandra Piras; Marta Struga; Małgorzata Wrzosek; Grażyna Kubiak-Tomaszewska; Anna E. Koziol; Oleksandra Savchenko; Tadeusz Lis; Joanna Stefanska; Piotr Tomaszewski; Michał Skrzycki; Daniel Szulczyk. Synthesis and Biological Evaluation of Novel Indole-Derived Thioureas. Molecules 2018, 23, 2554 .
AMA StyleGiuseppina Sanna, Silvia Madeddu, Gabriele Giliberti, Sandra Piras, Marta Struga, Małgorzata Wrzosek, Grażyna Kubiak-Tomaszewska, Anna E. Koziol, Oleksandra Savchenko, Tadeusz Lis, Joanna Stefanska, Piotr Tomaszewski, Michał Skrzycki, Daniel Szulczyk. Synthesis and Biological Evaluation of Novel Indole-Derived Thioureas. Molecules. 2018; 23 (10):2554.
Chicago/Turabian StyleGiuseppina Sanna; Silvia Madeddu; Gabriele Giliberti; Sandra Piras; Marta Struga; Małgorzata Wrzosek; Grażyna Kubiak-Tomaszewska; Anna E. Koziol; Oleksandra Savchenko; Tadeusz Lis; Joanna Stefanska; Piotr Tomaszewski; Michał Skrzycki; Daniel Szulczyk. 2018. "Synthesis and Biological Evaluation of Novel Indole-Derived Thioureas." Molecules 23, no. 10: 2554.
Giuseppina Sanna; Silvia Madeddu; Gabriele Giliberti; Sandra Piras; Marta Struga; Małgorzata Wrzosek; Grażyna Kubiak-Tomaszewska; Anna E. Koziol; Oleksandra Savchenko; Tadeusz Lis; Joanna Stefanska; Piotr Tomaszewski; Michał Skrzycki; Daniel Szulczyk. Synthesis and Biological Evaluation of Novel Indole-Derived Thioureas. Molecules 2018, 23, 1 .
AMA StyleGiuseppina Sanna, Silvia Madeddu, Gabriele Giliberti, Sandra Piras, Marta Struga, Małgorzata Wrzosek, Grażyna Kubiak-Tomaszewska, Anna E. Koziol, Oleksandra Savchenko, Tadeusz Lis, Joanna Stefanska, Piotr Tomaszewski, Michał Skrzycki, Daniel Szulczyk. Synthesis and Biological Evaluation of Novel Indole-Derived Thioureas. Molecules. 2018; 23 (10):1.
Chicago/Turabian StyleGiuseppina Sanna; Silvia Madeddu; Gabriele Giliberti; Sandra Piras; Marta Struga; Małgorzata Wrzosek; Grażyna Kubiak-Tomaszewska; Anna E. Koziol; Oleksandra Savchenko; Tadeusz Lis; Joanna Stefanska; Piotr Tomaszewski; Michał Skrzycki; Daniel Szulczyk. 2018. "Synthesis and Biological Evaluation of Novel Indole-Derived Thioureas." Molecules 23, no. 10: 1.
4-Chloro-3-nitrophenylthioureas 1–30 were synthesized and tested for their antimicrobial and cytotoxic activities. Compounds exhibited high to moderate antistaphylococcal activity against both standard and clinical strains (MIC values 2–64 μg/mL). Among them derivatives with electron-donating alkyl substituents at the phenyl ring were the most promising. Moreover, compounds 1–6 and 8–19 were cytotoxic against MT-4 cells and various other cell lines derived from human hematological tumors (CC50 ≤ 10 μM). The influence of derivatives 11, 13 and 25 on viability, mortality and the growth rate of immortalized human keratinocytes (HaCaT) was observed.
Anna Bielenica; Giuseppina Sanna; Silvia Madeddu; Gabriele Giliberti; Joanna Stefańska; Anna E. Kozioł; Oleksandra Savchenko; Paulina Strzyga-Łach; Alicja Chrzanowska; Grażyna Kubiak-Tomaszewska; Marta Struga. Disubstituted 4-Chloro-3-nitrophenylthiourea Derivatives: Antimicrobial and Cytotoxic Studies. Molecules 2018, 23, 2428 .
AMA StyleAnna Bielenica, Giuseppina Sanna, Silvia Madeddu, Gabriele Giliberti, Joanna Stefańska, Anna E. Kozioł, Oleksandra Savchenko, Paulina Strzyga-Łach, Alicja Chrzanowska, Grażyna Kubiak-Tomaszewska, Marta Struga. Disubstituted 4-Chloro-3-nitrophenylthiourea Derivatives: Antimicrobial and Cytotoxic Studies. Molecules. 2018; 23 (10):2428.
Chicago/Turabian StyleAnna Bielenica; Giuseppina Sanna; Silvia Madeddu; Gabriele Giliberti; Joanna Stefańska; Anna E. Kozioł; Oleksandra Savchenko; Paulina Strzyga-Łach; Alicja Chrzanowska; Grażyna Kubiak-Tomaszewska; Marta Struga. 2018. "Disubstituted 4-Chloro-3-nitrophenylthiourea Derivatives: Antimicrobial and Cytotoxic Studies." Molecules 23, no. 10: 2428.
