• Journal of Physiology & Pathology in Korean Medicine
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• v.17 no.1
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• pp.183-189
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• 2003

Platycodi Radix, the root of Platycodon grandiflorum, commonly known as Doraji, is used as a traditional oriental medicine. Extracts from the roots of P. grandiflorum have been reported to have wide ranging health benefits. We investigated the effects of an aqueous extract from the roots of P. grandiflorum (AEPG) on the cell proliferation of human lung carcinoma A549 cells in order to understand its anti-proliferative mechanism. AEPG treatment resulted in the inhibition of cell proliferation in a concentration-dependent manner. This anti-proliferative effect of A549 cells by AEPG treatment was associated with morphological changes such as membrane shrinking, cell rounding up and inhibition of cell migration. DNA flow cytometric histograms showed that populations of both Sand G2/M phase of the cell cycle were increased by AEPG treatment in a concentration-dependent manner. AEPG treatment induced a marked accumulation of tumor suppressor p53 and a concomitant induction of cyclin-dependent kinase (Cdk) inhibitor p21 and p27. In addition, SSS treatment resulted in down-regulation of Cdk2 and Cdk4 expression. The present results indicated that AEPG-induced inhibition of lung cancer cell proliferation is associated with the blockage of S to G2/M phase progression the induction of apoptosis. Taken together, these findings suggest that P. grandiflorum has strong potential for development as an agent for prevention against human lung cancer.

• Korean Journal of Medicinal Crop Science
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• v.7 no.3
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• pp.172-176
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• 1999

The saponins are considered the main effective components in Platycodon grandiflorum (Jacq.) A. DC.. In order to obtain the basic information for producing the high quality medicinal plant and processing, the crude saponin contents were analyzed with platycodi radix, the root of Platycodon grandiflorum by different cultivating years, parts, harvesting times and drying methods. The crude saponin contents were decreased by increasing cultivating years. The crude saponin contents were 2.74% in tail of root and 1.65 % in head of root, respectively. Besides, the contents of the crude saponin in cortex were 1.8 times more than that in core of root. The crude saponin contents in different harvesting times were 2.82% and 2.74% at March 10 and December 10, showing higher than that being harvested at June 10 and September 10. The crude saponin contents among drying methods were not significantly different at 5% level DMRT, but the hot air drying after steam showed the least crude saponin.

• Korean Journal of Medicinal Crop Science
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• v.10 no.3
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• pp.200-205
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• 2002

Platycodin D was isolated from n-butanol extract of Platycodi radix(Platycodon grandiflorum and identified by the spectroscopic analysis using $^1H$ and $^{13}C$ NMR techniques. A new method of analysis of platycodin D by high performance liquid chromatography(HPLC) was established using a reversed phase system with YMC-Pack ODS-AM( 250 X 4.6 mm) column and 30% acetonitrile as a mobile phase. Evaporative light scattering detector was used as detector. The kinds of extraction solvents and methods were examined to determine the efficient extraction condition and HPLC analysis was carried out to establish the optimum drying condition for the root of Platycodon grandiflorum. The contents of Platycodin D was highest as 0.083% when platycodon roots were dried at $60^{\circ}C$ using dry oven.

• 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.

• Journal of Life Science
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• v.19 no.12
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• pp.1802-1807
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• 2009

Platycodin D, a major component of Platycodi radix, is known to have various activities including anti-inflammatory, anti-hyperlipidemic, anti-tumor activities and others. Recently, it was reported that platycodin D inhibits fat accumulation and adipogenesis. The aim of this study was to investigate whether various adipogenic regulators are modulated by platycodin D treatment during the adipogenesis of 3T3-L1 cells. mRNA levels of terminal markers of adipogenesis such as ADIPOQ (adiponectin) and GLUT (glucose transporter) 4, which were quantified by real time PCR, were decreased by platycodin D treatment. mRNA expression of PPAR (peroxisome proliferator-activated receptor) $\gamma$ and C/EBP (CCAAT/enhaner binding protein) $\alpha$, which are central transcription factors of adipogenesis, were also decreased by platycodin D treatment. To elucidate the detailed molecular mechanism of platycodin D-induced inhibition of adipogenesis, we analyzed mRNA expression of upstream regulators of PPAR$\gamma$ and C/EPB$\alpha$. mRNA levels of the pro-adipogenic regulators, KROX20 and KLF (Kruppel-like factor) 15 were markedly down-regulated by platycodin D treatment. On the other hand, mRNA expression of CHOP (C/EBP homologous protein), an anti-adipogenic regulator, was significantly up-regulated by platycodin D treatment. mRNA levels of other pro-adipogenic regulators, C/EBP$\beta$ and C/EPB$\delta$, were not affected by platycodin D treatment, and another anti-adipogenic regulator, C/EBP$\gamma$ was also not affected by platycodin D treatment. Taken together, these results suggest that platycodin D-induced inhibition of adipogenesis is mediated by gene interactions including the down-regulation of pro-adipogenic regulators, KROX20 and KLF15, and the up-regulation of an anti-adipogenic regulator, CHOP.

