• Title/Summary/Keyword: Protopanaxadiol ginsenosides

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Increase in the Contents of Ginsenosides in Raw Ginseng Roots in Response to Exposure to 450 and 470 nm Light from Light-Emitting Diodes

  • Park, Sang-Un;Ahn, Deok-Jong;Jeon, Hyeon-Jeong;Kwon, Tae-Ryong;Lim, Hyoun-Sub;Choi, Bo-Seong;Baek, Kwang-Hyun;Bae, Han-Hong
    • Journal of Ginseng Research
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    • v.36 no.2
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    • pp.198-204
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    • 2012
  • An light-emitting diode (LED)-based light source was used as a monochromatic light source to determine the responses of raw ginseng roots (Panax ginseng Meyer) to specific emission spectra with respect to the production of ginsenosides. The ginsenoside content in the ginseng roots changed in response to the LED light treatments at $25^{\circ}C$ relative to the levels in the control roots that were treated in the dark or at $4^{\circ}C$ for 7 d. Ginseng roots were exposed to LEDs with four different peak emission wavelengths, 380, 450, 470, and 660 nm, in closed compartments. Compared with the control $4^{\circ}C$-treated roots, roots that were treated with 450 and 470 nm light showed a significantly increased production of ginsenosides (p<0.05), with increases of 64.9% and 74.1%, respectively. The contents of the ginsenosides $Rb_2$, Rc, and $Rg_1$ were significantly higher (p<0.05) in the 450 and 470 nm-treated root samples. The ratio of protopanaxadiol ginsenosides ($Rb_1$, $Rb_2$, Rc, and Rd) to protopanaxatriol ginsenosides ($Rb_1$, $Rb_2$, Re, and Rf) was significantly higher (p<0.05) in the 450 and 470 nm-treated root samples than in the control $4^{\circ}C$-treated roots. This is the first report that demonstrates the increase and conversion of ginsenosides in raw ginseng roots in response to exposure to LED light.

Non-clinical pharmacokinetic behavior of ginsenosides

  • Won, Hyo-Joong;Kim, Hyun Il;Park, Taejun;Kim, Hyeongmin;Jo, Kanghee;Jeon, Hyojin;Ha, Seo Jun;Hyun, Jung Min;Jeong, Aeri;Kim, Jung Sik;Park, Ye Jin;Eo, Yun Ho;Lee, Jaehwi
    • Journal of Ginseng Research
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    • v.43 no.3
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    • pp.354-360
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    • 2019
  • Ginsenosides, the major active ingredients of ginseng and other plants of the genus Panax, have been used as natural medicines in the East for a long time; in addition, their popularity in the West has increased owing to their various beneficial pharmacological effects. There is therefore a wealth of literature regarding the pharmacological effects of ginsenosides. In contrast, there are few comprehensive studies that investigate their pharmacokinetic behaviors. This is because ginseng contains the complicated mixture of herbal materials as well as thousands of constituents with complex chemical properties, and ginsenosides undergo multiple biotransformation processes after administration. This is a significant issue as pharmacokinetic studies provide crucial data regarding the efficacy and safety of compounds. Moreover, there have been many difficulties in the development of the optimal dosage regimens of ginsenosides and the evaluation of their interactions with other drugs. Therefore, this review details the pharmacokinetic properties and profiles of ginsenosides determined in various animal models administered through different routes of administration. Such information is valuable for designing specialized delivery systems and determining optimal dosing strategies for ginsenosides.

Ginseng saponins and the treatment of osteoporosis: mini literature review

  • Siddiqi, Muhammad Hanif;Siddiqi, Muhammad Zubair;Ahn, Sungeun;Kang, Sera;Kim, Yeon-Ju;Sathishkumar, Natarajan;Yang, Dong-Uk;Yang, Deok-Chun
    • Journal of Ginseng Research
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    • v.37 no.3
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    • pp.261-268
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    • 2013
  • The ginseng plant (Panax ginseng Meyer) has a large number of active ingredients including steroidal saponins with a dammarane skeleton as well as protopanaxadiol and protopanaxatriol, commonly known as ginsenosides, which have antioxidant, anticancer, antidiabetic, anti-adipocyte, and sexual enhancing effects. Though several discoveries have demonstrated that ginseng saponins (ginsenosides) as the most important therapeutic agent for the treatment of osteoporosis, yet the molecular mechanism of its active metabolites is unknown. In this review, we summarize the evidence supporting the therapeutic properties of ginsenosides both in vivo and in vitro, with an emphasis on the different molecular agents comprising receptor activator of nuclear factor kappa-B ligand, receptor activator of nuclear factor kappa-B, and matrix metallopeptidase-9, as well as the bone morphogenetic protein-2 and Smad signaling pathways.

