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Anti-inflammatory polyoxygenated cyclohexene derivatives from Uvaria macclurei
Yexin Cheng1, Hailong Li1, Dan Wu1
1State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin 300353, People's Republic of China.
This study isolated novel compounds from Uvaria macclurei, with (-)-zeylenone demonstrating significant anti-inflammatory effects by reducing nitric oxide (NO) production and inflammatory gene expression.
Area of Science:
- Natural Product Chemistry
- Pharmacology
- Medicinal Chemistry
Background:
- Uvaria macclurei is a plant source of bioactive compounds.
- Polyoxygenated cyclohexene derivatives possess potential therapeutic properties.
Purpose of the Study:
- To isolate and characterize novel compounds from Uvaria macclurei.
- To evaluate the anti-inflammatory activities of isolated compounds.
Main Methods:
- Isolation and structure elucidation using spectroscopic and circular dichroism analyses.
- In vitro anti-inflammatory assays on lipopolysaccharide (LPS)-stimulated RAW 264.7 cells.
- In vivo sepsis model in mice.
Main Results:
- Five new compounds (macclureins A-E) and 15 known analogues were isolated.
- (-)-Zeylenone exhibited potent inhibition of nitric oxide (NO) production (IC50 = 20.18 μM).
- (-)-Zeylenone downregulated pro-inflammatory factors (IFN-γ, iNOS, IL-6, TNF-α) via the NF-κB pathway and alleviated sepsis severity in mice.
Conclusions:
- (-)-Zeylenone is a promising anti-inflammatory agent.
- The study highlights the potential of Uvaria macclurei as a source of novel anti-inflammatory compounds.
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