scholarly journals The Anti-Biofilm Efficacy of Caffeic Acid Phenethyl Ester (CAPE) In Vitro and a Murine Model of Oral Candidiasis

2021 ◽  
Vol 11 ◽  
Author(s):  
Patrícia Pimentel de Barros ◽  
Rodnei Dennis Rossoni ◽  
Maíra Terra Garcia ◽  
Valéria de Lima Kaminski ◽  
Flávio Vieira Loures ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Caffeic Acid ◽  
Murine Model ◽  
Untreated Control ◽  
Oral Candidiasis ◽  
Caffeic Acid Phenethyl Ester ◽  
Control Group ◽  
Untreated Control Group ◽  
Immunomodulatory Effects

Candida albicans is the main fungal species associated with the development of oral candidiasis. Currently, therapeutic options for these infections are limited by the adverse effects of antifungal drugs and by the emergence of drug resistant strains. Thus, the development of new antifungal agents is needed for the prevention and treatment of oral Candida infections. Caffeic acid phenethyl ester (CAPE) is a natural compound from propolis polyphenolic groups that exhibits many pharmacological properties. In this study, we investigated whether CAPE can have antifungal and immunomodulatory effects on oral candidiasis. Preliminary tests to assess the antifungal activity of CAPE were performed using the Minimum Inhibitory Concentration (MIC) assay that demonstrated inhibition in a range from 16 to 32 μg/mL, confirming its antifungal activity on several C. albicans strains isolated from the oral cavity. Subsequently, we analyzed Candida spp biofilms formed in vitro, in which CAPE treatment at 5 x MIC caused a reduction of 68.5% in the total biomass and ~2.60 Log in the viable cell count (CFU/mL) in relation to the untreated biofilm (p<0.0001). Next, RNA was extracted from untreated and CAPE-treated biofilms and analyzed by real-time qPCR. A series of genes analyzed (ALS1, ECE1, EPA1, HWP1, YWP1, BCR1, BGR1, CPH1, EFG1, NDT80, ROB1, TEC1, UME6, SAP2, SAP5, PBL2, and LIP9) were downregulated by CAPE compared to the untreated control group (p<0.0001). In in vivo studies using Galleria mellonella, the treatment with CAPE prolonged survival of larvae infected by C. albicans by 44.5% (p < 0.05) and accompanied by a 2.07-fold increase in the number of hemocytes. Flow cytometry revealed the most prominent increases were in types P2 and P3 hemocytes, granular cells, which phagocytize pathogens. In addition, CAPE treatment decreased the fungal load in the hemolymph and stimulated the expression of antifungal peptide genes such as galiomicin and gallerimycin. The antifungal and immunomodulatory activities observed in G. mellonella were extended to a murine model of oral candidiasis, in which CAPE decreased the levels of C. albicans colonization (~2 log CFU/mL) in relation to the untreated control group. In addition, CAPE treatment significantly reduced pseudomembranous lesions, invasion of hyphae on epithelium surfaces, tissue damage and inflammatory infiltrate (p < 0.05). CAPE was also able to increase the expression of β-defensin 3 compared to the infected and untreated group by 3.91-fold (p < 0.0001). Taken together, these results show that CAPE has both antifungal and immunomodulatory effects, making it a promising natural antifungal agent for the treatment and prevention of candidiasis and shows impact to oral candidiasis.

scholarly journals Doxorubicin-induced myocardial failure in rats with malignant neoplasm: Protective role of fullerenol C60(OH)24

2008 ◽  
Vol 62 (3) ◽  
pp. 197-204 ◽  
Author(s):  
Rade Injac ◽  
Aleksandar Djordjevic ◽  
Borut Strukelj
Keyword(s):  
Untreated Control ◽  
Malignant Neoplasm ◽  
In Vivo Studies ◽  
Control Group ◽  
High Dose ◽  
Sprague Dawley ◽  
Untreated Control Group ◽  
Cardiac Damage

