Saponins as modulators of nuclear receptors

Zhang, Tiehua; Zhong, Shuning; Li, Tiezhu; Zhang, Jie

doi:10.1080/10408398.2018.1514580

Cited by 122 publications

(48 citation statements)

References 137 publications

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“…NRs comprise seven subfamilies, namely, thyroid hormone receptor-like (NR1), retinoid X receptor-like (NR2), estrogen receptor-like (NR3), nerve growth factor IB-like (NR4), steroidogenic factor-like (NR5), germ cell nuclear factor-like (NR6), miscellaneous (NR0), etc. ( Zhang et al, 2020c ). From N-terminus to C-terminus, NRs share common structure features and are composed of an activation function-1 (AF-1) domain, a DNA-binding domain (DBD), a ligand-binding domain (LBD), a ligand-dependent activation function-2 (AF-2) domain, as well as a hinge region linking the DBD and the LBD ( Figure 1 ) ( El-Gendy et al, 2018 ).…”

Section: Introductionmentioning

confidence: 99%

Natural Products Targeting Liver X Receptors or Farnesoid X Receptor

She

Pang

et al. 2022

Front. Pharmacol.

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Nuclear receptors (NRs) are a superfamily of transcription factors induced by ligands and also function as integrators of hormonal and nutritional signals. Among NRs, the liver X receptors (LXRs) and farnesoid X receptor (FXR) have been of significance as targets for the treatment of metabolic syndrome-related diseases. In recent years, natural products targeting LXRs and FXR have received remarkable interests as a valuable source of novel ligands encompassing diverse chemical structures and bioactive properties. This review aims to survey natural products, originating from terrestrial plants and microorganisms, marine organisms, and marine-derived microorganisms, which could influence LXRs and FXR. In the recent two decades (2000–2020), 261 natural products were discovered from natural resources such as LXRs/FXR modulators, 109 agonists and 38 antagonists targeting LXRs, and 72 agonists and 55 antagonists targeting FXR. The docking evaluation of desired natural products targeted LXRs/FXR is finally discussed. This comprehensive overview will provide a reference for future study of novel LXRs and FXR agonists and antagonists to target human diseases, and attract an increasing number of professional scholars majoring in pharmacy and biology with more in-depth discussion.

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Section: Introductionmentioning

confidence: 99%

Natural Products Targeting Liver X Receptors or Farnesoid X Receptor

She

Pang

et al. 2022

Front. Pharmacol.

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“…ginseng ), ginsenosides have been widely used in cancer treatment with reduced side effects [ 9 – 11 ]. Ginsenoside Rh2 can be divided into 20( S )-ginsenoside Rh2 (20( S )-Rh2) and 20( R )-ginsenoside Rh2 (20( R )-Rh2) according to different orientations of the hydroxyl group at C-20 position [ 12 , 13 ]. Tumor-associated macrophages (TAMs) are confirmed to play crucial roles in modulating the tumor microenvironment and promoting tumor metastases [ 14 ].…”

Section: Introductionmentioning

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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“…Star anise (Illicium verum, Hooker f.), a member of the Magnoliaceae or Magnolia family, is mainly distributed in southern China (Quan, 2017; Rocha, 2016). Owing to the numerous bioactive and volatile compounds, such as trans ‐anethole, estragole, and limonene from star anise essential oil (SAEO), it has the potential to be broadly used in food and medicine fields (Pranoto et al., 2005; Rocha, 2016; Tongnuanchan & Benjakul, 2014; Zhang, Zhong, Li, & Zhang, 2020). However, the hydrophobic property and instability of SAEO make the edible films lack of a continuous basal lamina and reduce the biological activity.…”

Section: Introductionmentioning

confidence: 99%

Theoretical and experimental investigation of sodium alginate composite films containing star anise ethanol extract/hydroxypropyl‐β‐cyclodextrin inclusion complex

Zhang

Guan

Zhang

et al. 2021

Journal of Food Science

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The aim of this study is to prepare composite films incorporated with star anise ethanol extract (SAEE)/hydroxypropyl‐β‐cyclodextrin (HP‐β‐CD) inclusion complex. The effects of sodium alginate concentration on mechanical properties of films are tested. Sodium alginate, SAEE, and SAEE/HP‐β‐CD inclusion complex‐based composite films are characterized in terms of UV‐visible spectroscopy, microstructure characterizations, including transmission electron microscopy, scanning electronic microscopy, Fourier transform infrared, and 1H NMR analysis, and molecular modeling calculations. With various stoichiometries, the complexes of sodium alginate/SAEE/HP‐β‐CD are compared through both theoretical and experimental analyses. Molecular simulations are applied to predict the possible orientations of SAEE inside the HP‐β‐CD cavity and the optimal stoichiometry of the complex formation. According to the simulation, the system of sodium alginate/SAEE (or SAEE/HP‐β‐CD inclusion complex) in a 3:1 stoichiometry reaches the lowest total energy and achieves a balance in complex system. In addition, the composite films can maintain high‐content vitamin C and reduce weight loss rate of fresh‐cut Chinese yam. In conclusion, coinciding with the experimental results, the molecular modeling successfully calculates the reasonable molecular structure and molecular behavior of sodium alginate/SAEE/HP‐β‐CD inclusion complex. The composite films in this study have the potential to be used for food packaging applications.Practical ApplicationIn this paper, we present composite films incorporated with star anise ethanol extract (SAEE)/hydroxypropyl‐β‐cyclodextrin (HP‐β‐CD) inclusion complex for the use of fresh‐cut Chinese yam preservation. The present study demonstrates a successful application of molecular modeling to predict the geometry of the final complex. It can serve as a powerful tool to calculate the energy of association between inclusion complex and sodium alginate molecules.

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Saponins as modulators of nuclear receptors

Cited by 122 publications

References 137 publications

Natural Products Targeting Liver X Receptors or Farnesoid X Receptor

Natural Products Targeting Liver X Receptors or Farnesoid X Receptor

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

Theoretical and experimental investigation of sodium alginate composite films containing star anise ethanol extract/hydroxypropyl‐β‐cyclodextrin inclusion complex

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