Isothiocyanates in Cancer Therapeutics - A Molecular Perspective

Isothiocyanates (ITCs) are naturally occurring organo-sulfur compounds. They occur widely in different plant sources, being most abundant in Brassicaceae family. Several of them have been demonstrated to possess significant bioactivities and health benefits including anticancer, anti-inflammatory, and antimicrobial activities. ITCs have very high electrophilicity and nucleophilicity due to the carbon and sulfur atom, respectively. Thus, chemical structure plays a prominent role in their bioactivities and ability to inhibit tumorigenesis. ITCs are potent against many forms of cancers and tumors. ITCs as drug conjugates and in combination therapies as antitumor therapeutic agents have shown promising prospects for clinical applications. Evaluation of possible ways to retain and/or enhance conversion of plant-derived GLSs into beneficial ITCs, can aid in enhancing nutritive and anticancer properties of ITC rich dietary plant sources. This review presents a comprehensive account of ITCs, their structure-activity relationship, specific biological functions to inhibit tumorigenesis and mechanism of action of different ITCs. Some examples on the use of ITC-drug conjugates and their use in combination therapies as promising anticancer therapeutics are highlighted. Further, methods to enhance nutritive properties through the conversion of glucosinolates (GLSs) into beneficial ITCs have also been proposed.