The therapeutic utility of the anthracycline antibiotic doxorubicin is limited due to its cardiotoxicity. Our aim was to investigate the efficacy of fullerenol C60(OH)24 in preventing single, high-dose doxorubicin-induced cardiotoxicity in rats with malignant neoplasm. In vitro and in vivo studies have shown that fullerenol C60(OH)24, has strong antioxidative potential. Experiment was performed on adult female Sprague Dawley rats with chemically induced mammary carcinomas. All 32 rats (2-5 groups) received i.p. applications of 1-methyl-l-nitrosourea (MNU; 50 mg/kg body weight) on the 50th and 113th day of age. Animals were randomly divided into five groups as follows: (1) Untreated control group - rats received saline only; (2) Cancer control group - rats received MNU and saline; (3) Dox group - rats received MNU and Dox 8 mg/kg; (4) Full/Dox group -rats received MNU and Full 100 mg/kg 30 min before Dox 8 mg/kg; (5) Full group - rats received MNU and Full 100 mg/kg. Tumor incidence was 4.94 +- 0.576 per rat. The animals were sacrificed 2 days after the application of doxorubicin and/or fullerenol, and the serum activities of CK, LDH and ?-HBDH, as well as the levels of MDA, GSH, GSSG, GSH-Px, SOD, CAT, GR and TAS in the heart, were determined. The results obtained from the enzymatic activity in the serum show that the administration of a single dose of 8 mg/kg in all treated groups induces statistically significant damage. There are significant changes in the enzymes of LDH and CK (p < 0.05), after an i.p. administration of doxorubicin/fullerenol and fullerenol. Comparing all groups with untreated control group, point to the conclusion that in the case of a lower oc-HBDH/LDH ratio, results in more serious the liver parenchymal damage. The results revealed that doxorubicin induced oxidative damage and that the fullerenol antioxidative influence caused significant changes in MDA, GSH, GSSG, GSH-Px, SOD, CAT, GR and TAS level in the heart (p < 0.05). Ultra structural analysis of heart tissues from rats treated with doxorubicin and indicated that the hearts of the rats were protected from doxorubicin-induced subcellular damage. Doxorubicin/fullerenol rats did not appear to show significant cardiac damage although occasional focal loss of cristae in the mitochondria was observed. Therefore, it is suggested that fullerenol might be a potential cardioprotector in doxorubicin-treated individuals.

scholarly journals In vitro evaluation of antimicrobial activity of 1-lauroyl-rac-glycerol on Candidaalbicans biofilms

2016 ◽  
Author(s):  
Emily Chen ◽  
Dalia Seleem ◽  
Bruna Benso ◽  
Vanessa Pardi ◽  
Ramiro M Murata
Keyword(s):  
Antifungal Activity ◽  
Biological Activities ◽  
Oral Candidiasis ◽  
Coconut Oil ◽  
Positive Control ◽  
Control Group ◽  
Vehicle Control Group ◽  
Culture Models ◽  
Candida Albicans Biofilms

Monolaurin (also known as glycerol monolaurate) is a natural compound found in coconut oil and is known for its protective biological activities as an antimicrobial agent. The nature of oral candidiasis and the increased antifungal resistance, culminate the need for investigating novel antifungal therapeutic agents. In this study, we examine the antifungal activity of monolaurin against Candida albicans biofilms (strain ATCC: SC5314/MYA2876) in vitro and how monolaurin may alter specific host inflammatory markers, such as gene expression of inflammatory cytokines IL-1α and IL-1β, as illustrated in co-culture models. The results from three groups were compared: 1- monolaurin (in the range of 3.9-2500 μM), positive control fluconazole (322 μM), and vehicle control group 1% Ethanol (v/v) The MIC and MFC of monolaurin were in the range 62.5-125 µM and 125-250 µM, respectively. The results show significant reduction in Log (CFU/ ml) of biofilms treated with 1250 and 2500 µM of 1- monolaurin when compared to the control groups. There was also a significant down-regulation of IL-1α and IL-1β in the biofilms treated with monolaurin. It can be concluded that monolaurin has a potential antifungal activity against C. albicans and can modulate the host’s pro-inflammatory response.

scholarly journals In vitro evaluation of antimicrobial activity of 1-lauroyl-rac-glycerol on Candidaalbicans biofilms

2016 ◽  
Author(s):  
Emily Chen ◽  
Dalia Seleem ◽  
Bruna Benso ◽  
Vanessa Pardi ◽  
Ramiro M Murata
Keyword(s):  
Antifungal Activity ◽  
Biological Activities ◽  
Oral Candidiasis ◽  
Coconut Oil ◽  
Positive Control ◽  
Control Group ◽  
Vehicle Control Group ◽  
Culture Models ◽  
Candida Albicans Biofilms

