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  1. Article ; Online: Antibacterial and Antibiofilm Activity of Myrtenol against Staphylococcus aureus

    Laísa Cordeiro / Pedro Figueiredo / Helivaldo Souza / Aleson Sousa / Francisco Andrade-Júnior / José Barbosa-Filho / Edeltrudes Lima

    Pharmaceuticals, Vol 13, Iss 133, p

    2020  Volume 133

    Abstract: The increase in Staphylococcus aureus resistance to conventional antibacterials and persistent infections related to biofilms, as well as the low availability of new antibacterial drugs, has made the development of new therapeutic alternatives necessary. ...

    Abstract The increase in Staphylococcus aureus resistance to conventional antibacterials and persistent infections related to biofilms, as well as the low availability of new antibacterial drugs, has made the development of new therapeutic alternatives necessary. Medicinal plants are one of the main sources of bioactive molecules and myrtenol is a natural product with several biological activities, although its antimicrobial activity is little explored. Based on this, the objective of this study was to evaluate the antibacterial activity of myrtenol against S. aureus , determining the minimum inhibitory and bactericidal concentrations (MIC and MBC), investigating the possible molecular target through the analysis of molecular docking. It also aimed to evaluate the effect of its combination with antibacterial drugs and its activity against S. aureus biofilms, in addition to performing an in silico analysis of its pharmacokinetic parameters. Myrtenol showed MIC and MBC of 128 µg/mL (bactericidal action) and probably acts by interfering with the synthesis of the bacterial cell wall. The effects of the association with antibacterials demonstrate favorable results. Myrtenol has remarkable antibiofilm activity and in silico results indicate a good pharmacokinetic profile, which make myrtenol a potential drug candidate for the treatment of infections caused by S. aureus .
    Keywords myrtenol ; Staphylococcus aureus ; antibacterial ; molecular docking ; antibiofilm ; checkerboard method ; Medicine ; R ; Pharmacy and materia medica ; RS1-441
    Subject code 630
    Language English
    Publishing date 2020-06-01T00:00:00Z
    Publisher MDPI AG
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  2. Article ; Online: Isoeugenol and Hybrid Acetamides against Candida albicans Isolated from the Oral Cavity

    Daianne Medeiros / José Oliveira-Júnior / Jefferson Nóbrega / Laísa Cordeiro / Jeane Jardim / Helivaldo Souza / Gracielle Silva / Petrônio Athayde-Filho / José Barbosa-Filho / Luciana Scotti / Edeltrudes Lima

    Pharmaceuticals, Vol 13, Iss 291, p

    2020  Volume 291

    Abstract: Isougenol is a phytoconstituent found in several essential oils. Since many natural products are potent antimicrobials, the synthesis of hybrid molecules—combining the chemical skeleton of the phytochemical with synthetic groups—can generate substances ... ...

    Abstract Isougenol is a phytoconstituent found in several essential oils. Since many natural products are potent antimicrobials, the synthesis of hybrid molecules—combining the chemical skeleton of the phytochemical with synthetic groups—can generate substances with enhanced biological activity. Based on this, the objective of this study was to evaluate the antifungal activity of isoeugenol and hybrid acetamides against Candida albicans isolated from the oral cavity. The methodologies used were the determination of minimum inhibitory concentration (MIC), minimum fungicidal concentration (MFC), action on fungal micromorphology, interaction test with nystatin by the checkerboard method and molecular docking study with important enzymes in the maintenance of fungal viability. The synthetic molecules did not demonstrate significant antifungal activity in vitro. The isoeugenol MIC and MFC varied between 128 and 256 µg/mL, being the phytoconstituent able to interfere in the formation of blastoconid and chlamydoconid structures, important in the pathogenic process of the species. The molecular docking study revealed that isoeugenol is a potential inhibitor of the enzymes 14-α-demethylase and delta-14-sterol reductase, interfering in the fungal cell membrane biosynthesis. Thus, this research provides clearer expectations for future pharmacological studies with isoeugenol and derived molecules, aiming at its therapeutic application against infections caused by Candida spp.
    Keywords Candida albicans ; isoeugenol ; checkerboard method ; molecular docking ; antifungal activity ; oral candidiasis ; Medicine ; R ; Pharmacy and materia medica ; RS1-441
    Subject code 540
    Language English
    Publishing date 2020-10-01T00:00:00Z
    Publisher MDPI AG
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  3. Article ; Online: Terpinen-4-ol as an Antibacterial and Antibiofilm Agent against Staphylococcus aureus

    Laísa Cordeiro / Pedro Figueiredo / Helivaldo Souza / Aleson Sousa / Francisco Andrade-Júnior / Daianne Medeiros / Jefferson Nóbrega / Daniele Silva / Evandro Martins / José Barbosa-Filho / Edeltrudes Lima

    International Journal of Molecular Sciences, Vol 21, Iss 4531, p

    2020  Volume 4531

    Abstract: Staphylococcus aureus is able to rapidly develop mechanisms of resistance to various drugs and to form strong biofilms, which makes it necessary to develop new antibacterial drugs. The essential oil of Melaleuca alternifolia is used as an antibacterial, ... ...

