Apoptotic and antioxidant effects in HCT-116 colorectal carcinoma cells by a spiro-acridine compound, AMTAC-06

Duarte, Sâmia Sousa; Silva, Daiana Karla Frade; Lisboa, Thaís; Gouveia, Rildésia S. V.; Andrade, Camyla Caroliny Neves de; Sousa, Valgrícia Matias de; Ferreira, Rafael Carlos; Moura, Ricardo Olímpio de; Gomes, Joilly Nilce Santana; Silva, Patrícia Mirella da; Azeve, Fátima de Lourdes Assunção Araújo de; Keesen, Tatjana Souza Lima; Gonçalves, Juan Carlos Ramos; Batista, Leônia Maria; Sobral, Marianna Vieira

doi:10.1007/s43440-022-00357-0

Cited by 10 publications

(7 citation statements)

References 50 publications

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“…These HaCaT cells are human epidermal keratinocytes that were used for the investigation of multistep carcinogenesis in human cells [57]. This cell line was chosen as a control based on its extensive use as a model for colorectal cancer research up to this point [58][59][60][61][62].…”

Section: Discussionmentioning

confidence: 99%

In Vitro Assessment of the Synergistic Effect of Aspirin and 5-Fluorouracil in Colorectal Adenocarcinoma Cells

et al. 2023

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Although remarkable progress has been made, colorectal cancer remains a significant global health issue. One of the most challenging aspects of cancer treatment is the resistance of tumor cells to classical chemotherapy. Conventional therapy for colorectal cancer often involves the use of 5-fluorouracil as a chemotherapeutic agent. Aspirin, a drug used primarily to prevent cardiovascular complications, became a focus of attention due to its potential use as an antitumor agent. The purpose of the study was to evaluate the potential synergistic cytotoxic effects of aspirin and 5-fluorouracil on colorectal adenocarcinoma cells. The viability of cells, the impact on the morphology and nuclei of cells, the potential antimigratory effect, and the impact on the expression of the major genes associated with cell apoptosis (Bcl-2, Bax, Bad), as well as caspases 3 and 8, were evaluated. The results indicated that the two compounds exerted a synergistic effect, causing a reduction in cell viability accompanied by changes characteristic of the apoptosis process—the condensation of nuclei and the reorganization of actin filaments in cells, the reduction in the expression of the Bcl-2 gene, and the increase in the expression of Bax and Bad genes, along with caspases 3 and 8. Considering all these findings, it appears that aspirin may be investigated in depth in order to be used in conjunction with 5-fluorouracil to increase antitumor activity.

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Section: Discussionmentioning

confidence: 99%

In Vitro Assessment of the Synergistic Effect of Aspirin and 5-Fluorouracil in Colorectal Adenocarcinoma Cells

et al. 2023

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“…Acridine-based agents represent a family of heterocyclic compounds which are currently undergoing significant research because of their potential anticancer activity. The pleiotropic mechanism of the antiproliferative effect of acridine derivatives, including topoisomerase II inhibition [ 57 ], cell cycle arrest in S phase [ 58 ] and G2/M phase [ 59 ], tubulin polymerization inhibition [ 60 ], DNA damage [ 61 ] and apoptosis induction [ 58 ] have been documented.…”

Section: Discussionmentioning

confidence: 99%

Chalcone-Acridine Hybrid Suppresses Melanoma Cell Progression via G2/M Cell Cycle Arrest, DNA Damage, Apoptosis, and Modulation of MAP Kinases Activity

Gazdova

Michalková

Kello

et al. 2022

IJMS

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This study was focused on investigating the antiproliferative effects of chalcone hybrids in melanoma cancer cells. Among seven chalcone hybrids, the chalcone-acridine hybrid 1C was the most potent and was selected for further antiproliferative mechanism studies. This in vitro study revealed the potent antiproliferative effect of 1C via cell cycle arrest and apoptosis induction. Cell cycle arrest at the G2/M phase was associated with modulation of expression or phosphorylation of specific cell cycle-associated proteins (cyclin B1, p21, and ChK1), tubulins, as well as with the activation of the DNA damage response pathway. Chalcone 1C also induced apoptosis accompanied by mitochondrial dysfunction evidenced by a decrease in mitochondrial membrane potential, increase in Bax/Bcl-xL ratio and cytochrome c release followed by caspase 3/7 activation. In addition, increased phosphorylation of MAP kinases (Erk1/2, p38 and JNK) was observed in chalcone 1C-treated melanoma cells. The strong antiproliferative activities of this chalcone-acridine hybrid suggest that it may be useful as an antimelanoma agent in humans.

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“…[60] Therefore, reducing of ROS levels can negatively modulate these processes leading to an antiproliferative effect. [61][62][63] Treatment of SK-MEL-28 cells with EO-LM for 24 hours compared to the control significantly reduced ROS production (Figure 5) when incubated with 33 μg/mL (25.23 � 0.9 %) and 66 μg/mL (25.39 � 0.17 %). On the other hand, in the positive control (H 2 O 2 ) it is possible to observe a significant increase in the fluorescence intensity of the DCF (96.3 � 2.5 %) (p < 0.0001).…”

Section: Quantification Of Reactive Oxygen Species (Ros)mentioning

confidence: 97%

Assessment of the in Vitro Antimelanoma Potential of Lippia microphylla Cham (Verbenaceae) Essential Oil

de Oliveira Lopes,

Neves de Andrade,

Sousa Duarte

et al. 2023

Chemistry & Biodiversity

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Essential oils stand out among natural products for their complex composition, frequently described in the literature with a range of biological effects. This study evaluated the cytotoxic activity against several human cancer cell lines of essential oils extracted from the leaves of Lippia microphylla (EO‐LM) Cham. (Verbenaceae). The melanoma cell line SK‐MEL‐28 was the most sensitive to the EO‐LM, presenting an IC50 of 33.38 ± 1.16 µg/mL. Afterward, the effects of EO‐LM on the cell cycle, induction of apoptosis, and production of reactive oxygen species (ROS) were evaluated. We stated a significant increase in the sub‐G1 population, indicating apoptosis, later confirmed by an increase of SK‐MEL‐28 cells labeled with Annexin V‐FITC and by the formation of apoptotic bodies and membrane blebs, observed by confocal microscopy. Additionally, EO‐LM reduced the production of ROS, indicating antioxidant activity. Therefore, EO‐LM exhibits anti‐melanoma activity in vitro, suggesting its potential as an anticancer agent.

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Apoptotic and antioxidant effects in HCT-116 colorectal carcinoma cells by a spiro-acridine compound, AMTAC-06

Cited by 10 publications

References 50 publications

In Vitro Assessment of the Synergistic Effect of Aspirin and 5-Fluorouracil in Colorectal Adenocarcinoma Cells

In Vitro Assessment of the Synergistic Effect of Aspirin and 5-Fluorouracil in Colorectal Adenocarcinoma Cells

Chalcone-Acridine Hybrid Suppresses Melanoma Cell Progression via G2/M Cell Cycle Arrest, DNA Damage, Apoptosis, and Modulation of MAP Kinases Activity

Assessment of the in Vitro Antimelanoma Potential of Lippia microphylla Cham (Verbenaceae) Essential Oil

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