Background: Tocotrienols (TTs) are vitamin E derivatives naturally occurring in several
plants and vegetable oils. Like Tocopherols (TPs), they comprise four isoforms, α, β, γ and δ, but unlike
TPs, they present an unsaturated isoprenoid chain. Recent studies indicate that TTs provide important
health benefits, including neuroprotective, anti-inflammatory, anti-oxidant, cholesterol lowering and immunomodulatory
effects. Moreover, they have been found to possess unique anti-cancer properties.
Objective: The purpose of this review is to present an overview of the state of the art of TTs role in
cancer prevention and treatment, as well as to describe recent patents proposing new methods for TTs
isolation, chemical modification and use in cancer prevention and/or therapy.
Methods: Recent literature and patents focusing on TTs anti-cancer applications have been identified
and reviewed, with special regard to their scientific impact and novelty.
Results: TTs have demonstrated significant anti-cancer activity in multiple tumor types, both in vitro
and in vivo. Furthermore, they have shown synergistic effects when given in combination with standard
anti-cancer agents or other anti-tumor natural compounds. Finally,
new purification processes and
transgenic sources have been designed in order to improve TTs production, and novel TTs formulations
and synthetic derivatives have been developed to enhance their solubility and bioavailability.
Conclusion: The promising anti-cancer effects shown by TTs in several preclinical studies may open
new opportunities for therapeutic interventions in different tumors. Thus, clinical trials aimed at confirming
TTs chemopreventive and tumor-suppressing activity, particularly in combination with standard
therapies, are urgently needed.