Monolaurin (also known as glycerol monolaurate) is a natural compound found in coconut oil and is known for its protective biological activities as an antimicrobial agent. The nature of oral candidiasis and the increased antifungal resistance, culminate the need for investigating novel antifungal therapeutic agents. In this study, we examine the antifungal activity of monolaurin against Candida albicans biofilms (strain ATCC: SC5314/MYA2876) in vitro and how monolaurin may alter specific host inflammatory markers, such as gene expression of inflammatory cytokines IL-1α and IL-1β, as illustrated in co-culture models. The results from three groups were compared: 1- monolaurin (in the range of 3.9-2500 μM), positive control fluconazole (322 μM), and vehicle control group 1% Ethanol (v/v) The MIC and MFC of monolaurin were in the range 62.5-125 µM and 125-250 µM, respectively. The results show significant reduction in Log (CFU/ ml) of biofilms treated with 1250 and 2500 µM of 1- monolaurin when compared to the control groups. There was also a significant down-regulation of IL-1α and IL-1β in the biofilms treated with monolaurin. It can be concluded that monolaurin has a potential antifungal activity against C. albicans and can modulate the host’s pro-inflammatory response.

scholarly journals In vitroevaluation of antifungal activity of monolaurin againstCandida albicansbiofilms

PeerJ ◽  
2016 ◽  
Vol 4 ◽  
pp. e2148 ◽  
Author(s):  
Dalia Seleem ◽  
Emily Chen ◽  
Bruna Benso ◽  
Vanessa Pardi ◽  
Ramiro M. Murata
Keyword(s):  
Gene Expression ◽  
Antifungal Activity ◽  
Inflammatory Cytokines ◽  
Biological Activities ◽  
Oral Candidiasis ◽  
Rna Extraction ◽  
Morphological Characteristics ◽  
Control Group ◽  
Culture Model

Monolaurin (also known as glycerol monolaurate) is a natural compound found in coconut oil and is known for its protective biological activities as an antimicrobial agent. The nature of oral candidiasis and the increased antifungal resistance demand the search for novel antifungal therapeutic agents. In this study, we examine the antifungal activity of monolaurin againstCandida albicansbiofilms (strain ATCC:SC5314/MYA2876)in vitroand investigate whether monolaurin can alter gene expression of host inflammatory cytokines, IL-1αand IL-1β. In a co-culture model, oral fibroblast cells were cultured simultaneously withC. albicansfor 24 hrs followed by the exposure to treatments of monolaurin (3.9–2,500 µM), positive control fluconazole (32.2 µM), and vehicle control group (1% ethanol), which was a model used to evaluate the cytotoxicity of monolaurin on fibroblasts as well as to analyze morphological characteristics of biofilms through fluorescence microscopy. In addition, the co-culture model was used for RNA extraction of oral fibroblasts to assess gene expression of host inflammatory cytokines, using quantitative real-time PCR. Our results showed the MIC and MFC of monolaurin were in the range 62.5–125 µM and 125–250 µM, respectively. Biofilm antifungal assay showed significant reduction in Log (CFU/ml) of biofilms treated with 1,250 and 2,500 µM of 1-monolaurin when compared to the control groups . There was also a significant down-regulation of IL-1αand IL-1βin the co-culture treated with monolaurin. It can be concluded that monolaurin has a potential antifungal activity againstC. albicansand can modulate the pro-inflammatory response of the host.

scholarly journals Orodispersible Film Loaded with Enterococcus faecium CRL183 Presents Anti-Candida albicans Biofilm Activity In Vitro

Pharmaceutics ◽  
2021 ◽  
Vol 13 (7) ◽  
pp. 998
Author(s):  
Virgínia Barreto Lordello ◽  
Andréia Bagliotti Meneguin ◽  
Sarah Raquel de Annunzio ◽  
Maria Pía Taranto ◽  
Marlus Chorilli ◽  
...  
Keyword(s):  
Candida Albicans ◽  
Antifungal Activity ◽  
Enterococcus Faecium ◽  
Potato Starch ◽  
Oral Candidiasis ◽  
Candida Spp ◽  
Sem Images ◽  
Control Film ◽  
In Vitro Antifungal Activity

