Molecules (Basel, Switzerland), 2021-07, Vol.26 (15), p.4644
2021
Details
- Autor(en) / Beteiligte
- Titel
- Germacranolides from Carpesium divaricatum : Some New Data on Cytotoxic and Anti-Inflammatory Activity
- Ist Teil von
- Molecules (Basel, Switzerland), 2021-07, Vol.26 (15), p.4644
- Ort / Verlag
- Switzerland: MDPI AG
- Erscheinungsjahr
- 2021
- Link zum Volltext
- Quelle
- EZB Electronic Journals Library
- Beschreibungen/Notizen
- Sieb. & Zucc., a traditional medicinal plant used as an inflammation-relieving remedy, is a rich source of terpenoids. At least 40 germacrane-type sesquiterpene lactones, representatives of four different structural groups, were isolated from the plant. Cytotoxicity against cancer cells in vitro is the most frequently described biological activity of the compounds. However, little is known about the selectivity of the cytotoxic effect. The anti-inflammatory activity of the germacranolides is also poorly documented. The objective of the present study was to assess the cytotoxic activity of selected germacranolides-derivatives of 4,5,8,9-tetrahydroxy-3-oxo-germacran-6,12-olide towards cancer and normal cell lines (including cells of different p53 status). Moreover, to assess the anti-inflammatory effect of the compounds, the release of four proinflammatory cytokines/chemokines (IL-1β, IL-8, TNF-α and CCL2) by lipopolysaccharide-stimulated human neutrophils was measured by ELISA. The investigated sesquiterpene lactones demonstrated nonselective activity towards prostate cancer (Du145 and PC3) and normal prostate epithelial cells (PNT2) as well as against melanoma cells (A375 and HTB140) and keratinocytes (HaCaT). Cytotoxic activity against osteosarcoma cells was independent of their p53 status. In sub-cytotoxic concentrations (0.5-2.5 µM) the studied compounds significantly decreased cytokine/chemokine release by lipopolysaccharide-stimulated human leukocytes.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 1420-3049eISSN: 1420-3049DOI: 10.3390/molecules26154644Titel-ID: cdi_doaj_primary_oai_doaj_org_article_ca788f45fb764e82a7b67378ba8894f5
- Format
- –
- Schlagworte
- anti-inflammatory, Anti-inflammatory agents, Anti-Inflammatory Agents - chemistry, Anti-Inflammatory Agents - classification, Anti-Inflammatory Agents - isolation & purification, Anti-Inflammatory Agents - pharmacology, Antineoplastic Agents, Phytogenic - chemistry, Antineoplastic Agents, Phytogenic - classification, Antineoplastic Agents, Phytogenic - isolation & purification, Antineoplastic Agents, Phytogenic - pharmacology, Apoptosis, Asteraceae - chemistry, Asteraceae - metabolism, Biological activity, Biomedical materials, Bone cancer, Carpesium, Cell Line, Cell Line, Tumor, Cell Survival - drug effects, Chemokine CCL2 - genetics, Chemokine CCL2 - immunology, Chemokines, Colorectal cancer, Cytokines, Cytotoxicity, Cytotoxins - chemistry, Cytotoxins - classification, Cytotoxins - isolation & purification, Cytotoxins - pharmacology, Doxorubicin - pharmacology, Drug dosages, Epithelial cells, Epithelium, Gene Expression Regulation, Neoplastic, germacranolides, Herbal medicine, Humans, IL-1β, Inflammation, Inhibitory Concentration 50, Interleukin 8, Interleukin-1beta - genetics, Interleukin-1beta - immunology, Interleukin-8 - genetics, Interleukin-8 - immunology, Inuleae, Investigations, Keratinocytes, Lactones, Leukocytes, Leukocytes (neutrophilic), Lipopolysaccharides, Lipopolysaccharides - antagonists & inhibitors, Lipopolysaccharides - pharmacology, Medicinal plants, Melanoma, Monocyte chemoattractant protein 1, Neutrophils, Neutrophils - cytology, Neutrophils - drug effects, Neutrophils - immunology, Osteosarcoma, Osteosarcoma cells, Plant Components, Aerial - chemistry, Plant Components, Aerial - metabolism, Plant Extracts - chemistry, Plants, Medicinal, Poland, Primary Cell Culture, Prostate cancer, Selectivity, Sesquiterpene lactones, Sesquiterpenes, Germacrane - chemistry, Sesquiterpenes, Germacrane - classification, Sesquiterpenes, Germacrane - isolation & purification, Sesquiterpenes, Germacrane - pharmacology, Signal Transduction, Terpenes, Toxicity, Transcription factors, Tumor cell lines, Tumor Necrosis Factor-alpha - genetics, Tumor Necrosis Factor-alpha - immunology, Tumor necrosis factor-α, Tumor Suppressor Protein p53 - genetics, Tumor Suppressor Protein p53 - immunology