Prosopis juliflora leave extracts induce cell death of MCF-7, HepG2, and LS-174T cancer cell lines

Elbehairi, Serag Eldin I.; Ahmed, Ahmed Ezzat; Alshati, Ali; Alkahtani, Mohammed Ali; Alfaifi, Mohammad Y.; Alsyaad, Khalid M.; Alalmie, Ali Yahya A.; Ahamed, Mohammed M Elimam; Moustafa, Mahmoud; Alhag, Sadeq K.; Al‐Abd, Ahmed M.; Abbas, Ahmed M.

doi:10.17179/excli2020-2830

Cited by 7 publications

(4 citation statements)

References 29 publications

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“…The most promising compounds ( 10 and 13 ) were explored for cell cycle distribution to determine the intracellular mode of action of these compounds. The cells and vehicle control were treated with each pre calculated IC 50 s for 48 h, were stained with propidium iodide, and observed for cell cycle distribution by flow cytometry [ 33 ]. As shown in Figure 2 , compound 10- treated A549 cells increased the G1 and G2 phase from 32.88 ± 2.04% to 34.66 ± 2.80% and from 29.13 ± 2.31% to 33.01 ± 2.28%, respectively, but decreased the cell distribution in the S phase from 38.48 ± 3.71% to 32.32 ± 1.51%, compared to the control cells.…”

Section: Resultsmentioning

confidence: 99%

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Cell Cycle Arrest and Apoptosis-Inducing Ability of Benzimidazole Derivatives: Design, Synthesis, Docking, and Biological Evaluation

et al. 2022

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In the current study, new benzimidazole-based 1,3,4-oxadiazole derivatives have been synthesized and characterized by NMR, IR, MS, and elemental analysis. The final compounds were screened for cytotoxicity against MDA-MB-231, SKOV3, and A549 cell lines and EGFR for inhibitory activities. Compounds 10 and 13 were found to be the most active against all the tested cell lines, comparable to doxorubicin, and exhibited significant inhibition on EGFR kinase, with IC50 0.33 and 0.38 μM, respectively, comparable to erlotinib (IC50 0.39 μM). Furthermore, these two compounds effectively suppressed cell cycle progression and induced cell apoptosis in MDA-MB-231, SKOV3, and A549 cell lines. The docking studies revealed that these compounds showed interactions similar to erlotinib at the EGFR site. It can be concluded that the synthesized molecules effectively inhibit EGFR, can arrest the cell cycle, and may trigger apoptosis and therefore, could be used as lead molecules in the development of new anticancer agents targeting EGFR kinase.

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Section: Resultsmentioning

confidence: 99%

“…The analysis was performed according to our previously published work [ 33 ]. Details regarding the procedure are provided in the Supplementary Material .…”

Section: Methodsmentioning

confidence: 99%

Cell Cycle Arrest and Apoptosis-Inducing Ability of Benzimidazole Derivatives: Design, Synthesis, Docking, and Biological Evaluation

et al. 2022

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“…The effect of selected compounds on cell cycle phase distribution was determined by flow cytometry using the same protocol described elsewhere [ 44 ]. Briefly, MCF-7, A549, and SKOV3 followed the same protocol displayed by Elbehairi et al [ 44 ].…”

Section: Methodsmentioning

confidence: 99%

In Vitro and In Silico Evaluation of Antiproliferative Activity of New Isoxazolidine Derivatives Targeting EGFR: Design, Synthesis, Cell Cycle Analysis, and Apoptotic Inducers

Alminderej,

Ghannay,

Elsamani

et al. 2023

Pharmaceuticals

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A series of novel enantiopure isoxazolidine derivatives were synthesized and evaluated for their anticancer activities against three human cancer cell lines such as human breast carcinoma (MCF-7), human lung adenocarcinoma (A-549), and human ovarian carcinoma (SKOV3) by employing MTT assay. The synthesized compounds were characterized by NMR and elemental analysis. Results revealed that all the synthesized compounds displayed significant inhibition towards the tested cell lines. Among them, 2g and 2f, which differ only by the presence of an ester group at the C-3 position and small EDG (methyl) at the C-5 position of the phenyl ring (2g), were the most active derivatives in attenuating the growth of the three cells in a dose-dependent manner. The IC50 for 2g were 17.7 ± 1 µM (MCF-7), 12.1 ± 1.1 µM (A-549), and 13.9 ± 0.7 µM (SKOV3), and for 2f were 9.7 ± 1.3µM (MCF-7), 9.7 ± 0.7µM (A-549), and 6.5 ± 0.9µM (SKOV3), respectively, which were comparable to the standard drug, doxorubicin. The enzymatic inhibition of 2f and 2g against EGFR afforded good inhibitory activity with IC50 of 0.298 ± 0.007 μM and 0.484 ± 0.01 µM, respectively, close to the positive control, Afatinib. Compound 2f arrested the cell cycle in the S phase in MCF-7 and SKOV3 cells, and in the G2/M phase in the A549 cell; however, 2g induced G0/G1 phase cell cycle arrest, and inhibited the progression of the three cancer cells, together with significant apoptotic effects. The docking study of compounds 2f and 2g into EGFR ATP-active site revealed that it fits nicely with good binding affinity. The pharmacokinetic and drug-likeness scores revealed notable lead-like properties. At 100 ns, the dynamic simulation investigation revealed high conformational stability in the EGFR binding cavity.

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“…The cells were rinsed once using PBS and five times using distilled water. The full procedure was conducted as described by Elbehairi and his coworkers ( Elbehairi et al, 2020 ).…”

Section: Methodsmentioning

confidence: 99%

Bioactivity and molecular docking of lactones isolated from Centaurea pseudosinaica Czerep

Alamri¹,

Sobahi²,

Althagbi³

et al. 2023

Saudi Pharmaceutical Journal

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Prosopis juliflora leave extracts induce cell death of MCF-7, HepG2, and LS-174T cancer cell lines

Cited by 7 publications

References 29 publications

Cell Cycle Arrest and Apoptosis-Inducing Ability of Benzimidazole Derivatives: Design, Synthesis, Docking, and Biological Evaluation

Cell Cycle Arrest and Apoptosis-Inducing Ability of Benzimidazole Derivatives: Design, Synthesis, Docking, and Biological Evaluation

In Vitro and In Silico Evaluation of Antiproliferative Activity of New Isoxazolidine Derivatives Targeting EGFR: Design, Synthesis, Cell Cycle Analysis, and Apoptotic Inducers

Bioactivity and molecular docking of lactones isolated from Centaurea pseudosinaica Czerep

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