• Title/Summary/Keyword: ginsenoside compound K

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Changes in Growth Characteristics, Biological Activity and Active Compound Contents in Ginseng of Different Ages (재배년수에 따른 인삼의 생육특성, 생리활성, 성분의 변화)

  • Moon, Ji Won;Jang, In Bae;Yu, Jin;Jang, In Bok;Seo, Su Jeoung;Lee, Sung Woo
    • Korean Journal of Medicinal Crop Science
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    • v.27 no.6
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    • pp.383-389
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    • 2019
  • Background: Ginseng has been used as a medicine and functional food since ancient times. It is a perennial crop, and its whose commercial valuse increases with growing period and is affected by the atmosphere and soil environment. Methods and Results: In a selected field, we measured air temperature under a shade structure and soil physicochemical properties, and determied plant and root growth as well as ginsenoside and total polyphenol content of one- to five-year-old ginsengs plants. Although air temperature above 30℃ was recored for more than 37 days, no marked growth inhibition of ginseng was detected. Among all soil physicochemical properties, except for pH, were within the allowable range the shortage increases with ginseng years. In five-year-old ginseng, the quantity is about 9.7% higher than the average weight by standard, indicating that is not affected by temperature when grown under a shade structure. Three-year-old ginseng contained the highest total ginsenoside and total polyphenol levels and exhibited the greatest DPPH radical scavenging activity. Conclusions: The total ginsenoside and protopanaxadiol/protopanaxatriol ratio were both low at five-year-old ginseng plants, which was attributed to rapid growth of the root system in five-year-oid plants. There were no significant differences in total polyphenol content and antioxidant activity between.

Enzymatic bioconversion of ginseng powder increases the content of minor ginsenosides and potentiates immunostimulatory activity

  • Park, Jisang;Kim, Ju;Ko, Eun-Sil;Jeong, Jong Hoon;Park, Cheol-Oh;Seo, Jeong Hun;Jang, Yong-Suk
    • Journal of Ginseng Research
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    • v.46 no.2
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    • pp.304-314
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    • 2022
  • Background: Ginsenosides are biologically active components of ginseng and have various functions. In this study, we investigated the immunomodulatory activity of a ginseng product generated from ginseng powder (GP) via enzymatic bioconversion. This product, General Bio compound K-10 mg solution (GBCK10S), exhibited increased levels of minor ginsenosides, including ginsenoside-F1, compound K, and compound Y. Methods: The immunomodulatory properties of GBCK10S were confirmed using mice and a human natural killer (NK) cell line. We monitored the expression of molecules involved in immune responses via enzyme-linked immunosorbent assay, flow cytometry, NK cell-targeted cell destruction, quantitative reverse-transcription real-time polymerase chain reaction, and Western blot analyses. Results: Oral administration of GBCK10S significantly increased serum immunoglobulin M levels and primed splenocytes to express pro-inflammatory cytokines such as interleukin-6, tumor necrosis factor-α, and interferon-γ. Oral administration of GBCK10S also activated NK cells in mice. Furthermore, GBCK10S treatment stimulated a human NK cell line in vitro, thereby increasing granzyme B gene expression and activating STAT5. Conclusion: GBCK10S may have potent immunostimulatory properties and can activate immune responses mediated by B cells, Th1-type T cells, and NK cells.

