Nanodelivery of natural isothiocyanates as a cancer therapeutic

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Natural isothiocyanates (ITCs) are phytochemicals abundant in cruciferous vegetables with the general structure, R–N=C=S. They are bioactive organosulfur compounds derived from the hydrolysis of glucosinolates by myrosinase. A significant number of isothiocyanates have been isolated from different plant sources that include broccoli, Brussels sprouts, cabbage, cauliflower, kale, mustard, wasabi, and watercress. Several ITCs have been demonstrated to possess significant pharmacological properties including: antioxidant, anti-inflammatory, anti-cancer and antimicrobial activities. Due to their chemopreventive effects on many types of cancer, ITCs have been regarded as a promising anti-cancer therapeutic agent without major toxicity concerns. However, their clinical application has been hindered by several factors including their low aqueous solubility, low bioavailability, instability as well as their hormetic effect. Moreover, the typical dietary uptake of ITCs consumed for promotion of good health may be far from their bioactive (or cytotoxic) dose necessary for cancer prevention and/or treatment. Nanotechnology is one of best options to attain enhanced efficacy and minimize hormetic effect for ITCs. Nanoformulation of ITCs leads to enhance stability of ITCs in plasma and emphasize on their chemopreventive effects. This review provides a summary of the potential bioactivities of ITCs, their mechanisms of action for the prevention and treatment of cancer, as well as the recent research progress in their nanodelivery strategies to enhance solubility, bioavailability, and anti-cancer efficacy.
Original languageEnglish
Pages (from-to)125-140
Number of pages16
JournalFree Radical Biology & Medicine
Early online date10 Mar 2021
Publication statusPublished - 1 May 2021


  • Allyl isothiocyanate
  • Apoptosis
  • Benzyl isothiocyanate
  • Cancer cells
  • Cancer therapeutic
  • Nanodelivery system
  • Nanoparticle
  • Natural isothiocyanates
  • Phenethyl isothiocyanate
  • Sulforaphane

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