scholarly journals Successful Release of Voriconazole and Flavonoids from MAPLE Deposited Bioactive Surfaces

2019 ◽  
Vol 9 (4) ◽  
pp. 786
Author(s):  
Irina Negut ◽  
Anita Visan ◽  
Camelia Popescu ◽  
Rodica Cristescu ◽  
Anton Ficai ◽  
...  
Keyword(s):  
Thin Films ◽  
Antifungal Activity ◽  
Active Form ◽  
Culture Collection ◽  
American Type Culture Collection ◽  
Laser Source ◽  
Laser Evaporation ◽  
Bioactive Substances ◽  
Chemical Structures

We explored the potential of biomimetic thin films fabricated by means of matrix-assisted pulsed laser evaporation (MAPLE) for releasing combinations of active substances represented by flavonoids (quercetin dihydrate and resveratrol) and antifungal compounds (amphotericin B and voriconazole) embedded in a polyvinylpyrrolidone biopolymer; the antifungal activity of the film components was evaluated using in vitro microbiological assays. Thin films were deposited using a pulsed KrF* excimer laser source which were structurally characterized using atomic force microscopy (AFM) and Fourier transform infrared spectroscopy (FTIR). High-quality thin films with chemical structures similar to dropcast ones were created using an optimum laser fluence of ~80 mJ/cm2. Bioactive substances were included within the polymer thin films using the MAPLE technique. The results of the in vitro microbiology assay, which utilized a modified disk diffusion approach and were performed using two fungal strains (Candida albicans American Type Culture Collection (ATCC) 90028 and Candida parapsilosis American Type Culture Collection (ATCC) 22019), revealed that voriconazole was released in an active form from the polyvinylpyrrolidone matrix. The results of this study show that the MAPLE-deposited bioactive thin films have a promising potential for use in designing combination devices, such as drug delivery devices, and medical device surfaces with antifungal activity.

scholarly journals In Vitro Activities of Garenoxacin (BMS-284756) against 170 Clinical Isolates of Nine Pasteurella Species

2002 ◽  
Vol 46 (9) ◽  
pp. 3068-3070 ◽  
Author(s):  
Ellie J. C. Goldstein ◽  
Diane M. Citron ◽  
C. Vreni Merriam ◽  
Yumi A. Warren ◽  
Kerin L. Tyrrell ◽  
...  
Keyword(s):  
Pasteurella Multocida ◽  
Active Agent ◽  
Culture Collection ◽  
Clinical Isolates ◽  
American Type Culture Collection ◽  
Dilution Method ◽  
Agar Dilution Method ◽  
Agar Dilution

ABSTRACT The in vitro susceptibilities of 170 clinical isolates plus 12 American Type Culture Collection strains of Pasteurella species comprising nine species and three Pasteurella multocida subspecies were studied by an agar dilution method. Garenoxacin (BMS-284756), a new des-fluoro(6) quinolone, was active at ≤0.06 μg/ml against all isolates, including four β-lactamase-producing strains, with >90% of the strains susceptible to ≤0.008 μg/ml. Garenoxacin was generally 1 to 2 dilutions more active than levofloxacin and moxifloxacin and was the most active agent tested. Cefoxitin required 1 μg/ml for inhibition of 51 of 182 (29%) of strains, and 3 strains (also β-lactamase producers) were resistant to doxycycline.

scholarly journals Characterization of Sucrose Thin Films for Biomedical Applications

2011 ◽  
Vol 2011 ◽  
pp. 1-6 ◽  
Author(s):  
S. L. Iconaru ◽  
F. Ungureanu ◽  
A. Costescu ◽  
M. Costache ◽  
A. Dinischiotu ◽  
...  
Keyword(s):  
Thin Films ◽  
Photoelectron Spectroscopy ◽  
Biomedical Applications ◽  
Culture Collection ◽  
Gravimetric Analysis ◽  
Osteoblast Cells ◽  
Glass Substrates ◽  
Evaporation Technique ◽  
Partially Unfolded

