Bergamottin, a natural furanocoumarin abundantly present in grapefruit juice, suppresses the invasiveness of human glioma cells via inactivation of Rac1 signaling

Luo, Wenzheng; Song, Zhenyu; Sun, Hongwei; Liang, Junxin; Zhao, Shanshan

doi:10.3892/ol.2017.7641

Cited by 10 publications

(10 citation statements)

References 26 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Inactivation of Rac 1 is also responsible for NF-κB inactivation [39]. Bergamottin exhibits antimetastatic behavior in U87 and U251 human glioma cells through Rac1 inactivation and MMP-9 downregulation [26].…”

Section: Nf-κb Inactivationmentioning

confidence: 99%

“…A significant advance in the investigation of the anticancer properties of furanocoumarins was the revelation of their antiproliferative activity arresting cell-cycle capture and causing cell death [ 23 , 24 , 25 ]. At the cellular levels, furanocoumarins appear to affect actin filaments, which might be valuable in metastasis prevention [ 26 ].…”

Section: Bioavailability Of Furocoumarinsmentioning

confidence: 99%

“…NF-κB and signal transducer and activator of transcription 3 (STAT3) association triggers inflammation and cancer [ 25 ]. Bergamottin enhances tumor necrosis factor (TNF) induced apoptosis in U87 and U251 via NF-κB and STAT3 inhibition [ 26 ]. The blocking of NF-κB activity by psoralen (80 μg/mL) leads to inhibition of FADD like IL-1β converting enzyme inhibitory protein (c-FLIP) and inhibitor of apoptosis proteins (IAP), activation of Bax, JNKs, and blocking G1/S phase in KBv200 and K562 [ 27 ].…”

Section: Mechanistic Insightsmentioning

confidence: 99%

See 2 more Smart Citations

Anticancer Potential of Furanocoumarins: Mechanistic and Therapeutic Aspects

Ahmed

Khan

Aschner

et al. 2020

IJMS

128

View full text Add to dashboard Cite

Cancer is one of the most extreme medical conditions in both developing and developed countries around the world, causing millions of deaths each year. Chemotherapy and/or radiotherapy are key for treatment approaches, but both have numerous adverse health effects. Furthermore, the resistance of cancerous cells to anticancer medication leads to treatment failure. The rising burden of cancer overall requires novel efficacious treatment modalities. Natural medications offer feasible alternative options against malignancy in contrast to western medication. Furanocoumarins’ defensive and restorative impacts have been observed in leukemia, glioma, breast, lung, renal, liver, colon, cervical, ovarian, and prostate malignancies. Experimental findings have shown that furanocoumarins activate multiple signaling pathways, leading to apoptosis, autophagy, antioxidant, antimetastatic, and cell cycle arrest in malignant cells. Additionally, furanocoumarins have been shown to have chemo preventive and chemotherapeutic synergistic potential when used in combination with other anticancer drugs. Here, we address different pathways which are activated by furanocoumarins and their therapeutic efficacy in various tumors. Ideally, this review will trigger interest in furanocoumarins and their potential efficacy and safety as a cancer lessening agents.

show abstract

Section: Nf-κb Inactivationmentioning

confidence: 99%

Section: Bioavailability Of Furocoumarinsmentioning

confidence: 99%

Section: Mechanistic Insightsmentioning

confidence: 99%

See 1 more Smart Citation

Anticancer Potential of Furanocoumarins: Mechanistic and Therapeutic Aspects

Ahmed

Khan

Aschner

et al. 2020

IJMS

128

View full text Add to dashboard Cite

show abstract

“…In human neuroblastoma SH-SY5Y cells, bergamot essential oils (BEOs) were also found to exhibit significant anti-proliferative effects [67] and it was hypothesized that bergamottin and 5-geranyloxy-7-methoxycoumarin may have substantially contributed to the BEO-induced anti-proliferative effects. Bergamottin also exhibited anti-invasive activity in human glioma cells through the inactivation of Rac1 activity and the downregulation of MMP-9 [68].…”

