Fraxinellone: From pesticidal control to cancer treatment

Bailly, Christian; Vergoten, Gérard

doi:10.1016/j.pestbp.2020.104624

Cited by 17 publications

(12 citation statements)

References 69 publications

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“…Previous reports have confirmed the anti-inflammatory and neuroprotective effects of FRA in vivo (Hou et al, 2018;Bailly and Vergoten, 2020;Lei et al, 2020). However, there are few studies on the anti-tumor effects of FRA.…”

Section: Discussionmentioning

confidence: 81%

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Fraxinellone Has Anticancer Activity by Inducing Osteosarcoma Cell Apoptosis via Promoting Excessive Autophagy Flux

Zhang

2021

Front. Pharmacol.

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Osteosarcoma is a malignant bone tumor that is easy to metastasize in the early stage and has a very poor prognosis. Fraxinellone (FRA) is one of the main components isolated from the D. dasycarpus plant. Its anti-inflammatory and neuroprotective effects have been confirmed, but the research on the anti-cancer effect of FRA and its potential mechanism is relatively scarce. In this study, we found that FRA inhibited the proliferation and migration of osteosarcoma cells HOS and MG63 in a dose-dependent manner. Immunofluorescence, fluorescence staining and western blotting analysis showed that FRA could simultaneously induce osteosarcoma cell apoptosis and increase autophagy flux. Subsequent turnaround experiments suggested that the pro-apoptotic effect of FRA was achieved through excessive autophagy flux. The results of the xenograft orthotopic model further supported the anti-cancer effects of FRA, indicating that FRA treatment inhibited the growth of osteosarcoma, and the pro-apoptotic and autophagy effects of FRA were also proved in vivo. These studies provide new ideas for the future treatment of osteosarcoma and offer theoretical support for the anti-cancer mechanism of FRA.

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Section: Discussionmentioning

confidence: 81%

“…Fraxinellone (FRA) is a degradable limonin isolated from the root bark of the Dictamnus plant, which has relatively strong insecticidal activity (Bailly and Vergoten, 2020). In addition, the natural product also has anti-inflammatory and immunomodulatory effects (Lei et al, 2020).…”

Section: Discussionmentioning

confidence: 99%

Fraxinellone Has Anticancer Activity by Inducing Osteosarcoma Cell Apoptosis via Promoting Excessive Autophagy Flux

Zhang

2021

Front. Pharmacol.

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“…-Mazz., Scutellaria barbata D. Don, and Dictamnus dasycarpus Turcz., respectively, and all three ingredients have been reported to have some palliative effects on psoriasis ( Yang et al, 2018 ; Wu L. et al, 2020 ; Wu X. et al, 2020 ; Dimitris et al, 2020 ). Furthermore, fraxinellone, a main active ingredient in Dictamnus dasycarpus Turcz., shows potent anti-inflammatory and immunomodulatory effects that are hepatoprotective and can treat proliferative diseases ( Bailly and Vergoten, 2020 ). Additionally, osthole, a principal component of Cnidium monnieri (L.) Cusson, exerted inhibitory effects on hypoxic HCT116 cells that may be associated with eukaryotic initiation factor 2 alpha phosphorylation-mediated apoptosis and the translational repression of hypoxia-inducible factor-1 (HIF-1) ( Peng and Chou, 2022 ).…”

Section: Resultsmentioning

confidence: 99%

Banzhilian formula alleviates psoriasis-like lesions via the LCN2/MMP-9 axis based on transcriptome analysis

Xing

Yan²,

Guo³

et al. 2023

Front. Pharmacol.

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Introduction: Oral Banzhilian formula (BZLF) is effective in the clinical treatment of psoriasis. However, the effectiveness and mechanism of different drug delivery routes deserve further study.Methods: First, we established the mouse model of psoriasis using imiquimod (IMQ), and high-performance liquid chromatography (HPLC) was used for the quality control of BZLF. Secondly, Total RNA Sequencing and bioinformatics analysis were used to explore the regulatory mechanism of BZLF in improving psoriatic lesions. Finally, further verification was based on animal experiments.Results: we externally applied BZLF for skin lesions in an imiquimod-induced psoriasis mouse model and found that BZLF alleviated psoriasis-like skin lesions while inhibiting the expression of Ki67 and inflammatory factors (Il17a, Tnf-α, S100a7 and Cxcl1) in skin lesions. Transcriptome sequencing results suggested that BZLF inhibited signalling pathways closely related to psoriatic inflammation, such as the IL-17 signalling pathway, chemokine signalling pathway, TNF signalling pathway, and NF-kappa B signalling pathway, and the protein-protein interaction (PPI) network identified LCN2 as one of the core target genes and screened out its regulated downstream gene MMP9.Discussion: Our findings suggest that the anti-psoriatic mechanism of BZLF involved in downregulating the LCN2/MMP-9 axis.

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“…In addition to interfering with PD-1 and PD-L1 binding, there are some small molecules that also inhibit the expression and translation of PD-1/PD-L1 or degrade PD-1/PD-L1. For example, fraxinellone, which is isolated from the antitumor herb, Dictamnus dasycarpus , suppresses the synthesis of HIF-1α and STAT3 to reduce the expression of PD-L1, thereby restricting proliferation and angiogenesis in tumor cells 22 , 23 . In addition, translation of PD-L1 has been reported to be inhibited by eFT508 (tomivosertib).…”

Section: Small Molecule Drugs Directly Targeting Immune Checkpointsmentioning

confidence: 99%

Development of small molecule drugs targeting immune checkpoints

Chen,

Zhao,

Liu

et al. 2024

Cancer Biol Med

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Immune checkpoint inhibitors (ICIs) are used to relieve and refuel anti-tumor immunity by blocking the interaction, transcription, and translation of co-inhibitory immune checkpoints or degrading co-inhibitory immune checkpoints. Thousands of small molecule drugs or biological materials, especially antibody-based ICIs, are actively being studied and antibodies are currently widely used. Limitations, such as anti-tumor efficacy, poor membrane permeability, and unneglected tolerance issues of antibody-based ICIs, remain evident but are thought to be overcome by small molecule drugs. Recent structural studies have broadened the scope of candidate immune checkpoint molecules, as well as innovative chemical inhibitors. By way of comparison, small molecule drug-based ICIs represent superior oral bioavailability and favorable pharmacokinetic features. Several ongoing clinical trials are exploring the synergetic effect of ICIs and other therapeutic strategies based on multiple ICI functions, including immune regulation, anti-angiogenesis, and cell cycle regulation. In this review we summarized the current progression of small molecule ICIs and the mechanism underlying immune checkpoint proteins, which will lay the foundation for further exploration.

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Fraxinellone: From pesticidal control to cancer treatment

Cited by 17 publications

References 69 publications

Fraxinellone Has Anticancer Activity by Inducing Osteosarcoma Cell Apoptosis via Promoting Excessive Autophagy Flux

Fraxinellone Has Anticancer Activity by Inducing Osteosarcoma Cell Apoptosis via Promoting Excessive Autophagy Flux

Banzhilian formula alleviates psoriasis-like lesions via the LCN2/MMP-9 axis based on transcriptome analysis

Development of small molecule drugs targeting immune checkpoints

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