Abstract
Platycodin D has diverse pharmacological activities. An efficient and economical mechanism for obtaining platycosides (platycodin D in particular) would be very useful. Balloon flower leaf extract (BFLE) was obtained by recycling leaves discarded from Platycodi radix production, as they have a high platycoside E content. A recombinant β-glycosidase from Caldicellulosiruptor owensensis was characterized and applied to BFLE for platycoside bioconversion. The enzyme specifically hydrolyzed the glucose residue at the C-3 position in platycosides and was suitable for platycodin D production. Under optimized reaction conditions, β-glycosidase from C. owensensis completely converted platycoside E from BFLE into platycodin D with the highest concentration and productivity reported so far. These results greatly improve the production process for deglycosylated platycosides.
Highlights
Balloon flower (Platycodon grandiflorum) has been known as a health food and a conventional medicine for treating bronchitis, tuberculosis, asthma, diabetes and other inflammatory diseases in Northeast Asia
Platycodin D is comprised of a pentacyclic triterpene aglycone and two-sided sugar components that contain one glucose molecule at the C-3 and the oligosaccharide residue consisting of arabinose-rhamnose-xylose-apiose at C-28
The C. owensensis β-glycosidase was expressed in Escherichia coli BL 21 with a soluble form
Summary
Balloon flower (Platycodon grandiflorum) has been known as a health food and a conventional medicine for treating bronchitis, tuberculosis, asthma, diabetes and other inflammatory diseases in Northeast Asia. Platycodin D, a major platycoside in the root of Platycodon grandiflorum (Platycodi radix), has shown diverse pharmaceutical effects such as anti-tumor [1,2], anti-inflammatory [3,4], anti-allergy [5,6] and anti-obesity [7,8] activities. Platycodin D is comprised of a pentacyclic triterpene aglycone and two-sided sugar components that contain one glucose molecule at the C-3 and the oligosaccharide residue consisting of arabinose-rhamnose-xylose-apiose at C-28. It can be converted by deglycosylation from platycoside E and platycodin D3 (Figure 1), which account for about 20 and 3% of the total platycosides in Platycodi radix and have two and one more glucose molecules at C-3, respectively [9]. Deglycosylation of saponins improves their biological activity because of their resulting smaller molecular weight, better permeability through the cell membrane and higher bioavailability [10,11]
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