scholarly journals Antifungal Activity of the Phenolic Compounds Ellagic Acid (EA) and Caffeic Acid Phenethyl Ester (CAPE) against Drug-Resistant Candida auris

2021 ◽  
Vol 7 (9) ◽  
pp. 763
Author(s):  
Fernanda Cristina Possamai Rossatto ◽  
Nagendran Tharmalingam ◽  
Iliana E. Escobar ◽  
Pedro Alves d’Azevedo ◽  
Karine Rigon Zimmer ◽  
...  
Keyword(s):  
Caffeic Acid ◽  
Ellagic Acid ◽  
Galleria Mellonella ◽  
Treatment Options ◽  
Caffeic Acid Phenethyl Ester ◽  
Biological Properties ◽  
Current Treatment ◽  
Drug Resistant ◽  
Candida Auris ◽  
Fungal Cell

Candida auris is an emerging healthcare-associated fungal pathogen that has become a serious global health threat. Current treatment options are limited due to drug resistance. New therapeutic strategies are required to target this organism and its pathogenicity. Plant polyphenols are structurally diverse compounds that present a vast range of biological properties. In the present study, plant-derived molecules ellagic acid (EA) and caffeic acid phenethyl ester (CAPE) were investigated for their antifungal and antivirulence activities against Candida auris. We also tested against C. albicans. The minimum inhibitory concentration (MIC) for EA ranged from 0.125 to 0.25 µg/mL and for CAPE ranged from 1 to 64 µg/mL against drug-resistant C. auris strains. Killing kinetics determined that after 4 h treatment with CAPE, there was a complete reduction of viable C. auris cells compared to fluconazole. Both compounds might act by modifying the fungal cell wall. CAPE significantly reduced the biomass and the metabolic activity of C. auris biofilm and impaired C. auris adhesion to cultured human epithelial cells. Furthermore, both compounds prolonged the survival rate of Galleria mellonella infected by C. auris (p = 0.0088 for EA at 32 mg/kg and p = 0.0028 for CAPE at 4 mg/kg). In addition, EA at 4 μg/mL prolonged the survival of C. albicans-infected Caenorhabditis elegans (p < 0.0001). CAPE was not able to prolong the survival of C. albicans-infected C. elegans. These findings highlight the antifungal and antivirulence effects of EA and CAPE against C. auris, and warrant further investigation as novel antifungal agents against drug-resistant infections.

scholarly journals Identification of Antifungal Compounds against Multidrug Resistant Candida auris Utilizing a High Throughput Drug Repurposing Screen

2021 ◽  
Author(s):  
Yu-Shan Cheng ◽  
Jose Santinni Roma ◽  
Min Shen ◽  
Caroline Mota Fernandes ◽  
Patricia S. Tsang ◽  
...  
Keyword(s):  
High Throughput ◽  
High Throughput Screening ◽  
Treatment Options ◽  
Drug Repurposing ◽  
Multidrug Resistant ◽  
Current Treatment ◽  
Drug Combinations ◽  
Serine Palmitoyltransferase ◽  
Candida Auris ◽  
Pharmacologically Active

Candida auris is an emerging fatal fungal infection that has resulted in several outbreaks in hospitals and care facilities. Current treatment options are limited by the development of drug resistance. Identifying new pharmaceuticals to combat these drug-resistant infections will thus be required to overcome this unmet medical need. We have established a bioluminescent ATP-based assay to identify new compounds and potential drug combinations showing effective growth inhibition against multiple strains of multidrug resistant Candida auris. The assay is robust and suitable for assessing large compound collections by high throughput screening. Utilizing this assay, we conducted a screen of 4,314 approved drugs and pharmacologically active compounds which yielded 25 compounds including 6 novel anti-Candida auris compounds and 13 sets of potential two drug combinations. Among the drug combinations, the serine palmitoyltransferase inhibitor myriocin demonstrated a combinational effect with flucytosine against all tested isolates during screening. This combinational effect was confirmed in 13 clinical isolates of Candida auris.

scholarly journals Caffeic Acid Phenethyl Ester (CAPE) Induced Apoptosis in Serous Ovarian Cancer OV7 Cells by Deregulation of BCL2/BAX Genes

