Cytotoxic and apoptotic effects of chalcone derivatives of 2‐acetyl thiophene on human colon adenocarcinoma cells

Vasconcelos, Alana de; Campos, Vinícius Farias; Nedel, Fernanda; Seixas, Fabiana Kömmling; Dellagostin, Odir A.; Smith, Kevin R.; Pereira, Cláudio Martin Pereira de; Stefanello, Francieli Moro; Collares, Tiago; Barschak, Alethéa Gatto

doi:10.1002/cbf.2897

Cited by 49 publications

(23 citation statements)

References 36 publications

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“…Some chalcones displayed marked antiproliferative effects, via apoptosis and autophagy induction (32) others enhance TRAILinduced apoptosis (37) or ROS production (38) etc. Numerous chalcones derivate mentioned in the previous section induced apoptosis via inner mitochondrial pathway through overexpression of Bax protein and active caspase-3 (28,34,35). Our results indicated that chalcone analog treatment of HCT-116 cells caused overexpression of active, mitochondrial pro-apoptotic Bax protein and active caspase-3 compared to the control cells.…”

Section: Discussionsupporting

confidence: 50%

Antitumor Effects of Vanillin Based Chalcone Analogues in Vitro

Luković¹,

Mitrović²,

Popović³

et al. 2020

Acta Poloniae Pharmaceutica - Drug Research

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Colorectal cancer (CRC) is the third most common malignancy worldwide. CRC represents 13% of all malignant tumors and it may be expected to overcome the mortality rate of patients with heart diseases in the near future (1, 2). Approximately, one half of the population in Western countries develops a colorectal tumor by the age of 70 (3, 4). However, this type of cancer is more frequent among younger population, due to obesity, bad nutritional habits, smoking and lack of physical activity (5). Colorectal cancer develops as a polyp or adenoma in the intestinal mucosa. Malignant transformation of benign changes depends on its size and histological presentation (1). In previous years, the survival rate of patients with metastatic colorectal cancer increased significantly due to the development and the application of new chemotherapy regimens (6). There are several types of cell deaths, of which two are the main types: apoptosis and necrosis. Apoptosis, a programmed cell death, is character

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Section: Discussionsupporting

confidence: 50%

Antitumor Effects of Vanillin Based Chalcone Analogues in Vitro

Luković¹,

Mitrović²,

Popović³

et al. 2020

Acta Poloniae Pharmaceutica - Drug Research

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“…Morever thiophene containing chalcones ( Figure 1) were reported in various studies that it have bioactive potential such as antibacterial, apoptotic, anti-angiogenic and radical scavenging agent (11)(12)(13)(14)(15). On the other hand, there is no study on the antifungal and anti-biofilm activities of the 1,3di(thiophen-2-yl)prop-2-en-1-one (4) according to our literature survey.…”

Section: Introductionmentioning

confidence: 88%

“1,3-di(thiophen-2-yl) prop-2-en-1-one” kalkon türevinin antifungal, anti-biyofilm ve anti-kanser aktivitelerinin belirlenmesi

Tutar¹,

Çelik²,

Gezegen³

et al. 2017

Cumhuriyet Medical Journal

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Our study aims to determine antifungal and anti-biofilm activity potential of five chalcone derivatives, which have been already reported in the literature, against Candida albicans and Candida tropicalis. In addition, it aimed to determine antioxidant property and anti-cancer activity of 1,3-di(thiophen-2-yl)prop-2-en-1-one chalcone derivative, whose antimicrobial activity was revealed within the study, in human breast cancer cell line (MCF-7) and human bone cancer cell line (MG63). Method: Chalcones used in the study were diluted two times in dimethyl sulfoxide (DMSO) and prepared at concentration between 1000-15 µg/mL. Antifungal and anti-biofilm activity of chalcones determined by using microdilution method. Radical scavenging activity was tested by employing 2, 2-diphenyl-1-picrylhydrazyl (DPPH). The cell viability was assessed using the cleavage of tetrazolium salts added to the culture medium. Results: In our study, MIC values of "1,3-di(thiophen-2-yl) prop-2-en-1-one", which showed its antimicrobial activity on C. albicans and C. tropicalis, were found to be 0.06 mg/mL for both organisms, whereas its MBC values were found to be 0.12 mg/mL and 0.50 mg/mL respectively. MBIC activities were found to be 0.06 and 0.25 mg/mL respectively, whereas MBEC values were found to be 1 mg/mL. When MIC was applied to 48-hours biofilm formation, it was observed that the formation has decreased by 83% and 81%. IC50 value of "1,3-di(thiophen-2-yl) prop-2-en-1-one" was found to be 13,52 µg / mL. Regarding MCF-7 and MG63 cell line at 5 µg / mL concentration, 30% and 65% preserve its viability after 24 hours of incubation respectively. Conclusions: According to these results, it can be said that chalcone compound that include thiophen ring has shown an inhibiting effect on the multiplication and both on the formation of the biofilm of C. albicans and C. tropicalis strains. The results of the study revealed that chalcone compound may be valuable as an antifungal, anti-biofilm and anti-cancer agent.

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“…2). We anticipated that due to the well known bioisosterism of thiophene ring with benzene the newly designed molecules (B) would retain the PDE4 inhibitory properties of A. Additionally, in view of the fact that the thiophene ring being integral part of several anticancer agents/drugs [7,8] as well as cytotoxic/apoptotic agents [9] we expected potential apoptosis inducing properties of B.…”

Section: Introductionmentioning

confidence: 98%