scholarly journals Antifungal Activity of Linear and Disulfide-Cyclized Ultrashort Cationic Lipopeptides Alone and in Combination with Fluconazole against Vulvovaginal Candida spp.

Pharmaceutics ◽  
2021 ◽  
Vol 13 (10) ◽  
pp. 1589
Author(s):  
Paulina Czechowicz ◽  
Damian Neubauer ◽  
Joanna Nowicka ◽  
Wojciech Kamysz ◽  
Grażyna Gościniak
Keyword(s):  
Antifungal Activity ◽  
Synergistic Effect ◽  
Antimicrobial Activities ◽  
The Other ◽  
In Vivo Studies ◽  
Antifungal Compounds ◽  
Candida Spp ◽  
Anticandidal Activity ◽  
Toxic Concentrations

Vulvovaginal candidiasis (VVC) occurs in over 75% of women at least once during their lifetime and is an infection that significantly affects their health. Candida strains resistant to standard azole antifungal therapy and relapses of VVC are more and more common. Hypothetically, biofilm is one of the main reasons of relapses and failure of the therapy. Ultrashort cationic lipopeptides (USCLs) exhibit high antimicrobial activities. Our previous study on USCLs revealed that disulfide cyclization can result in selective antifungal compounds. Therefore, four USCL were selected and their antifungal activity were studied on 62 clinical strains isolated from VVC. The results confirmed previous premises that cyclic analogs have increased selectivity between fungal cells and keratinocytes and improved anticandidal activity compared to their linear analogs against both planktonic and biofilm cultures. On the other hand, linear lipopeptides in combination with fluconazole showed a synergistic effect. It was found that the minimum inhibitory concentrations of the tested compounds in combination with fluconazole were at least four times lower than when used separately. Our results indicate that combination therapy of VVC with USCLs and fluconazole at low non-toxic concentrations can be beneficial owing to the synergistic effect. However, further in vivo studies are needed to confirm this hypothesis.

scholarly journals Antifungal Activity of Linear and Disulfide-Cyclized Ultrashort Cationic Lipopeptides Alone and in Combination with Fluconazole Against Vulvovaginal Candida spp.

2021 ◽  
Author(s):  
Paulina Czechowicz ◽  
Damian Neubauer ◽  
Joanna Nowicka ◽  
Wojciech Kamysz ◽  
Grażyna Gościniak
Keyword(s):  
Antifungal Activity ◽  
Combination Therapy ◽  
Synergistic Effect ◽  
Antimicrobial Activities ◽  
The Other ◽  
Antifungal Compounds ◽  
Candida Spp ◽  
Anticandidal Activity ◽  
Toxic Concentrations

Abstract Vulvovaginal candidiasis (VVC) occurs in over 75% of women at least once during their lifetime and is an infection that significantly affects their health. Candida strains resistant to standard azole antifungal therapy and relapses of VVC are more and more common. Hypothetically, biofilm is one of the main reasons of relapses and failure of the therapy. Ultrashort cationic lipopeptides (USCLs) exhibit high antimicrobial activities. Our previous study on USCLs revealed that disulfide cyclization can result in selective antifungal compounds. Therefore, four USCL were selected and their antifungal activity were studied on 62 clinical strains isolated from VVC. The results showed that cyclic analogs have increased selectivity between fungal cells and keratinocytes and improved anticandidal activity than their linear analogs against both planktonic and biofilm cultures. On the other hand, linear lipopeptides in combination with fluconazole showed the synergistic effect. It was found that the minimum inhibitory concentrations of the tested compounds in combination with fluconazole were at least four times lower than when used separately. Our results indicate that combination therapy of VVC with USCLs and fluconazole at low non-toxic concentrations can be beneficial owing to the synergistic effect. However, further in vivo studies are needed to confirm this hypothesis.

scholarly journals EVALUATION OF ANTIFUNGAL AND ANTIBACTERIAL ACTIVITY OF SOME NEW BENZIMIDAZOLE DERIVATIVES

2018 ◽  
Vol 48 (2) ◽  
pp. 125-129
Author(s):  
K. ZOMORODIAN ◽  
S. KHABNADIDEH ◽  
L. ZAMANI ◽  
K. PAKSHIR ◽  
M. TAJADDOD
Keyword(s):  
Antifungal Activity ◽  
Fungal Infections ◽  
Antimicrobial Activities ◽  
Antifungal Drugs ◽  
In Vivo Studies ◽  
Benzimidazole Derivatives ◽  
Dilution Method ◽  
Gram Positive ◽  
Meta Position

