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Acarbose
Acarbose is a useful drug for the treatment of type II insulin-independent diabetes and is the first alpha-glucosidase inhibitor available in the US (known as Precose, Bayer Corporation). It was approved by the Food and Drug Administration (FDA) in September 1995 for use as monotherapy in patients with non-insulin-dependent diabetes mellitus (NIDDM). Found as one of the components in a complex mixture of pseudo-oligosaccharides isolated from culture broths of the Actinoplanes strain SE 50/110, acarbose shows potent inhibitory activity against sucrase, maltase, dextrinase, and glucoamylase. It also shows inhibitory activity, although to a relatively lower extent, against alpha-amylase and other amylose-degrading enzymes.
Structurally, acarbose represents a pseudotetrasaccharide, consisting of an unsaturated aminocyclitol, valienamine, a deoxyhexose and maltose. The pseudodisaccharide core structure, known as acarviosine, which is composed of valienamine and the deoxyhexose, is postulated to be essential for its biological activity. The core unit acarviosine is also linked to a variable number of glucose residues resulting in several other components in the complex mixture of acarbose. The formation of these components is highly dependent on the composition of the carbon source available in the culture medium. Media containing glucose and maltose will result in a specifically high yield of acarbose and the lower components, while media with high concentration of starch will yield longer pseudooligosaccharide species.
