Tocopheryl Succinate—Versatile Functions due to Its Unique Physicochemical Properties

Abstract

Summary ␣ -Tocopheryl succinate (TS), a succinyl ester of ␣ -tocopherol ( ␣ -T), has no antioxidant activity, but it does have unique physicochemical properties and shows versatile biological functions. The physicochemical properties of TS affect the structure and function of lipid membranes, and the ability to form bilayer vesicles by itself suggests that TS can become a new carrier in the field of drug delivery systems. The ability to induce apoptosis is a most attractive property of TS. Because TS shows higher cytotoxicity on various cancer cells than on normal cells in vitro , prevents tumor growth, and extends survival in vivo , much attention has been paid to TS as a new type of anti-cancer drug. Activation of various signal transduction factors is also a well-known function of TS. In particular, protein kinase C (PKC), which acts in upstream in the signal transduction, is thought to play an important role in the effects of TS. Our theoretical computational study indicates that TS activates PKC by direct interaction with PKC due to its high structural flexibility.

Intestinal Epithelial Cells Absorb γ‐Tocotrienol Faster than α‐Tocopherol

“…The most significant finding in this study was that c-tocotrienol was more readily transferred to the intestinal cell membrane than a-tocopherol in the Caco2 cell model or in the rat administration experiments. This result is in accordance with the previous finding that tocotrienol isomers were more readily incorporated into various kinds of culture cells than tocopherol isomers [12,14,[25][26][27][28]. Those studies concluded that the inter-membrane mobility of c-tocotrienol was greater than that of tocopherol isomers [27].…”

“…However, various bioactivities, beyond antioxidant functions, of tocopherol and tocotrienol isomers, have recently been reported [35,36]. Several biological activities of tocotrienol isomers were reported to be more effective than those of tocopherol isomers [12,[26][27][28]. Further information about the digestive behaviors of tocopherol and tocotrienol isomers will be needed in the near future so that their advanced use can be considered.…”