• Journal of Life Science
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• v.23 no.3
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• pp.389-398
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• 2013

Platycodin D is a major constituent of triterpene saponins, which is found in the root of Platycodon grandiflorum, Platycodi Radix, which is widely used in traditional Oriental medicine for the treatment of many chronic inflammatory diseases. Several pharmacological effects of this compound have been reported recently, such as anti-inflammation, immunogenicity, anti-adipogenesis, lowered cholesterol, and anti-cancer activity. However, the mechanism by which this action occurs is poorly understood. In this study, we found that platycodin D greatly increased the potential of the anti-proliferative effect in various cancer cell lines. Our data revealed that platycodin D treatment resulted in a time- and concentration-response growth inhibition of U937 cells by inducing apoptosis, as evidenced by the formation of apoptotic bodies, chromatin condensation, and the accumulation of cells in the sub-G1 phase. Apoptosis induction of U937 cells by platycodin D correlated with an increase in the Bax/Bcl-2 ratio and caused the down-regulation of IAP family members. In addition, platycodin D treatment resulted in proteolytic activation of caspase-3, the concomitant degradation of poly(ADP-ribose) polymerases, and the collapse of the mitochondria membrane potential (${\Delta}{\Psi}_m$). However, the cytotoxic effects induced by platycodin D treatment were significantly inhibited by z-DEVD-fmk, a caspase-3 inhibitor, which demonstrated the important role that caspase-3 played in the observed cytotoxic effect. These findings suggest that platycodin D may be a potential chemotherapeutic agent for use in the control of human leukemia U937 cells. These findings also provided important new insights into possible molecular mechanisms of the anti-cancer activity of platycodin D.

• Nutrition Research and Practice
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• v.5 no.3
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• pp.198-204
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• 2011

Target herbal ingredient (THI) is an extract made from two herbs, Scutellariae Radix and Platycodi Radix. It has been developed as a treatment for metabolic diseases such as hyperlipidemia, atherosclerosis, and hypertension. One component of these two herbs has been reported to have anti-inflammatory, anti-hyperlipidemic, and anti-obesity activities. However, there have been no reports about the effects of the mixed extract of these two herbs on metabolic diseases. In this study, we investigated the metabolic effects of THI using a diet-induced obesity (DIO) mouse model. High-fat diet (HFD) mice were orally administered daily with 250 mg/kg of THI. After 10 weeks of treatment, the THI-administered HFD mice showed reduction of body weights and epididymal white adipose tissue weights as well as improved glucose tolerance. In addition, the level of total cholesterol in the serum was markedly reduced. To elucidate the molecular mechanism of the metabolic effects of THI in vitro, 3T3-L1 cells were treated with THI, after which the mRNA levels of adipogenic transcription factors, including C/$EBP{\alpha}$ and $PPAR{\gamma}$, were measured. The results show that the expression of these two transcription factors was down regulated by THI in a dose-dependent manner. We also examined the combinatorial effects of THI and swimming exercise on metabolic status. THI administration simultaneously accompanied by swimming exercise had a synergistic effect on serum cholesterol levels. These findings suggest that THI could be developed as a supplement for improving metabolic status.

• Korean Journal of Pharmacognosy
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• v.41 no.2
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• pp.147-152
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• 2010

The capability of the solvents for extracting the bioactive saponins from the roots of Platycodon grandiflorum (Campanulaceae) was investigated to obtain an ideal extract which contained bioactive saponins with high quality and high quantity. The content of eight representative saponins in extracts, such as deapioplatycoside E, platycoside E, platyconic acid A and platycodin D, platycodin $D_3$, platycodin $D_2$, polygalacin $D_2$, polygalacin D were analyzed simultaneousely by the modified HPLC analytical method. The validation test of the modified qualitative and quantitative analytical method employing the ELSD equipped HPLC for eight representative saponins in the roots extract of P. grandiflorum showed a good linearity, precision and accuracy. the correlation coefficient ($r^2$) values of the calbration curves for each saponins were observed to be over 0.9990. LOD and LOQ of each saponin was calculated as $0.10{\mu}g{\sim}0.40{\mu}g$ (LOD) and $0.40{\mu}g{\sim}0.80{\mu}g$ (LOQ), respectively. Recovery rates of each saponin were also calculated as over 98%, respectively. With exception of two saponins, platyconic acid A and platycodin D, The content of eight saponins in extracts was decreased proportionally to the increment of the water ratio of solvent for extraction. Consequently, as aquous alcohol was used as a solvent for extracting the saponin components from powdered roots of P. grandiflorum, the water content in the aquous alcohol was seemed to be a critical factor for extracting efficacy. The 60-80% ratio of alcohol in the aquous alcohol were deduced to be suitable and recommendable for the preparation of roots extract of P. grandiflorum which contained saponins with high quality and high quantity.