Evaluation of chemopreventive action of Ginsenoside Rp1

Kumar, Ashok; Kumar, Madhu; Panwar, M. S.; Samarth, Ravindra M.; Park, Tae Yoon; Park, Myung Hwan; Kimura, Hiroshi

doi:10.1002/biof.5520260104

Cited by 21 publications

(26 citation statements)

References 43 publications

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“…In addition, Rg3 has recently been used as a new anti-tumor drug in China, and reported to exhibit anti-angiogenic and anti-tumor activities such as the regulation of tumor invasion and metastasis (Yue et al, 2006). Ginsenoside Rp1, a semi-synthesized Rg3 derivative, is known to be more stable and less toxic, and has stronger anti-tumor activity than Rg3 (Kumar et al, 2006;Park et al, 2008;Kim and Cho, 2009;Kumar et al, 2009). However, no detailed mechanisms of G-Rp1 responsible for regulation of tumor growth and progression have been clearly reported to date.…”

Section: Discussionmentioning

confidence: 99%

“…G-Rp1 of 97% purity was prepared using established protocols (Kumar et al, 2006;Park et al, 2008). The stock solution (10 mM) of G-Rp1 was dissolved in 100% dimethyl sulfoxide.…”

Section: Reagentsmentioning

confidence: 99%

“…Previous studies have reported that ginsenoside Rp1 (GRp1) possesses the potential chemopreventive and antimetastatic activities (Kumar et al, 2006;Park et al, 2008;Kumar et al, 2009). These studies suggest that G-Rp1 can alter the signaling pathways and sequentially regulate the ex-www.biomolther.org pression and/or activation of cell mitogenesis-related proteins.…”

Section: G-rp1 Inhibition Of Cell Proliferation Is Mediated By Inductmentioning

confidence: 99%

See 2 more Smart Citations

Ginsenoside Rp1 Inhibits Proliferation and Migration of Human Lung Cancer Cells

Hong¹,

Cho²,

Seo³

2011

Biomolecules and Therapeutics

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Section: Discussionmentioning

confidence: 99%

“…G-Rp1 of 97% purity was prepared using established protocols (Kumar et al, 2006;Park et al, 2008). The stock solution (10 mM) of G-Rp1 was dissolved in 100% dimethyl sulfoxide.…”

Section: Reagentsmentioning

confidence: 99%

Section: G-rp1 Inhibition Of Cell Proliferation Is Mediated By Inductmentioning

confidence: 99%

See 1 more Smart Citation

Ginsenoside Rp1 Inhibits Proliferation and Migration of Human Lung Cancer Cells

Hong¹,

Cho²,

Seo³

2011

Biomolecules and Therapeutics

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“…Furthermore, Rp1 has C 20 -dehydroxy and saturated side chains whereas Rg3, Rg5 and Rh2 have unsaturated double bonds (17). Rp1 has been shown to have chemopreventive effects on mouse skin papilloma (18). Rp1 is proved to be 10x more active and is more stable than Rg3 and Rh2.…”

Section: Introductionmentioning

confidence: 99%

“…All other chemicals were obtained from Nakalai Tesque (Kyoto, Japan). Rp1 was prepared as reported (17,18). Briefly, ginsenoside Rg5 was prepared in a high yield by citric acid hydrolysis of protopanaxadiol ginsenosides fraction in ethanol, and followed by silica gel column chromatographic purification.…”

