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Compositional analysis of major saponins and anti-inflammatory activitiy of steam-processed platycodi radix under pressure
Abstract
Platycosides are the saponins in Platycodi Radix and they have several beneficial effects such as anti-inflammatory 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 °C, 1, 2, 3, 6 and 9 h), the contents of several platycosides such as platycoside E, platycodin D3, 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 deapi-platycoside E, deapi-platycodin D3, 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.
... Platycoside analysis HPLC chromatograms of puffed and non-puffed doraji with the same moisture content of 6.0 g of water/100 g of doraji at different puffing pressures are shown in Fig. 5. Levels of platycosides were reduced after the puffing process to a nearly undetectable level at (27). It was shown that the linkage between sugars at C-28 is easily degraded by heat and pressure (28). In this study, HPLC analysis indicated that the puffing process may cleave C-28 residues, resulting in decreased levels of platycosides. ...
... The platycoside contents in doraji puffed at 980 kPa were much lower than in non-puffed doraji. The result was in agreement with a report that the platycoside composition was changed by processing under steam and pressure (28). In this study, the puffing pressure was a major factor that affected the extraction yield, crude saponin content, platycoside content, and antioxidant activity. ...
Effects of moisture content and puffing pressure on the extraction yield, crude saponin content, antioxidant activity, and platycoside content of puffed 21-year-old doraji were investigated. Sliced doraji was dried to 4.0, 6.0, and 8.0 g of water/100 g of sample, then puffed at pressures of 686, 784, 882, and 980 kPa. The extraction yield, crude saponin, and antioxidant activity of puffed doraji, compared with non-puffed doraji, increased from 35.9 to 52.7 g/100 g of dried doraji, from 34.4 to 70.5 mg/g of dried doraji, and from 34.0 to 138.1 mg of vitamin C equivalent (VCE)/g of dried doraji, respectively. Levels of the major platycosides, platycoside E, platycodin D, and D3 of puffed doraji were reduced as the puffing pressure increased. Puffing can be a favorable unit process resulting in a higher extraction yield, total crude saponin content, and antioxidant activity of doraji. © 2015, The Korean Society of Food Science and Technology and Springer Science+Business Media Dordrecht.
Saponins can be classified as triterpenoid (C30) or steroidal (C27), based on their carbon nucleus (aglycone). Sugar residues are linked to the aglycone, conferring an amphiphilic nature on these molecules, which is relevant for their biological activities. Saponins include a large variety of molecules that find several applications in pharmacology. Saponins have been shown to display immunoadjuvant, anti-inflammatory, antiplatelet, hypocholesterolemic, antitumoral, anti-HIV, antibacterial, insecticide, fungicide and anti-leishmanial activities. Anti-inflammatory medicines are increasingly demanded to treat various forms of arthritis in aging and obese populations and to help reduce the doses and duration of conventional corticotherapy with less side effects and without immunosuppression. The vaccine market for both human and veterinary uses is close to US$ 15 billion, progressively inflated by the recurrent threat of global pandemics.This paper provides an overview of recent advances (main focus on the last five years) on plant saponins that show anti-inflammatory and/or immunoadjuvant activities: source plants, isolation procedures, mechanism of action and biotechnological approaches towards sustainable production of bioactive saponins. Special attention is given to ginseng and Quillaja saponins. Strategies based on plant cultivation, cell and tissue culture, elicitation, and metabolic engineering for improved production of saponins are described. Future directions for research in the field and strategies to overcome bottlenecks are also discussed.
An extract of heat-processed Achyranthes fauriei roots showed more potent cytotoxic activity against human hepatoma SK-Hep-1 cells than that of the crude plant. Employing a bioassay-linked HPLC-ELSD (high performance liquid chromatography-evaporative light scattering detector) method, followed by silica gel column chromatography, a cytotoxic triterpenoid saponin, chikusetsusaponin IVa was isolated. It is contributive to the increased cytotoxic activity of the heat-processed. The amount of chikusetsusaponin IVa from the roots of Achyranthes fauriei was significantly increased after heat-processing.
Our previous report stated that kikyo-to, a Japanese herbal medicine, consisting of the roots of Platycodon grandiflorum and Glycyrrhiza sp., stimulates the pancreatic exocrine secretion of conscious rats. The present study focused on the effective components of kikyo-to and the mechanism of stimuli to pancreatic secretion of rats. When 10 to 100 mg of platycodin D, a saponin from the root of Platycodon grandiflorum, was intragastrically administered, the pancreatic secretion of rats was stimulated. At the same time, the plasma CCK concentration increased. On the other hand, the stimulative effects of glycyrrhizin, a saponin from the root of Glycyrrhiza sp. were weak compared to platycodin D. The effects of 10 mg/kg of platycodin D on pancreatic secretion were inhibited by loxiglumide (50 mg/kg, i.g.), a CCK receptor antagonist. In contrast, the suppressive effect of atropine (300 micrograms/kg/h, i.v.) on pancreatic secretion was reduced by administering 10 mg/kg of platycodin D. In addition, up to 1 mM of platycodin D did not inhibit the trypsin activities in vitro. In conclusion, kikyo-to serves to stimulate pancreatic exocrine secretion mainly because platycodin D causes gastrointestinal hormones, particularly, CCK to be released from the duodenum.