Sucrose is a natural osmolyte accumulated in the cells of organisms as they adapt to environmental stress. In vitro sucrose increases protein stability and forces partially unfolded structures to refold. Thin films of sucrose (C12H22O11) were deposited on thin cut glass substrates by the thermal evaporation technique (P∼10−5torr). Characteristics of thin films were put into evidence by Fourier Transform Infrared Spectroscopy (FTIR), X-ray Photoelectron Spectroscopy (XPS), scanning electron microscopy (SEM), and differential thermal analysis and thermal gravimetric analysis (TG/DTA). The experimental results confirm a uniform deposition of an adherent layer. In this paper we present a part of the characteristics of sucrose thin films deposited on glass in medium vacuum conditions, as a part of a culture medium for osteoblast cells. Osteoblast cells were used to determine proliferation, viability, and cytotoxicity interactions with sucrose powder and sucrose thin films. The osteoblast cells have been provided from the American Type Culture Collection (ATCC) Centre. The outcome of this study demonstrated the effectiveness of sucrose thin films as a possible nontoxic agent for biomedical applications.

scholarly journals Evaluation of the antifungal activity by plant extracts against Colletotrichum gloeosporioides Penz

2008 ◽  
Vol 32 (2) ◽  
pp. 420-428 ◽  
Author(s):  
Polyanna Alves Silva ◽  
Denilson Ferreira Oliveira ◽  
Ney Robson Taironi do Prado ◽  
Douglas Antônio de Carvalho ◽  
Gilvane Aparecida de Carvalho
Keyword(s):  
Antifungal Activity ◽  
Freeze Drying ◽  
Colletotrichum Gloeosporioides ◽  
Plantago Lanceolata ◽  
Stevia Rebaudiana ◽  
Tween 80 ◽  
In Vitro Assays ◽  
Bioactive Substances ◽  
Stevia Rebaudiana Bertoni

Aiming to develop more efficient and environmental friendly methods than those available to control Colletotrichum gloeosporioides Penz, which causes blister spot in coffee trees, a search for plants able to produce substances active against such pathogen was carried out. Thus, extracts of 48 plant species, collected at Alto Rio Grande region, in Minas Gerais, were prepared and submitted to in vitro assays with that fungus. The best results were obtained with the extracts prepared from Digitalis lanata Ehrh, Origanum manjorona L., Plantago lanceolata Hook. and Stevia rebaudiana (Bertoni) Bertoni, which inhibited C. gloeosporioides spores germination. After dilution of some active extracts with aqueous 1 % Tween 80 solution in a 1:2 or 1:3 ratio (extract:aqueous solution), their antifungal activity vanished. Some of the active extracts were also submitted to freeze drying and none of them presented any alteration in their antifungal activity. Concluding, several plants presented potential to be used in the search for new bioactive substances to control C. gloeosporioides, especially O. manjorona L., which inhibited 96 % of the fungus spores germination.

scholarly journals Comparison of In Vitro Activities of Camptothecin and Nitidine Derivatives against Fungal and Cancer Cells

1999 ◽  
Vol 43 (12) ◽  
pp. 2862-2868 ◽  
Author(s):  
Maurizio Del Poeta ◽  
Shih-Fong Chen ◽  
Daniel Von Hoff ◽  
Christine C. Dykstra ◽  
Mansukh C. Wani ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Mammalian Cells ◽  
Topoisomerase I ◽  
Active Form ◽  
Antifungal Drugs ◽  
Water Soluble ◽  
Yeast Cells ◽  
Original Structure ◽  
Camptothecin Analogs