The extensive use of antifungal drugs and their resistance against fungal infections have led to discover new antimicrobial compounds. We previously described synthesis of some new derivatives of 2-methylbenzimidazole (1a-5a) and 5,6dimethylbenzimidazol (1b-5b). Here we evaluated the antimicrobial activities of these compounds against different species of micro organisms including gram positive and gram negative bacteria as well as fungi. Broth micro-dilution method as recommended by clinical and laboratory standard institute (CLSI) was used for this purpose. The results show compounds 2-Methyl-1-(3-methylbenzyl)-1H-benzo [d]imidazole (5a) and 5,6-Dimethyl-1-(3-methyl benzyl)-1H-benzo[d]imidazole (5b) had the best antifungal activity against the examined fungi and gram positive bacteria. Moreover these two compounds inhibited the growth of azole resistant strains. By comparison the relationship between the structures and activities of the tested compounds revealed that the presence of methyl residue in meta position of benzyl group enhance the antifungal activity. Regarding a broad spectrum antifungal activities of some of the tested compounds, they might be a good candidate for further in vivo studies to evaluate their pharmacological activity and toxicity as a novel antifungal agents.

scholarly journals Standardization of a method to study angiogenesis in a mouse model

2013 ◽  
Vol 85 (4) ◽  
pp. 1483-1487
Author(s):  
DAVID FEDER ◽  
FABIO F. PERRAZO ◽  
EDIMAR C. PEREIRA ◽  
SILVANA FORSAIT ◽  
CECILIA K.R. FEDER ◽  
...  
Keyword(s):  
Quantitative Analysis ◽  
Animal Models ◽  
The Other ◽  
In Vivo Studies ◽  
Specific Method ◽  
Test Results ◽  
Hemoglobin Content ◽  
Physiological Conditions ◽  
Adult Organism

In the adult organism, angiogenesis is restricted to a few physiological conditions. On the other hand, uncontrolled angiogenesis have often been associated to angiogenesis-dependent pathologies. A variety of animal models have been described to provide more quantitative analysis of in vivo angiogenesis and to characterize pro- and antiangiogenic molecules. However, it is still necessary to establish a quantitative, reproducible and specific method for studies of angiogenesis factors and inhibitors. This work aimed to standardize a method for the study of angiogenesis and to investigate the effects of thalidomide on angiogenesis. Sponges of 0.5 x 0.5 x 0.5 cm were implanted in the back of mice groups, control and experimental (thalidomide 200 mg/K/day by gavage). After seven days, the sponges were removed. The dosage of hemoglobin in sponge and in circulation was performed and the ratio between the values was tested using nonparametric Mann-Whitney test. Results have shown that sponge-induced angiogenesis quantitated by ratio between hemoglobin content in serum and in sponge is a helpful model for in vivo studies on angiogenesis. Moreover, it was observed that sponge-induced angiogenesis can be suppressed by thalidomide, corroborating to the validity of the standardized method.

RhBMP-2 and -7 combined with absorbable collagen sponge carrier enhance ectopic bone formation: An in vivo bioassay

2011 ◽  
Vol 5 (1) ◽  
pp. 85-92
Author(s):  
Kanok Preativatanyou ◽  
Sittisak Honsawek
Keyword(s):  
Bone Formation ◽  
Synergistic Effect ◽  
Expression System ◽  
Collagen Sponge ◽  
In Vivo Studies ◽  
Blood Vessel Invasion ◽  
New Bone Formation ◽  
Absorbable Collagen Sponge ◽  
In Vivo Bioassay

Abstract Background: Recombinant human bone morphogenetic proteins (rhBMPs) have been characterized especially chondrogenic and osteogenic activity both in vitro and in vivo studies. However, delivery of more than one growth factor by sustained release carrier to orthopedic site has yet been questionable in terms of efficacy and synergism. Objective: Evaluate osteoinductivity and synergistic effect of rhBMP-2 and -7 using absorbable collagen sponge (ACS) carrier system in vivo. Methods: cDNA of BMP-2 and -7 active domains were cloned and expressed in Escherichia coli BL21 StarTM (DE3) using pRSETc expression system. Then, the purified rhBMPs were loaded onto ACS and evaluated by in vivo rat subcutaneous bioassay. Two and eight weeks postoperatively, all treated groups were histologically verified for evidence of new bone formation and neovascularization by hematoxylin-eosin staining and light microscopy. Results: The Wistar rat treated with rhBMP-2 or -7/ACS exhibited new bone formation, compared to ACS control. The group treated with ACS supplemented with both rhBMP-2 and -7 significantly showed the osteoid matrix very well-organized into trabeculae-like structure with significant blood vessel invasion. Conclusion: The osteogenic induction of rhBMPs was combined with ACS carrier in the in vivo bioassay. In addition, the combination of both two potent recombinant osteoinductive cytokines, rhBMP-2 and -7, with ACS carrier demonstrated synergistic effect and might be a more promising and effective choice for therapeutic applications.