On the basis of recently reported biologically active 3-(trifluoromethyl)phenylthioureas, a series of diaryl derivatives incorporating 1H-tetrazol-5-yl (1a-11a, 1a'-11a') and 1,3-thiazolidin-4-one (1b-11b) scaffolds were synthesized. The synthesis pathway was confirmed by an X-ray crystallographic studies of 3a', 6a, 8a, 6b and 8b. The cytotoxicity against MT-4 cells and anti-HIV properties of new derivatives were evaluated. As compared to initial thiourea connections, the cyclisation reduced the cytotoxicity of compounds by 2-15 times. The most promising N-(4-nitrophenyl)-1H-tetrazol-5-amine 7a was found to be more active than the origin thiourea. Its cytotoxicity was evaluated on A549, HTB-140 and HaCaT cell lines using MTT assay. The compound shows significant influence on cancer, but not on normal cells. Obtained results can provide some constructive data for further designing of novel family of potentially bioactive analogs.
Anna Bielenica; Daniel Szulczyk; Wioletta Olejarz; Silvia Madeddu; Gabriele Giliberti; Ilona B. Materek; Anna E. Koziol; Marta Struga. 1 H -Tetrazol-5-amine and 1,3-thiazolidin-4-one derivatives containing 3-(trifluoromethyl)phenyl scaffold: Synthesis, cytotoxic and anti-HIV studies. Biomedicine & Pharmacotherapy 2017, 94, 804 -812.
AMA StyleAnna Bielenica, Daniel Szulczyk, Wioletta Olejarz, Silvia Madeddu, Gabriele Giliberti, Ilona B. Materek, Anna E. Koziol, Marta Struga. 1 H -Tetrazol-5-amine and 1,3-thiazolidin-4-one derivatives containing 3-(trifluoromethyl)phenyl scaffold: Synthesis, cytotoxic and anti-HIV studies. Biomedicine & Pharmacotherapy. 2017; 94 ():804-812.
Chicago/Turabian StyleAnna Bielenica; Daniel Szulczyk; Wioletta Olejarz; Silvia Madeddu; Gabriele Giliberti; Ilona B. Materek; Anna E. Koziol; Marta Struga. 2017. "1 H -Tetrazol-5-amine and 1,3-thiazolidin-4-one derivatives containing 3-(trifluoromethyl)phenyl scaffold: Synthesis, cytotoxic and anti-HIV studies." Biomedicine & Pharmacotherapy 94, no. : 804-812.
Thiourea derivatives have been reported to possess many biological activities, among them antiviral and antitumoral properties. As part of our continuing effort to develop new active compounds, we report the synthesis and the evaluation of new fifteen thiourea derivatives with 1,3-benzothiazol-2-yl moiety, among them a group of biologically active (1-7) also underwent cyclisation to 1,3-thiazolidin-4-ones. Molecular structure of four compounds (4, 13, 15 and 3a) was determined by an X-ray crystallography. We here report the evaluation of their cytotoxicity against human leukaemia/lymphoma- and solid tumour-derived cell lines and of their antiviral activity against HIV-1 and representatives of ssRNA and dsDNA viruses. Derivative 5 showed an interesting activity against HIV-1 wild type and against variants carrying clinically relevant mutations. A colorimetric enzyme immunoassay clarified its mode of action as a non-nucleoside inhibitor of the reverse transcriptase.This article is protected by copyright. All rights reserved.
Anna Bielenica; Giuseppina Sanna; Silvia Madeddu; Marta Struga; Michał Jóźwiak; Anna E. Kozioł; Aleksandra Sawczenko; Ilona B. Materek; Alessandra Serra; Gabriele Giliberti. New thiourea and 1,3-thiazolidin-4-one derivatives effective on the HIV-1 virus. Chemical Biology & Drug Design 2017, 90, 883 -891.
AMA StyleAnna Bielenica, Giuseppina Sanna, Silvia Madeddu, Marta Struga, Michał Jóźwiak, Anna E. Kozioł, Aleksandra Sawczenko, Ilona B. Materek, Alessandra Serra, Gabriele Giliberti. New thiourea and 1,3-thiazolidin-4-one derivatives effective on the HIV-1 virus. Chemical Biology & Drug Design. 2017; 90 (5):883-891.
Chicago/Turabian StyleAnna Bielenica; Giuseppina Sanna; Silvia Madeddu; Marta Struga; Michał Jóźwiak; Anna E. Kozioł; Aleksandra Sawczenko; Ilona B. Materek; Alessandra Serra; Gabriele Giliberti. 2017. "New thiourea and 1,3-thiazolidin-4-one derivatives effective on the HIV-1 virus." Chemical Biology & Drug Design 90, no. 5: 883-891.
