Coumarin polysulfides inhibit cell growth and induce apoptosis in HCT116 colon cancer cells

Saidu, Nathaniel Edward Bennett; Valente, Sérgio; Bana, Emilie; Kirsch, Gilbert; Bagrel, Denyse; Montenarh, Mathias

doi:10.1016/j.bmc.2011.12.032

Cited by 63 publications

(30 citation statements)

References 41 publications

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“…Elinos-Báez et al reported that 7-hydroxycoumarin inhibits anti-apoptotic Bcl-2 expression in lung cancer cells and promotes the expression of pro-apoptotic Bcl-2-associated X protein (Bax) (8). Other studies identified that coumarin is able to induce cervical and colon cancer cell apoptosis by activating the mitochondrial pathway and the caspase-3-dependent apoptotic pathway, to downregulate the anti-apoptotic NF-κB, Bcl-2 and Bcl-xL, and upregulate caspase-3 to promote the release of cytochrome (cyt) c (9,10). The coumarin derivative psoralidin is also able to enhance the role of tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) in promoting the apoptosis and necrosis of HeLa cervical cancer cells (11).…”

Section: Introductionmentioning

confidence: 99%

7,8-Dihydroxycoumarin inhibits A549 human lung adenocarcinoma cell proliferation by inducing apoptosis via suppression of Akt/NF-κB signaling

Wang

Pan

et al. 2013

Experimental and Therapeutic Medicine

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The Akt/NF-κB pathways are involved in numerous anti-apoptotic and drug-resistance events that occur in non-small cell lung cancer (NSCLC). In the present study, the role of 7,8-dihydroxycoumarin in the regulation of the anti-apoptotic Akt and NF-κBp65 signaling pathways was explored. A549 human lung adenocarcinoma cells were exposed to 7,8-dihydroxycoumarin with a final concentration of 25, 50 and 100 μmol/l for 48 h. Quantitative polymerase chain reaction (PCR) and western blotting were performed to detect mRNA and protein expression, respectively. The MTT assay was performed to detect cell proliferation. The results demonstrated that anti-apoptotic phospho-Akt1 (pAkt1), phospho-IκBα (pIκBα), NF-κBp65 and Bcl-2 were inhibited and pro-apoptotic caspase-3 was upregulated in a concentration-dependent manner. At a concentration of 100 μmol/l, the anti-apoptotic NF-κBp65 and Bcl-2 mRNA expression levels decreased 0.12 (5.82/48.5, treated/control)-fold and 0.17 (6.7/39.4, treated/control)-fold, respectively. The pro-apoptotic caspase-3 mRNA was upregulated 4.43 (39.4/8.9, treated/control)-fold. The anti-apoptotic pAkt1, pIκBα, NF-κBp65 and Bcl-2 proteins were downregulated, with blot grayscale values of 7.3 (vs. 52.4 control), 4.3 (vs. 42.2 control), 5.08 (vs. 44.5 control) and 5.92 (vs. 38.5 control), respectively. The proapoptotic caspase-3 was upregulated to a blot grayscale value of 27.8 (vs. 5.8 control). The proliferative activity of A549 cells was reduced significantly compared with that of the control cells (83.7, 27.2 and 9.5 vs. 100%, respectively; P<0.05 for each). 7,8-Dihydroxycoumarin plays an important role in the induction of apoptosis via suppression of Akt/NF-κB signaling in A549 human lung adenocarcinoma cells in a concentration-dependent manner. 7,8-Dihydroxycoumarin may be a candidate naturally-occurring drug for the treatment and prevention of lung adenocarcinoma.

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Section: Introductionmentioning

confidence: 99%

7,8-Dihydroxycoumarin inhibits A549 human lung adenocarcinoma cell proliferation by inducing apoptosis via suppression of Akt/NF-κB signaling

Wang

Pan

et al. 2013

Experimental and Therapeutic Medicine

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“…The animal studies revealed that expressions of NF-κB, TNF-α, Stat3, NF-E2 related factor 2, IL-2, IL-1β were found to be low which were otherwise induced in the adenocarcinoma. Saidu et al (2012) investigated the novel compounds dicoumarin polysulphides for their anticancer action in HCT116 colon cancer cells. The study suggested that coumarin tetrasulphides showed best activity by accumulating the cells in G2/M phase that finally underwent apoptosis through intrinsic pathway.…”

Section: Citrus Limonoids Mechanism Of Anticancer Activity Referencesmentioning

confidence: 99%

An insight into the role of citrus bioactives in modulation of colon cancer

Kaur

2015

Journal of Functional Foods

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“…Among all these versatile biological activities, coumarins are notably accounted for their anticancer activities . There are innumerable pathways wherein coumarin triggers the cancer such as cell cycle arrest, angiogenesis inhibition, kinase inhibition, telomerase inhibition, antimitotic activity, monocarboxylate transporters inhibition, carbonic anhydrase inhibition, aromatase inhibition and sulfatase inhibition . Daphnetin, one of the coumarin derivative was found to inhibit protein kinase specifically EGF receptor including cAMP dependent protein kinase (PKA) and protein kinase C (PKC) .…”

Section: Introductionmentioning

confidence: 99%

Microwave‐Expedited Green Synthesis, Photophysical, Computational Studies of Coumarin‐3‐yl‐thiazol‐3‐yl‐1,2,4‐triazolin‐3‐ones and Their Anticancer Activity

et al. 2018

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Mild and efficient synthesis of 5‐methyl‐4‐[(2Z)‐4‐(2‐oxo‐2H‐chromen‐3‐yl)‐2‐(4‐arylimino)thiazol‐3(2H)‐yl]‐2‐(4‐aryl)‐2H‐1,2,4‐triazol‐3(4H)‐ones 7(h–s) has been developed using microwave assisted multicomponent route. The molecular structures of these novel compounds were characterized and the photophysical and thermal properties were investigated elaborately using absorption, fluorescence, fluorescence decay lifetimes and thermo gravimetric analysis. Solvatochromism was studied as a function of polarity of the solvents. The ground and excited states of electronic geometric optimizations were computed using density functional theory (DFT and TD‐DFT). The orientation of atomic orbitals and their energies were supported by HOMO‐LUMO calculations. Electrostatic potential (ESP) maps indicated the electron density predicting the reactive sites. Compounds 7(h–s) were docked into the epidermal growth factor receptor (EGFR) tyrosine kinase domain which formed a stable complex with good C‐score values. The title compounds were evaluated for their anticancer activity against A549, MDA‐MBA‐231, HeLa and K562 cancer cell lines which showed sensitivity against most of the tested compounds.

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Coumarin polysulfides inhibit cell growth and induce apoptosis in HCT116 colon cancer cells

Cited by 63 publications

References 41 publications

7,8-Dihydroxycoumarin inhibits A549 human lung adenocarcinoma cell proliferation by inducing apoptosis via suppression of Akt/NF-κB signaling

7,8-Dihydroxycoumarin inhibits A549 human lung adenocarcinoma cell proliferation by inducing apoptosis via suppression of Akt/NF-κB signaling

An insight into the role of citrus bioactives in modulation of colon cancer

Microwave‐Expedited Green Synthesis, Photophysical, Computational Studies of Coumarin‐3‐yl‐thiazol‐3‐yl‐1,2,4‐triazolin‐3‐ones and Their Anticancer Activity

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