• Journal of Ginseng Research
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• v.42 no.2
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• pp.123-132
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• 2018

Ginseng has gained its popularity as an adaptogen since ancient days because of its triterpenoid saponins, known as ginsenosides. These triterpenoid saponins are unique and classified as protopanaxatriol and protopanaxadiol saponins based on their glycosylation patterns. They play many protective roles in humans and are under intense research as various groups continue to study their efficacy at the molecular level in various disorders. Ginsenosides Rb1 and Rg1 are the most abundant ginsenosides present in ginseng roots, and they confer the pharmacological properties of the plant, whereas ginsenoside Rg3 is abundantly present in Korean Red Ginseng preparation, which is highly known for its anticancer effects. These ginsenosides have a unique mode of action in modulating various signaling cascades and networks in different tissues. Their effect depends on the bioavailability and the physiological status of the cell. Mostly they amplify the response by stimulating phosphotidylinositol-4,5-bisphosphate 3-kinase/protein kinase B pathway, caspase-3/caspase-9-mediated apoptotic pathway, adenosine monophosphate-activated protein kinase, and nuclear factor kappa-light-chain-enhancer of activated B cells signaling. Furthermore, they trigger receptors such as estrogen receptor, glucocorticoid receptor, and N-methyl-$\text\tiny{D}$-aspartate receptor. This review critically evaluates the signaling pathways attenuated by ginsenosides Rb1, Rg1, and Rg3 in various tissues with emphasis on cancer, diabetes, cardiovascular diseases, and neurodegenerative disorders.

• Bulletin of the Korean Chemical Society
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• v.28 no.7
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• pp.1187-1194
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• 2007

The three major active isoflavonoids (calycosin-7-O-β -glucoside, isomucronulatol 7-O-β-glucoside, formononetin) and two main saponins (astragaloside I, astragaloside IV) in an extract of Radix Astragali were determined using rapid, sensitive, reliable HPLC/UV and LC-ESI-MS/MS methods. The separation conditions employed for HPLC/UV were optimized using a phenyl-hexyl column (4.6 × 150 mm, 5 μm) with the gradient elution of acetonitrile and water as the mobile phase at a flow rate of 1.0 mL/min and a detection wavelength of 230 nm. The specificity of the peaks was determined using a triple quadrupole tandem mass spectrometer equipped with an electrospray ionization (ESI) source that was operated in multiple reaction monitoring (MRM) in the positive mode. These methods were fully validated with respect to the linearity, accuracy, precision, recovery and robustness. The HPLC/UV method was applied successfully to the quantification of three major isoflavonoids in the extract of Radix Astragali. The results indicate that the established HPLC/UV and LC-ESI-MS/MS methods are suitable for the quantitative analysis and quality control of multi-components in Radix Astragali.

• Archives of Pharmacal Research
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• v.9 no.1
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• pp.29-38
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• 1986

The effects of ginseng saponins on the sarcolemmal $Na^{+}$, $K^{+}$-ATPase were compared to gypsophila saponin, sodium dodecylsulfate (SDS), and Triton X-100 to elucidate whether the effects are due to the membrane distruption, using a highly enriched preparation of cardiac sarcolemma prepared from dog ventricular myocardium. About 26% and 29% of vesicles in the preparation, enriched in ouabain-sensitive $Na^{+}$, $K^{+}$-ATP ase, $\beta$-adrenergic and muscarinic receptors are rightside-out and inside-out orientation, respectively. Ginseng saponins (triol>total> diol) inhibited $Na^{+}$, $K^{+}$-ATP ase activity, $Na^{+}$, $K^{+}$-ATPase activity and [$^{3}$H]ouabain binding of sarcolemmal vesicles. However, gypsophila saponin, SDS (0.4$\mu$g/$\mu$g protein) and Triton X-100 (0.6 $\mu$g/$\mu$g protein) caused about 1.35 and 1.40-fold increase in $Na^{+}$, $K^{+}$-ATPase activity and [$^{3}$H] oubain binding, respectively. Especially, the activating effect of gypsophila saponin on membrane Na+, K+ ATPase was detected at gypsophila saponin to sarcolemmal protein ratios as high as 100. Low dose of ginseng saponin (3$\mu$g/$\mu$g protein) decreased the phosphorylation sites and the concentration of ouabain binding sites (Bmax) without affecting the turnover number and affinity for ouabain binding, while gypsophila saponin, SDS(0.4 ug/ug protein), ahd Triton X-100 (0.6$\mu$g/$\mu$g protein) increased the Bmax. The results suggest that ginseng saponins cause a decrease in the number of active sites by interacting directly with $Na^{+}$, $K^{+}$-ATPase before disruption of membrane barriers of sarcolemmal vesicles.

