Small benzothiazole molecule induces apoptosis and prevents metastasis through DNA interaction and c-MYC gene supression in diffuse-type gastric adenocarcinoma cell line

Mesquita, Felipe Pantoja; Pinto, Laine Celestino; Soares, Bruno Moreira; Portilho, Adrhyann Jullyanne de Sousa; Silva, Emerson Lucena da; Ramos, Ingryd Nayara de Farias; Khayat, André Salim; Moreira-Nunes, Caroline Aquino; Bezerra, Mirna Marques; Chazin, Eliza de Lucas; Vasconcelos, Thatyana R. A.; Burbano, Rommel Rodrı́guez; Moraes, Maria Elisabete Amaral de; Montenegro, Raquel Carvalho

doi:10.1016/j.cbi.2018.08.006

Cited by 12 publications

(6 citation statements)

References 65 publications

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“…In addition, luciferase assay demonstrated that MSI1 was able to directly bind to the consensus sequence of c-Myc 3′-UTR in OSCC cells. As a type of oncogene, c-Myc phosphoprotein can interact with the pre-replicative complex at the S phase of the cell cycle, and c-Myc silencing can cause cell-cycle arrest at the S phase and promote apoptosis in cancer cells, as previously shown in gastric cancer and esophageal SCC (28,29). Thus, MSI1 appears to cause cell cycle arrest in part by inhibiting the expression of c-Myc.…”

Section: Discussionmentioning

confidence: 72%

Knockdown of MSI1 inhibits the proliferation of human oral squamous cell carcinoma by inactivating STAT3 signaling

et al. 2019

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Musashi RNA-binding protein 1 (MSI1) is highly expressed in several types of cancer; however, its role in oral squamous cell carcinoma (OSCC) remains unknown. The purpose of this study was to investigate the probable mechanism underlying the involvement of MSI1 in OSCC. The results demonstrated that MSI1 was upregulated in OSCC tissues, but not in adjacent healthy tissues. MSI1 silencing resulted in decreased cell proliferative, invasive and migrative capacity. In addition, MSI1 silencing led to cell cycle arrest at the S phase, downregulation of c-Myc and cyclin D1, and upregulation of p21 and p27 levels. Additional studies demonstrated that MSI1 suppression inhibited the activation of signal transducer and activator of transcription 3 (STAT3) signaling. Accordingly, the findings of the present study suggested that MSI1 silencing can suppress OSCC cell proliferation and progression, in part by inhibiting the activation of the c-Myc/STAT3 pathway.

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Section: Discussionmentioning

confidence: 72%

Knockdown of MSI1 inhibits the proliferation of human oral squamous cell carcinoma by inactivating STAT3 signaling

et al. 2019

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“…One study found that the benzothiazole derivative carbamate showed antiproliferative activity against NT2/D1 cells 27 . And a report found that AFN01 (benzothiazole derivative) inhibited cell proliferation in a model gastric cancer cell line 28 . In this study, we examined the responses of OVCAR420 and SKOV3 cells to different concentrations of Rosline.…”

Section: Discussionmentioning

confidence: 99%

“…27 And a report found that AFN01 (benzothiazole derivative) inhibited cell proliferation in a model gastric cancer cell line. 28 In this study, we examined the responses of OVCAR420 and SKOV3 cells to different concentrations of Rosline. We found that Rosline dose-dependently inhibited the proliferation of ovarian cancer cells and blocked the cell cycle.…”

Section: Discussionmentioning

confidence: 99%

Rosline promotes p21 expression to inhibit ovarian cancer cell proliferation via p53‐independent pathway

