The present invention provides novel compositions and methods for their production and use in modulating arginine metabolism to treat biological conditions. The biological condition is preferably one associated with dysregulated arginine metabolism and/or abnormal endogenous levels of substances resulting from or involved in arginine metabolism. The subject invention provides compositions that modulate levels of arginine or levels of substances that are derived from arginine in vivo via pre-selected signal transduction/metabolic pathways. In one embodiment, compositions comprising arginine and a glycoside are provided. The compositions and methods of the invention are able to select and prompt a particular metabolic pathway in which the arginine is to be used as a substrate.