Dimeric Furanones with a Unique Polycyclic Spiro Skeleton from Hawk Tea.

Area of Science:

• Natural Product Chemistry
• Medicinal Chemistry
• Organic Chemistry

Background:

• Hawk tea (likely *Hieracium pilosella*) is a source of bioactive natural products.
• Furanone derivatives are known for diverse biological activities.
• Novel chemical scaffolds are crucial for drug discovery.

Purpose of the Study:

• To isolate and characterize novel furanone derivatives from hawk tea.
• To evaluate the cytotoxic and mechanistic effects of these compounds against cancer cell lines.

Main Methods:

• Isolation and purification of compounds using chromatographic techniques.
• Structure elucidation via high-resolution electrospray ionization mass spectrometry (HR-ESIMS), nuclear magnetic resonance (NMR), electronic circular dichroism (ECD), and single-crystal X-ray diffraction.
• Cytotoxicity assays against AsPC-1, HCT-116, and L02 cells.
• Mechanistic studies including autophagy induction, migration inhibition, and cell cycle analysis.

Main Results:

• Six novel furanone derivatives, hawktealides A-F (1-6), with a unique 5/6/5 tricyclic spiro-system were identified.
• Compounds 1-3 demonstrated concentration-dependent cytotoxicity against AsPC-1 and HCT-116 cancer cells.
• Hawktealide A (1) exhibited significant potency against AsPC-1 cells and induced autophagy, inhibited migration, and caused cell cycle arrest in these cells.

Conclusions:

• Novel furanone derivatives, hawktealides A-F, were successfully isolated and characterized.
• Hawktealides A-C possess significant cytotoxic activity against human cancer cell lines.
• Hawktealide A demonstrates promising anti-cancer potential through multiple mechanisms, warranting further investigation.