Two new triterpenoid saponins, platycoside D [3-O-beta-D-glucopyranosyl-(1-->6)-beta-D-glucopyranosyl-(1-->6)-beta-D- glucopyranosyl-2 beta, 3 beta, 16 alpha, 23-tetrahydroxyolean-12-ene-28-oic acid 28-O-beta-D- apiofuranosyl-(1-->3)-beta-D-xylopyranosyl-(1-->4)-alpha-L-rhamnop yranosyl- (1-->2)-alpha-L-arabinopyranoside] and platycoside E [3-O-beta-D-glucopyranosyl-(1-->6)-beta-D-glucopyranosyl- (1-->6)-beta-D-glucopyranosyl-2 beta,3 beta,16 alpha,23,24-pentahydroxyolean-12-ene-28-oic acid 28-O-beta-D-apiofuranosyl-(1-->3)-beta-D-xylopyranosyl-(1-->4)-alp ha-L- rhamnopyranosyl-(1-->2)-alpha-L-arabinopyranoside] were isolated from the roots of Platycodon grandiflorum. Structural determination is based on spectral and chemical evidence.
Thirteen commercial samples of Platycodi radix of Platycodon grandiflorum, were collected from China (5 kinds), Korea (5 kinds), and Japan (3 kinds) along with 8 kinds of botanically cultivated Platycodi radix, 3 kinds of wild Platycodi radix collected from different places in Japan. HPLC analysis showed that the commercial botanical and wild samples of P. radix all contained platycodins and a total of twelve peaks were identified by co-HPLC anlaysis with authentic samples isolated earlier from this laboratory. The peak purity and identify were checked with a PDA. The contents of the major saponins, platycodins A, C, D were determined and the peak-area ratios of platycodins A, C, D were shown to be correlated with their sources of origin. The commercial samples from China and Korea each gave a distinct HPLC pattern with peak-area ratio of platycodins A, C, D at 1:2:3 and 2:4:1, respectively. HPLC analysis showed that those on the Japanese market were either imported from China or Korea based upon their HPLC patterns while the Japanese botanical garden or wild type samples gave a higher total saponin content with the peak-area ratio of platycodins A, C, D at 1:2:1.
We investigated the effects of aqueous extract from Platycodi radix (AEPR), a traditional drug used to treat acute lung inflammatory disease, on lipopolysaccharide (LPS)-induced inflammation in A549 human cultured airway epithelial cells. Nuclear factor-kappaB (NF-kappaB) and its inhibitory regulator, inhibitory kappaB (I-kappaB), play crucial roles in LPS-induced inflammatory response. We show that LPS-induced nuclear translocation of NF-kappaBp65 is inhibited by AEPR. LPS-induced expression of I-kappaBalpha, which is expressed by LPS-induced activation of NF-kappaB, is inhibited by AEPR as well. Besides LPS-induced expression of a group of genes, such as tumor necrosis factor-alpha (TNF-alpha), inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2), are repressed by AEPR. We also found that expression of heat shock protein 70 (Hsp70), which has an anti-inflammatory activity, is increased by AEPR plus LPS. These results suggest that AEPR may act as a therapeutic agent for inflammatory disease through regulating the activity of NF-kappaB and expression of inflammatory genes.
Adhesion molecules play an important role in the development of atherogenesis and are produced by endothelial cells after being stimulated with various inflammatory cytokines. This study examined the effect of saponins that were isolated from the roots of Platycodon grandiflorum A. DC (Campanulaceae), Changkil saponins (CKS), on the cytokine-induced monocyte/human endothelial cell interaction, which is a crucial early event in atherogenesis. CKS significantly inhibited the TNFalpha-induced increase in monocyte adhesion to endothelial cells as well as decreased the protein and mRNA expression levels of vascular adhesion molecule-1 and intercellular cell adhesion molecule-1 on endothelial cells. Furthermore, CKS significantly inhibited the TNFalpha-induced production of intracellular reactive oxygen species (ROS) and activation of NF-kappaB by preventing IkappaB degradation and inhibiting IkappaB kinase activity. Overall, CKS has anti-atherosclerotic and anti-inflammatory activity, which is least in part the result of it reducing the cytokine-induced endothelial adhesion to monocytes by inhibiting intracellular ROS production, NF-kappaB activation, and cell adhesion molecule expression in endothelial cells.
Platycodon grandiflorum A. DC (Campanulaceae) is a traditional medicinal plant. Its root, Platycodi Radix, contains an abundant amount of saponin glycosides, platycodins, of which platycodin D is one of the major components. The chemical structures of platycodins can be modified by various types of chemical processing, but a modification mediated with microorganisms has been not reported yet. In this study, platycodin D was modified to several partially degraded platycodin glycosides after treatment with a crude enzyme extract from Aspergillus niger (A. niger). The modified platycodin D possessed a shorter sugar side-chain, and presented a remarkably reduced V79-4 cell (Chinese hamster lung fibroblasts) cytotoxicity and erythrocyte hemolytic toxicity, whereas the nitrite-scavenging activity was increased in the modified platycodin D. Sensory scores for pungency, bitterness and after-taste were improved as well in the modified platycodin D. Results suggest that A. niger mediated modification yielded a novel partially degraded platycodin glycoside which possesses increased bioactivities and improved sensory values, yet with reduced toxic profiles.