Development of New Materials of Ginseng by Nanoparticles

  • Yang, Deok Chun;Mathiyalagan, Ramya;Yang, Dong Uk;Perez, Zuly Elizabeth Jimenez;Hurh, Joon;Ahn, Jong Chan
    • Proceedings of the Plant Resources Society of Korea Conference
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    • 2018.04a
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    • pp.3-3
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    • 2018
  • For centuries, Panax ginseng Meyer (Korean ginseng) has been widely used as a medicinal herb in Korea, China, and Japan. Ginsenosides are a class of triterpene saponins and recognized as the bioactive components in Korean ginseng. Ginsenosides, which can be classified broadly as protopanaxadiols (PPD), protopanaxatriols (PPT), and oleanolic acids, have been shown to flaunt a vast array of pharmacological activities such as immune-modulatory, anti-inflammatory, anti-tumor, anti-diabetic, and antioxidant effects. In recent years, a number of ginseng and ginsenoside researches have increasingly gained wide attention owing to its unique pharmacological properties. Although good efficacies of ginsenosides have been reported, lack of target specific delivery into tumor sites, low solubility, and low bioavailability due to modifications in gastro-intestinal environments limit their biomedical application in clinical trials. As a result to this major challenge, nanotechnology and drug delivery techniques play a significant role to solve this problematic issue. Thus, we reported the preparation of poly-ethylene glycol (PEG) and glycol chitosan (GC) functionalized to ginsenoside (Compound K and PPD) conjugates via hydrolysable ester bonds with improved aqueous solubility and pH-dependent drug release. In vitro cytotoxicity assays revealed that PEG-CK, and PPD-CK conjugates exhibited lower cytotoxicity compared to bare CK and PPD in HT29 cells. However, GC-CK conjugates exhibited higher and similar cytotoxicity in HT29 and HepG2 cells. Furthermore, GC-CK-treated RAW264.7 cells did not exhibit significant cell death at higher concentration of treatment which supports the biocompatibility of the polymer conjugates. They also inhibited nitric oxide production in lipopolysaccharide (LPS)-induced RAW64.7 cells. In addition to polymer-ginsenoside conjugates, silver (AgNps) and gold nanoparticles (AuNps) have been successfully synthesized by green chemistry using different m. The biosynthesized nanoparticles demonstrated antimicrobial efficacy, anticancer, anti-inflammatory, antioxidant activity, biofilm inhibition, and anticoagulant effect. Special interest on the effective delivery methods of ginsenoside to treatment sites is the focus of metal nanoparticle research.In short, nano-sizing of ginsenoside results in an increased water solubility and bioavailability. The use of nano-sized ginsenoside and P. ginseng mediated metallic nanoparticles is expected to be effective on medical platform against various diseases in the future.

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Fermentation of red ginseng extract by the probiotic Lactobacillus plantarum KCCM 11613P: ginsenoside conversion and antioxidant effects

  • Jung, Jieun;Jang, Hye Ji;Eom, Su Jin;Choi, Nam Soon;Lee, Na-Kyoung;Paik, Hyun-Dong
    • Journal of Ginseng Research
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    • v.43 no.1
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    • pp.20-26
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    • 2019
  • Background: Ginsenosides, which are bioactive components in ginseng, can be converted to smaller compounds for improvement of their pharmacological activities. The conversion methods include heating; acid, alkali, and enzymatic treatment; and microbial conversion. The aim of this study was to determine the bioconversion of ginsenosides in fermented red ginseng extract (FRGE). Methods: Red ginseng extract (RGE) was fermented using Lactobacillus plantarum KCCM 11613P. This study investigated the ginsenosides and their antioxidant capacity in FRGE using diverse methods. Results: Properties of RGE were changed upon fermentation. Fermentation reduced the pH value, but increased the titratable acidity and viable cell counts of lactic acid bacteria. L. plantarum KCCM 11613P converted ginsenosides $Rb_2$ and $Rb_3$ to ginsenoside Rd in RGE. Fermentation also enhanced the antioxidant effects of RGE. FRGE reduced 2,2-diphenyl-1-picrylhydrazyl radical scavenging activity and reducing power; however, it improved the inhibition of ${\beta}$-carotene and linoleic acid oxidation and the lipid peroxidation. This suggested that the fermentation of RGE is effective for producing ginsenoside Rd as precursor of ginsenoside compound K and inhibition of lipid oxidation. Conclusion: This study showed that RGE fermented by L. plantarum KCCM 11613P may contribute to the development of functional food materials.

