Pharmacological Effects of Prenylated Flavonoids in Cancer

Prenylated flavonoids represent a unique subclass of polyphenolic compounds characterised by the addition of a hydrophobic prenyl moiety, which confers enhanced cellular permeability and target affinity. Among them, xanthohumol and related derivatives have emerged as promising candidates for cancer prevention and therapy. These molecules exert multimodal pharmacological effects, including the induction of programmed cell death, suppression of mitochondrial function in malignant cells, arrest of cell cycle progression, inhibition of angiogenesis, and attenuation of metastasis through matrix metalloproteinase regulation. Mechanistic studies reveal that these effects are mediated by modulation of key signalling pathways such as NF-κB, PI3K/Akt, Nrf2 and Notch, as well as by the activation of autophagic processes. Preclinical data underscore their capacity to overcome multidrug resistance and to synergise with established chemotherapeutics. Ongoing efforts focus on optimising bioavailability, minimising off-target actions, and translating these phytochemicals into clinically viable formulations.

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Pharmacological Effects of Prenylated Flavonoids in Cancer publication trend

The graph below shows the total number of articles in pharmacological effects of prenylated flavonoids in cancer across all publications each year (not limited to Nature Index journals).

Technical terms

Prenylated flavonoid: Flavonoid substituted with a lipophilic prenyl group that enhances cellular uptake and bioactivity.

Xanthohumol: A prenylated chalcone from Humulus lupulus with documented anticancer properties.

Apoptosis: Programmed cell death mechanism essential for the elimination of cancerous cells.

MMP (Matrix metalloproteinase): Enzyme family that degrades extracellular matrix components, facilitating tumour invasion and metastasis.

NF-κB: Transcription factor that controls genes involved in inflammation and cell survival, often dysregulated in cancer.

Nrf2: Transcription factor that orchestrates cellular antioxidant responses by inducing detoxification enzymes.

References

1. Antioxidant Potential of Xanthohumol in Disease Prevention: Evidence from Human and Animal Studies. Antioxidants (2024).
2. Xanthohumol hinders invasion and cell cycle progression in cancer cells through targeting MMP2, MMP9, FAK and P53 genes in three-dimensional breast and lung cancer cells culture. Cancer Cell International (2023).
3. Anticancer Activity and Mechanism of Xanthohumol: A Prenylated Flavonoid From Hops (Humulus lupulus L.). Frontiers in Pharmacology (2018).
4. Xanthohumol Inhibits Notch Signaling and Induces Apoptosis in Hepatocellular Carcinoma. PLOS ONE (2015).