Apoptotic effect of synthetic 2′,4′,5′-trimethoxychalcones in human K562 and Jurkat leukemia cells

Costa, Aline; Chiaradia-Delatorre, Louise Domeneghini; Bubniak, Lorena dos Santos; Mascarello, Alessandra; Marzarotto, M A L; Moraes, Ana Carolina Rabello de; Stumpf, Taisa Regina; Cordeiro, Mabel Mariela Rodríguez; Yunes, Rosendo A.; Nunes, Ricardo José; Santos-Silva, Maria Cláudia

doi:10.1007/s00044-014-1002-4

Cited by 9 publications

(6 citation statements)

References 38 publications

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“…Similar to our data, various studies demonstrated upregulation of the pro-apoptotic proteins Bax [54][55][56] and Bak [54,55] with downregulation of Bcl-2 [54,55,57] and Bcl-x [54,55,57]. Concordantly, in leukemia and cervical cancer cells, exposure to naphthyl chalcones [58], 2 ,4 ,5 -trimethoxychalcones [59] as well as coumarin-chalcone hybrids [36] induced apoptosis via the caspase-dependent pathway; the chalcones reduced Bcl-2 expression, while Bax and caspase-3 expression was upregulated, thus triggering the intrinsic pathway and inducing apoptosis.…”

Section: Discussionsupporting

confidence: 90%

Novel Nitrogen-Based Chalcone Analogs Provoke Substantial Apoptosis in HER2-Positive Human Breast Cancer Cells via JNK and ERK1/ERK2 Signaling Pathways

Rizeq

Gupta

Kheraldine

et al. 2021

IJMS

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Natural chalcones possess antitumor properties and play a role as inducers of apoptosis, antioxidants and cytotoxic compounds. We recently reported that novel nitrogen chalcone-based compounds, which were generated in our lab, have specific effects on triple-negative breast cancer cells. However, the outcome of these two new compounds on human epidermal growth factor receptor 2 (HER2)-positive breast cancer remains nascent. Thus, we herein investigated the effects of these compounds (DK-13 and DK-14) on two HER2-positive breast cancer cell lines, SKBR3 and ZR75. Our data revealed that these compounds inhibit cell proliferation, deregulate cell-cycle progression and significantly induce cell apoptosis in both cell lines. Furthermore, the two chalcone compounds cause a significant reduction in the cell invasion ability of SKBR3 and ZR75 cancer cells. In parallel, we found that DK-13 and DK-14 inhibit colony formation of both cell lines in comparison to their matched controls. On the other hand, we noticed that these two compounds can inhibit angiogenesis in the chorioallantoic membrane model. The molecular pathway analysis of chalcone compounds exposed cells revealed that these compounds inhibit the expression of both JNK1/2/3 and ERK1/2, the major plausible molecular pathways behind these events. Our findings implicate that DK-13 and DK-14 possess effective chemotherapeutic outcomes against HER2-positive breast cancer via the ERK1/2 and JNK1/2/3 signaling pathways.

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Section: Discussionsupporting

confidence: 90%

Novel Nitrogen-Based Chalcone Analogs Provoke Substantial Apoptosis in HER2-Positive Human Breast Cancer Cells via JNK and ERK1/ERK2 Signaling Pathways

Rizeq

Gupta

Kheraldine

et al. 2021

IJMS

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“…The mechanism of action involves the reduction of cell proliferation which has been shown by a reduction in the expression of cell proliferation marker Ki67. Cell death induced by 2′,4′,5′-trimethoxychalcones was due to induction of apoptosis through the reduction of the mitochondrial membrane potential, reduction in Bcl-2 expression, increase in Bax expression, increase in active caspase-3, and activating the intrinsic pathway and execution phase of apoptosis [ 16 ].…”

Section: Molecular Insights Of Anticancer Chalconesmentioning

confidence: 99%

Chalcone Scaffold in Anticancer Armamentarium: A Molecular Insight

Das

Manna

2016

Journal of Toxicology

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“…Chalcones were recrystallized from hot ethanol to obtain pure substances at yields between 53% and 98%. The structures of chalcones ( Figure 1) were confirmed through comparisons of their melting points and nuclear magnetic resonance spectra with those previously published for chalcones from A, C and P series (CHIARADIA et al, 2008a), chalcones B (NAVARINI et al, 2009;BORCHHARDT et al, 2010), chalcones D , chalcones J (COSTA et al, 2014), chalcones L and R (CHIARADIA et al, 2012), chalcones M (SALUM et al, 2013), chalcones N (MIELCKE et al, 2012 and chalcones T (CHIARADIA et al, 2008b).…”

Section: Synthesis Of Chalconesmentioning

confidence: 55%

Chalcones to control Alternaria alternata in murcott tangor fruits

Camargos¹,

Perina²,

Carvalho³

et al. 2016

Biosci. J.

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Alternaria brown spot (ABS), caused by the fungus Alternaria alternata pathotype tangerine, is one of the main phytosanitary problems for mandarin growers. About 15 applications per year of harmful fungicides are required for controlling ABS disease in citrus orchards. As chalcones seem to be less toxic to humans and environment than the commercial fungicides in use, this study initially aimed at synthesizing 137 chalcones through aldolic condensations between benzaldehydes and acetophenones. The resulting chalcones were screened for activity against A. alternata through a fungal growth assay that was carried out in 96-cell polypropylene plates, using the same concentration to all studied substances. The four active chalcones underwent conidia germination and mycelial growth, which confirmed the antifungal activity of the compounds. These chalcones were then poured onto Murcott tangor fruit that had been inoculated with conidia of the fungus. All four chalcones reduced the ABS progress to values significantly smaller (P≤0.05) than that observed for the control. Statistical calculations showed that the best results were afforded by two compounds, bearing a 2,4,5-trimethoxyphenyl group at position 3 of prop-2-enal and a 3-nitro-or 3-hydroxyphenyl group at position 1 of the aldehyde. Such compounds reduced the incidence of the disease in Murcott tangor fruit to values that did not differ statistically from those obtained with a commercial fungicide.

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Apoptotic effect of synthetic 2′,4′,5′-trimethoxychalcones in human K562 and Jurkat leukemia cells

Cited by 9 publications

References 38 publications

Novel Nitrogen-Based Chalcone Analogs Provoke Substantial Apoptosis in HER2-Positive Human Breast Cancer Cells via JNK and ERK1/ERK2 Signaling Pathways

Novel Nitrogen-Based Chalcone Analogs Provoke Substantial Apoptosis in HER2-Positive Human Breast Cancer Cells via JNK and ERK1/ERK2 Signaling Pathways

Chalcone Scaffold in Anticancer Armamentarium: A Molecular Insight

Chalcones to control Alternaria alternata in murcott tangor fruits

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