Induction of antimicrobial peptides from Rana dybowskii under Rana grylio virus stress, and bioactivity analysis

2012 ◽  
Vol 58 (7) ◽  
pp. 848-855 ◽  
Author(s):  
Shu-Jing Yang ◽  
Xiang-Hong Xiao ◽  
Yi-Gang Xu ◽  
Dan-Dan Li ◽  
Long-Hui Chai ◽  
...  
Keyword(s):  
Antimicrobial Peptides ◽  
Antimicrobial Activities ◽  
The Other ◽  
Degenerate Primers ◽  
Cdna Sequences ◽  
Gram Positive Bacteria ◽  
Pathogen Invasion ◽  
Peptide Precursors ◽  
Rana Dybowskii

The skin glands of Ranidae are a rich source of antimicrobial peptides. In this study, the genomic RNA of Rana dybowskii was extracted from its skin while under Rana grylio virus stress. Five new cDNA sequences encoding 5 mature peptides, Ranatuerin-2YJ (GLMDIFKVAVNKLLAAGMNKPRCKAAHC), Dybowskin-YJb (IIPLPLGYFAKKP), Dybowskin-YJa (IIPLPLGYFAKKKKKKDPVPLDQ), Temperin-YJa (VLPLLETCSMTCWENNQTFGK), and Temperin-YJb (VLPLVGNLLNDLLGK), were obtained by reverse transcription polymerase chain reaction with a pair of degenerate primers designed according to the conserved terminal sequences of cDNA encoding antimicrobial peptide precursors of genus Rana. The antimicrobial activities of the peptides were analyzed, and the results demonstrated that all these peptides showed a significant anti-Rana grylio virus activity, and the virus was gradually cleared with the increase in gene expression. Among the 5 peptides obtained in this work, Ranatuerin-2YJ also showed a broad-spectrum anti-Gram-positive bacteria and anti-Gram-negative bacteria activity with a minimal inhibitory concentration of 22.5 µg/mL and 7.64% hemolysis activity, both of which were significantly lower (p < 0.05) than that of the other peptides. Moreover, Ranatuerin-2YJ was widely distributed in the skin, liver, spleen, and blood of R. dybowskii, while the other 4 peptides could only be cloned from the skin, indicating that the Ranatuerin-2YJ in vivo plays an important role in the protection against pathogen invasion.

The influence of photodynamic therapy parameters on the inactivation of Candida spp: in vitro and in vivo studies

Laser Physics ◽  
2014 ◽  
Vol 24 (4) ◽  
pp. 045601 ◽  
Author(s):  
F Alves ◽  
E G Mima ◽  
L N Dovigo ◽  
V S Bagnato ◽  
J H Jorge ◽  
...  
Keyword(s):  
Photodynamic Therapy ◽  
In Vivo Studies ◽  
Candida Spp

scholarly journals Non-toxic Cobalt(III) Schiff Base Complexes with Broad Spectrum Antifungal Activity

2020 ◽  
Author(s):  
Angelo Frei ◽  
A. Paden King ◽  
Gabrielle J. Lowe ◽  
Amy K. Cain ◽  
Francesca L. Short ◽  
...  
Keyword(s):  
Schiff Base ◽  
Antifungal Activity ◽  
Broad Spectrum ◽  
Bacterial Infections ◽  
Fungal Infections ◽  
Antifungal Drugs ◽  
New Drugs ◽  
Schiff Base Complexes ◽  
In Vivo Studies

