Bioactive sesquiterpenes from Inula helenium
| Autor: | Zi Wu, Haitao Cheng, Xiao-Qin Zheng, Jie Xu, Ruiying Yuan, Qiang Wang, Jiachuan Lei, Jianqing Yu, Yijun Tu, Xin-Xin Zhang |
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| Rok vydání: | 2021 |
| Předmět: |
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 |
| Zdroj: | Bioorganic Chemistry. 114:105066 |
| ISSN: | 0045-2068 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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