Improved Bioactivity of 3-O-β-D-Glucopyranosyl Platycosides in Biotransformed Platycodon grandiflorum Root Extract by Pectinase from Aspergillus aculeatus

Abstract

Platycodon grandiflorus A.DC., known as bellflower or balloon flower, belongs to the genus Platycodon of the family Campanulaceae. It is a perennial herb native to East Asia. Platycodi radix (PR), the root of Platycodon grandiflorum, contains a mixture of different chemical compounds that may act individually, additively, or synergistically to improve human health. The main bioactive compounds of PR are platycodin saponins. PR is eaten as a side dish in Korean cuisine and is also used in desserts, teas, flavored liquors, and as a dietary supplements for the treatment of pulmonary diseases and respiratory disorders such as cough, asthma, bronchitis, cold, sore throat, tonsillitis, tuberculosis, inflammation, and chest congestion [1]. Furthermore, PR has been used as a traditional herbal treatment for hyperlipidemia, hypertension, and diabetes [2]. The root extract is reported to have hepatoprotective [3], anti-inflammatory [3], anti-lipidemic [4], anti-hypercholesterolemic [5], and antiobesity properties [6]. PR extract-derived platycosides are composed of pentacyclic triterpenes with two side sugar moieties. One of the sugars is a β-glucopyranose residue that is linked by a glycosidic bond at C-3 in the triterpenoid structure, whereas the other is an oligosaccharide (apiofuranosyl-xylopyranosyl-rhamnopranosylarabinofuranosyl residue) attached to the ester linkage at C-28.There are three types of saponins, each determined by the type of residue at C-24 in the triterpenoid structure. Platycodigenin-type saponins, one of the three, have a hydroxymethyl group at C-24 (Fig. 1A). Another, polygalacic acid-type saponins, have a methyl group at C-24 (Fig. 1B). The last, platyconic acid-type saponins, have a carboxyl group at C-24 (Fig. 1C). All three types share the same structure except for the residue in C-24, while the differences in functionality depend on the residue of C-24 in the triterpenoid structure.Deglycosylated saponins, obtained through the biotransformation of glycosylated saponins, exert stronger biological effects than their glycosylated forms [7,8]. Glycosylated saponins with more than three sugar residues are poorly absorbed in the intestine, whereas deglycosylated saponins, with less than two sugar residues, function Platycodon grandiflorum (balloon flower) root (Platycodi radix, PR) is used as a health supplement owing to its beneficial bioactive properties. In the present study, the anti-inflammatory, antioxidant, and whitening effects of deglycosylated platycosides (saponins) from PR biotransformed by pectinase from Aspergillus aculeatus were investigated. The bioactivities of the platycosides improved when the number of sugar moieties attached to the aglycone platycosides was decreased. The deglycosylated saponins exhibited higher lipoxygenase inhibitory activities (anti-inflammatory activities) than the precursor platycosides and the anti-inflammatory compound baicalein. The 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity of the pectinasetreated PR extract was higher than that of...

Biotransformation and pharmacological activities of platycosides from Platycodon grandiflorum roots

“…The crude enzyme from Rhizopus oryzae , a food-available fungus is a new fermentation microorganic strain to obtain deapiosylated platycosides ( Shin, Kil, Lee, & Oh, 2021 ). Compared with a previous study that β -glucosidase from Dictyoglomus turgidum converted platycosides into deglucosylated ones ( Kang, Kim, Shin, Ko, & Oh, 2019 ), Ju et al (2021) reported that pectinase from Aspergillus aculeatus can biotansformate glycosylated platycosides into 3- O - β-D -glucopyranosyl platycosides ( Fig. 6 ).…”

“…Increasing researches showed that platycosides could be transformed into deglycosylated, dehydroxylated, acetylated and hydroxylated metabolites in vivo and in vitro ( Zhang, Song, Liu, & Guo, 2022 ). Similar to ginsenosides, deglycosylated platycosides, obtained through the biotransformation of glycosylated saponins, showed biological effects better than their glycosylated forms ( Ju, Lee, Lee, Kim, & Oh, 2021 , Kang, Kim, Shin, Ko, & Oh, 2019 , Shin, Kil, Lee, & Oh, 2021 ). Deapiosylated platycosides or secondary glycosides such as the anti-inflammatory, antioxidant activities, expectorant effects, were more active than those of the precursor glycosylated platycosides ( Shin, Kil, Lee, & Oh, 2021 ).…”

Ethnopharmacology, phytochemistry, pharmacology and product application of Platycodon grandiflorum: A review

“…These ingredients play a synergistic role in whitening the skin through the anti-inflammatory and antioxidant effects of Jiegeng and can be used to develop healthy and effective skincare products and cosmetics ( Ma et al, 2021 ). The Jiegeng methanol extract was converted by pectinase to obtain 3- O - β - D -glucopyranosyl platycosides can synergically exert anti-inflammatory, antioxidant, and whitening effects, and is a good raw material for making whitening cosmetics ( Ju et al, 2021 ). The Japanese Kao Cosmetics Company has launched whitening essences, whitening essence milk, and other whitening products containing P. grandiflorum -whitening active ingredients.…”

Integrated metabolomic and transcriptomic analysis reveals variation in the metabolites and genes of Platycodon grandiflorus roots from different regions

“…Platycodon grandiflorum root (PG) is popularly known as “Jiegeng” in China, “Doraji” in Korea, “Kikyo” in Japan, and “Huridunzhaga” in Mongolia 3 and has been widely used to prepare side dishes and kimchi in northeast China and Korea 4,5 . Several studies have indicated that the starch of PG can be made into a high‐quality pastry, and PG extracts can be used as active components in anti‐ageing cosmetics and whitening body lotion 6 . PG is a traditional Asian herbal medicine with a long history of use; it is widely used for the treatment of cough, phlegm, sore throat, and other pulmonary and respiratory disorders in clinics 7,8 …”

“…that the starch of PG can be made into a high-quality pastry, and PG extracts can be used as active components in anti-ageing cosmetics and whitening body lotion. 6 PG is a traditional Asian herbal medicine with a long history of use; it is widely used for the treatment of cough, phlegm, sore throat, and other pulmonary and respiratory disorders in clinics. 7,8 In China, Platycodon grandiflorum is a popular medicinal and food homology plant that is used as a clinical medicine as well as food ingredient; 7 it was first recorded in the famous book Shen Nong Ben Cao Jing.…”