Section: Bergamottin and Cancermentioning

confidence: 99%

Pharmacological Utilization of Bergamottin, Derived from Grapefruits, in Cancer Prevention and Therapy

Arfuso

Sethi

et al. 2018

IJMS

View full text Add to dashboard Cite

Cancer still remains one of the leading causes of death worldwide. In spite of significant advances in treatment options and the advent of novel targeted therapies, there still remains an unmet need for the identification of novel pharmacological agents for cancer therapy. This has led to several studies evaluating the possible application of natural agents found in vegetables, fruits, or plant-derived products that may be useful for cancer treatment. Bergamottin is a furanocoumarin derived from grapefruits and is also a well-known cytochrome P450 inhibitor. Recent studies have demonstrated potent anti-oxidative, anti-inflammatory, and anti-cancer properties of grapefruit furanocoumarin both in vitro and in vivo. The present review focuses on the potential anti-neoplastic effects of bergamottin in different tumor models and briefly describes the molecular targets affected by this agent.

show abstract

“… 30 Bergamottin is able to suppress human glioma cells’ invasiveness through the inactivation of the Rac1 pathway. 31 Bergamottin presents an anti-tumor function in lung adenocarcinoma by the stimulation of mitochondrial membrane potential loss, cell cycle arrest, and apoptosis, and the decrease of cell invasion and migration in vitro and in vivo. 32 Bergamottin is able to inhibit lung cancer cells’ metastasis by the attenuation of epithelial-to-mesenchymal transition and several oncogenes signaling cascades.…”

Section: Discussionmentioning

confidence: 99%

Bergamottin Induces DNA Damage and Inhibits Malignant Progression in Melanoma by Modulating miR-145/Cyclin D1 Axis

Zhao¹,

Liao²

2021

OTT

View full text Add to dashboard Cite

Background Melanoma is a prevalent skin cancer with the high rate of metastasis and mortality, affecting the increasing number of people worldwide. Bergamottin (BGM) is a natural furanocoumarin derived from grapefruits and presents the potential anti-cancer activity in several tumor models. However, the role of BGM in the development of melanoma remains unclear. Here, we aimed to explore the effect of BGM on the DNA damage and progression of melanoma. Methods The effect of BGM on the melanoma progression was analyzed by CCK-8 assays, colony formation assays, transwell assays, Annexin V-FITC Apoptosis Detection Kit, cell-cycle analysis, in vivo tumorigenicity analysis. The mechanism investigation was performed using luciferase reporter gene assays, qPCR assays, and Western blot analysis. Results We identified that BGM repressed cell proliferation, migration, and invasion of melanoma cells. BGM induced cell cycle arrest at the G0/G1 phase and enhanced apoptosis of melanoma cells. The DNA damage in the melanoma cells was stimulated by the BGM treatment. Meanwhile, BGM was able to up-regulate the expression of miR-145 and miR-145 targeted Cyclin D1 in the melanoma cells. Furthermore, BGM inhibited the progression of melanoma by targeting miR-145/Cyclin D1 axis in vitro. BGM attenuated the tumor growth of melanoma in vivo. Conclusion Thus, we conclude that BGM induces DNA damage and inhibits tumor progression in melanoma by modulating the miR-145/Cyclin D1 axis. Our finding provides new insights into the mechanism by which BGM modulates the development of melanoma. BGM may be applied as a potential anti-tumor candidate for the clinical treatment of melanoma.

show abstract

Bergamottin, a natural furanocoumarin abundantly present in grapefruit juice, suppresses the invasiveness of human glioma cells via inactivation of Rac1 signaling

Cited by 10 publications

References 26 publications

Anticancer Potential of Furanocoumarins: Mechanistic and Therapeutic Aspects

Anticancer Potential of Furanocoumarins: Mechanistic and Therapeutic Aspects

Pharmacological Utilization of Bergamottin, Derived from Grapefruits, in Cancer Prevention and Therapy

Bergamottin Induces DNA Damage and Inhibits Malignant Progression in Melanoma by Modulating miR-145/Cyclin D1 Axis

Contact Info

Product

Resources

About