Resistance to currently available antifungal drugs has quietly been on the rise but overshadowed by the alarming spread of antibacterial resistance. There is a striking lack of attention to the threat of drug resistant fungal infections, with only a handful of new drugs currently in development. Given that metal complexes have proven to be useful new chemotypes in the fight against diseases such as cancer, malaria, and bacterial infections, it stands to reason to explore their possible utility in treating fungal infections. Herein we report a series of cobalt(III) Schiff base complexes with broad spectrum antifungal activity. Some of these complexes (1-3) show minimum inhibitory concentrations (MIC) in the low micro- to nanomolar range against a series of Candida and Cryptococcus yeasts. Additionally, we demonstrate that these compounds show no cytotoxicity against both bacterial and human cells. Finally, we report first in vivo toxicity data on these compounds in Galleria mellonella, showing that doses as high as 266 mg/kg are tolerated without adverse effects, paving the way for further in vivo studies of these complexes. <br>

scholarly journals Insects as a source of phenolic compounds and potential health benefits

2021 ◽  
pp. 1-12
Author(s):  
M.C. Nino ◽  
L. Reddivari ◽  
C. Osorio ◽  
I. Kaplan ◽  
A.M. Liceaga
Keyword(s):  
Phenolic Compounds ◽  
De Novo ◽  
Health Benefits ◽  
Antimicrobial Activities ◽  
In Vivo Studies ◽  
Plant Phenolics ◽  
Potential Health ◽  
Bioactive Potential

The use of insects in traditional medicine and unveiling the chemical structure of the bright pigments in butterfly wings led to the discovery of bioactive phenolic compounds in the insect bodies. These metabolites have been found not only due to the insect absorption and metabolisation of the plant-derived phenolic present in their diet, but also from the ability of insects to synthesise phenolic compounds de novo through the sclerotisation process. Plant phenolics are secondary metabolites involved in the protection of tissues against UV radiation, herbivores, and pathogens, as well as pigmentation of fruits and flowers. These bioactive compounds exhibit antioxidant, anti-inflammatory, anticancer, and antimicrobial activities, demonstrated through in vitro and in vivo studies. This bioactive potential is thought to occur due to their chemical characteristics that allow them to stabilise reactive oxygen species (ROS), chelate prooxidant metal ions, interact with key enzymes and signal cascades involved in biological pathways. Bioactivity of plant phenolics and both in vitro, in vivo studies, suggest that the dietary compounds absorbed by the insect maintain their chemical and bioactive properties. Further characterisation of the phenolic composition in edible insects and evaluation of their bioactive capacity as well as their bioavailability, could result in discovering additional health benefits of entomophagy apart from macro-nutritional (e.g. protein) content.

scholarly journals Synthesis and Evaluation of Bioactivity of 6-[(2-Pyridinyloxy)](Benzo)Imidazo[2,1-b][1,3]Thiazine Derivatives

2021 ◽  
Vol 12 (4) ◽  
pp. 5031-5044
Keyword(s):  
Antifungal Activity ◽  
The Other ◽  
Albino Rats ◽  
Target Compound ◽  
Mild Conditions ◽  
In Vivo Experiments ◽  
Nmr Spectrometry ◽  
Suppression Index

A series of new 6-[(pyridine-2-yl)oxy]-6,7-dihydro-5H-imidazo[2,1-b]thiazines 4a-l and their benzoannelated derivatives 4m-r was synthesized by the reaction between 3-hydroxy(benzo)imidazo[2,1-b][1,3]thiazines and substituted 2-chloropyridines under the mild conditions with the yield 53-74 %. The structure of the target compound was proven by the results of 1H NMR, 13C NMR spectrometry, and LC-MS. In silico evaluation of these drug-like compounds proved that many of them comply with the Lipinski ‘rule of five’ and the Veber rule. Antibacterial, antifungal, and anti-inflammatory activity of all synthesized compounds were investigated in the in vitro and in vivo experiments. According to the bio screening results, the compounds 6-[(5-сhloropyridin-2-yl)oxy]-6,7-dihydro-5H-imidazo[2,1-b][1,3]thiazine 4a, 6-[(3,5-dichloropyridin-2-yl)oxy]-6,7-dihydro-5H-imidazo[2,1-b][1,3]thiazine 4e and 6-{[3-chloro-5-(trifluoromethyl)pyridin-2-yl]oxy}-2,3-diphenyl-6,7-dihydro-5H-imidazo[2,1-b][1,3]thiazine 4l proved antifungal activity against Candida albicans. On the other hand, 3-[(3,5-dichloropyridin-2-yl)oxy]-3,4-dihydro-2H-benzo[4,5]imidazo[2,1-b][1,3]thiazine 4q proved the best antifungal activity against Aspergillus niger K 9 (MIC=15.62 µg/ml) and comparatively high antiedema activity against the carrageenan-induced edema of the hind paws of albino rats (the inflammation suppression index was 39.1 %).

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