• Asian Pacific Journal of Cancer Prevention
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• v.15 no.13
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• pp.5455-5461
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• 2014

Background: Saponins are a major active component for the traditional Chinese medicine, Rubus parvifolius L., which has shown clear antitumor activities. However, the specific effects and mechanisms of saponins of Rubus parvifolius L. (SRP) remain unclear with regard to human chronic myeloid leukemia cells. The aim of this study was to investigate inhibition of proliferation and apoptosis induction effects of SRP in K562 cells and further elucidate its regulatory mechanisms. Materials and Methods: K562 cells were treated with different concentrations of SRP and MTT assays were performed to determine cell viability. Apoptosis induction by SRP was determined with FACS and DAPI staining analysis. Western blotting was used to detect expression of apoptosis and survival related genes. Specific inhibitors were added to confirm roles of STAT3 and AMPK pathways in SRP induction of apoptosis. Results: Our results indicated that SRP exhibited obvious inhibitory effects on the growth of K562 cells, and significantly induced apoptosis. Cleavage of pro-apoptotic proteins was dramatically increased after SRP exposure. SRP treatment also increased the activities of AMPK and JNK pathways, and inhibited the phosphorylation expression level of STAT3 in K562 cells. Inhibition of the AMPK pathway blocked the activation of JNK by SRP, indicating that SRP regulated the expression of JNK dependent oon the AMPK pathway. Furthermore, inhibition of the latter significantly conferred resistance to SRP pro-apoptotic activity, suggesting involvement of the AMPK pathway in induction of apoptosis. Pretreatment with a STAT3 inhibitor also augmented SRP induced growth inhibition and cell apoptosis, further confirming roles of the STAT3 pathway after SRP treatment. Conclusions: Our results demonstrated that SRP induce cell apoptosis through AMPK activation and STAT3 inhibition in K562 cells. This suggests the possibility of further developing SRP as an alternative treatment option, or perhaps using it as adjuvant chemotherapeutic agent for chronic myeloid leukemia therapy.

• Asian Pacific Journal of Cancer Prevention
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• v.15 no.24
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• pp.10911-10916
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• 2015

Background: Tumor metastases are the main reasons for oncotherapy failure. Paris polyphylla (Chinese name: Chonglou) has traditionally been used for its anti-cancer actions. In this article, we focus on the regulation of human lung cancer A549 cell metastases and invasion by Paris polyphylla steroidal saponins (PPSS). Materials and Methods: Cell viability was evaluated in A549 cells by MTT assay. Effects of PPSS on invasion and migration were investigated by wound-healing and matrigel invasion chamber assays. Adhesion to type IV collagen and laminin was evaluated by MTT assay. Expression and protease activity of two matrix metalloproteinases (MMPs), MMP-2 and MMP-9, were analyzed by Western blotting and gelatin zymography, respectively. Results: PPSS exerted growth inhibitory effects on A549 cells, and effectively inhibited A549 cell adhesion, migration and invasion in a concentration-dependent manner. Western blotting and gelatin zymography analysis revealed that PPSS inhibited the expression and secretion of MMP-2 and MMP-9 in A549 cells. Conclusions: PPSS has the potential to suppress the migration, adhesion and invasion of A549 cells. PPSS could be a potential candidate for interventions against lung cancer metastases.

• Korean Journal of Medicinal Crop Science
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• v.9 no.1
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• pp.21-25
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• 2001

Major saponins in ginseng were analysed using reverse phase high performance liquid chromatography with binary mobile phase gradient control system instead of normal phase column. The optimum condition were as following : reverse phase column; ${\mu}{\beta}ondapak\;C_{18}$ column (Waters, $3.9mm{\times}300\;mm,\;5{\mu}m$), methyl cyanaide/water binary mobile phase gradient control system, solvent flow rate; 1.5 ml/min, and UV($203{\mu}m$ ) detector. The complete separation of ginsenoside $Rb_1,\;Rb_2,\;Rc,\;Rd,\;Re,\;Rf\;and\;Rg_1$ was achieved within 55 min. The Regression coefficients of the calibration curves for seven ginsenosides were 0.99.

• Journal of Life Science
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• v.19 no.1
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• pp.138-146
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• 2009

Garlic (Allium sativum) are an agronomically important genus because of their sulfur flavour components. The majority of the volatiles flavour principles are generated through the enzymatic hydrolysis of the non-volatile organosulfur compounds. However, these compounds may be possible sources of new novel bioacuve and therapeutic principles. Garlic has strong antioxidant activity, and epidemiological studies support the fad that diets rich of garlic may prevent some of the chronic diseases. The health cares of garlic likely arise from a wide variety of components, which may work synergistically. The chemical changes of garlic composition makes it plausible that a variation in processing can lead to acquisition of differential chemical compositions of garlic products. Especially highly unstable allicin can easily disappear during processing and are quickly transformed into a various organosulfur compounds. Various supplements of garlic, particularly aged garlic extract (AGE), are known to possess a promising antioxidant potential and are effective in prevention of chronic diseases because of the bioactive constituents. Although all of active ingredients of AGE are not elucidated, water-soluble components of AGE, including S-allylcysteine, S-allylmercaptane, steroid saponins, tetrahydro-${\beta}$-carboline derivatives, and fructosyl-arginine, appears to be associated with the pharmacological effects of AGE. Consequently, the allicin free garlic components such as S-allylcysteine, S-allylmercaptane, steroid saponins, tetrahydro-${\beta}$-carboline derivatives, and fructosyl-arginine can be applicable to standardization of the quality of commercial garlic products. This review provides an insight into garlic's biomarkers and presents evidence that they may either prevent or delay chronic disease associated with aging.

