• 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.

• Proceedings of the Plant Resources Society of Korea Conference
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• 2012.05a
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• pp.20-20
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• 2012

Isoprenoids represent the most diverse group of metabolites, which are functionally and structurally identified in plant organism to date. Ginsenosides, glycosylated triterpenes, are considered to be the major pharmaceutically active ingredient of ginseng. Its backbones, categorized as protopanaxadiol (PPD), protopanaxatriol (PPT), and oleanane saponin, are synthesized via the isoprenoid pathway by cyclization of 2,3-oxidosqualene mediated with dammarenediol synthase or beta-amyrin synthase. The rate-limiting 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMGR), which is the first committed step enzyme catalyzes the cytoplasmic mevalonate (MVA) pathway for isoprenoid biosynthesis. DXP reductoisomerese (DXR), yields 2-C-methyl-D-erythritol 4-phosphate (MEP), is partly involved in isoprenoid biosynthesis via plastid. Squalene synthase and squalene epoxidase are involved right before the cyclization step. The triterpene backbone then undergoes various modifications, such as oxidation, substitution, and glycosylation. Here we will discuss general biosynthesis pathway for the production of ginsenoside and its modification based on their subcellular biological functions.

• Archives of Pharmacal Research
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• v.14 no.4
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• pp.352-356
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• 1991

The anti-platelet activity of ilexoside D isolated from the roots of Ilex pubescens Hook. et Arn. was investigated in in vitro and ex vivo models of platelet aggregation induced by ADP, thrombin or collagen in rats. In vitro ilexoside D inhibited more effectively platelet aggregation induced by ADP and thrombin than by collagen as compared with aspirin. Ex vivo ilexoside D also inhibited platelet aggregation induced by ADP and collagen, but not by thrombin, and the inhibitory action of ilexoside D was more effective than that of aspirin. However, in vitro ilexoside D inhibited very poorly the generation of malonyldialdehyde, which is known to be concomitantly released with thromboxane $A_2$ during platelet aggregation. These results suggest that the anti-platelet activity of ilexoside D may not be responsible for prostaglandin synthesis in platelets.

• Journal of Life Science
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• v.26 no.1
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• pp.59-67
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• 2016

Platycodon grandiflorum A. De Candolle (Korean name, ‘Doraji’) is a perennial plant containing various triterpenoid saponins. The roots of this plant have traditionally been used as a food material in Korea. Here, we prepared a fermented P. grandiflorum extract (PG). Although it was previously reported that P. grandiflorum A. extract has a variety of physiological functionalities, including anti-inflammatory and anti-oxidant activities, little is known about its vascular functions. In this study, we executed a series of experiments to identify the effect of PG on endothelial cells. PG at a high concentration (100 μg/ml) was found to induce cell detachment, whereas PG at a low concentration (0.1 μg/ml) appeared to promote cell proliferation and migration in bovine aortic endothelial cells. The cell detachment induced by the high concentration was not associated with cell death, such as apoptosis, necrosis, and autophagy. In addition, we found that PG at the high concentration formed a small vesicular structure called an endothelial microparticle (EMP). The EMP was prepared by centrifugal fractionation and determined with flow cytometry and a microscope. Interestingly, PG-induced cell detachment was found to be mediated by EMP. We furthermore determined that PG at the low concentration activated Akt, a crucial cell-signaling molecule, and then controlled cell proliferation and migration. Overall, our findings suggest that PG at low doses maintains vascular stability by promoting endothelial cell proliferation, and enhances the efficacy of wound healing by cell proliferation and migration activity.

