- 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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- Blank mixed micelle, and preparation method and applications thereof
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The invention discloses blank mixed micelle, and a preparation method and applications thereof. The blank mixed micelle comprises an amphiphilic copolymer and ginsenoside represented by formula I, ishigh in efficiency, is safe, is stable, is high in targeting performance, is excellent in homogeneity, is stable in quality, is convention in preparation technology, can be used for coating one or a plurality of active substances in drugs or cosmetics and health care substances, and is capable of forming mixed micelle containing loaded active substances. Compared with conventional nanometer micelle, the blank mixed micelle possesses following advantages: the mixed micelle loaded with active substances is excellent in drug forming performance, multiple drug resistance, stability, homogeneity, and safety performance, and is small in particle size; and the curative effect of loaded active drugs on drug resistant cells is better.
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Paragraph 0231; 0232; 0233; 0234
(2018/09/08)
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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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p. 4515 - 4520
(2009/04/08)
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