Anna Bielenica; Karolina Stępień; Aleksandra Sawczenko; Tadeusz Lis; Anna E. Koziol; Silvia Madeddu; David Collu; Filippo Iuliano; Anita Kośmider; Marta Struga. Synthesis, Structural Studies and Biological Evaluation of Halogen Derivatives of 1,3-Disubstituted Thiourea. Letters in Drug Design & Discovery 2017, 14, 636 -646.
AMA StyleAnna Bielenica, Karolina Stępień, Aleksandra Sawczenko, Tadeusz Lis, Anna E. Koziol, Silvia Madeddu, David Collu, Filippo Iuliano, Anita Kośmider, Marta Struga. Synthesis, Structural Studies and Biological Evaluation of Halogen Derivatives of 1,3-Disubstituted Thiourea. Letters in Drug Design & Discovery. 2017; 14 (6):636-646.
Chicago/Turabian StyleAnna Bielenica; Karolina Stępień; Aleksandra Sawczenko; Tadeusz Lis; Anna E. Koziol; Silvia Madeddu; David Collu; Filippo Iuliano; Anita Kośmider; Marta Struga. 2017. "Synthesis, Structural Studies and Biological Evaluation of Halogen Derivatives of 1,3-Disubstituted Thiourea." Letters in Drug Design & Discovery 14, no. 6: 636-646.
Nucleoside analogues play an important role in antiviral, antibacterial and antineoplastic chemotherapy. Herein we report the synthesis, structural characterization and biological activity of some 4′-C -methyl- and -phenyl dioxolane-based nucleosides. In particular, α and β anomers of all natural nucleosides were obtained and characterized by NMR, HR-MS and X-ray crystallography. The compounds were tested for antimicrobial activity against some representative human pathogenic fungi, bacteria and viruses. Antitumor activity was evaluated in a large variety of human cancer cell-lines. Although most of the compounds showed non-significant activity, 23α weakly inhibited HIV-1 multiplication. Moreover, 22α and 32α demonstrated a residual antineoplastic activity, interestingly linked to the unnatural α configuration. These results may provide structural insights for the design of active antiviral and antitumor agents.
Silvia Franchini; Umberto M. Battisti; Claudia Sorbi; Annalisa Tait; Andrea Cornia; Lak Shin Jeong; Sang Kook Lee; Jayoung Song; Roberta Loddo; Silvia Madeddu; Giuseppina Sanna; Livio Brasili. Synthesis, structural characterization and biological evaluation of 4′-C-methyl- and phenyl-dioxolane pyrimidine and purine nucleosides. Archives of Pharmacal Research 2016, 40, 537 -549.
AMA StyleSilvia Franchini, Umberto M. Battisti, Claudia Sorbi, Annalisa Tait, Andrea Cornia, Lak Shin Jeong, Sang Kook Lee, Jayoung Song, Roberta Loddo, Silvia Madeddu, Giuseppina Sanna, Livio Brasili. Synthesis, structural characterization and biological evaluation of 4′-C-methyl- and phenyl-dioxolane pyrimidine and purine nucleosides. Archives of Pharmacal Research. 2016; 40 (5):537-549.
Chicago/Turabian StyleSilvia Franchini; Umberto M. Battisti; Claudia Sorbi; Annalisa Tait; Andrea Cornia; Lak Shin Jeong; Sang Kook Lee; Jayoung Song; Roberta Loddo; Silvia Madeddu; Giuseppina Sanna; Livio Brasili. 2016. "Synthesis, structural characterization and biological evaluation of 4′-C-methyl- and phenyl-dioxolane pyrimidine and purine nucleosides." Archives of Pharmacal Research 40, no. 5: 537-549.
Anna Bielenica; Ewa Kedzierska; Sylwia Fidecka; Hanna Maluszyńska; Barbara Miroslaw; Anna E. Koziol; Joanna Stefanska; Silvia Madeddu; Gabriele Giliberti; Giuseppina Sanna; Marta Struga. Synthesis, Antimicrobial and Pharmacological Evaluation of Thioureaderivatives of 4H-1,2,4-triazole. Letters in Drug Design & Discovery 2015, 12, 263 -276.
AMA StyleAnna Bielenica, Ewa Kedzierska, Sylwia Fidecka, Hanna Maluszyńska, Barbara Miroslaw, Anna E. Koziol, Joanna Stefanska, Silvia Madeddu, Gabriele Giliberti, Giuseppina Sanna, Marta Struga. Synthesis, Antimicrobial and Pharmacological Evaluation of Thioureaderivatives of 4H-1,2,4-triazole. Letters in Drug Design & Discovery. 2015; 12 (4):263-276.
Chicago/Turabian StyleAnna Bielenica; Ewa Kedzierska; Sylwia Fidecka; Hanna Maluszyńska; Barbara Miroslaw; Anna E. Koziol; Joanna Stefanska; Silvia Madeddu; Gabriele Giliberti; Giuseppina Sanna; Marta Struga. 2015. "Synthesis, Antimicrobial and Pharmacological Evaluation of Thioureaderivatives of 4H-1,2,4-triazole." Letters in Drug Design & Discovery 12, no. 4: 263-276.