Xiao

et al. 2023

J of Obstet and Gynaecol

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Aim To investigate the effect of benzothiazole derivatives (Rosline) on ovarian cancer and the potential mechanism. Methods Ovarian cancer tissues were collected clinically and immunohistochemistry was used to detect the expression of p53 and p21. Ovarian cancer cells were exposed to 0, 2.5, 5, 10 μmol/L Rosline for 24 h. 100 nmol/L Pifithrin‐α pre‐incubation was used to inhibit the transcriptional activity of p53. CCK‐8 and BrdU assays were used to detect the effects of different concentrations of rosline on the proliferation and cell cycle of OVCAR420 and SKOV3 cells. Flow cytometry assay was used to detect cell cycle. The transcriptional and translational expression of p21 and p53 were detected by RT‐qPCR and Western blot. Results p21 was expressed in ovarian cancer tissues without p53 expression. Rosline inhibits the proliferation of ovarian cancer cells and blocks the cell cycle progression. Meanwhile, Rosline promotes p21 expression in ovarian cancer cells at both mRNA and protein levels, but with no significant effect on p53 expression. Besides, Rosline promotes p21 expression, inhibits cell proliferation, and blocks the cell cycle via the p53‐independent pathway. Conclusion Rosline promoted p21 expression thereby inhibiting cell proliferation and blocks the cell cycle via p53‐independent pathway.

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“…10 The control was composed of a normal gastric cell line. 11 Cells were cultured in Dulbecco's modified Eagle's Medium (Gibco®) supplemented with 10% fetal bovine serum (Gibco®), 1% penicillin and streptomycin, in a 5% CO 2 air humidified atmosphere at 37°C.…”

Section: Cell Culturementioning

confidence: 99%

“…The apoptotic profile was considered to be when cells presented bright green nuclei (activation of caspase 3/7). 11…”

Section: Caspase 3/7 Activitymentioning

confidence: 99%

Kinase inhibitor screening reveals aurora‐a kinase is a potential therapeutic and prognostic biomarker of gastric cancer

Mesquita

Silva

Souza

et al. 2021

J of Cellular Biochemistry

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Gastric cancer is one of the most common and deadly types of cancer in the world, and poor prognosis with treatment failure is widely reported in the literature. In this context, kinases have been considered a relevant choice for targeted therapy in gastric cancer. Here, we explore the antiproliferative and antimigratory effects of the AURKA inhibitor and the prognostic and therapeutic value as a biomarker of gastric cancer. A total of 145 kinase inhibitors were screened to evaluate the cytotoxic or cytostatic effects in the gastric cancer cell line. Using the Alamar Blue assay, flow cytometry, quantitative polymerase chain reaction, and observation of caspase 3/7 activity and cell migration, we investigated the antiproliferative, proapoptotic, and antimigratory effects of the AURKA inhibitor. Moreover, AURKA overexpression was evaluated in the gastric cell lines and the gastric tumor tissue. Out of the 145 inhibitors, two presented the highest antiproliferative effect. Both molecules can induce apoptosis by the caspases 3/7 pathway in addition to inhibiting cancer cell migration, mainly the AURKA inhibitor. Moreover, molecular docking analysis revealed that GW779439X interacts in the active site of the AURKA enzyme with similar energy as a well-described inhibitor.Our study identified AURKA overexpression in the gastric cancer cell line and gastric tumor tissue, revealing that its overexpression in patients with cancer is correlated with low survival. Therefore, it is feasible to suggest AURKA as a potential marker of gastric cancer, besides providing robust information for diagnosis and estimated survival of patients. AURKA can be considered a new molecular target used in the prognosis and therapy of gastric cancer.

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Small benzothiazole molecule induces apoptosis and prevents metastasis through DNA interaction and c-MYC gene supression in diffuse-type gastric adenocarcinoma cell line

Cited by 12 publications

References 65 publications

Knockdown of MSI1 inhibits the proliferation of human oral squamous cell carcinoma by inactivating STAT3 signaling

Knockdown of MSI1 inhibits the proliferation of human oral squamous cell carcinoma by inactivating STAT3 signaling

Rosline promotes p21 expression to inhibit ovarian cancer cell proliferation via p53‐independent pathway

Kinase inhibitor screening reveals aurora‐a kinase is a potential therapeutic and prognostic biomarker of gastric cancer

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