ABSTRACT The activities of a series of camptothecin and nitidine derivatives that might interact with topoisomerase I were compared against yeast and cancer cell lines. Our findings reveal that structural modifications to camptothecin derivatives have profound effects on the topoisomerase I-drug poison complex in cells. Although the water-soluble anticancer agents topotecan and irinotecan are less active than the original structure, camptothecin, other derivatives or analogs with substitutions that increase compound solubility have also increased antifungal activities. In fact, a water-soluble prodrug appears to penetrate into the cell and release its active form; the resulting effect in complex with Cryptococcus neoformanstopoisomerase I is a fungicidal response and also potent antitumor activity. Some of the compounds that are not toxic to wild-type yeast cells are extremely toxic to the yeast cells when the C. neoformans topoisomerase I target is overexpressed. With the known antifungal mechanism of a camptothecin-topoisomerase I complex as a cellular poison, these findings indicate that drug entry may be extremely important for antifungal activity. Nitidine chloride exhibits antifungal activity against yeast cells through a mechanism(s) other than topoisomerase I and appears to be less active than camptothecin analogs against tumor cells. Finally, some camptothecin analogs exhibit synergistic antifungal activity against yeast cells in combination with amphotericin B in vitro. Our results suggest that camptothecin and/or nitidine derivatives can exhibit potent antifungal activity and that the activities of camptothecin derivatives with existing antifungal drugs may be synergistic against pathogenic fungi. These new compounds, which exhibit potent antitumor activities, will likely require further structural changes to find more selective activity against fungal versus mammalian cells to hold promise as a new class of antifungal agents.

scholarly journals Atividade antibacteriana in vitro de pimentas e pimentões (Capsicum sp.) sobre quatro bactérias toxinfectivas alimentares

2010 ◽  
Vol 12 (1) ◽  
pp. 8-12 ◽  
Author(s):  
H.H Carvalho ◽  
J.M Wiest ◽  
F.T Cruz
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Enterococcus Faecalis ◽  
Salmonella Enteritidis ◽  
Culture Collection ◽  
American Type Culture Collection ◽  
Porto Alegre

Determinou-se in vitro a Intensidade de Atividade de Inibição Bacteriana (IINIB) e a Intensidade de Atividade de Inativação Bacteriana (IINAB), através de Testes de Diluição em Sistema de Tubos Múltiplos, de extratos de oito pimentas do gênero Capsicum, etnograficamente acessadas na região metropolitana de Porto Alegre/RS/BR, frente a inóculos bacterianos padronizados (American Type Culture Collection - ATCC), respectivamente Staphylococcus aureus (25923), Enterococcus faecalis (19433), Salmonella enteritidis (13076) e Escherichia coli (11229), em doses-desafio = 10(7) UFC mL-1. Quatro destas plantas, pimenta calabresa ("pool" Capsicum sp), pimenta-de-jardim (C.annuum), pimenta dedo-de-moça (C. baccatum) e pimenta malagueta (C. frutescens), apresentaram atividades de inibição e inativação seletivas, em ordem decrescente, para salmonela, coliforme fecal, enterococo e estafilococo. As demais, pimenta cambuci (C. baccatum) e os pimentões (C. annuum) amarelo, verde e vermelho, apresentaram nenhuma atividade. Discute-se a validade da ferramenta etnográfica na prospecção de fatores de proteção anti-bacteriana em plantas, bem como a influência da inibição/inativação na preditividade do diagnóstico bacteriológico.

scholarly journals Structure-activity relationships of cadinane-type sesquiterpene derivatives against wood-decay fungi

Holzforschung ◽  
2005 ◽  
Vol 59 (6) ◽  
pp. 620-627 ◽  
Author(s):  
Chi-Lin Wu ◽  
Shih-Chang Chien ◽  
Sheng-Yang Wang ◽  
Yueh-Hsiung Kuo ◽  
Shang-Tzen Chang
Keyword(s):  
Antifungal Activity ◽  
Wide Spectrum ◽  
Wood Decay ◽  
Wood Preservatives ◽  
Decay Fungi ◽  
Structure Activity Relationships ◽  
Chemical Structures ◽  
Structure Activity ◽  
Wood Decay Fungi

