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In Vitro-In Vivo Dose Response of Ursolic Acid, Sulforaphane, PEITC, and Curcumin in Cancer Prevention

A Correction to this article was published on 06 February 2018

This article has been updated

Abstract

According to the National Center of Health Statistics, cancer was the culprit of nearly 600,000 deaths in 2016 in the USA. It is by far one of the most heterogeneous diseases to treat. Treatment for metastasized cancers remains a challenge despite modern diagnostics and treatment regimens. For this reason, alternative approaches are needed. Chemoprevention using dietary phytochemicals such as triterpenoids, isothiocyanates, and curcumin in the prevention of initiation and/or progression of cancer poses a promising alternative strategy. However, significant challenges exist in the extrapolation of in vitro cell culture data to in vivo efficacy in animal models and to humans. In this review, the dose at which these phytochemicals elicit a response in vitro and in vivo of a multitude of cellular signaling pathways will be reviewed highlighting Nrf2-mediated antioxidative stress, anti-inflammation, epigenetics, cytoprotection, differentiation, and growth inhibition. The in vitro-in vivo dose response of phytochemicals can vary due, in part, to the cell line/animal model used, the assay system of the biomarker used for the readout, chemical structure of the functional analog of the phytochemical, and the source of compounds used for the treatment study. While the dose response varies across different experimental designs, the chemopreventive efficacy appears to remain and demonstrate the therapeutic potential of triterpenoids, isothiocyanates, and curcumin in cancer prevention and in health in general.

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Change history

  • 06 February 2018

    The citation of the author name “Ah-Ng Tony Kong” in PubMed is not the author’s preference. Instead of “Kong AT”, the author prefers “Kong AN”.

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Acknowledgments

The authors express sincere gratitude to all of the members of Dr. Kong’s laboratory for their helpful discussions.

Funding

This work was supported in part by institutional funds and by R01-CA200129 from the National Cancer Institute (NCI), R01-AT009152 from the National Center for Complementary and Integrative Health (NCCIH) and R01-AT007065 from NCCIH and the Office of Dietary Supplements (ODS).

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Correspondence to Ah-Ng Kong.

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Guest Editors: Ah-Ng Kong and Chi Chen

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Ramirez, C.N., Li, W., Zhang, C. et al. In Vitro-In Vivo Dose Response of Ursolic Acid, Sulforaphane, PEITC, and Curcumin in Cancer Prevention. AAPS J 20, 19 (2018). https://doi.org/10.1208/s12248-017-0177-2

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KEY WORDS

  • triterpenoids
  • isothiocyanates
  • curcumin
  • chemoprevention
  • phytochemical