Molecules ◽  
2020 ◽  
Vol 25 (15) ◽  
pp. 3514 ◽  
Author(s):  
Anna Kleczka ◽  
Robert Kubina ◽  
Radosław Dzik ◽  
Krzysztof Jasik ◽  
Jerzy Stojko ◽  
...  
Keyword(s):  
Ovarian Cancer ◽  
Caffeic Acid ◽  
Caffeic Acid Phenethyl Ester ◽  
Biological Properties ◽  
New Drugs ◽  
Pcr Analysis ◽  
Ovarian Cancer Cells ◽  
Cell Nuclei ◽  
Anticancer Properties ◽  
Induced Apoptosis

Ovarian cancer has the worst prognosis among all gynecological cancers. Therefore, it seems reasonable to seek new drugs that may improve the effectiveness of treatment or mitigate the adverse effects of chemotherapy. Caffeic acid phenethyl ester (CAPE) has many beneficial biological properties. The aim of the study was to assess the anticancer properties of CAPE against serum ovarian carcinoma cells. The morphology of the cells was evaluated in H-E staining and in transmission electron microscopy. The cytotoxic and proapoptotic activity of CAPE was investigated by using the XTT-NR-SRB assay, qRT-PCR analysis of BAX/BCL2 expression, and by cytometric evaluation. CAPE causes constriction in OV7 cells, numerous granulomas were observed in the cytoplasm, the cell nuclei were pyknotic. Autophagosomal vacuoles could suggest the occurrence of aponecrosis. CAPE significantly decreased the lysosomal activity and the total synthesis of cellular proteins. CAPE exhibited, dose and time dependent, cytotoxic activity against OV7 serum ovarian cancer cells. In OV7 cells CAPE induced apoptosis via dysregulation of BAX/BCL2 balance, while activated proapoptotic BAX gene expression level was 10 times higher than BCL2.

scholarly journals Antimicrobial and Antibiofilm Activity against Streptococcus mutans of Individual and Mixtures of the Main Polyphenolic Compounds Found in Chilean Propolis

2019 ◽  
Vol 2019 ◽  
pp. 1-7 ◽  
Author(s):  
Jorge Jesús Veloz ◽  
Marysol Alvear ◽  
Luis A. Salazar
Keyword(s):  
Caffeic Acid ◽  
Streptococcus Mutans ◽  
Caffeic Acid Phenethyl Ester ◽  
Biological Properties ◽  
Tooth Surface ◽  
Dilution Method ◽  
Antibiofilm Activity ◽  
Biofilm Thickness ◽  
Low Concentrations ◽  
Important Health

Dental caries is multifactorial disease and an important health problem worldwide. Streptococcus mutans is considered as a major cariogenic agent in oral cavity. This bacteria can synthetize soluble and insoluble glucans from sucrose by glucosyltransferases enzymes and generate stable biofilm on the tooth surface. Biological properties of Chilean propolis have been described and it includes antimicrobial, antifungal, and antibiofilm activities. The main goal of this study was to quantify the concentrations of main flavonoids presents in Chilean propolis and compare some biological properties such as antimicrobial and antibiofilm activity of individual compounds and the mixture of this compounds, against S. mutans cultures. Chilean propolis was studied and some polyphenols present in this extract were quantified by HPLC-DAD using commercial standards of apigenin, quercetin, pinocembrin, and caffeic acid phenethyl ester (CAPE). MIC for antimicrobial activity was determined by serial dilution method and biofilm thickness on S. mutans was quantified by confocal microscopy. Pinocembrin, apigenin, quercetin, and caffeic acid phenethyl ester (CAPE) are the most abundant compounds in Chilean propolis. These polyphenols have strong antimicrobial and antibiofilm potential at low concentrations. However, pinocembrin and apigenin have a greater contribution to this action. The effect of polyphenols on S. mutans is produced by a combination of mechanisms to decrease bacterial growth and affect biofilm proliferation due to changes in their architecture.

scholarly journals The Future Perspectives of Drug Repurposing and Treatment for the Drug Resistant Breast Cancer: A Review

