- The preparation of ginsenoside Rg5, its antitumor activity against breast cancer cells and its targeting of PI3K
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Ginsenosides have been reported to possess various pharmacological effects, including anticancer effects. Nevertheless, there are few reports about the antitumor activity and mechanisms of ginsenoside Rg5 against breast cancer cells. In the present study, the major ginsenoside Rb1 was transformed into the rare ginsenoside Rg5 through enzymatic bioconversion and successive acid-assisted high temperature and pressure processing. Ginsenosides Rb1, Rg3, and Rg5 were investigated for their antitumor effects against five human cancer cell lines via the MTT assay. Among them, Rg5 exhibited the greatest cytotoxicity against breast cancer. Moreover, Rg5 remarkably suppressed breast cancer cell proliferation through mitochondria-mediated apoptosis and autophagic cell death. LC3B-GFP/Lysotracker and mRFP-EGFP-LC3B were utilized to show that Rg5 induced autophagosome-lysosome fusion. Western blot assays further illustrated that Rg5 decreased the phosphorylation levels of PI3K, Akt, mTOR, and Bad and suppressed the PI3K/Akt signaling pathway in breast cancer. Moreover, Rg5-induced apoptosis and autophagy could be dramatically strengthened by the PI3K/Akt inhibitor LY294002. Finally, a molecular docking study demonstrated that Rg5 could bind to the active pocket of PI3K. Collectively, our results revealed that Rg5 could be a potential therapeutic agent for breast cancer treatment.
- Liu, Yannan,Fan, Daidi
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- Conversion of ginsenoside RB1 into six types of highly bioactive ginsenoside Rg3 and its derivatives by FeCl3 catalysis
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Ginsenoside Rb1 is an important saponin of ginseng(s); however, Rb1, with 3-O- and 20-O-sugar moieties, has low bioavailability. Here, we report the derivatization of ginsenoside Rb1 to completely generate six types of highly bioactive minor ginsenoside R
- Yu, Hongshan,Wang, Yu,Liu, Chunying,Yang, Jiamei,Xu, Longquan,Li, Guanheng,Song, Jianguo,Jin, Fengxie
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p. 901 - 906
(2018/09/10)
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- Manufacturing method for mass-production of 20(S)-ginsenoside Rg3
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The present invention relates to a method for selectively mass-producing 20(S)-ginsenoside Rg3 from ginsenoside Rd. The 20(S)-ginsenoside Rg3 rarely exists in white ginseng or red ginseng, and exists as an S-type isomer or an R-type isomer even though exiting in a small amount. Thus, an amount thereof refined as a single material is very low, and thus a use thereof is not easy. However, according to the present invention, 20(S)-ginsenoside Rg3 is mass-produced by using only ginsenoside Rd which can be easily separated from leaves of ginsengs, and thus addition of ginsenoside which may be generated from Rc, Re, Rf, and the like can be relatively prevented compared to when extracts of ginsengs, red ginsengs, or the like are used. A relative production amount of 20(R)-ginsenoside Rg3 is low. Thus, purification is easy, and mass-production is easy.(AA) Before steaming(BB) Example 1-1 (dry steaming, 120 anddeg;C, 2 hours, 0.13MPa)(CC) Example 1-2 (dry steaming, 120 anddeg;C, 4 hours, 0.13MPa)(DD) Example 1-3 (dry steaming, 120 anddeg;C, 6hours, 0.13MPa)COPYRIGHT KIPO 2018
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Paragraph 0029; 0031-0043
(2018/08/30)
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- Microwave degradation of floatation-enriched ginsenoside extract from Panax quinquefolium L. Leaf
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Even though the degradation of ginsenosides has been thoroughly studied in animals and in vitro using acids, enzymes, and intestinal bacteria, a new degradation method is established for obtaining the ginsenosides Rg3, Rh2 and their
- Bai, Yuping,Zhao, Lisha,Qu, Chenling,Meng, Xiangzhe,Zhang, Hanqi
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experimental part
p. 10252 - 10260
(2010/07/18)
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- The chemical and hydroxyl radical scavenging activity changes of ginsenoside-Rb1 by heat processing
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The chemical and hydroxyl radical ({radical dot}OH) scavenging activity changes of ginsenoside Rb1 (Rb1) by heat processing were investigated in this study. Rb1 was changed into 20(S)-Rg3, 20(R)-Rg3,
- Lee, Yong Jae,Kim, Hyun Young,Kang, Ki Sung,Lee, Jin Gyun,Yokozawa, Takako,Park, Jeong Hill
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body text
p. 4515 - 4520
(2009/04/08)
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- Metabolism of 20(S)- and 20(R)-ginsenoside Rg3 by human intestinal bacteria and its relation to in vitro biological activities.
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When ginsenoside Rg3 was anaerobically incubated with human fecal microflora, all specimens metabolized ginsenoside Rg3 to ginsenoside Rh2 and protopanaxadiol. The main metabolite was ginsenoside Rh2. 20(S)-ginsenoside Rg3 was quickly transformed to 20(S)
- Bae, Eun-Ah,Han, Myung Joo,Choo, Min-Kyung,Park, Sun-Young,Kim, Dong-Hyun
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- Synthesis of ginsenoside Rg3, a minor constituent of Ginseng radix.
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Glycosylation of 12beta-acetoxy-dammar-24-en-3beta,20(S)-diol (4), with hepta-O-acetyl-alpha-sophorosyl bromide (5) under catalysis by Ag2CO3 or Ag2O afforded a chromatographically unseparated mixture of the alpha- and beta-linked octaacetates 6 and 7 in an approximately 2.5:1 ratio. After deprotection and chromatographic purification, the free alpha- (8) and beta-glycosides (9) were obtained. Sophoroside 9 was identical in all respects with ginsenoside Rg3, the minor component of Ginseng Radix rubra. All compounds were fully characterized by 1H and 13C NMR spectroscopy.
- Anufriev,Malinovskaya,Denisenko,Uvarova,Elyakov,Kim,Baek
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p. 179 - 182
(2007/10/03)
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- Malonyl-ginsenosides Rb1, Rb2, Rc and Rd, four new malonylated dammarane-type triterpene oligoglycosides from Ginseng Radix
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Four new malonylated dammarane-type triterpene oligoglycosides, named malonyl-ginsenosides Rb1 (1), Rb2 (2), Rc (3), and Rd (4), were isolated from Ginseng Radix, the root of Panax ginseng, and their structures were elucidated on the basis of chemical and physicochemical evidence.
- Kitagawa,Taniyama,Hayashi,Yoshikawa
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p. 3353 - 3356
(2007/10/02)
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