Ginsenosides Inhibit Endothelium - dependent Contraction in the Spontaneously Hypertensive Rat Aorta isn vitro (선천성 고혈압 랫드에서 ginsenosides에 의한 내피의존성수축의 억제작용)

  • 김낙두;최원선
    • Journal of Ginseng Research
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    • v.21 no.2
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    • pp.125-132
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    • 1997
  • Our previous study showed that in vivo treatment of spontaneously hypertensive rats (SHR) with protopanaxatriol ginsenosides (PPT) reduces the blood pressure and inhibits the con- tractions induced by endothelium-derived contracting factor (prostaglandin endoperoxide ($PGH_2$) and superoxide anion) in aorta isolated from SHR. The aim of the present study is to examine whether PPT improves endothelial functions in the isolated thoracic aorta of SHR in vitro. Treatments of aortic rings with PPT, purified ginsenoside $Rg_1$ ($Rg_1$) or indomethacin normalized endotheliuln-dependent relaxation to acetylcholine, but not with protopanaxadiol ginsenosides (PPD) and purified ginsenoside Rb1 (Rb1). The effects of PPT were dose-dependent. PGH,- and oxygen free radical-inducted contractions in rat aorta without endothelium were inhibited by PPT or $Rg_1$, but not by PPD or $Rb_1$. Contractions induced by PGF2$\alpha$, U-46619, a stable thromboxane A2 agonist or KCI (60 mM) were not inhibited by PPT, $Rg_1$ or $Rb_1$. These findings demonstrate that PPT but not PPD scavenges the oxygen-derived free radicals and/or antagonize the effects of $PGH_2$ in the vascular smooth muscle and may explain the hypotensive effect of ginseng in the SHR.

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Ginsenoside profiles and related gene expression during foliation in Panax ginseng Meyer

  • Kim, Yu-Jin;Jeon, Ji-Na;Jang, Moon-Gi;Oh, Ji Yeon;Kwon, Woo-Saeng;Jung, Seok-Kyu;Yang, Deok-Chun
    • Journal of Ginseng Research
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    • v.38 no.1
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    • pp.66-72
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    • 2014
  • Panax ginseng is one of the most important medicinal plants in Asia. Triterpene saponins, known as ginsenosides, are the major pharmacological compounds in P. ginseng. The present study was conducted to evaluate the changes in ginsenoside composition according to the foliation stage of P. ginseng cultured in a hydroponic system. Among the three tested growth stages (closed, intermediate, and opened), the highest amount of total ginsenoside in the main and fine roots was in the intermediate stage. In the leaves, the highest amount of total ginsenoside was in the opened stage. The total ginsenoside content of the ginseng leaf was markedly increased in the transition from the closed to intermediate stage, and increased more slowly from the intermediate to opened leaf stage, suggesting active biosynthesis of ginsenosides in the leaf. Conversely, the total ginsenoside content of the main and fine roots decreased from the intermediate to opened leaf stage. This suggests movement of ginsenosides during foliation from the root to the leaf, or vice versa. The difference in the composition of ginsenosides between the leaf and root in each stage of foliation suggests that the ginsenoside profile is affected by foliation stage, and this profile differs in each organ of the plant. These results suggest that protopanaxadiol- and protopanaxatriol(PPT)-type ginsenosides are produced according to growth stage to meet different needs in the growth and defense of ginseng. The higher content of PPT-type ginsenosides in leaves could be related to the positive correlation between light and PPT-type ginsenosides.

Complete $^1H$-NMR and $^{13}C$-NMR spectral analysis of the pairs of 20(S) and 20(R) ginsenosides

  • Yang, Heejung;Kim, Jeom Yong;Kim, Sun Ok;Yoo, Young Hyo;Sung, Sang Hyun
    • Journal of Ginseng Research
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    • v.38 no.3
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    • pp.194-202
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    • 2014
  • Background: Ginsenosides, the major ingredients of Panax ginseng, have been studied for many decades in Asian countries as a result of their wide range of pharmacological properties. The less polar ginsenosides, with one or two sugar residues, are not present in nature and are produced during manufacturing processes by methods such as heating, steaming, acid hydrolysis, and enzyme reactions. $^1H$-NMR and $^{13}C$-NMR spectroscopic data for the identification of the less polar ginsenosides are often unavailable or incomplete. Methods: We isolated 21 compounds, including 10 pairs of 20(S) and 20(R) less polar ginsenosides (1-20), and an oleanane-type triterpene (21) from a processed ginseng preparation and obtained complete $^1H$-NMR and $^{13}C$-NMR spectroscopic data for the following compounds, referred to as compounds 1-21 for rapid identification: 20(S)-ginsenosides Rh2 (1), 20(R)-Rh2 (2), 20(S)-Rg3 (3), 20(R)-Rg3 (4), 6'-O-acetyl-20(S)-Rh2 [20(S)-AcetylRh2] (5), 20(R)-AcetylRh2 (6), 25-hydroxy-20(S)-Rh2 (7), 25-hydroxy-20(S)-Rh2 (8), 20(S)-Rh1 (9), 20(R)-Rh1 (10), 20(S)-Rg2 (11), 20(R)-Rg2 (12), 25-hydroxy-20(S)-Rh1 (13), 25-hydroxy-20(R)-Rh1 (14), 20(S)-AcetylRg2 (15), 20(R)-AcetylRg2 (16), Rh4 (17), Rg5 (18), Rk1 (19), 25-hydroxy-Rh4 (20), and oleanolic acid 28-O-b-D-glucopyranoside (21).

