The in Vitro Structure-Related Anti-Cancer Activity of Ginsenosides and Their Derivatives

Dong, Hang; Bai, Li; Wong, Vincent Kam Wai; Zhou, Hua; Wang, Jing Rong; Liu, Yan; Jiang, Zhi‐Hong; Liu, Liang

doi:10.3390/molecules161210619

Cited by 79 publications

(57 citation statements)

References 15 publications

(14 reference statements)

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…The tumor suppressive ability of G-Rh2 is related to the inhibition of cell proliferation and metastasis, and induction of apoptosis . However, studies using different cell line models have reported conflicting data (Choi et al, 2011;Dong et al, 2011;Chung et al, 2013;Tang et al, 2013;Fatmawati et al, 2014;Guo et al, 2014;You et al, 2014a). We previously reported that G-Rh2 can inhibit the proliferation of human lung adenocarcinoma A549 cells as well as cause cell cycle arrest in the G1 phase in a dose-dependent manner.…”

Section: Introductionmentioning

confidence: 99%

JNK pathway and relative transcriptional factor were involved in ginsenoside Rh2-mediated G1 growth arrest and apoptosis in human lung adenocarcinoma A549 cells

et al. 2016

View full text Add to dashboard Cite

ABSTRACT. Ginsenoside Rh2 has been shown to have an antitumor effect on a wide range of cancers. A previous study has shown that ginsenoside Rh2 can inhibit the proliferation of the human lung adenocarcinoma A549 cell line in a dose-dependent manner by activating caspase-8/3 activity to promote apoptosis. However, the association of the JNK signaling pathways and transcription factors with ginsenoside Rh2 in the suppression of non-small cell lung cancer has not yet been reported. In this study, we found that ginsenoside Rh2 can activate the JNK/MAPKs signaling pathway and increase the phosphorylation and transcriptional activity of the transcription factors AP-1 and ATF2. Ginsenoside Rh2 also reduced the expression of transcription factors E2F1 and c-Myc. Furthermore, ginsenoside Rh2 affected the expression levels of cyclin D1 and the CDK4 protein, which are key regulatory factors of the G1/S cyclin-dependent kinase. The anti-proliferative and induced apoptotic effects of ginsenoside Rh2 on A549 cell provide evidence to support the application of traditional Chinese medicine to lung cancer treatment.

show abstract

Section: Introductionmentioning

confidence: 99%

JNK pathway and relative transcriptional factor were involved in ginsenoside Rh2-mediated G1 growth arrest and apoptosis in human lung adenocarcinoma A549 cells

et al. 2016

View full text Add to dashboard Cite

show abstract

“…Moreover, the pharmacological effects of PPD are similar to or stronger than those of Rh2 and Rg3 (Hasegawa et al, 2000;Lee et al, 2000;Popovich & Kitts, 2004). Previous studies indicated that PPD showed powerful pleiotropic anti-cancer effects in several cancer cell lines and the capability of inhibiting metastasis (Li et al, 2006;Liu et al, 2007;Dong et al, 2011;Zhu et al, 2011), thus becomes a potential therapeutic agent in the prevention and treatment of cancer (Popovich & Kitts, 2002;Yu et al, 2007;Usami et al, 2008). As such, it is currently undergoing phase I clinical trials in China.…”

Section: (S)-protopanaxadiol (Ppd) Is Mainly Derived From Ginsengmentioning

confidence: 99%

A nanoparticulate drug-delivery system for 20(S)-protopanaxadiol: formulation, characterization, increased oral bioavailability and anti-tumor efficacy

Han

et al. 2015

Drug Delivery

View full text Add to dashboard Cite

As with many other hydrophobic anticancer agents, 20(S)-protopanaxadiol (PPD) has a very low oral bioavailability. In this study, a precipitation-combined ultrasonication technique was used to prepare PPD nanosuspensions. The mean particle size of the nanosuspensions was approximately 222 ± 12 nm, the drug payload achieved 50% after lyophilization and the maximum PPD concentration can reach 100 mg/ml, which is over 30 000 times the solubility of PPD in aqueous solution (3 mg/ml). After oral administration, the C max and AUC last values of PPD nanosuspensions were approximately 3.66-fold and 3.48-fold as those of PPD coarse suspensions, respectively. In contrast to the free drug solution, PPD nanosuspensions showed higher in vitro anti-tumor activity against HepG-2 cells (an IC 50 value of 1.40 versus 5.83 mg/ml at 24 h, p50.01). The in vivo study in H22-tumor-bearing mice demonstrated that PPD nanosuspensions showed good anti-tumor efficacy with an inhibition rate of 79.47% at 100 mg/kg, while 50 mg/kg of cyclophosphamide was displayed as positive control, and the inhibition rate was 87.81%. Considering the highest drug payload, oral bioavailability reported so far, significant anti-tumor efficacy and excellent safety of encapsulated drugs, PPD nanosuspensions could be used in potential effective strategies for anticancer therapy; further investigation is ongoing.

show abstract

“…16 For example, the less polar ginsenosides demonstrate higher cytotoxic activity against several cancer cells. 14,17 Despite established anti-neoplastic properties of ginsenosides, a link between ginseng sapogenins structure and its anticancer activity as well as its mode of action in TN breast cancer has not been established. Hence, we designed this study to compare the anti-cancer effects of PPD, PPT, 2H-PPD, and 2H-PPT in TN breast cancer by using MDA-MB-231 cells.…”

mentioning

confidence: 99%

Inhibitory effects of ginseng sapogenins on the proliferation of triple negative breast cancer MDA-MB-231 cells

Kwak

Park

Lee

et al. 2014

Bioorganic & Medicinal Chemistry Letters

View full text Add to dashboard Cite

The in Vitro Structure-Related Anti-Cancer Activity of Ginsenosides and Their Derivatives

Cited by 79 publications

References 15 publications

JNK pathway and relative transcriptional factor were involved in ginsenoside Rh2-mediated G1 growth arrest and apoptosis in human lung adenocarcinoma A549 cells

JNK pathway and relative transcriptional factor were involved in ginsenoside Rh2-mediated G1 growth arrest and apoptosis in human lung adenocarcinoma A549 cells

A nanoparticulate drug-delivery system for 20(S)-protopanaxadiol: formulation, characterization, increased oral bioavailability and anti-tumor efficacy

Inhibitory effects of ginseng sapogenins on the proliferation of triple negative breast cancer MDA-MB-231 cells

Contact Info

Product

Resources

About