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Extracts of two germplasm lines of St. Johns wort (SJW; Hypericum perforatum L.) selected for enhanced hypericin and hyperforin content were evaluated for potential activity against colon cancer.  Bioactivity was assessed in signaling pathways of tumor necrosis factor-a (TNF-?) and nuclear transcription factor-?B (NF-?B) in HT-29 colon cancer cells. Both extracts and the hypericin standard significantly inhibited growth of HT-29 cells. Levels of active NF-?B were reduced in cells treated with either of the plant extracts or hypericin, but the purified hyperforin standard was comparatively ineffective. The combination of TNF-? and SJW treatments had significantly higher cytotoxic effects, and reduced the expression of NF-?B, inhibitor of NF-?Bs (I?Ba), I?B kinase b (IKKb), and TNF receptor-1. These observations indicate the potential of SJW as a source of cancer therapies, including those that act synergistically with TNF-?. The phytochemical complexity of SJW tissues necessitates consistent, optimized plant extracts for optimal results and the data indicate that additional, possibly unidentified, phytochemicals from SJW have potential in the treatment or prevention of colon cancer.

Optimized St. John's Wort (Hypericum perforatum L.) Germplasm Lines Exert Cytotoxicity in HT-29 Colon Cancer Cells via Downregulation of NF-?B