• Journal of Haehwa Medicine
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• v.21 no.2
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• pp.63-72
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• 2013

To develop a new anti-skin aging cosmetics or functional foods by using antioxidative activity and collagenase inhibitor, a potent collagenase or elastase inhibitor was screened from various extracts of medicinal plants and its optimal extraction condition was investigated. And antioxidative activity, antimicrobial activity and inhibitory of effect against collagenase activity were investigated. In the these results, we selected the Sanguisorba (Sanguisorba officinalis L.) that presents a potential biological activities. Sanguisorba which is very rich in triterpenoid saponin and tannins was recently reported its anti-oxidant activities and phytoestogenic activities in vivo test and many clinical studies. The experiments were carried out in vitro to determine anti-oxidant activities of Sanguisorba extracts on DPPH radical scavenging activity assay, Superoxidase scavenging activity assay, Elastase and collagenase activity assay. It show that the Sanguisorba extracts have the most significant anti-oxidant on free radical scavenging activity assay, and also inhibited significantly activities of elastase, collagenase. Further, Sanguisorba extracts are activated Type I collagen protein expression in CCD-986sk cells. These result suggest that the Sanguisorba extracts on DPPH radical scavenging activity assay, Superoxidase scavenging activity assay, elastase and collagenase activity assay, Type I collagen protein expression in CCD-986sk cells effected could be developed cosmetic ingredients for anti-aging.

• KOREAN JOURNAL OF CROP SCIENCE
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• v.41 no.spc1
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• pp.123-144
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• 1996

This review deals briefly with the various medicinal components(mainly saikosaponins), their biological activities and the variation of their contents by different cultivation environment and plant parts in Bupleurum species. Bupleuri radix, a crude drug, is the root of Bupleurum falcatum L. (Korea, Japan), B. chinense(China), and their related species (Umbelliferae). There are over 120 species in Bupleurum genus throughout world, mainly Asian area, and over 5 species in Korea, investigated up to now. These plants contain many physiological active compounds and the principal components are saikosaponins. Major activities of this crude drug and saikosaponins are the anti-inflammatory and antihepatotoxic activities. Saikosaponins and their derivatives in Bupleurum spp. have been chemically studied, isolated and identified over 70 compounds in over 50 species. Other components, physiologically active ones, also have been investigated, which are the groups of lignan, flavonoid, essential oil, polyacetylene, polysaccharide, etc. Saikosaponins belong to the group of triterpenoid saponin chemotaxonomically and occur the accumulation and turnover in plant tissues through secondary metabolism, mevalonic acid pathway. The contents and kinds of saikosaponins and other components in Bupleurum spp. plants are various due to different species and growing environments, as the plant growth characters and yield are various. Most of medicinal plants as well as Bupleurum species are very useful as agricultural products and traditional medicines, and also are very valuable as genetic resources and natural products. So we need to collect, evaluate, preserve, and utilize various medicinal plants, and also to under-stand secondary metabolism and improve the breeding and cultivation techniques for the safe production of crude drugs with high quality and yielding.

• Biomolecules & Therapeutics
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• v.21 no.5
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• pp.332-337
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• 2013

Microglial activation plays an important role in the development and progression of various neurological disorders such as cerebral ischemia, multiple sclerosis, and Alzheimer's disease. Thus, controlling microglial activation can serve as a promising therapeutic strategy for such brain diseases. In the present study, we showed that kalopanaxsaponin A, a triterpenoid saponin isolated from Kalopanax pictus, inhibited inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), and tumor necrosis factor (TNF)-${\alpha}$ expression in lipopolysaccharide (LPS)-stimulated microglia, while kalopanaxsaponin A increased anti-inflammatory cytokine interleukin (IL)-10 expression. Subsequent mechanistic studies revealed that kalopanaxsaponin A inhibited LPS-induced DNA binding activities of NF-${\kappa}B$ and AP-1, and the phosphorylation of JNK without affecting other MAP kinases. Furthermore, kalopanaxsaponin A inhibited the intracellular ROS production with upregulation of anti-inflammatory hemeoxygenase-1 (HO-1) expression. Based on the previous reports that JNK pathway is largely involved in iNOS and proinflammatory cytokine gene expression via modulating NF-${\kappa}B$/AP-1 and ROS, our data collectively suggest that inhibition of JNK pathway plays a key role in anti-inflammatory effects of kalopanaxsaponin A in LPS-stimulated microglia.

