Anticancer compound derived from flowers

Researchers from the University of Birmingham have produced a compound with anticancer properties directly from the flowering garden plant known as feverfew, which is grown in many UK gardens and also commonly sold in health food shops as a remedy for migraine and other aches and pains.

The team were investigating a compound called parthenolide, which was identified by scientists as having anticancer properties several years ago. The compound appears to work by increasing the levels of reactive oxygen species (ROS) in cells; cancer cells already have higher levels of these unstable molecules, so when parthenolide increases levels of these to a critical point, the process causes the cells to die.

Although available commercially, parthenolide is extremely expensive, with poor ‘drug-like’ properties, and has not progressed beyond basic research. Now the Birmingham team has developed a method for producing parthenolide directly from plants, as well as modifying it to produce a number of compounds that killed cancer cells in in vitro experiments.

The study was initiated by Dr Angelo Agathanggelou from the university’s Institute of Cancer and Genomic Studies, who is investigating new ways to treat chronic lymphocytic leukaemia (CLL) — a type of cancer which typically affects older people. He explained, “There are several effective treatments for CLL, but after a time the disease in some patients becomes resistant. We were interested in finding out more about the potential of parthenolide.”

Drawing together researchers from the Institute of Cancer and Genomic Studies and School of Chemistry, along with drug discovery companies Sygnature Discovery and ApconiX, the multidisciplinary study saw feverfew plants cultivated in the university’s Winterbourne Botanic Garden. Cultivation and harvesting was partially overseen by Lee Hale, Head of Winterbourne Botanic Garden, who noted, “After trials on related plant species within the Asteraceae family it soon became apparent that Tanacetum parthenium — feverfew — provided the optimum levels of parthenolide.”

Feverfew cultivation effort, Winterbourne Botanic Garden, prior to harvesting feverfew; (inset) recrystallised PTL.

With expertise from the School of Chemistry, the team was able to extract the compound from the flowers and modify it so it could be used to kill CLL cells in the laboratory. This makes the compound much more promising as a drug that could be used in the clinic for CLL patients, the researchers wrote in the journal MedChemComm.

“This research is important not only because we have shown a way of producing parthenolide that could make it much more accessible to researchers, but also because we’ve been able to improve its ‘drug-like’ properties to kill cancer cells,” said Professor John Fossey of the University’s School of Chemistry. “It’s a clear demonstration that parthenolide has the potential to progress from the flowerbed into the clinic.”

Top image credit: ©stock.adobe.com/au/nadin333

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