8-Chrysoeriol, as a potential BCL-2 inhibitor triggers apoptosis of SW1990 pancreatic cancer cells

Zhang, Yiwen; Li, Zhimei; Min, Qiuxia; Abulizi, Palida; Zhang, Yiyuan; Tang, Ruotian; Chen, Lixia; Li, Hua

doi:10.1016/j.bioorg.2018.01.042

Cited by 26 publications

(17 citation statements)

References 22 publications

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“…Docking experiments and enzymatic assays have demonstrated that chrysoeriol is able also to bind and inhibit two kinases, VEGFR2 (vascular endothelial growth factor 2) and c-Met, both important for tumor progression and resistance to drugs [149]. 8-chrysoeriol, a derivate of chrysoeriol, can promote apoptosis by binding to the BH3 domain of Bcl2 antiapoptotic proteins, that are highly expressed in cancer cells, blocking their activity and inducing cells death [150]. Only few mechanistic studies were carried out, using breast cancer, myeloma, and lung carcinoma cell lines.…”

Section: Chrysoeriolmentioning

confidence: 99%

Citrus Flavones: An Update on Sources, Biological Functions, and Health Promoting Properties

Barreca

Mandalari

Calderaro

et al. 2020

Plants

101

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Citrus spp. are among the most widespread plants cultivated worldwide and every year millions of tons of fruit, juices, or processed compounds are produced and consumed, representing one of the main sources of nutrients in human diet. Among these, the flavonoids play a key role in providing a wide range of health beneficial effects. Apigenin, diosmetin, luteolin, acacetin, chrysoeriol, and their respective glycosides, that occur in concentrations up to 60 mg/L, are the most common flavones found in Citrus fruits and juices. The unique characteristics of their basic skeleton and the nature and position of the substituents have attracted and stimulated vigorous investigations as a consequence of an enormous biological potential, that manifests itself as (among other properties) antioxidant, anti-inflammatory, antiviral, antimicrobial, and anticancer activities. This review analyzes the biochemical, pharmacological, and biological properties of Citrus flavones, emphasizing their occurrence in Citrus spp. fruits and juices, on their bioavailability, and their ability to modulate signal cascades and key metabolic enzymes both in vitro and in vivo. Electronic databases including PubMed, Scopus, Web of Science, and SciFinder were used to investigate recent published articles on Citrus spp. in terms of components and bioactivity potentials.

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Section: Chrysoeriolmentioning

confidence: 99%

Citrus Flavones: An Update on Sources, Biological Functions, and Health Promoting Properties

Barreca

Mandalari

Calderaro

et al. 2020

Plants

101

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“…Strategies to inhibit Bcl-2-like proteins include the use of antisense oligonucleotides, antibodies, peptides or small molecule inhibitors, each of which with their pros and cons have recently been fully reviewed in literature [39,92,104]. Among these strategies, due to their smaller size and high specificity to bind to the three-dimensional structurally conserved hydrophobic cleft present on anti-apoptotic Bcl-2 family proteins [92], the use of BH3-domain-mimicking peptides looks like the most promising alternative [39] and has led to the development of a series of small molecules that bind to the hydrophobic cleft of anti-apoptotic Bcl2-proteins as competitive inhibitors [104] that are currently under different clinical and preclinical stages of development for cancer treatment [39,89,91,105]. (Figure 5) (Table 6 and Table 7).…”

Section: Bcl-2 As a Target For Cancer Treatmentmentioning

confidence: 99%

Bcl-2 Inhibition to Overcome Resistance to Chemo- and Immunotherapy

García-Aranda

Pérez-Ruiz

Redondo

2018

IJMS

119

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According to the World Health Organization (WHO), cancer is a leading cause of death worldwide. The identification of novel targets for cancer treatment is an area of intense work that has led Bcl-2 over-expression to be proposed as one of the hallmarks of cancer and Bcl-2 inhibition as a promising strategy for cancer treatment. In this review, we describe the different pathways related to programmed cell death, the role of Bcl-2 family members in apoptosis resistance to anti-cancer treatments, and the potential utility of Bcl-2 inhibitors to overcome resistance to chemo- and immunotherapy.

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“…Using molecular docking, several bioactive compounds from Annona muricata Linn were shown to be potential inhibitors of anti-apoptotic proteins, such as Bcl-2, Bcl-w and Mcl-1 (Mohamad Rosdi et al, 2018). In a structure-based virtual ligand screening, 8-chrysoeriol, a bioactive flavonoid, was identified to bind directly to Bcl-2, similar to BH3 mimetics, and to trigger apoptosis in pancreatic cancer cells (Zhang et al, 2018). Our results verified that ALO could target the anti-apoptotic protein Bcl-2 in glioma cells but not in other cancer cells.…”

Section: Discussionmentioning

confidence: 99%

Identification of Aloperine as an anti-apoptotic Bcl2 protein inhibitor in glioma cells

Wei

Chen

et al. 2019

PeerJ

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Objective Aloperine (ALO), an alkaloid isolated from the leaves of Sophora alopecuroides, has been suggested to exhibit anti-inflammatory and anti-tumor properties and is traditionally used to treat various human diseases, including cancer. However, limited information is available about the mechanisms that determine the anti-tumor activities of ALO. Methods Herein, through comprehensive bioinformatics methods and in vitro functional analyses, we evaluated the detailed anti-tumor mechanisms of ALO. Results Using the databases Bioinformatics analysis tool for molecular mechanism of traditional Chinese medicine and PubChem Project, we identified the potential targets of ALO. A protein–protein interaction network was constructed to determine the relationship among these probable targets. Functional enrichment analysis revealed that ALO is potentially involved in the induction of apoptosis. In addition, molecular docking demonstrated that ALO expectedly docks into the active pocket of the Bcl2 protein, suggesting Bcl2 as a direct target of ALO. Moreover, western blot and qPCR analysis showed that ALO downregulated Bcl2 expression in human glioma cell lines, SK-N-AS and U118. Using flow cytometry methods, we further confirmed that ALO significantly promotes apoptosis in SK-N-AS and U118 cell lines, similar to the effect induced by ABT-737, a well-known Bcl2 inhibitor. In addition, Bcl-2 overexpression could rescue ALO-induced Bcl-2 inhibition and suppress pro-apoptotic effects in glioma cells. Conclusion Taken together, these findings suggest that the natural agent ALO effectively enhances apoptosis by acting as a potential Bcl2 inhibitor in human glioma cells.

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8-Chrysoeriol, as a potential BCL-2 inhibitor triggers apoptosis of SW1990 pancreatic cancer cells

Cited by 26 publications

References 22 publications

Citrus Flavones: An Update on Sources, Biological Functions, and Health Promoting Properties

Citrus Flavones: An Update on Sources, Biological Functions, and Health Promoting Properties

Bcl-2 Inhibition to Overcome Resistance to Chemo- and Immunotherapy

Identification of Aloperine as an anti-apoptotic Bcl2 protein inhibitor in glioma cells

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