Aim: To investigate the action mechanism of a novel chemical structural aminotetralin derivate, 2-Amino-Nonyl-6-Methoxyl-Tetralin Muriate (10b), against Candida albicans (C albicans) in the ergosterol biosynthetic pathway.
Methods: Antifungal susceptibility test of 10b was carried out using broth microdilution method, the action mechanism of 10b against C albicans was investigated by GC-MS spectrometry and real-time RT-PCR assay, and cytotoxicity of 10b in vitro was assessed by MTS/PMS reduction assay.
Results: 10b reduced the ergosterol content markedly, and the 50% ergosterol content inhibitory concentration (ECIC(50) value) was 0.08 microg/mL. Although the sterol composition of 10b-grown cells was completely identical with that of erg24 strain, the content of ergosta-8,14,22-trienol in 10b-grown cells was much higher than that in erg24 strain. Real-time RT-PCR assay revealed a global upregulation of sterol metabolism genes. In addition, the 50% inhibitory concentration (IC(50) value) of 10b was 11.30 microg/mL for murine embryonic fibroblasts and 35.70 microg/mL for human normal liver cells.
Conclusion: 10b possessed a mode of action different from that of azoles and morpholines, whose targets were sterol C-14 reductase (encoded by ERG24 gene) and sterol C-5 desaturase (encoded by ERG3) related enzyme. Although 10b seemed to reduce MTS/PMS reduction in a dose dependent manner, IC(50) value for mammalian cells was much higher than 50% minimum inhibitory concentration (MIC(50)) value for C albicans. This indicates that the formulation is preliminarily safe and warrants further study for possible human applications.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4007502 | PMC |
| http://dx.doi.org/10.1038/aps.2009.157 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Antifungal Susceptibility of Dermatophyte Isolates from Patients with Chronic and Recurrent Dermatophytosis.
Indian Dermatol Online J
December 2024
Department of Microbiology, Yenepoya Medical College, (Deemed to be University), Mangalore, Karnataka, India.
Background: The widespread occurrence of chronic and recurrent dermatophytosis has significantly affected the quality of life for patients in India and beyond. Identifying the causative dermatophytes and understanding their antifungal susceptibility can aid clinicians in tailoring effective antifungal therapies.
Materials And Methods: Patients with chronic and recurrent dermatophytosis were enrolled, and conventional fungal cultures were conducted on skin scrapings.
Exploring the ROS-mediated anti-cancer potential in human triple-negative breast cancer by garlic bulb extract: A source of therapeutically active compounds.
J Tradit Complement Med
November 2024
Department of Biotechnology, Era's Lucknow Medical College and Hospital, Era University, Lucknow, 226003, India.
Background And Aim: L. has been used medicinally and traditionally since antiquity. This study sought to examine the ethanolic extract (ASEE) in inducing apoptosis in human triple-negative breast cancer (TNBC) MDA-MB-231 cells and the molecular interactions of the identified components with cell death markers using method.
View Article and Find Full Text PDFComparative study on organoleptic properties and volatile organic compounds in turmeric, turmeric essential oil, and by-products using E-nose, HS-GC-IMS, and HS-GC-MS.
Food Chem X
January 2025
Collage of Food Science and Technology, Hebei Agricultural University, Baoding, China.
The properties, applications, and in vitro bioactivities of turmeric, turmeric essential oil (TEO), and turmeric essential oil by-products (TEO-BP) were evaluated using sensory analysis, gas chromatography-mass spectrometry (GC-MS), gas chromatography-ion mobility spectrometry (GC-IMS), and electronic nose techniques. A total of 62 and 66 volatile organic compounds (VOCs), primarily terpenoids and sesquiterpenoids, were identified by GC-MS and GC-IMS, respectively. Distillation temperature, particularly at 90 °C, significantly influenced the color and organoleptic properties of TEO, with variations in VOC profiles driving these differences.
View Article and Find Full Text PDFChanges in functional activities and volatile flavor compounds of fermented mung beans, cowpeas, and quinoa started with Bacillus amyloliquefaciens SY07.
Food Res Int
February 2025
State Key Laboratory of Food Nutrition and Safety, College of Food Science and Engineering, Tianjin University of Science and Technology, Tianjin 300457 PR China. Electronic address:
In this work, the functional activities including α-glucosidase, α-amylase, angiotensin converting enzyme (ACE) inhibitory activity, and antioxidant activity of mixed grains (mung beans, cowpeas, and quinoa) fermented with Bacillus amyloliquefaciens SY07 were investigated. The volatile flavor of the mixed grains collected every 12 h during 72 h-fermentation were further detected as well. The inhibition on α-glucosidase and α-amylase reached up to 89.
View Article and Find Full Text PDFThe processing of shaking and standing improves the taste quality of summer black tea.
Food Res Int
February 2025
State Key Laboratory of Tea Plant Biology and Utilization, Anhui Agricultural University, China; Key Laboratory of Tea Biology and Tea Processing of Ministry of Agriculture and Rural Affairs, Anhui Agricultural University, China; International Joint Research Laboratory of Tea Chemistry and Health Effects of Ministry of Education, Anhui Agricultural University, China. Electronic address:
Shaking and standing (SS) enhances the aroma intensity and quality of black tea (BT). However, its contribution to the taste remains unknown, and the interaction mechanism between the aroma and taste perception of black tea is also undisclosed. Here, the metabolomics and sensory evaluation-assisted flavor analysis were employed to investigate the changes in non-volatiles induced by SS, and the interaction mechanism between aroma and taste perception.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!