    Abstract Staphylococcus aureus is able to rapidly develop mechanisms of resistance to various drugs and to form strong biofilms, which makes it necessary to develop new antibacterial drugs. The essential oil of Melaleuca alternifolia is used as an antibacterial, a property believed to be mainly due to the presence of terpinen-4-ol. Based on this, the objective of this study was to evaluate the antibacterial and antibiofilm potential of terpinen-4-ol against S. aureus . The Minimal Inhibitory and Minimal Bactericidal Concentrations (MIC and MBC) of terpinen-4-ol were determined, and the effect of its combination with antibacterial drugs as well as its activity against S. aureus biofilms were evaluated. In addition, an in silico analysis of its pharmacokinetic parameters and a molecular docking analysis were performed. Terpinen-4-ol presented a MIC of 0.25% ( v/v ) and an MBC of 0.5% ( v/v ) (bactericidal action); its association with antibacterials was also effective. Terpinen-4-ol has good antibiofilm activity, and the in silico results indicated adequate absorption and distribution of the molecule in vivo. Molecular docking indicated that penicillin-binding protein 2a is a possible target of terpinen-4-ol in S. aureus . This work highlights the good potential of terpinen-4-ol as an antibacterial product and provides support for future pharmacological studies of this molecule, aiming at its therapeutic application.
    Keywords terpinen-4-ol ; Staphylococcus aureus ; antibacterial ; antibiofilm ; molecular docking ; checkerboard method ; Biology (General) ; QH301-705.5 ; Chemistry ; QD1-999
    Language English
    Publishing date 2020-06-01T00:00:00Z
    Publisher MDPI AG
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  4. Article ; Online: Potential of 2-Chloro- N -(4-fluoro-3-nitrophenyl)acetamide Against Klebsiella pneumoniae and In Vitro Toxicity Analysis

    Laísa Cordeiro / Hermes Diniz-Neto / Pedro Figueiredo / Helivaldo Souza / Aleson Sousa / Francisco Andrade-Júnior / Thamara Melo / Elba Ferreira / Rafael Oliveira / Petrônio Athayde-Filho / José Barbosa-Filho / Abrahão Oliveira-Filho / Edeltrudes Lima

    Molecules, Vol 25, Iss 3959, p

    2020  Volume 3959

    Abstract: Klebsiella pneumoniae causes a wide range of community and nosocomial infections. The high capacity of this pathogen to acquire resistance drugs makes it necessary to develop therapeutic alternatives, discovering new antibacterial molecules. Acetamides ... ...

    Abstract Klebsiella pneumoniae causes a wide range of community and nosocomial infections. The high capacity of this pathogen to acquire resistance drugs makes it necessary to develop therapeutic alternatives, discovering new antibacterial molecules. Acetamides are molecules that have several biological activities. However, there are no reports on the activity of 2-chloro- N -(4-fluoro-3-nitrophenyl)acetamide. Based on this, this study aimed to investigate the in vitro antibacterial activity of this molecule on K. pneumoniae , evaluating whether the presence of the chloro atom improves this effect. Then, analyzing its antibacterial action more thoroughly, as well as its cytotoxic and pharmacokinetic profile, in order to contribute to future studies for the viability of a new antibacterial drug. It was shown that the substance has good potential against K. pneumoniae and the chloro atom is responsible for improving this activity, stabilizing the molecule in the target enzyme at the site. The substance possibly acts on penicillin-binding protein, promoting cell lysis. The analysis of cytotoxicity and mutagenicity shows favorable results for future in vivo toxicological tests to be carried out, with the aim of investigating the potential of this molecule. In addition, the substance showed an excellent pharmacokinetic profile, indicating good parameters for oral use.
    Keywords 2-chloro- N -(4-fluoro-3-nitrophenyl)acetamide ; Klebsiella pneumoniae ; antibacterial ; toxicity ; minimum inhibitory concentration ; Organic chemistry ; QD241-441
    Subject code 540
    Language English
    Publishing date 2020-08-01T00:00:00Z
    Publisher MDPI AG
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  5. Article ; Online: (R)-(+)-β-Citronellol and (S)-(−)-β-Citronellol in Combination with Amphotericin B against Candida Spp.

