Quinoxaline derivatives as new inhibitors of coxsackievirus B5

Carta, Antonio; Sanna, Giuseppina; Briguglio, Irene; Madeddu, Silvia; Vitale, Gabriella; Piras, Sandra; Corona, Paola; Peana, Alessandra Tiziana; Laurini, Erik; Fermeglia, Maurizio; Pricl, Sabrina; Serra, A.; Carta, Elisa; Loddo, Roberta; Giliberti, Gabriele

doi:10.1016/j.ejmech.2017.12.083

Cited by 37 publications

(30 citation statements)

References 47 publications

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“…BHK cells were seeded in 96-well plates at an initial density of 6×10 5 [13]. Compound's activity against CV-B4, Sb-1, VV, VSV, hRSV A2 and HSV-1 was determined by plaque reduction assays in infected cell monolayers as described previously [14]. Briefly, monolayer of Vero-76 cells was grown overnight on 24-well plate.…”

Section: Cytotoxicity Assaysmentioning

confidence: 99%

Biological activities of essential oil extracted from leaves of Atalantia sessiflora Guillauminin Vietnam

Donadu

et al. 2020

J Infect Dev Ctries

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Introduction: The present study aimed to determine the chemical compositions and bioactivities of the essential oil of Atalantia sessiflora Guillaumin (A. sessiflora), including antibacterial, antimycotic, antitrichomonas, anti-inflammatory and antiviral effects. Methodology: The essential oil from leaves of A. sessiflora was extracted by hydrodistillation using a Clevenger apparatus. Chemical compositions of oil were identified by GC/MS. Antimicrobial and antitrichomonas activity were determined by the microdilution method; anti-inflammatory and antiviral were determined by the MTT method. Results: The average yield of oil was 0.46 ± 0.01% (v/w, dry leaves). A number of 45 constituents were identified by GC/MS. The essential oil comprised four main components. The oil showed antimicrobial activities against Gram-positive strains as Staphylococcus; Gram-negative bacteria such as Klebsiella pneumoniae and Escherichia coli; and finally four Candida species. Enterococcus faecalis and Pseudomonas aeruginosa were least susceptible to the oil of A. sessiflora, as seen in their MIC and MLC values over 16% (v/v). Activity against Trichomonas vaginalis was also undertaken, showing IC50, IC90 and MLC values of 0.016, 0.03 and 0.06% (v/v) respectively, after 48 hours of incubation. The oil of A. sessiflora displayed activity against the nitric oxide generation with the IC50 of 95.94 ± 6.18 µg/mL. The oil was completely ineffective against tested viruses, ssRNA+, ssRNA-, dsRNA, and dsDNA viruses. Conclusions: This is the first yet comprehensive scientific report about the chemical compositions and pharmacological properties of the essential oil of A. sessiflora. Further studies should be done to evaluate the safety and toxicity of A. sessiflora oil.

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Section: Cytotoxicity Assaysmentioning

confidence: 99%

Biological activities of essential oil extracted from leaves of Atalantia sessiflora Guillauminin Vietnam

Donadu

et al. 2020

J Infect Dev Ctries

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“…After a 3 or 4-days incubation at 37 °C, cell viability was determined by the MTT method, as described earlier [ 47 ]. Compound’s activity against CV-B5, Sb-1, VSV, VV, HSV-1 and RSV was determined by plaque reduction assays in infected Vero-76 cell monolayers, as described earlier [ 48 , 49 ]. Concentrations resulting in 50% inhibition (CC 50 or EC 50 ) were determined by linear regression analysis.…”

Section: Methodsmentioning

confidence: 99%

Synthesis and Biological Evaluation of Novel Indole-Derived Thioureas

et al. 2018

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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.

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“…Activities of essential oils and compounds against CV-B4, Sb-1, VV, VSV, hRSV A2, and HSV-1 was determined by plaque reduction assays in infected cell monolayers as described previously [47]. Briefly, Vero-76 cells were cultured in 24-well tissue culture plate and with approximately 50/100 PFU/well of virus.…”

Section: Viruses and Antiviral Assaysmentioning

confidence: 99%

Biological Activities of Essential Oils from Leaves of Paramignya trimera (Oliv.) Guillaum and Limnocitrus littoralis (Miq.) Swingle

Doan

et al. 2020

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.

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Quinoxaline derivatives as new inhibitors of coxsackievirus B5

Cited by 37 publications

References 47 publications

Biological activities of essential oil extracted from leaves of Atalantia sessiflora Guillauminin Vietnam

Biological activities of essential oil extracted from leaves of Atalantia sessiflora Guillauminin Vietnam

Synthesis and Biological Evaluation of Novel Indole-Derived Thioureas

Biological Activities of Essential Oils from Leaves of Paramignya trimera (Oliv.) Guillaum and Limnocitrus littoralis (Miq.) Swingle

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