Bioorganic & medicinal chemistry, 2014-08, Vol.22 (15), p.4198-4203
2014
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- Autor(en) / Beteiligte
- Titel
- Topoisomerase II inhibitors from the roots of Stellera chamaejasme L
- Ist Teil von
- Bioorganic & medicinal chemistry, 2014-08, Vol.22 (15), p.4198-4203
- Ort / Verlag
- England: Elsevier Ltd
- Erscheinungsjahr
- 2014
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- Three new compounds, including one daphnane diterpene (1), one sesquiterpene (6), and one lignan (7) have been isolated from the Stellera chamaejasme L., together with five other known compounds, including four daphnane diterpenenoids (2–5) and one lignan (8). The structures of the new compounds were elucidated by spectroscopic analysis. The cytotoxicities of compounds 1–8 towards human lung adenocarcinoma cells (A549 cells) were evaluated using a sulforhodamine B assay. All of the compounds displayed significant cytotoxicity, with IC50 values in the ranging of 0.2nM to 2.0μM. Mechanistic studies revealed that the antitumor activities of compounds 1–3 and 7 were derived from their inhibition of topoisomerase II (Topo II). Furthermore, as a Topo II inhibitor, compound 1 was found to effectively induced G2-M phase cell cycle arrest and apoptosis in cancer cells.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0968-0896eISSN: 1464-3391DOI: 10.1016/j.bmc.2014.05.042Titel-ID: cdi_proquest_miscellaneous_1549200716
- Format
- –
- Schlagworte
- Antineoplastic Agents, Phytogenic - chemistry, Antineoplastic Agents, Phytogenic - isolation & purification, Antineoplastic Agents, Phytogenic - pharmacology, Apoptosis, Apoptosis - drug effects, Cell Line, Tumor, Cell Proliferation - drug effects, Cytotoxic activity, DNA Topoisomerases, Type II - chemistry, DNA Topoisomerases, Type II - metabolism, G2 Phase Cell Cycle Checkpoints - drug effects, Humans, M Phase Cell Cycle Checkpoints - drug effects, Magnetic Resonance Spectroscopy, Molecular Conformation, Plant Roots - chemistry, Plant Roots - metabolism, Stellera chamaejasme L, Thymelaeaceae - chemistry, Thymelaeaceae - metabolism, Topoisomerase II, Topoisomerase II Inhibitors - chemistry, Topoisomerase II Inhibitors - isolation & purification, Topoisomerase II Inhibitors - pharmacology