Antitumor and immunomodulatory effects of ginsenoside Rh2 and its octyl ester derivative in H22 tumor-bearing mice

Chen, Fang; Sun, Yong; Zheng, Shilian; Qin, Yan; McClements, David Julian; Hu, Jiang‐Ning; Deng, Zeyuan

doi:10.1016/j.jff.2017.03.013

Cited by 53 publications

(29 citation statements)

References 40 publications

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“…Our present study herein tried to synthesize short‐chain fatty acid ester of M1 in vitro to favor the potential of different forms of ester of M1. Accordingly, in murine H22 cell test in vitro, we observed less cytotoxicity of M1‐O than M1, which is in agreement with previous study . This could be demonstrated that esterification of M1 may represent a detoxification reaction, just as cholesterol esterification .…”

supporting

confidence: 92%

“…In particular, mono‐ and dioctyl ginsenoside Rh2 was extensively investigated in previous studies. One of the main benefits of esterification of ginsenoside Rh2 was enhanced cellular uptake, which was confirmed not only in tumor cell line but also in normal counterparts . However, comparing with ginsenoside Rh2, ginsenoside M1 is universally accepted as one of the main metabolites after oral administrations of ginseng .…”

mentioning

confidence: 97%

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Octyl ester of ginsenoside compound K as novel anti‐hepatoma compound: Synthesis and evaluation on murine H22 cells in vitro and in vivo

et al. 2017

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Ginsenoside compound K (M1) is the active form of major ginsenosides deglycosylated by intestinal bacteria after oral administration. However, M1 was reported to selectively accumulate in liver and transform to fatty acid esters. Ester of M1 was not excreted by bile as M1 was, which means it was accumulated in the liver longer than M1. This study reported a synthetic method of M1-O, a mono-octyl ester of M1, and evaluated the anticancer property against murine H22 cell both in vitro and in vivo. As a result, both M1 and M1-O showed a dose-dependent manner in cytotoxicity assay in vitro. At lower dose of 12.5 μm, M1-O showed moderate detoxification. Instead, M1-O exhibited significantly higher inhibition in H22-bearing mice than M1. M1-O induced murine H22 tumor cellular apoptosis in caspase-dependent pathway given that pan-caspase inhibitor, Z-VAD-FMK, could reverse the cytotoxicity induced by M1-O. Additionally, pro- and anti-apoptosis proteins, Bcl-2 and Bax, altered and consequently induced increased expression of cleaved caspase-3. Interestingly, cyclophosphamide regimen significantly induced atrophy of spleen and thymus, main immune organs, while M1-O treatment greatly alleviated this atrophy. Collectively, we propose M1-O as a candidate for live cancer treatment.

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supporting

confidence: 92%

mentioning

confidence: 97%

Octyl ester of ginsenoside compound K as novel anti‐hepatoma compound: Synthesis and evaluation on murine H22 cells in vitro and in vivo

et al. 2017

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“…6 Structures of dammarane-type triterpenoid ginsenosides (30)(31)(32)(33) with potential anticancer activity. ly) for 15 d. This indicates that G-Rh2 mediates its antitumor activity partially through modulation of the immune system [103]. No obvious toxicity was observed in the mice used in these in vivo studies [102,103].…”

Section: Dammarane-type Triterpenoids Ii: Ginsenosidesmentioning

confidence: 76%

“…ly) for 15 d. This indicates that G-Rh2 mediates its antitumor activity partially through modulation of the immune system [103]. No obvious toxicity was observed in the mice used in these in vivo studies [102,103].…”

Section: Dammarane-type Triterpenoids Ii: Ginsenosidesmentioning

confidence: 76%

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Natural Product Triterpenoids and Their Semi-Synthetic Derivatives with Potential Anticancer Activity

Ren

Kinghorn

2019

Planta Med

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Triterpenoids are distributed widely in higher plants and are of interest because of their structural diversity and broad range of bioactivities. In particular, there is a very large literature on the propensity of a variety of triterpenoids to act as potential anticancer agents. In the present review, the anticancer potential is summarized for naturally occurring triterpenoids and their semi-synthetic derivatives, including examples of lupane-, oleanane-, ursane-, and cucurbitane-type pentacyclic triterpenoids, along with dammarane-type tetracyclic triterpenes including ginsenosides and their sapogenins and dichapetalins, which have been characterized as antitumor leads from higher plants. Preliminary structure-activity relationships and reported mechanisms of the antineoplastic-related activity are included. Prior studies for triterpenoids of plant origin are supportive of additional work being conducted on the more detailed biological and mechanistic evaluation for the progression of this type of natural products as possible cancer chemotherapeutic agents.

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Ginsenosides from Korean red ginseng modulate T cell function via the regulation of NF-AT-mediated IL-2 production

Vinh

Park

Duy

et al. 2018

Food Sci Biotechnol

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Korean red ginseng is a traditional health food frequently used to prevent or treat various diseases worldwide. In this study, we evaluated the immunomodulatory activities of eleven compounds (1-11) isolated from Korean red ginseng, focusing on T cell function. First, the effects of the eleven compounds were studied on the regulation of IL-2, a potent T cell growth factor. Compounds 5, 7, and 9 significantly increased IL-2 secretion in phorbol 12-myristate 13-acetate (PMA)/ionomycin (Io)-induced EL-4 T cells. Next, we examined the effects of compounds 5, 7, and 9 on the regulation of transcription factors related to IL-2 production in T cells. Compound 9 significantly increased the PMA/Io-induced promoter activity of nuclear factor of activated T cells (NF-AT) in EL-4 T cells, but did not have any significant effects on the promoters of NF-jB. These results suggest that compound 9 activates T cell function via the regulation of NF-AT-mediated IL-2 production.

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Antitumor and immunomodulatory effects of ginsenoside Rh2 and its octyl ester derivative in H22 tumor-bearing mice

Cited by 53 publications

References 40 publications

Octyl ester of ginsenoside compound K as novel anti‐hepatoma compound: Synthesis and evaluation on murine H22 cells in vitro and in vivo

Octyl ester of ginsenoside compound K as novel anti‐hepatoma compound: Synthesis and evaluation on murine H22 cells in vitro and in vivo

Natural Product Triterpenoids and Their Semi-Synthetic Derivatives with Potential Anticancer Activity

Ginsenosides from Korean red ginseng modulate T cell function via the regulation of NF-AT-mediated IL-2 production

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