Section: Introductionmentioning

confidence: 99%

Molecular mechanisms of ginsenoside Rp1-mediated growth arrest and apoptosis

Kumar

Kumar²,

Park³

et al. 2009

Int J Mol Med

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Abstract. Ginsenoside Rp1, a semi-synthesized ginseng saponin, was shown to have chemopreventive action and antimetastatic potential. However, the molecular mechanisms of Rp1 on cell growth and death are not fully understood. In this study, the antiproliferative effect of Rp1 on HeLa cells in vitro was investigated. Treatment with Rp1 at 40 μM inhibited the proliferation and partial accumulation of cells at the G1 phase. Rp1-mediated G1 arrest was accompanied by decreased expression of cyclin D1, E, and A and increased expression of p21 without any significant change in p53 or phospho-p53 (Ser15). On the other hand, prolonged incubation with Rp1 at 40 μM caused apoptosis and activation of caspase-3, -8, and -9. The participation of these three caspases in apoptosis was more clearly shown in experiments using inhibitors, which markedly prevented Rp1-induced apoptosis in the case of each caspase. Cleavage of the polyADP-ribose polymerase, often used as an apoptotic marker, was also found in Rp1-induced apoptosis. Among Bcl-2 family proteins (Bad, Bax, Bid, Bcl-2), Bax and Bid were activated by Rp1 treatment, which resulted in the release of cytochrome c from mitochondria, following activation of caspase-9. These observations indicate that multiple cell cycle regulatory proteins and apoptosis-inducing proteins are regulated by Rp1 and contribute to Rp1-induced growth arrest and apoptosis. IntroductionA number of plant glycosides were reported to have biological activities (1-4). The chronic intake of Panax ginseng C.A.Meyer has been associated with a decreased incidence of cancers that lack organ specificity, as well as cancers of the lung, stomach, liver, colorectum, and pancreas (5,6). Panax ginseng ingredients with anticarcinogenic and antimutagenic activities were identified as minor components in red ginseng (steamed and air-dried Panax ginseng) including ginsenosides Rg3, Rg5 and Rh2 (7,8). The molecular mechanisms of active ingredients were also studied (9-13). Among ginsenosides, Rg3 was developed as an anticancer drug for treating lung and liver cancers in China (14). Ginsenoside Rg5 showed more potent chemopreventive and antitumor action than ginsenoside Rg3 (7,15), but was somewhat unstable in a pure form (16). Therefore, we need to synthesize ginsenosides Rp1 [3-O-ß-D-Glucopyranosyl (1→2)-ß-D-glucopyranosyl dammarane-3ß, 12ß-diol] with chemopreventive activity and stability, to improve the anti-tumor activity of Rg3 and its congeners by chemical modifications.Various types of ginsenosides consist of totally different molecules on the basis of their chemical structure, such as the number of sugars attached to the backbone and part of the side chain of the molecules. Furthermore, Rp1 has C 20 -dehydroxy and saturated side chains whereas Rg3, Rg5 and Rh2 have unsaturated double bonds (17). Rp1 has been shown to have chemopreventive effects on mouse skin papilloma (18). Rp1 is proved to be 10x more active and is more stable than Rg3 and Rh2. Ginsenoside Rp1 was prepared on a large scale and high yield as a ...

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Ginsenoside Rp1 from Panax ginseng Exhibits Anti-cancer Activity by Down-regulation of the IGF-1R/Akt Pathway in Breast Cancer Cells

Kang

Song

Woo

et al. 2011

Plant Foods Hum Nutr

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Cancer prevention is effective and reduces health care costs because cancer is often a preventable disease that can be affected by lifestyle factors. Therefore, researchers are interested in discovering natural compounds that have anticancer activities, such as delaying the development of cancer and preventing its progression. One such natural agent is ginseng (Panax ginseng), which is traditionally used in some parts of the world as a popular remedy for various diseases including cancer. We hypothesized that the ginsenoside Rp1, a component of ginseng, reduces cancer cell proliferation through inhibition of the insulin-like growth factor 1 receptor (IGF-1R)/Akt pathway. We first tested the efficacy of Rp1 against human breast cancer cell lines. Treatment with Rp1 inhibited breast cancer cell proliferation and inhibited both anchorage-dependent and -independent breast cancer cell colony formation. In addition, treatment with 20 μM Rp1 induced cycle arrest and apoptosis-mediated cell growth suppression. Our findings further indicated that Rp1 decreased the stability of the IGF-1R protein in breast cancer cells. Therefore, we suggest that Rp1 has potential as an anticancer drug and that IGF-1R is an important target for treatment and prevention of breast cancer.

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Evaluation of chemopreventive action of Ginsenoside Rp1

Cited by 21 publications

References 43 publications

Ginsenoside Rp1 Inhibits Proliferation and Migration of Human Lung Cancer Cells

Ginsenoside Rp1 Inhibits Proliferation and Migration of Human Lung Cancer Cells

Molecular mechanisms of ginsenoside Rp1-mediated growth arrest and apoptosis

Ginsenoside Rp1 from Panax ginseng Exhibits Anti-cancer Activity by Down-regulation of the IGF-1R/Akt Pathway in Breast Cancer Cells

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