Abstract Cadinane-type sesquiterpenes have a wide spectrum of biological activity, but their use as wood preservatives and the structure-activity relationships of their derivatives have not yet been reported. A total of 13 compounds were synthesized from T-cadinol, T-muurolol, and α-cadinol and their chemical structures were confirmed by IR, MS, and 1H and 13C NMR. The antifungal properties of 16 compounds against three wood-decay fungi were evaluated in vitro. α-Cadinol showed strong antifungal activity against Lenzites betulina, Trametes versicolor, and Laetiporus sulphureus (total mean IC50 0.10 mM). Among the derivatives synthesized, 3β-ethoxy-T-muurolol (0.24 mM), 4ξH-cadinan-10β-ol (0.25 mM), 4ξH-muurolan-10β-ol (0.29 mM), and 4ξH-cadinan-10α-ol (0.25 mM) showed good antifungal activity against all fungi tested. Correlation was observed between the antifungal activity of the compounds tested and log P. Furthermore, the presence of an unsaturated double bond and oxygen-containing functional groups in the compounds plays a key role in their antifungal activity. The stereo configuration of cadinane-type sesquiterpenes also influences their antifungal activity. Understanding how the structure of natural compounds relates to their antifungal function is important and may facilitate their application as novel wood preservatives.

scholarly journals Atividade antimicrobiana in vitro do látex da Jatropha multifida L.

2021 ◽  
Vol 10 (10) ◽  
pp. e334101017511
Author(s):  
Daniglayse Santos Vieira ◽  
Irinaldo Diniz Basílio Junior ◽  
Rossana Teotonio de Farias Moreira ◽  
Rodrigo José Nunes Calumby ◽  
Rafael Aleixo dos Santos Silva ◽  
...  
Keyword(s):  
Culture Collection ◽  
American Type Culture Collection ◽  
E Coli ◽  
Jatropha Multifida

Jatropha multifida L., conhecida popularmente como mertiolate, é um arbusto, cujas flores vermelhas com anteras amareladas, parecem pequenas peças de coral e caule com presença de látex. É usada na medicina popular para tratar diversas afecções, como feridas infectadas, úlceras e dermatoses. O objetivo do estudo foi verificar a atividade antimicrobiana do látex in natura e liofilizado da J. multifida. Trata-se de pesquisa quantitativa, do tipo experimental. O látex foi coletado no município de Igreja Nova – Alagoas, utilizando-se o método de sangria, em que se realizou cortes oblíquos no caule, obtendo-se o extrato in natura. Já para obtenção do extrato em pó, utilizou-se a liofilização do material in natura. Para avaliação da atividade antimicrobiana foi empregado o método de microdiluição em caldo para determinação da Concentração Inibitória Mínima (CIM), seguido de plaqueamento em ágar para obtenção da Concentração Bactericida Mínima (CBM) dos extratos frente aos microrganismos padronizados pela American Type Culture Collection – ATCC: S. aureus (25923) S. epidermidis (31488), E. faecalis (29212), P. aeruginosa (27853), E. coli (25922), E. aerogenes (13048) e Concentração Fungicida Mínima (CFM) para C. albicans (24433). Os resultados apontaram que ambos os extratos do látex da J. multifida apresentaram uma atividade antimicrobiana moderada contra a maioria das cepas bacterianas testadas e uma atividade fúngica fraca frente a C. albicans, com destaque para o extrato liofilizado. Conclui-se que os extratos foram mais promissores contra as cepas de S. aureus, S. epidermidis, E. faecalis e P. aeruginosa, abrindo possibilidades para evolução de estudos complementares.

scholarly journals Crinipellins A and I, Two Diterpenoids from the Basidiomycete Fungus Crinipellis rhizomaticola, as Potential Natural Fungicides