Background: Probiotic bacteria have been emerging as a trustworthy choice for the prevention and treatment of Candida spp. infections. This study aimed to develop and characterize an orodispersible film (ODF) for delivering the potentially probiotic Enterococcus faecium CRL 183 into the oral cavity, evaluating its in vitro antifungal activity against Candida albicans. Methods and Results: The ODF was composed by carboxymethylcellulose, gelatin, and potato starch, and its physical, chemical, and mechanical properties were studied. The probiotic resistance and viability during processing and storage were evaluated as well as its in vitro antifungal activity against C. albicans. The ODFs were thin, resistant, and flexible, with neutral pH and microbiologically safe. The probiotic resisted the ODF obtaining process, demonstrating high viability (>9 log10 CFU·g−1), up to 90 days of storage at room temperature. The Probiotic Film promoted 68.9% of reduction in fungal early biofilm and 91.2% in its mature biofilm compared to the group stimulated with the control film. Those results were confirmed through SEM images. Conclusion: The probiotic ODF developed is a promising strategy to prevent oral candidiasis, since it permits the local probiotic delivery, which in turn was able to reduce C. albicans biofilm formation.

Caffeic acid phenethyl ester attenuates allergic airway inflammation and hyperresponsiveness in murine model of ovalbumin-induced asthma

Life Sciences ◽  
2008 ◽  
Vol 82 (13-14) ◽  
pp. 797-805 ◽  
Author(s):  
Won-Kyo Jung ◽  
Da-Young Lee ◽  
Yung Hyun Choi ◽  
Sung Su Yea ◽  
Inhak Choi ◽  
...  
Keyword(s):  
Airway Inflammation ◽  
Caffeic Acid ◽  
Murine Model ◽  
Allergic Airway Inflammation ◽  
Caffeic Acid Phenethyl Ester

Effect of caffeic acid phenethyl ester on gastric acid secretion in vitro

2005 ◽  
Vol 521 (1-3) ◽  
pp. 139-143 ◽  
Author(s):  
Francesca Borrelli ◽  
Inmaculada Posadas ◽  
Raffaele Capasso ◽  
Gabriella Aviello ◽  
Valeria Ascione ◽  
...  
Keyword(s):  
Acid Secretion ◽  
Gastric Acid Secretion ◽  
Gastric Acid ◽  
Caffeic Acid ◽  
Caffeic Acid Phenethyl Ester

Evaluation of anti-allergic properties of caffeic acid phenethyl ester in a murine model of systemic anaphylaxis

2008 ◽  
Vol 226 (1) ◽  
pp. 22-29 ◽  
Author(s):  
Sae-Gwang Park ◽  
Da-Young Lee ◽  
Su-Kil Seo ◽  
Soo-Woong Lee ◽  
Se-Kwon Kim ◽  
...  
Keyword(s):  
Caffeic Acid ◽  
Murine Model ◽  
Caffeic Acid Phenethyl Ester ◽  
Systemic Anaphylaxis

Formulation development of folic acid conjugated PLGA nanoparticles for improved cytotoxicity of Caffeic acid phenethyl ester

2021 ◽  
Vol 09 ◽  
Author(s):  
Harshad S Kapare ◽  
Sathiyanarayanan L ◽  
Arulmozhi S ◽  
Kakasaheb Mahadik
Keyword(s):  
Folic Acid ◽  
Drug Release ◽  
Caffeic Acid ◽  
Caffeic Acid Phenethyl Ester ◽  
Therapeutic Effects ◽  
Formulation Development ◽  
Sustained Drug Release ◽  
Active Constituent

Background: Honey bee propolis is one of the natural product reported in various traditional systems of medicines including Ayurveda. Caffeic acid phenethyl ester (CAPE) is an active constituent of propolis which is well known for its anticancer potential. The therapeutic effects of CAPE are restricted owing to its less aqueous solubility and low bioavailability. Objective: In this study CAPE loaded folic acid conjugated nanoparticle system (CLFPN) was investigated to enhance solubility, achieve sustained drug release and improved cytotoxicity of CAPE. Methods: Formulation development, characterization and optimization were carried out by design of experiment approach. In vitro and in vivo cytotoxicity study was carried out for optimized formulations. Results: Developed nanoparticles showed particle size and encapsulation efficiency of 170 ± 2 - 195 ± 3 nm and 75.66 ± 1.52 - 78.80 ± 1.25 % respectively. Optimized formulation CLFPN showed sustained drug release over a period of 42 h. GI50 concentration was decreased by 46.09% for formulation as compared to CAPE in MCF-7 cells indicating targeting effect of CLFPN. An improved in vitro cytotoxic effect was reflected in in-vivo Daltons Ascites Lymphoma model by reducing tumor cells count. Conclusion: The desired nanoparticle characteristic with improved in vivo and in vitro cytotoxicity was shown by developed formulation. Thus it can be further investigated for biomedical applications.

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