• Applied Biological Chemistry
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• v.19 no.4
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• pp.233-242
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• 1976

In this paper, new methods for the determination of the total and the individual saponin glucosides were proposed. One of them was a colorimetric method following Two-dimensional Thin layer chromatography. And the method employing Thinchrograph TFG-10 or Densitorol DMU-33C followed the separation of the saponins by means of a preparative thin layer chromatography. In accordance with the density of the chromatogram of each saponin, Thinchrogram or Densitogram of the individual saponin fraction was plotted and determined.

• Journal of Ginseng Research
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• v.40 no.4
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• pp.366-374
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• 2016

Background: In this study, we screened and identified an endophyte JG09 having strong biocatalytic activity for ginsenosides from Platycodon grandiflorum, converted ginseng total saponins and ginsenoside monomers, determined the source of minor ginsenosides and the transformation pathways, and calculated the maximum production of minor ginsenosides for the conversion of ginsenoside Rb1 to assess the transformation activity of endophyte JG09. Methods: The transformation of ginseng total saponins and ginsenoside monomers Rb1, Rb2, Rc, Rd, Rg1 into minor ginsenosides F2, C-K and Rh1 using endophyte JG09 isolated by an organizational separation method and Esculin-R2A agar assay, as well as the identification of transformed products via TLC and HPLC, were evaluated. Endophyte JG09 was identified through DNA sequencing and phylogenetic analysis. Results: A total of 32 ${\beta}$-glucosidase-producing endophytes were screened out among the isolated 69 endophytes from P. grandiflorum. An endophyte bacteria JG09 identified as Luteibacter sp. effectively converted protopanaxadiol-type ginsenosides Rb1, Rb2, Rc, Rd into minor ginsenosides F2 and C-K, and converted protopanaxatriol-type ginsenoside Rg1 into minor ginsenoside Rh1. The transformation pathways of major ginsenosides by endophyte JG09 were as follows: $Rb1{\rightarrow}Rd{\rightarrow}F2{\rightarrow}C-K$; $Rb2{\rightarrow}C-O{\rightarrow}C-Y{\rightarrow}C-K$; $Rc{\rightarrow}C-Mc1{\rightarrow}C-Mc{\rightarrow}C-K$; $Rg1{\rightarrow}Rh1$. The maximum production rate of ginsenosides F2 and C-K reached 94.53% and 66.34%, respectively. Conclusion: This is the first report about conversion of major ginsenosides into minor ginsenosides by fermentation with P. grandiflorum endophytes. The results of the study indicate endophyte JG09 would be a potential microbial source for obtaining minor ginsenosides.

• Biomedical Science Letters
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• v.26 no.2
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• pp.66-74
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• 2020

This study was carried out to investigate the protective effect of crude saponin from Platycodon grandiflorum on Clinical chemical parameters in male rats acutely exposed to 2,3,7,8-tetrachlorodibenzo-ρ-dioxin (TCDD). Crude saponin was prepared from Korean Platycodon grandiflorum with Diaion HP-20 adsorption chromatography after extraction of 80% ethanol at 75℃. The crude saponin was confirmed by thin layer chrmatography. When compared with ginseng saponins, the crude saponin had both a few number of saponins and a broad distribution. Forty male rats (200±20 g) were divided into 4 groups. Normal control (NC) group received vehicle and saline; TCDD-treated (TT) group received TCDD (40 ㎍/kg, single dose) intraperitoneally; Platycodon grandiflorum saponin (PG5 and PG10) groups received crude saponin 5 mg/kg and 10 mg/kg (p.o), respectively, for 2 weeks before 1 week of TCDD-exposure. Increase of body weight was retarded greatly by TCDD-exposure. Body weight of animals in TT group was significantly decrease after 2 days of TCDD-exposure. However, body weights of animals in PG groups increased through the experimental perimental period, although the increasing rate was slower than that of NC group. Increases in contents of blood glucose, total cholesterol and triglyceride (TG) and activities of amylase, lipase, AST, ALT and LDH by toxic action of TCDD were significantly attenuated by crude saponin from Platycodon grandiflorum (P<0.05). In conclusion, these results suggest that crude saponin prepared from Korean Platycodon grandiflorum might be a member of useful protective agents against TCDD, which is one of the environmental hormones.