• Journal of Microbiology and Biotechnology
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• v.31 no.6
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• pp.847-854
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• 2021

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 the non-treated PR extract. The trolox-equivalent antioxidant capacity (TEAC) assay showed improved values as the saponins were hydrolyzed. The tyrosinase inhibitory activities (whitening effects) of deglycosylated platycosides were higher than those of the precursor platycosides. Furthermore, 3-O-β-ᴅ-glucopyranosyl platycosides showed higher anti-inflammatory, antioxidant, and whitening activities than their precursor glycosylated platycosides. Therefore, 3-O-β-ᴅ-glucopyranosyl platycosides may improve the beneficial effects of nutritional supplements and cosmetic products.

• Journal of Microbiology and Biotechnology
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• v.30 no.6
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• pp.946-954
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• 2020

Platycodon grandiflorum root (Platycodi radix) saponins, platycosides, have been used as health supplements and food items for the treatment of respiratory disorders and pulmonary diseases. Deglycosylated saponins have been known to exert stronger biological effects than their glycosylated forms. In the present study, glycosylated platycosides in Platycodi radix extract were biotransformed into deglycosylated 3-O-β-ᴅ-glucopyranosyl platycosides, including 3-O-β-ᴅ-glucopyranosyl platycodigenin, 3-O-β-ᴅ-glucopyranosyl polygalacic acid, and 3-O-β-ᴅ-glucopyranosyl platyconic acid, by pectinase from Aspergillus aculeatus. This is the first report on the quantitative enzymatic production of 3-O-β-ᴅ-glucopyranosyl platycosides. The chemical structures of 3-O-β-ᴅ-glucopyranosyl platycosides were identified with LC/MS. Moreover, the biotransformation pathways of the three types of platycosides in Platycodi radix into 3-O-β-ᴅ-glucopyranosyl platycosides were established.

• Journal of Microbiology and Biotechnology
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• v.32 no.4
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• pp.430-436
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• 2022

Platycosides, Platycodi radix (Platycodon grandiflorus root) saponins, are used as food supplements and exert diverse pharmacological activities. Deglycosylation of saponins enhances their biological efficacy, and deglycosylated platycosides are produced mainly through enzymatic hydrolysis. However, the types of available deglycosylated platycosides remain limited because of a lack of hydrolyzing enzymes that can act on specific glycosides in glycosylated platycosides. In this study, a crude enzyme from Aspergillus tubingensis converted platycoside E (PE) and polygalacin D₃ (PGD3) into deglucose-apiose-xylosylated (deGAX)-platycodin D (PD) and deGAX-polygalacin D (PGD), respectively. The products were identified through LC/MS analysis by specifically hydrolyzing all glucose residues at C-3, and apiose and xylose residues at C-28 of platycoside. The hydrolytic activity of the crude enzyme obtained after the cultivation of the fungus using citrus pectin and corn steep solid as carbon and nitrogen sources, respectively, in culture medium was increased compared with those using other carbon and nitrogen sources. The crude enzyme from A. tubingensis was the most effective in producing deGAX platycoside at pH 5.0 and 60℃. The crude enzyme produced 0.32 mg/ml deGAX-PD and 0.34 mg/ml deGAX-PGD from 1 mg/ml PE and 1 mg/ml PGD3 (at pH 5.0 and 60℃) for 12 and 10 h, with productivities of 32.0 and 42.5 mg/l/h and molar yields of 62.1 and 59.6%, respectively. To the best of our knowledge, this is the first study to produce deGAX platycosides from glycosylated platycosides.

• Natural Product Sciences
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• v.14 no.4
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• pp.274-280
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• 2008

Platycosides are the saponins in Platycodi Radix and they have several beneficial effects such as antiinflammatory and anti-obesity activities. This study was designed to determine the changes in the saponin composition in Platycodi Radix (platycosides) after being processed under steam and pressure and to investigate the anti-inflammatory effects of their extracts. The change of the platycoside compositions was investigated after 1, 2, 3, 6 and 9h heat processing of Platycodi Radices by using HPLC coupled with an evaporative light scattering detection (ELSD) system. After heat treatment ($125^{\circ}C$, 1, 2, 3, 6 and 9 h), the contents of several platycosides such as platycoside E, platycodin $D_3$, platycodin D, polygalacin D, and platycodin A decreased as the processing time was longer. While the total contents of the saponins decreased, the contents of deapi-forms of deapiplatycoside E, deapi-platycodin $D_3$, and deapi-platycodin D increased relatively. These results indicate that the linkage between apiose and xylose located at C-28 is labile to heat and pressure. The LPS-induced iNOS inhibitory activities of the samples treated for 1 and 2 hours were enhanced and after then, the activities were reduced. These results suggested that heat treatment of the samples affect the content of the total saponins and the saponin content may be the important criteria representing the anti-inflammatory activity.

• Preventive Nutrition and Food Science
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• v.19 no.2
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• pp.59-68
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• 2014

The extracts and pure saponins from the roots of Platycodon grandiflorum (PG) are reported to have a wide range of health benefits. Platycosides (saponins) from the roots of PG are characterized by a structure containing a triterpenoid aglycone and two sugar chains. Saponins are of commercial significance, and their applications are increasing with increasing evidence of their health benefits. The biological effects of saponins include cytotoxic effects against cancer cells, neuroprotective activity, antiviral activity, and cholesterol lowering effects. Saponins with commercial value range from crude plant extracts, which can be used for their foaming properties, to high purity saponins such as platycodin D, which can be used for its health applications (e.g., as a vaccine adjuvant). This review reveals that platycosides have many health benefits and have the potential to be used as a remedy against many of the major health hazards (e.g., cancer, obesity, alzheimer's) faced by populations around the world. Methods of platycoside purification and analysis are also covered in this review.

• Journal of the Korean Society of Food Science and Nutrition
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• v.45 no.7
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• pp.1017-1025
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• 2016

This study was performed in order to investigate changes in platycosides, as well as antimicrobial activities of bronchus diseases-inducing bacteria (Corynebacterium diphtheriae, Klebsiella pneumoniae, Staphylococcus aureus, and Streptococcus pyogenes) of Platycodon grandiflorum root (PGR) fermented by lactic acid bacteria (Leuconostoc mesenteroides N12-4, Leuc. mesenteroides N58-5, Lactobacillus plantarum N76-10, L. plantarum N56-12, Lactobacillus brevis N70-9, and L. brevis E3-8). Growth of L. plantarum on PGR was most active during lactic acid fermentation using different strains. Total platycoside, platycoside E, platycodin A, polygalacin $D_2$, polygalacin D, and diapioplatyco-side E contents of PGR fermented for 96 h at $37^{\circ}C$ by Leuc. mesenteroides and L. plantarum increased, whereas contents of platycodin D and platycodin $D_3$ were reduced. The antimicrobial activity on PGR fermented by L. plantarum N56-12 exhibited strong microbial proliferation for all four kinds of bronchus disease-inducing bacteria and was higher than that of non-fermented PGR extract. MIC of fermented PGR extract by L. plantarum N56-12 on C. diphtheriae, K. pneumoniae, S. aureus, and S. pyogenes were 45, 10, 50, and 25 mg/mL, respectively. Thus, this result shows that the antimicrobial activities of bronchus disease-inducing bacteria and platycoside content of PGR by L. plantarum N56-12 were higher than that of non-fermented PGR extract.