• The Korean Journal of Physiology and Pharmacology
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• v.21 no.3
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• pp.279-286
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• 2017

The root bark extract of Aralia taibaiensis is used traditionally for the treatment of diabetes mellitus in China. The total saponin extracted from Aralia Taibaiensis (sAT) has effective combined antihyperglycemic and hypolipidemic activities in experimental type 2 diabetic rats. However, the active compounds have not yet been fully investigated. In the present study, we examined effects of twelve triterpenoid saponins on AMP-activated protein kinase (AMPK) activation, and found that compound 28-O-${\beta}$-D-glucopyranosyl ester (AT12) significantly increased phosphorylation of AMPK and Acetyl-CoA carboxylase (ACC). AT12 effectively decreased blood glucose, triglyceride (TG), free fatty acid (FFA) and low density lipoprotein-cholesterol (LDL-C) levels in the rat model of type 2 diabetes mellitus (T2DM). The mechanism by which AT12 activated AMPK was subsequently investigated. Intracellular ATP level and oxygen consumption were significantly reduced by AT12 treatment. The findings suggested AT12 was a novel AMPK activator, and could be useful for the treatment of metabolic diseases.

• Asian Pacific Journal of Cancer Prevention
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• v.15 no.4
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• pp.1745-1749
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• 2014

Background: Platycodin D (PD), a triterpenoid saponin isolated from the Chinese medicinal herb Platycodonis radix, possesses anti-cancer effects in several cancer cell lines. The aim of this study was to evaluate its anticancer activities in hepatocellular carcinoma cells. Materials and Methods: MTT and colony formation assays were performed to evaluate cell proliferation, along with flow cytometry and Western blotting for apoptosis. Cell adhesion was tested by observing cellular morphology under a microscope, while the transwell assay was employed to investigate the cell migration and invasion. Results: PD concentration-dependently inhibited cell proliferation in both HepG2 and Hep3B cells, and significantly suppressed colony formation and induced apoptosis in HepG2 cells. The protein levels of cleaved poly ADP-ribose polymerase (PARP) and Bax were up-regulated while that of survivin was down-regulated after treatment with PD. Moreover, PD not only obviously suppressed the adhesion of HepG2 cells to Matrigel, but also remarkably depressed their migration and invasion induced by 12-O-tetradecanoylphorbol 13-acetate (TPA). Conclusions: PD presents anti-cancer potential in hepatocellular carcinoma cells via inducing apoptosis, and inhibiting cell adhesion, migration and invasion, indicating promising features as a lead compound for anti-cancer agent development.

• The Korean Journal of Physiology and Pharmacology
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• v.21 no.6
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• pp.609-616
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• 2017

Ardipusilloside-I is a natural triterpenoid saponin, which was isolated from Ardisia pusilla A. DC. The aim of the study was to evaluate the stimulation of ardipusilloside-I on gastrointestinal motility in vitro and in vivo. The experiment of smooth muscle contraction directly monitored the contractions of the isolated jejunal segment (IJS) in different contractile states, and the effects of ardipusilloside-I on myosin were measured in the presence of $Ca^{2+}$-calmodulin using the activities of 20 kDa myosin light chain ($MLC_{20}$) phosphorylation and myosin $Mg^{2+}$-ATPase. The effects of ardipusilloside-I on gastro emptying and intestinal transit in constipation-predominant rats were observed, and the MLCK expression in jejuna of constipated rats was determined by western blot. The results showed that, ardipusilloside-I increased the contractility of IJS in a dose-dependent manner and reversed the low contractile state (LCS) of IJS induced by low $Ca^{2+}$, adrenaline, and atropine respectively. There were synergistic effects on contractivity of IJS between ardipusilloside-I and ACh, high $Ca^{2+}$, and histamine, respectively. Ardipusilloside-I could stimulate the phosphorylation of $MLC_{20}$ and $Mg^{2+}$-ATPase activities of $Ca^{2+}$- dependent phosphorylated myosin. Ardipusilloside-I also stimulated the gastric emptying and intestinal transit in normal and constipated rats in vivo, respectively, and increased the MLCK expression in the jejuna of constipation-predominant rats. Briefly, the findings demonstrated that ardipusilloside-I could effectively excite gastrointestinal motility in vitro and in vivo.