ArticleJournal of natural products2018
Crystal Structures and Human Leukemia Cell Apoptosis Inducible Activities of Parthenolide Analogues Isolated from Piptocoma rufescens.
Article in Journal of natural products, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
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Who cites it
9 citing papers in PubMed, 16 citations in OpenAlex.
- Flavonoids and Sesquiterpene Lactones fromMetabolites · 2025Article
- Accessing the synthesis of natural products and their analogues enabled by the Barbier reaction: a review.RSC advances · 2024Review
- Strategies for the discovery of potential anticancer agents from plants collected from Southeast Asian tropical rainforests as a case study.Natural product reports · 2023Review
- Altereporenes A-E, five epoxy octa-hydronaphthalene polyketides produced by an endophytic fungusRSC advances · 2022Article
- Identification of a Covalent Importin-5 Inhibitor, Goyazensolide, from a Collective Synthesis of Furanoheliangolides.ACS central science · 2021Article
- Development of Potential Antitumor Agents from the Scaffolds of Plant-Derived Terpenoid Lactones.Journal of medicinal chemistry · 2020Article
- Plant-Derived Natural Products in Cancer Research: Extraction, Mechanism of Action, and Drug Formulation.Molecules (Basel, Switzerland) · 2020Review
- Phomretones A-F, CRSC advances · 2020Article
- Potential Anticancer Agents Characterized from Selected Tropical Plants.Journal of natural products · 2019Review
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
Abstract
The molecular structures of three parthenolide analogues, (-)-goyazensolide (1), (-)-15-deoxygoyazensolide (2), and (-)-ereglomerulide (3), isolated from the leaves of Piptocoma rufescens in a previous study were determined by X-ray analysis, and the absolute configuration of (-)-goyazensolide (1) was confirmed crystallographically using Cu Kα radiation at low temperature. Compounds 1-3, (+)-rufesolide A (4), and commercial parthenolide were found to be growth inhibitory toward MOLM-13 and EOL-1 human acute myeloid leukemia cells using PKC412 (midostaurin) as the positive control, with 1-3 being more active than parthenolide. Also, compounds 1-4 exhibited synergistic effects when tested with PKC412, but parthenolide did not show this type of activity. At a concentration lower than 2.0 μM, both 1 and 2 induced approximately 50% of the cells to become apoptotic at a late stage of the cell cycle, but no similar apoptotic effects were observed for 3, 4, or parthenolide. Leukemia cell apoptosis was induced by these compounds through the activation of caspase-3 and the inhibition of NF-κB, as indicated by immunoblotting analysis, and compounds 1 and 2 seem to be promising leads for development as potential antileukemic agents.
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Registered trials
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