20(S)-Protopanaxadiol blocks cell cycle progression by targeting epidermal growth factor receptor

Zhang, Tiehua; Liang, Yuan; Zuo, Peng; Jing, Siyuan; Li, Tiezhu; Wang, Yongjun; Lv, Chengyu; Li, Da; Zhang, Jie; Wei, Zhengyi

doi:10.1016/j.fct.2019.111017

Cited by 28 publications

(7 citation statements)

References 54 publications

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“…7,8 Natural products have attracted considerable attention for the wide range of human health benefits. 9,10 Dihydrochalcones are important natural products, which exhibit antioxidant, anti-inflammatory, antibacterial, antidiabetic, anticancer, and cardioprotective activities. 11,12 They are mainly present in the edible species of Lithocarpus, Rubus, Malus, and Averrhoa.…”

Section: Introductionmentioning

confidence: 99%

E Se tea alleviates acetaminophen-induced liver injury by activating the Nrf2 signaling pathway

Zhang

Zhao

et al. 2022

Food Funct.

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Section: Introductionmentioning

confidence: 99%

E Se tea alleviates acetaminophen-induced liver injury by activating the Nrf2 signaling pathway

Zhang

Zhao

et al. 2022

Food Funct.

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“…Reverse transcription and PCR amplification were carried out with TransScript one-step gDNA removal and cDNA synthesis supermix kit (Transgen Biotech Co., Ltd., Beijing, China). Quantitative real-time PCR was conducted using CFX96™ real-time system (Bio-rad®, Hercules, CA, USA) along with the primer pairs listed in the past article of our team [ 20 ]. The relative expression levels of mRNA were calculated by the 2 - ΔΔ CT method normalized with the GAPDH RNA level.…”

Section: Methodsmentioning

confidence: 99%

Identification of 20(S)-Ginsenoside Rh2 as a Potential EGFR Tyrosine Kinase Inhibitor

Liang

Zhao

Zou

et al. 2022

Oxidative Medicine and Cellular Longevity

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As the main active ingredients of Panax ginseng, ginsenosides possess numerous bioactivities. Epidermal growth factor receptor (EGFR) was widely used as a valid target in anticancer therapy. Herein, the EGFR targeting activities of 20(S)-ginsenoside Rh2 (20(S)-Rh2) and the relationship of their structure-activity were investigated. Homogeneous time-resolved fluorescence assay showed that 20(S)-Rh2 significantly inhibited the activity against EGFR kinase. 20(S)-Rh2 was confirmed to effectively inhibited cell proliferation in a dose-dependent manner by MTT assay. Furthermore, quantitative real-time PCR and western blotting analysis revealed that 20(S)-Rh2 inhibited A549 cells growth via the EGFR-MAPK pathway. Meanwhile, 20(S)-Rh2 could promote cell apoptosis, block cell cycle, and reduce cell migration of A549 cells, respectively. In silico, the result suggested that both hydrophobic interactions and hydrogen-bonding interactions could contribute to stabilize their binding. Molecular dynamics simulation showed that the side chain sugar moiety of 20(S)-Rh2 was too flexible to be fixed at the active site of EGFR. Collectively, these findings suggested that 20(S)-Rh2 might serve as a potential EGFR tyrosine kinase inhibitor.

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“…GROMACS was used to assess the binding stabilities of sanguinarine and chelerythrine with GR‐LBD. Firstly, CHARMM36 all‐atom force field was used to prepare the topology of GR‐LBD [29]. The topologies of sanguinarine and chelerythrine were obtained by CGenFF server.…”

Section: Methodsmentioning

confidence: 99%

In vitro Anti‐Inflammatory Potency of Sanguinarine and Chelerythrine via Interaction with Glucocorticoid Receptor

Zhang

Liang

et al. 2020

eFood

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As quaternary benzo[c]phenanthridine alkaloids, sanguinarine and chelerythrine possess multiple biological activities including anti-inflammatory effects. They have been confirmed to regulate gene expression of inflammatory-related cytokines at transcription level. This work aims to investigate the glucocorticoid-like anti-inflammatory effects of sanguinarine and chelerythrine, which may be mediated by Glucocorticoid Receptor (GR). Firstly, the interactions of GR with sanguinarine and chelerythrine were investigated by fluorescence polarization assay and the result showed that these two alkaloids could bind to GR with potent affinities. Luciferase reporter assay showed that sanguinarine was a weak GR agonist but chelerythrine failed to induce GR transcriptional activation in HeLa cells. These two alkaloids at high concentration showed similar tumor necrosis factor-a inhibitory potency to dexamethasone in RAW 264.7 cells, indicating their anti-inflammatory effects in vitro. In addition, the results of molecular docking and dynamics simulations showed that sanguinarine and chelerythrine could bind effectively with GR and might serve as its functional ligands. In conclusion, chelerythrine was speculated to be a selective GR modulator that might exhibit GR-mediated beneficial actions with reduced side effects.

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20(S)-Protopanaxadiol blocks cell cycle progression by targeting epidermal growth factor receptor

Cited by 28 publications

References 54 publications

E Se tea alleviates acetaminophen-induced liver injury by activating the Nrf2 signaling pathway

E Se tea alleviates acetaminophen-induced liver injury by activating the Nrf2 signaling pathway

Identification of 20(S)-Ginsenoside Rh2 as a Potential EGFR Tyrosine Kinase Inhibitor

In vitro Anti‐Inflammatory Potency of Sanguinarine and Chelerythrine via Interaction with Glucocorticoid Receptor

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