Inhibitory Effects of 12 Ginsenosides on the Activities of Seven Cytochromes P450 in Human Liver Microsomes

  • Jo, Jung Jae;Shrestha, Riya;Lee, Sangkyu
    • Mass Spectrometry Letters
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    • v.7 no.4
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    • pp.106-110
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    • 2016
  • Ginseng, a traditional herbal drug, has been used in Eastern Asia for more than 2000 years. Various ginsenosides, which are the major bioactive components of ginseng products, have been shown to exert numerous beneficial effects on the human body when co-administered with drugs. However, this may give rise to ginsenoside-drug interactions, which is an important research consideration. In this study, acassette assay was performed the inhibitory effects of 12 ginsenosides on seven cytochrome P450 (CYP) isoforms in human liver microsomes (HLMs) using LC-MS/MS to predict the herb-drug interaction. After incubation of the 12 ginsenosides with seven cocktail CYP probes, the generated specific metabolites were quantified by LC-MS/MS to determine their activities. Ginsenoside Rb1 and F2 showed strong selective inhibitory effect on CYP2C9-catalyzed diclofenac 4'-hydroxylation and CYP2B6-catalyzed bupropion hydroxylation, respectively. Ginsenosides Rd showed weak inhibitory effect on the activities of CYP2B6, 2C9, 2C19, 2D6, 3A4, and compound K, while ginsenoside Rg3 showed weak inhibitory effects on CYP2B6. Other ginsenosides, Rc, Rf, Rg1, Rh1, Rf, and Re did not show significant inhibitory effects on the activities of the seven CYPs in HLM. Owing to the poor absorption of ginsenosides after oral administration in vivo, ginsenosides may not have significant side effects caused by interaction with other drugs.

Ginsenoside Rb1 and compound K improve insulin signaling and inhibit ER stress-associated NLRP3 inflammasome activation in adipose tissue

  • Chen, Weijie;Wang, Junlian;Luo, Yong;Wang, Tao;Li, Xiaochun;Li, Aiyun;Li, Jia;Liu, Kang;Liu, Baolin
    • Journal of Ginseng Research
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    • v.40 no.4
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    • pp.351-358
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    • 2016
  • Background: This study was designed to investigate whether ginsenoside Rb1 (Rb1) and compound K (CK) ameliorated insulin resistance by suppressing endoplasmic reticulum (ER) stress-induced inflammation in adipose tissue. Methods: To induce ER stress, epididymal adipose tissue from mice or differentiated 3T3 adipocytes were exposed to high glucose. The effects of Rb1 and CK on reactive oxygen species production, ER stress, TXNIP/NLRP3 inflammasome activation, inflammation, insulin signaling activation, and glucose uptake were detected by western blot, emzyme-linked immunosorbent assay, or fluorometry. Results: Rb1 and CK suppressed ER stress by dephosphorylation of $IRE1{\alpha}$ and PERK, thereby reducing TXNIP-associated NLRP3 inflammasome activation in adipose tissue. As a result, Rb1 and CK inhibited IL-$1{\beta}$ maturation and downstream inflammatory factor IL-6 secretion. Inflammatory molecules induced insulin resistance by upregulating phosphorylation of insulin receptor substrate-1 at serine residues and impairing insulin PI3K/Akt signaling, leading to decreased glucose uptake by adipocytes. Rb1 and CK reversed these changes by inhibiting ER stress-induced inflammation and ameliorating insulin resistance, thereby improving the insulin IRS-1/PI3K/Akt-signaling pathway in adipose tissue. Conclusion: Rb1 and CK inhibited inflammation and improved insulin signaling in adipose tissue by suppressing ER stress-associated NLRP3 inflammation activation. These findings offered novel insight into the mechanism by which Rb1 and CK ameliorate insulin resistance in adipose tissue.

Differential effects of ginsenoside metabolites on slowly activating delayed rectifier K+ and KCNQ1 K+ channel currents

