Proapoptotic Activity of Achillea membranacea Essential Oil and Its Major Constituent 1,8-Cineole against A2780 Ovarian Cancer Cells

Abdalla, Ashraf N.; Shaheen, Usama; Abdallah, Qasem; Flamini, Guido; Bkhaitan, Majdi M.; Abdelhady, Mohamed; Ascrizzi, Roberta; Bader, Ammar

doi:10.3390/molecules25071582

Cited by 46 publications

(36 citation statements)

References 37 publications

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“…Treatment with up to 1 µM eucalyptol caused a dose-dependent increase in early apoptosis, while limiting necrosis. In addition, eucalyptol caused S phase arrest and dose-dependent increase in pre-G1 apoptotic events was also observed [245]. Eucalyptol induced cell death in prostate cancer cells expressing the tumor suppressor gene ANXA7.…”

Section: Eucalyptolmentioning

confidence: 79%

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Anti-Cancer Potential of Cannabinoids, Terpenes, and Flavonoids Present in Cannabis

Tomko

Whynot

Ellis

et al. 2020

Cancers

162

139

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In recent years, and even more since its legalization in several jurisdictions, cannabis and the endocannabinoid system have received an increasing amount of interest related to their potential exploitation in clinical settings. Cannabinoids have been suggested and shown to be effective in the treatment of various conditions. In cancer, the endocannabinoid system is altered in numerous types of tumours and can relate to cancer prognosis and disease outcome. Additionally, cannabinoids display anticancer effects in several models by suppressing the proliferation, migration and/or invasion of cancer cells, as well as tumour angiogenesis. However, the therapeutic use of cannabinoids is currently limited to the treatment of symptoms and pain associated with chemotherapy, while their potential use as cytotoxic drugs in chemotherapy still requires validation in patients. Along with cannabinoids, cannabis contains several other compounds that have also been shown to exert anti-tumorigenic actions. The potential anti-cancer effects of cannabinoids, terpenes and flavonoids, present in cannabis, are explored in this literature review.

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Section: Eucalyptolmentioning

confidence: 79%

“…Exhibited cytotoxic effects [148,243]. Induced apoptosis [244][245][246][247]. Induced cell cycle arrest [245,247].…”

Section: Eucalyptolmentioning

confidence: 99%

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Anti-Cancer Potential of Cannabinoids, Terpenes, and Flavonoids Present in Cannabis

Tomko

Whynot

Ellis

et al. 2020

Cancers

162

139

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“…Evading apoptosis is one of the most important hallmarks of cancer [ 54 ]. We quantified the apoptotic activity of HAA 2020 , dinaciclib, or their combination using annexin V FITC/PI, as previously mentioned [ 55 ]. MCF7 cells were seeded in 6-well plates at 5 × 10 5 cells/well.…”

Section: Methodsmentioning

confidence: 99%

Significance of Targeting VEGFR-2 and Cyclin D1 in Luminal-A Breast Cancer

et al. 2020

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The hormonal luminal-A is the most pre-dominant sub type of breast cancer (BC), and it is associated with a high level of cyclin D1 in Saudi patients. Tamoxifen is the golden therapy for hormonal BC, but resistance of cancer cells to tamoxifen contributes to the recurrence of BC due to many reasons, including high levels of AIB1 and cyclin D1. Overcoming drug resistance could be achieved by exploring alternative targetable therapeutic pathways and new drugs or combinations. The objective of this study was to determine the differentially enriched pathways in 12 samples of Saudi women diagnosed with luminal-A using the PamChip peptide microarray-based kinase activity profiling, and to compare the activity of HAA2020 and dinaciclib with tamoxifen in singles and combinations in the MCF7 luminal-A cell line. Our results of network and pathway analysis of the 12 samples highlighted the importance of VEGFR and CDKs in promoting luminal-A breast cancer. The activation of VEGF signaling via VEGFR-2 leads to activation of PI3K/AKT kinases and an increase of cell survival, and leads to activation of Hsp90, which induces the phosphorylation of FAK1, resulting in cytoskeleton remodeling. PLC-gamma 1 is also activated, leading to FAK-2 and PKC activation. Notably, the G1/S cell cycle phases and phosphorylation processes contribute to the top seven tumorigenesis processes in the 12 samples. Further, the MTT combination of HAA2020 and dinaciclib showed the best combination index (CI), was more clonogenic against MCF7 cells compared to the other combinations, and it also showed the best selectivity index (SI) in normal MRC5 cells. Interestingly, HAA2020 and dinaciclib showed a synergistic apoptotic and G1 cell cycle effect in MCF7 cells, which was supported by their synergistic CDK2, cyclin D1, and PCNA inhibition activities. Additionally, the combination showed VEGFR-2 and Hsp90 inhibition activities in MCF7 cells. The results show the significance of targeting VEGFR-2 and cyclin D1 in Saudi luminal-A breast cancer patients, and the effect of combining HAA2020 and dinaciclib on those targets in the MCF7 model. It also warrants further preclinical and in vivo investigations for the combination of HAA2020 and dinaciclib as a possible future second-line treatment for luminal-A breast cancers.

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“…After 24 h treatment. The PI-stained cells was used to analyse cells using flow cytometer (BC, FC500) 44 .…”

Section: Cell Cycle Analysismentioning

confidence: 99%

Pharmacophore-based virtual screening, synthesis, biological evaluation, and molecular docking study of novel pyrrolizines bearing urea/thiourea moieties with potential cytotoxicity and CDK inhibitory activities

Shawky

Ibrahim

Abourehab

et al. 2020

Journal of Enzyme Inhibition and Medicinal Chemistry

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In the current study, virtual screening of a small library of 1302 pyrrolizines bearing urea/thiourea moieties was performed. The top-scoring hits were synthesised and evaluated for their cytotoxicity against three cancer (MCF-7, A2780, and HT29) and one normal (MRC-5) cell lines. The results of the MTT assay revealed potent cytotoxic activities for most of the new compounds (IC 50 ¼ 0.16-34.13 lM). The drug-likeness study revealed that all the new compounds conform to Lipinski's rule. Mechanistic studies of compounds 18 b, 19a, and 20a revealed the induction of apoptosis and cell cycle arrest at the G 1 phase in MCF-7 cells. The three compounds also displayed potent inhibitory activity against CDK-2 (IC 50 ¼ 25.53-115.30 nM). Moreover, the docking study revealed a nice fitting of compound 19a into the active sites of CDK-2/6/9. These preliminary results suggested that compound 19a could serve as a promising scaffold in the discovery of new potent anticancer agents.

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Proapoptotic Activity of Achillea membranacea Essential Oil and Its Major Constituent 1,8-Cineole against A2780 Ovarian Cancer Cells

Cited by 46 publications

References 37 publications

Anti-Cancer Potential of Cannabinoids, Terpenes, and Flavonoids Present in Cannabis

Anti-Cancer Potential of Cannabinoids, Terpenes, and Flavonoids Present in Cannabis

Significance of Targeting VEGFR-2 and Cyclin D1 in Luminal-A Breast Cancer

Pharmacophore-based virtual screening, synthesis, biological evaluation, and molecular docking study of novel pyrrolizines bearing urea/thiourea moieties with potential cytotoxicity and CDK inhibitory activities

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