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Bioactive sesquiterpenes from Inula helenium
- Source :
- Bioorganic Chemistry. 114:105066
- Publication Year :
- 2021
- Publisher :
- Elsevier BV, 2021.
-
Abstract
- Twenty-one eudesmane-type sesquiterpenes, including five new compounds, were isolated from the roots of Inula helenium. The structures of the new compounds (1–5) were determined by extensive spectroscopic data interpretation, single-crystal X-ray diffraction analysis and ECD calculations. Six compounds can synergistically enhance cisplatin effect against ovarian cancer cells, the structure − activity relationship for the synergistic effect of these compounds with cisplatin was revealed for the first time, which provides useful clues to develop novel sensitizers to overcome drug resistance in cancer. In addition, fifteen sesquiterpenes exhibited significant anti-inflammatory activity, which provided promising candidates for development of anti-inflammatory agent.
- Subjects :
- Lipopolysaccharides
Cell Survival
medicine.drug_class
Chemosensitizer
Drug resistance
Pharmacology
Nitric Oxide
Sesquiterpene
01 natural sciences
Biochemistry
Anti-inflammatory
Mice
Structure-Activity Relationship
chemistry.chemical_compound
Drug Discovery
medicine
Animals
Humans
Molecular Biology
Cells, Cultured
Cell Proliferation
Cisplatin
Inula
Dose-Response Relationship, Drug
Molecular Structure
biology
010405 organic chemistry
Chemistry
Organic Chemistry
Cancer
medicine.disease
biology.organism_classification
Antineoplastic Agents, Phytogenic
0104 chemical sciences
Molecular Docking Simulation
010404 medicinal & biomolecular chemistry
RAW 264.7 Cells
Drug Screening Assays, Antitumor
Sesquiterpenes
Helenium
medicine.drug
Subjects
Details
- ISSN :
- 00452068
- Volume :
- 114
- Database :
- OpenAIRE
- Journal :
- Bioorganic Chemistry
- Accession number :
- edsair.doi.dedup.....9a9deb07d52e2437f621f8fbd7bdad33
- Full Text :
- https://doi.org/10.1016/j.bioorg.2021.105066