Back to Search
Start Over
Fluorescence-Based High Throughput Screening Technologies for Natural Chloride Ion Channel Blockers
- Source :
- Chemical Research in Toxicology. 31:1332-1338
- Publication Year :
- 2018
- Publisher :
- American Chemical Society (ACS), 2018.
-
Abstract
- Chloride channels represent a group of potential drug targets; their blockers showed significant protecting effect on impaired cells by modulating apoptosis, autophagy, and other cell signals. However, clinical drugs with chloride channel inhibitory properties have not yet been developed. Natural product extract becomes an underlying candidate satisfied the clinical requirements for its low toxicity, low cost, and abundant sources. Here, a fluorescence-based EYFP-H148Q/I153L-HeLa cell line model was constructed by molecular cloning and verified by real-time polymerase chain reaction and Western blotting assay. By using this chloride channel blocker screening model, seven hit compounds chosen from 6988 natural compounds showed the channel blocking activity. Then the hit compounds were further validated by electrophysiological patch-clamp analysis. Our study preliminarily identified PC-4 as a new chloride channel inhibitor and demonstrated the reliability and sensitivity of fluorescence-based high throughput screening technologies for discovery of biologically active compounds from natural herbal compounds.
- Subjects :
- 0301 basic medicine
Patch-Clamp Techniques
Recombinant Fusion Proteins
High-throughput screening
Green Fluorescent Proteins
Action Potentials
Toxicology
Chloride
Small Molecule Libraries
03 medical and health sciences
chemistry.chemical_compound
0302 clinical medicine
Chloride Channels
High-Throughput Screening Assays
medicine
Humans
Ion channel
Natural product
Biological activity
General Medicine
Chloride channel blocker
030104 developmental biology
chemistry
Biochemistry
Mutagenesis, Site-Directed
Chloride channel
030217 neurology & neurosurgery
HeLa Cells
medicine.drug
Subjects
Details
- ISSN :
- 15205010 and 0893228X
- Volume :
- 31
- Database :
- OpenAIRE
- Journal :
- Chemical Research in Toxicology
- Accession number :
- edsair.doi.dedup.....cab07985c5289636cf8cb307ffe7d8b5