Rebaudioside, a novel agent of glycoside clathration of pharmacons

Abstract

205 Glycyrrhizinic acid and stevioside, glycosides of higher terpenoids, are capable of in vivo formation of clathrates with pharmacons with various types of activity. This property of glycosides allows the effective dose to be substantially decreased (by a factor of 10– 100), with the basic activity being preserved and novel pharmacological effects appearing [1–6]. The plant Stevia rebaudiana Bertoni is known to produce not only stevioside I, but also rebaudioside A II, which can be obtained in an individual state. The carbon chain of rebaudioside is more branched than the corresponding structural fragment of stevioside. Considering the high capacity of stevioside for clathrate formation, it is conceivable that rebaudioside also forms clathrates. Note that rebaudioside, like stevioside, is nontoxic (LD 50 8000 mg/kg) and is included in food compositions as a sweetener [7, 8]. Our study described below has confirmed that rebaudioside has the aforementioned capacity for glycoside clathrate formation.