    Daniele Silva / Hermes Diniz-Neto / Laísa Cordeiro / Maria Silva-Neta / Shellygton Silva / Francisco Andrade-Júnior / Maria Leite / Jefferson Nóbrega / Maria Morais / Juliana Souza / Lyvia Rosa / Thamara Melo / Helivaldo Souza / Aleson Sousa / Gregório Rodrigues / Abrahão Oliveira-Filho / Edeltrudes Lima

    International Journal of Molecular Sciences, Vol 21, Iss 5, p

    2020  Volume 1785

    Abstract: The enantiomers (R)-(+)-β-citronellol and (S)-(−)-β-citronellol are present in many medicinal plants, but little is understood about their bioactivity against Candida yeasts. This study aimed to evaluate the behavior of positive and negative enantiomers ... ...

    Abstract The enantiomers (R)-(+)-β-citronellol and (S)-(−)-β-citronellol are present in many medicinal plants, but little is understood about their bioactivity against Candida yeasts. This study aimed to evaluate the behavior of positive and negative enantiomers of β-citronellol on strains of Candida albicans and C. tropicalis involved in candidemia. The minimum inhibitory concentration (MIC) and minimum fungicide concentration (MFC) were determined. The evaluation of growth kinetics, mechanism of action, and association studies with Amphotericin B (AB) using the checkerboard method was also performed. R-(+)-β-citronellol and S-(−)-β-citronellol presented a MIC 50% of 64 µg/mL and a MFC 50% of 256 µg/mL for C. albicans strains. For C. tropicalis , the isomers exhibited a MIC 50% of 256 µg/mL and a MFC 50% of 1024 µg/mL. In the mechanism of action assay, both substances displayed an effect on the fungal membrane but not on the fungal cell wall. Synergism and indifference were observed in the association of R-(+)-β-citronellol and AB, while the association between S-(−)-β-citronellol and AB displayed synergism, additivity, and indifference. In conclusion, both isomers of β-citronellol presented a similar profile of antifungal activity. Hence, they can be contemplated in the development of new antifungal drugs providing that further research is conducted about their pharmacology and toxicity.
    Keywords isomers ; (r)-(+)-β-citronellol ; (s)-(−)-β-citronellol ; candida spp ; antifungal activity ; Biology (General) ; QH301-705.5 ; Chemistry ; QD1-999
    Subject code 500
    Language English
    Publishing date 2020-03-01T00:00:00Z
    Publisher MDPI AG
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  6. Article ; Online: Th1-Biased Immunomodulation and In Vivo Antitumor Effect of a Novel Piperine Analogue

    Jephesson Santos / Monalisa Brito / Rafael Ferreira / Ana Paula Moura / Tatyanna Sousa / Tatianne Batista / Vivianne Mangueira / Fagner Leite / Ryldene Cruz / Giciane Vieira / Bruno Lira / Petrônio Athayde-Filho / Helivaldo Souza / Normando Costa / Robson Veras / José Maria Barbosa-Filho / Hemerson Magalhães / Marianna Sobral

    International Journal of Molecular Sciences, Vol 19, Iss 9, p

    2018  Volume 2594

    Abstract: Natural products have an important role as prototypes in the synthesis of new anticancer drugs. Piperine is an alkaloid amide with antitumor activity and significant toxicity. Then, the N-(p-nitrophenyl)acetamide piperinoate (HE-02) was synthesized, and ... ...

    Abstract Natural products have an important role as prototypes in the synthesis of new anticancer drugs. Piperine is an alkaloid amide with antitumor activity and significant toxicity. Then, the N-(p-nitrophenyl)acetamide piperinoate (HE-02) was synthesized, and tested for toxicological and antitumor effects. The toxicity was evaluated in vitro (on RAW 264.7 cells and mice erythrocytes) and in vivo (acute toxicity in mice). The Ehrlich ascites carcinoma model was used to evaluate the antitumor activity of HE-02 (6.25, 12.5 or 25 mg/kg, intraperitoneally, i.p.), as well as toxicity. HE-02 induced only 5.01% of hemolysis, and reduced the viability of RAW 264.7 cells by 49.75% at 1000 µg/mL. LD50 (lethal dose 50%) was estimated at around 2000 mg/kg (i.p.). HE-02 reduced Ehrlich tumor cell viability and peritumoral microvessels density. There was an increase of Th1 helper T lymphocytes cytokine profile levels (IL-1β, TNF-α, IL-12) and a decrease of Th2 cytokine profile (IL-4, IL-10). Moreover, an increase was observed on reactive oxygen species and nitric oxide production. Weak in vivo toxicological effects were recorded. Our data provide evidence that the piperine analogue HE-02 present low toxicity, and its antitumor effect involves modulation of immune system to a cytotoxic Th1 profile.
    Keywords cancer ; piperine analogue ; antitumor activity ; toxicity ; Biology (General) ; QH301-705.5 ; Chemistry ; QD1-999
    Language English
    Publishing date 2018-09-01T00:00:00Z
    Publisher MDPI AG
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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