Antiproliferative and apoptotic effects of diffractaic acid in A549 and AGS cancer cells

Kızıl, Hamit Emre; Ağar, Güleray

doi:10.1063/1.4981747

Cited by 2 publications

(4 citation statements)

References 7 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The obtained results confirm the consistency of flow cytometry and qPCR results. Moreover, our results are supported by a study in which diffractaic acid showed an apoptotic effect on A549 cells by increasing the expressions of caspase‐3 and P53 genes (Kızıl & Ağar, 2017). Altogether, it can be concluded that diffractaic acid triggers considerable apoptosis in A549 cells via the intrinsic apoptotic pathway.…”

Section: Discussionsupporting

confidence: 80%

“…that diffractaic acid has a significant antiproliferative effect on A549 (lung cancer) and AGS (gastric cancer) cell lines up to a concentration of 100 μg/mL (without calculating the IC 50 value), but has no toxic effect on healthy human umbilical cord vascular endothelial cells (HUVEC) up to 200 μg/mL for 48 h (Kızıl, 2016;Kızıl & A gar, 2017).…”

Section: Discussionmentioning

confidence: 99%

“…Diffractaic acid, a lichen secondary metabolite, has been claimed to be an anticancer agent performed with different cancer cells. Some preliminary cytotoxicity studies with diffractaic acid have been carried out (Brisdelli et al, 2013; Kızıl & Ağar, 2017; Truong et al, 2014). But, there is no detailed study that can reveal its anticancer mechanism of action in the literature.…”

Section: Discussionmentioning

confidence: 99%

“…Truong et al (2014) declared the potent cytotoxic effect of diffractaic acid on HeLa (human cervical carcinoma), NCI‐H460 (human lung cancer), and MCF‐7 (human breast cancer) cell lines at 100 μg/mL. In the literature, it has been reported that diffractaic acid has a significant antiproliferative effect on A549 (lung cancer) and AGS (gastric cancer) cell lines up to a concentration of 100 μg/mL (without calculating the IC 50 value), but has no toxic effect on healthy human umbilical cord vascular endothelial cells (HUVEC) up to 200 μg/mL for 48 h (Kızıl, 2016; Kızıl & Ağar, 2017). In another study, the IC 50 value of diffractaic acid on glioblastoma cells was reported as 35.67 μg/mL (Emsen et al, 2018).…”

Section: Discussionmentioning

confidence: 99%

See 3 more Smart Citations

Diffractaic acid exhibits thioredoxin reductase 1 inhibition in lung cancer A549 cells

Günaydın

Sulukoğlu

Kalın

et al. 2023

J of Applied Toxicology

View full text Add to dashboard Cite

Lung cancer is the leading cause of cancer‐related deaths all over the world. Therefore, it has gained importance in the development of new chemotherapeutic strategies to identify anticancer agents with low side effects, reliable, high anticancer potential, and specific to lung cancer cells. Thioredoxin reductase 1 (TrxR1) is an important therapeutic target for lung cancer treatment because of its overexpression in tumor cells. Here, we aimed to examine the anticancer effect of diffractaic acid, a lichen secondary metabolite, in A549 cells by comparing it with the commercial chemotherapeutic drug carboplatin and also to investigate whether the anticancer effect of diffractaic acid occurs via TrxR1‐targeting. The IC50 value of diffractaic acid on A549 cells was determined as 46.37 μg/mL at 48 h, and diffractaic acid had stronger cytotoxicity than carboplatin in A549 cells. qPCR results revealed that diffractaic acid promoted the intrinsic apoptotic pathway through the upregulation of the BAX/BCL2 ratio and P53 gene in A549 cells, which is consistent with the flow cytometry results. Furthermore, migration analysis results indicated that diffractaic acid impressively suppressed the migration of A549 cells. While the enzymatic activity of TrxR1 was inhibited by diffractaic acid in A549 cells, no changes were seen in the quantitative expression levels of gene and protein. These findings provide fundamental data on the anticancer effect of diffractaic acid on A549 cells targeting TrxR1 activity, suggesting that it could be considered a chemotherapeutic agent for lung cancer therapy.

show abstract

Section: Discussionsupporting

confidence: 80%

Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

See 2 more Smart Citations

Diffractaic acid exhibits thioredoxin reductase 1 inhibition in lung cancer A549 cells

Günaydın

Sulukoğlu

Kalın

et al. 2023

J of Applied Toxicology

View full text Add to dashboard Cite

show abstract

Diffractaic acid exerts anti-cancer effects on hepatocellular carcinoma HepG2 cells by inducing apoptosis and suppressing migration through targeting thioredoxin reductase 1

Sulukoğlu,

Günaydın,

Kalın

et al. 2024

Naunyn-Schmiedeberg's Arch Pharmacol

View full text Add to dashboard Cite

Hepatocellular carcinoma (HCC) represents one of the most common malignant tumors worldwide. Due to the limited number of available drugs and their side effects, the development of new chemotherapeutic strategies for HCC treatment has become increasingly important. This study is aimed at investigating whether diffractaic acid (DA), one of the secondary metabolites of lichen, exhibits a potential anticancer effect on HepG2 cells and whether its anticancer effect is mediated by inhibition of thioredoxin reductase 1 (TRXR1), which is a target of chemotherapeutic strategies due to overexpression in tumor cells including HCC. XTT assay results showed that DA exhibited strong cytotoxicity on HepG2 cells with an IC50 value of 78.07 µg/mL at 48 h. Flow cytometric analysis results revealed that DA displayed late apoptotic and necrotic effects on HepG2 cells. Consistent with these findings, real-time PCR results showed that DA did not alter the BAX/BCL2 ratio in HepG2 cells but upregulated the P53 gene. Moreover, the wound healing assay results revealed a strong anti-migratory effect of DA in HepG2 cells. Real-time PCR and Western blot analyses demonstrated that DA increased TRXR1 gene and protein expression levels, whereas enzyme activity studies disclosed that DA inhibited TRXR1. These findings suggest that DA has an anticancer effect on HepG2 cells by targeting the enzymatic inhibition of TRXR1. In conclusion, DA as a TRXR1 inhibitor can be considered an effective chemotherapeutic agent which may be a useful lead compound for the treatment of HCC.

show abstract

Antiproliferative and apoptotic effects of diffractaic acid in A549 and AGS cancer cells

Cited by 2 publications

References 7 publications

Diffractaic acid exhibits thioredoxin reductase 1 inhibition in lung cancer A549 cells

Diffractaic acid exhibits thioredoxin reductase 1 inhibition in lung cancer A549 cells

Diffractaic acid exerts anti-cancer effects on hepatocellular carcinoma HepG2 cells by inducing apoptosis and suppressing migration through targeting thioredoxin reductase 1

Contact Info

Product

Resources

About