2021 ◽  
Author(s):  
Panneerselvam Theivendren ◽  
Selvaraj Kunjiappan ◽  
Yashoda Mariappa Hegde ◽  
Kaveena Ravi ◽  
Sivakumar Vellaichamy ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Treatment Options ◽  
Survival Rates ◽  
Drug Repurposing ◽  
Current Treatment ◽  
New Drugs ◽  
Health Concern ◽  
Drug Resistant ◽  
The Future ◽  
New Treatment

Breast cancer is a major health concern as it is the second leading cause of death from cancer. There are several well-known risk factors that contribute to breast cancer. Despite the various treatment options available, complete cure is still difficult due to heterogenicity of BC subtypes. As a result, identifying BC subtypes is critical for determining the optimal treatment approach. Over the last several years, new drugs targeting particular therapeutic targets have resulted in significant advances in the treatment of breast cancer. Nonetheless, resistance to treatment is the “major” issue, and a significant increase in survival rates has been the main focus for researchers. The purpose of this review article is to provide a broad overview of the molecular basis of drug resistance in breast cancer, as well as a detailed assessment of current treatment options, potential new treatment methods for drug-resistant breast cancer and repurposed drugs used for treatment. The possibility of non-cancer drugs being studied for breast cancer in the future, as well as the obstacles and bottlenecks of drug repurposing, is also highlighted. Finally, we go through present problems and future prospects in drug-resistant breast cancer therapy.

scholarly journals The Pluripotent Activities of Caffeic Acid Phenethyl Ester

Molecules ◽  
2021 ◽  
Vol 26 (5) ◽  
pp. 1335
Author(s):  
Batoryna Olgierd ◽  
Żyła Kamila ◽  
Banyś Anna ◽  
Morawiec Emilia
Keyword(s):  
Wound Healing ◽  
Caffeic Acid ◽  
Honey Bee ◽  
Broad Spectrum ◽  
Caffeic Acid Phenethyl Ester ◽  
Biological Properties ◽  
Published Data ◽  
Compound A ◽  
Inflammatory Agent ◽  
Anti Cancer

Caffeic acid phenethyl ester (CAPE) is a strong antioxidant extracted from honey bee-hive propolis. The mentioned compound, a well-known NF-κB inhibitor, has been used in traditional medicine as a potent anti-inflammatory agent. CAPE has a broad spectrum of biological properties including anti-viral, anti-bacterial, anti-cancer, immunomodulatory, and wound-healing activities. This review characterizes published data about CAPE biological properties and potential therapeutic applications, that can be used in various diseases.

An Overview of Dementias

2012 ◽  
Vol 21 (3) ◽  
pp. 75-84
Author(s):  
Venkata Vijaya K. Dalai ◽  
Jason E. Childress ◽  
Paul E Schulz
Keyword(s):  
Clinical Presentation ◽  
Treatment Options ◽  
Current Treatment ◽  
Great Variability ◽  
Health Concern ◽  
Public Health Concern ◽  
Life Threatening ◽  
The Common ◽  
Neurodegenerative Dementias ◽  
Made In

Dementia is a major public health concern that afflicts an estimated 24.3 million people worldwide. Great strides are being made in order to better diagnose, prevent, and treat these disorders. Dementia is associated with multiple complications, some of which can be life-threatening, such as dysphagia. There is great variability between dementias in terms of when dysphagia and other swallowing disorders occur. In order to prepare the reader for the other articles in this publication discussing swallowing issues in depth, the authors of this article will provide a brief overview of the prevalence, risk factors, pathogenesis, clinical presentation, diagnosis, current treatment options, and implications for eating for the common forms of neurodegenerative dementias.

Initiation of Clozapine Therapy in a Patient With Preexisting Leukopenia: A Discussion of the Rationale of Current Treatment Options

2001 ◽  
Vol 13 (4) ◽  
pp. 233-237 ◽  
Author(s):  
Roger Boshes ◽  
Theo Manschreck ◽  
Jean Desrosiers ◽  
Steven Candela ◽  
Meredith Hanrahan-Boshes
Keyword(s):  
Treatment Options ◽  
Current Treatment ◽  
Clozapine Therapy
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