  • Choi, Sun-Hye;Lee, Byung-Hwan;Kim, Hyeon-Joong;Jung, Seok-Won;Hwang, Sung-Hee;Nah, Seung-Yeol
    • Journal of Ginseng Research
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    • v.37 no.3
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    • pp.324-331
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    • 2013
  • Channels formed by the co-assembly of the KCNQ1 subunit and the mink (KCNE1) subunit underline the slowly activating delayed rectifier $K^+$ channels ($I_{Ks}$) in the heart. This $K^+$ channel is one of the main pharmacological targets for the development of drugs against cardiovascular disease. Panax ginseng has been shown to exhibit beneficial cardiovascular effects. In a previous study, we showed that ginsenoside Rg3 activates human KCNQ1 $K^+$ channel currents through interactions with the K318 and V319 residues. However, little is known about the effects of ginsenoside metabolites on KCNQ1 $K^+$ alone or the KCNQ1 + KCNE1 $K^+$ ($I_{Ks}$) channels. In the present study, we examined the effect of protopanaxatriol (PPT) and compound K (CK) on KCNQ1 $K^+$ and $I_{Ks}$ channel activity expressed in Xenopus oocytes. PPT more strongly inhibited the $I_{Ks}$ channel currents than the currents of KCNQ1 $K^+$ alone in concentration- and voltage-dependent manners. The $IC_{50}$ values on $I_{Ks}$ and KCNQ1 alone currents for PPT were $5.18{\pm}0.13$ and $10.04{\pm}0.17{\mu}M$, respectively. PPT caused a leftward shift in the activation curve of $I_{Ks}$ channel activity, but minimally affected KCNQ1 alone. CK exhibited slight inhibition on $I_{Ks}$ and KCNQ1 alone $K^+$ channel currents. These results indicate that ginsenoside metabolites show limited effects on $I_{Ks}$ channel activity, depending on the structure of the ginsenoside metabolites.

Changes in the ginsenoside content during the fermentation process using microbial strains

  • Lee, So Jin;Kim, Yunjeong;Kim, Min-Gul
    • Journal of Ginseng Research
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    • v.39 no.4
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    • pp.392-397
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    • 2015
  • Background: Red ginseng (RG) is processed from Panax ginseng via several methods including heat treatment, mild acid hydrolysis, and microbial conversion to transform the major ginsenosides into minor ginsenosides, which have greater pharmaceutical activities. During the fermentation process using microbial strains in a machine for making red ginseng, a change of composition occurs after heating. Therefore, we confirmed that fermentation had occurred using only microbial strains and evaluated the changes in the ginsenosides and their chemical composition. Methods: To confirm the fermentation by microbial strains, the fermented red ginseng was made with microbial strains (w-FRG) or without microbial strains (n-FRG), and the fermentation process was performed to tertiary fermentation. The changes in the ginsenoside composition of the self-manufactured FRG using the machine were evaluated using HPLC, and the 20 ginsenosides were analyzed. Additionally, we investigated changes of the reducing sugar and polyphenol contents during fermentation process. Results: In the fermentation process, ginsenosides Re, Rg1, and Rb1 decreased but ginsenosides Rh1, F2, Rg3, and Compound Y (C.Y) increased in primary FRG more than in the raw ginseng and RG. The content of phenolic compounds was high in FRG and the highest in the tertiary w-FRG. Moreover, the reducing sugar content was approximately three times higher in the tertiary w-FRG than in the other n-FRG. Conclusion: As the results indicate, we confirmed the changes in the ginsenoside content and the role of microbial strains in the fermentation process.

Anti-inflammatory activity and toxicity of the compound K produced by bioconversion (생물전환에 의해 생성된 Compound K의 항염증 및 독성 효과)

  • Kim, MooSung;Shin, Hyun Young;Kim, Hyun-Gyeong;Kang, Ji Sung;Jung, Kyung-Hwan;Yu, Kwang-Won;Moon, Gi-Seong;Lee, Hyang-Yeol
    • Journal of the Korean Applied Science and Technology
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    • v.38 no.6
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    • pp.1466-1475
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    • 2021
  • Compound K (20-O-β-(D-glucopyranosyl)-20(S)-protopanaxadiol) is an active ingredient of ginsenosides. Compound K has been known to produce from biotransformation by β-glucosidase action of human intestinal microbes after oral admistration of ginseng. We have investigated the cytotoxicity of compound K obtained from bio-converted ginseng extract. As a result, compound K showed no significant cytotoxicity in the concentration of 0.001 to 1 ㎍/mL and inhibited the production of TNF-α, MCP-1, IL-6 and NO in RAW 264.7 cells induced by LPS inflamation. In the same concentration, HaCaT cells induced by inflammation with TNF-α and IFN-γ decreased IL-8 production due to compound K treatment. In the brine shrimp lethality assay, the LC50 of compound K was 0.37 mg/mL indicating some toxicity, but the bioconverted product containing 35% compound K showed relatively low toxicity with an LC50 of 0.87 mg/mL. These results suggest that the compound K enriched extract is a potential functional material for acne relief cosmetic products.