A Chemical Study of the Saponins and Flavonoids of Dwarf Ginseng (Panax trifolius L.) and Its Comparison to Related Species in the Araliaceae (왜생삼 (Panax trifolius L.)의 사포닌과 프라보노이드의 화학적 연구 및 오가과에 속하는 유연종과의 성분 비교연구)

  • Lee Taikwang M.;Marderosian Ara Der
    • Proceedings of the Ginseng society Conference
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    • 1988.08a
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    • pp.141-146
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    • 1988
  • Dwarf ginseng (Panax trifolius L.) is a member of the ginseng family (Araliaceae). which is indigenous to North America and is distributed from Southern Canada to the Northern United States. In total. nine compounds were isolated from the leaves of Dwarf gineng. Of these. four were identified as flavonoids and five were found to be ginsenosides. Two of the flavonoids were identified to be kaempferol-3. 7-dirhamnoside and kaempferol-3-gluco-7-rhamnoside. Four of the ginsenosides were identified as notoginsenoside-Fe. ginsenoside-Rd. ginsenoside-Rc and $ginsenoside-Rb_1$ The common aglycone of these ginsenosides was shown to be (20S)-protopanaxadiol. The identification of flavonoids and ginsenosides from the root. stem. leaf. flower and fruit of Dwarf ginseng was detected by Two-Dimensional Thin-Layer Chromatography (2D-TLC) and High Performance Liquid Chromatography (HPLC). The quantitation of flavonoids and ginsenosides from the root. stem. leaf. flower and fruit of Dwarf ginseng and related species such as Korean gineng (Panax ginseng C.A. Meyer) and American ginseng (Panax quinquefolium L.) was analyzed by HPLC only. Three flavonoids (Kaempferol derivatives) labelled compound 1 $(10.8\%)$, compound 3 ($2.8\%$), and compound 4 ($8.4\%)$ were found in the root of Dwarf ginseng but not found in the roots of Korean ginseng and American ginseng. This is the first time that flavonoids have been found and identified in roots of the ginseng family (Araliaceae).

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Drug-biomacromolecule interaction V

  • Kim, Chong-Kook;Ahn, Hae-Young;Han, Byung-Hoon;Hong, Soon-Keun
    • Archives of Pharmacal Research
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    • v.6 no.1
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    • pp.63-68
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    • 1983
  • The binding properties of three ginsenosides, Rb$_{1}$, Rc and Re, to bovine and human serum albumins have been examined by fluorescence probe technique. 1-anilinonphathalene-8-sulfonate (ANS) was used as the fluorescence probe. Protopanaxatriol glycoside, Re, did not quench the fluorscence of ANS to the bovine serum albumin. Competitive bindings between protopanaxadiol glycosides, Rb$_{1}$ and Rc are both 3.3 . The binding constants for Rb$_{1}$ and Rc with bovine serum albumin were 1.91 * 10$_{4}$M$_{-1}$ AND 1.04 * 10$^{[-994]}$ M$^{-1}$ , respectively. The ginsenosides, Rb$_{1}$, Rc and Re did not quench the fluorescence of ANS bound to human serum albumin.

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Molecular signaling of ginsenosides Rb1, Rg1, and Rg3 and their mode of actions

  • Mohanan, Padmanaban;Subramaniyam, Sathiyamoorthy;Mathiyalagan, Ramya;Yang, Deok-Chun
    • 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.

A comparative study on chemical composition of total saponins extracted from fermented and white ginseng under the effect of macrophage phagocytotic function

  • Xiao, Dan;Xiu, Yang;Yue, Hao;Sun, Xiuli;Zhao, Huanxi;Liu, Shuying
    • Journal of Ginseng Research
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    • v.41 no.3
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    • pp.379-385
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    • 2017
  • In this study, white ginseng was used as the raw material, which was fermented with Paecilomyces hepiali through solid culture medium, to produce ginsenosides with modified chemical composition. The characteristic chemical markers of the products thus produced were investigated using rapid resolution liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (RRLC-QTOF-MS). Chemical profiling data were obtained, which were then subjected to multivariate statistical analysis for the systematic comparison of active ingredients in white ginseng and fermented ginseng to understand the beneficial properties of ginsenoside metabolites. In addition, the effects of these components on biological activity were investigated to understand the improvements in the phagocytic function of macrophages in zebrafish. According to the established RRLC-QTOF-MS chemical profiling, the contents in ginsenosides of high molecular weight, especially malonylated protopanaxadiol ginsenosides, were slightly reduced due to the fermentation, which were hydrolyzed into rare and minor ginsenosides. Moreover, the facilitation of macrophage phagocytic function in zebrafish following treatment with different ginseng extracts confirmed that the fermented ginseng is superior to white ginseng. Our results prove that there is a profound change in chemical constituents of ginsenosides during the fermentation process, which has a significant effect on the biological activity of these compounds.