Molecules ◽  
2018 ◽  
Vol 23 (9) ◽  
pp. 2377 ◽  
Author(s):  
Jae Han ◽  
Mira Oh ◽  
Yu Lee ◽  
Jaehyuk Choi ◽  
Gyung Choi ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Ethyl Acetate ◽  
Culture Filtrate ◽  
Fungal Pathogens ◽  
Its Region ◽  
In Planta ◽  
Chemical Structures ◽  
Wide Range ◽  
Wheat Leaf

In the course of screening for microbes with antifungal activity, we found that the culture filtrate of the IUM00035 isolate exhibited strong antifungal activity against Magnaporthe oryzae and Colletotrichum coccodes in planta. Based on the phylogenetic analysis with the ITS region, the IUM00035 isolate was identified as Crinipellis rhizomaticola. To identify antifungal compounds from the C. rhizomaticola IUM00035 isolate, the culture filtrate of the isolate was partitioned with ethyl acetate and n-butanol and, consequently, two active compounds were isolated from the ethyl acetate extract. The chemical structures of the isolated compounds were determined as crinipellin A (1) and a new crinipellin derivative, crinipellin I (2), by NMR spectral analyses and a comparison of their NMR and MS data with those reported in the literature. Crinipellin A (1) exhibited a wide range of antifungal activity in vitro against C. coccodes, M. oryzae, Botrytis cinerea, and Phytophthora infestans (MICs = 1, 8, 31, and 31 µg/mL, respectively). Furthermore, when plants were treated with crinipellin A (1) (500 µg/mL) prior to inoculation with fungal pathogens, crinipellin A (1) exhibited disease control values of 88%, 65%, and 60% compared with non-treatment control against tomato late blight, pepper anthracnose, and wheat leaf rust, respectively. In contrast to crinipellin A (1), crinipellin I (2) showed weak or no activity (MICs > 250 µg/mL). Taken together, our results show that the C. rhizomaticola IUM00035 isolate suppresses the development of plant fungal diseases, in part through the production of crinipellin A (1).

scholarly journals Design, Synthesis, and Antimicrobial Activities of 1,2,3-Triazole Glycoside Clickamers

Molecules ◽  
2020 ◽  
Vol 25 (4) ◽  
pp. 790 ◽  
Author(s):  
Tamer El Malah ◽  
Hany F. Nour ◽  
Amira A. E. Satti ◽  
Bahaa A. Hemdan ◽  
Wael A. El-Sayed
Keyword(s):  
Staphylococcus Aureus ◽  
Antifungal Activity ◽  
Bacterial Resistance ◽  
Antimicrobial Activities ◽  
Biological Evaluation ◽  
Biologically Active ◽  
Spectroscopic Techniques ◽  
Reference Drug ◽  
Chemical Structures

Bacterial resistance remains a significant threat and a leading cause of death worldwide, despite massive attempts to control infections. In an effort to develop biologically active antibacterial and antifungal agents, six novel aryl-substituted-1,2,3-triazoles linked to carbohydrate units were synthesized through the Cu(I)-catalyzed azide-alkyne cycloaddition CuAAC of substituted-arylazides with a selection of alkyne-functionalized sugars. The chemical structures of the new derivatives were verified using different spectroscopic techniques. The novel clicked 1,2,3-triazoles were evaluated for in vitro antibacterial activity against Gram-positive Staphylococcus aureus and Gram-negative Pseudomonas aeruginosa, and the obtained results were compared with the activity of the reference antibiotic “Ampicillin”. Likewise, in vitro antifungal activity of the new 1,2,3-triazoles was investigated against Candida albicans and Aspergillus niger using “Nystatin” as a reference drug. The results of the biological evaluation pointed out that Staphylococcus aureus was more susceptible to all of the tested compounds than other examined microbes. In addition, some tested compounds exhibited promising antifungal activity.

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