Ionizing radiation induces epithelial–mesenchymal transition in human bronchial epithelial cells

Tang, Bo; Xi, Yue; Cui, Fengmei; Gao, Jin; Chen, Huiqin; Yu, Wentao; Yu, Ting

doi:10.1042/bsr20200453

Cited by 3 publications

(3 citation statements)

References 37 publications

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“…Cell adhesion was tested using a cell adhesion detection kit (Best Bio) according to the manufacturer's protocol. [ 19 ] In brief, cells were seeded into 12‐well plates, and different concentrations of 5e were added to the culture medium and cultured for 48 h. The day before the test, extracellular matrix coating solution (100 µl/well) was added to 96‐well plates and incubated at 4°C overnight. On the next day, the coating solution was removed and washed with a strip washing solution.…”

Section: Methodsmentioning

confidence: 99%

Synthesis and anticancer activity of ethyl 5‐amino‐1‐N‐substituted‐imidazole‐4‐carboxylate building blocks

Ruzi

Nie

Bozorov

et al. 2021

Archiv der Pharmazie

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A series of 5‐amino‐1‐N‐substituted‐imidazole‐4‐carboxylate building blocks was synthesized and assayed for their antiproliferative potential against human cancer cell lines, including HeLa (cervical), HT‐29, HCT‐15 (colon), A549 (lung), and MDA‐MB‐231 (breast) cells. The preliminary screening results revealed that several derivatives containing alkyl chains at the N‐1 position of the imidazole core demonstrate a certain inhibitory effect on growth and proliferation. A significant effect was observed following ethyl 5‐amino‐1‐dodecyl‐1H‐imidazole‐4‐carboxylate (5e) treatment for 72 h. The IC50 value for HeLa cells was 0.737 ± 0.05 μM, whereas that for HT‐29 cells was 1.194 ± 0.02 μM. Further investigations revealed that 5e significantly inhibited tumor cell colony formation and migration, and it exhibited antiadhesive effects on HeLa cells as well as antitubulin activity along with the induction of early apoptosis of HeLa and HT‐29 cells. In addition, derivative 5e significantly reduced the cell mitochondrial membrane potential in a dose‐dependent manner and induced early apoptosis of HeLa and HT‐29 cells, indicating that 5e may serve as a lead compound for further drug discovery and development.

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Section: Methodsmentioning

confidence: 99%

Synthesis and anticancer activity of ethyl 5‐amino‐1‐N‐substituted‐imidazole‐4‐carboxylate building blocks

Ruzi

Nie

Bozorov

et al. 2021

Archiv der Pharmazie

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“…Micro-CT has also been adopted to detect fibrosis-related lesions in bleomycin models ( Ask et al, 2008 ; De Langhe, et al, 2012 ). Considering that the lung tissue is particularly sensitive to cumulative doses of ionizing radiation ( Plathow et al, 2004 ; Graves et al, 2010 ; Tang et al, 2020 ), it needs to be kept in the mind that radiotoxicity may play a role for repeated micro-CT scanning. The excellent agreement found between in vivo MRI, in vivo micro-CT and standard histological measures of lung fibrosis in mice ( Velde et al, 2014 ) provides clear evidence in favor of MRI as imaging readout in the bleomycin model.…”

Section: Introductionmentioning

confidence: 99%

Magnetic resonance imaging and ultrasound elastography in the context of preclinical pharmacological research: significance for the 3R principles

et al. 2023

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The 3Rs principles—reduction, refinement, replacement—are at the core of preclinical research within drug discovery, which still relies to a great extent on the availability of models of disease in animals. Minimizing their distress, reducing their number as well as searching for means to replace them in experimental studies are constant objectives in this area. Due to its non-invasive character in vivo imaging supports these efforts by enabling repeated longitudinal assessments in each animal which serves as its own control, thereby enabling to reduce considerably the animal utilization in the experiments. The repetitive monitoring of pathology progression and the effects of therapy becomes feasible by assessment of quantitative biomarkers. Moreover, imaging has translational prospects by facilitating the comparison of studies performed in small rodents and humans. Also, learnings from the clinic may be potentially back-translated to preclinical settings and therefore contribute to refining animal investigations. By concentrating on activities around the application of magnetic resonance imaging (MRI) and ultrasound elastography to small rodent models of disease, we aim to illustrate how in vivo imaging contributes primarily to reduction and refinement in the context of pharmacological research.

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“…However, the development of acquired or intrinsic resistance poses limitations to the therapeutic success in cancer patients (60,61) . In addition, radiation therapy itself can have an impact on cancer cells by potentially inducing distant metastasis, promoting tumor migration, and enhancing the invasive capabilities of the cancer cells (62,63) . In contrast, NSCLC cells exhibit lower sensitivity to radiation therapy and are less responsive to current treatment modalities compared to SCLC cells.…”

Section: Treatment Options For Lung Cancer and Advanced-stage Nsclcmentioning

confidence: 99%

Photochemical reaction of renieramycins and evaluation of cytotoxicity against lung cancer cells

Sinsook

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Lung cancer causes more deaths than any other type of cancers, with the majority of patients diagnosed with non-small cell lung cancer (NSCLC). Lung cancer is a difficult disease to treat because of the drug resistant problem. Therefore, there is an immediate need for effective, safe, and easily accessible anti-lung cancer drug. Ecteinascidin 743 (Trabectedin or Yondelis?), a marine-derived tetrahydroisoquinoline alkaloid, is an approved drug for treating human lung cancer. This research was studied on the semi-syntheses of new renieramycins derivatives with similar structures to above drug for discovery and development of potent NSCLC cytotoxic agents. Renieramycins was extracted from Xestospongia sp., a blue sponge found at the vicinity of Si-Chang island, Chonburi, Thailand. Renieramycin M was reported as a major alkaloid possessing a bis-tetrahydroisoquinolinequinone as core structure. Regarding the previous report, renieramycin M shows cytotoxicity against NSCLC. Thus, structural modifications focusing on the transformation of substituents at carbon positions 7 and 8 of natural renieramycins including renieramycin M, N, and O were performed by photochemical reaction in conjugation with the reaction optimizations using various light sources�and solvents�to obtain the [1,3]-dioxole group at carbon positions 7 and 8, efficiently.�The result showed that the photochemical reaction with blue light in dichloromethane furnished the highest yield. Under this optimized photochemical reaction, renieramycin M transformed to renieramycin T and renieramycin N and O produced renieramycin U. The results of photochemical reaction support chemical transformations of natural renieramycins under the ocean with sunlight exposure. Furthermore, semi-syntheses of the ester derivatives of renieranycins containing a 4'-pyridinecarbonyl substituent at carbon position 22, using an esterification reaction and new derivatives from the sequential esterification and photochemical reaction containing both 4'-pyridinecarbonyl substituent at carbon position 22 and [1,3]-dioxole group at carbon positions 7 and 8 were conducted. The series of natural renieramycins and derivatives totally 10�compounds were evaluated their cytotoxicity against H292 and H460 NSCLC cell lines. As the results, 22-O-(4'-pyridinecarbonyl) jorunnamycin A exhibited IC50�at 3.52 ? 0.62 ?M and 3.98 ? 0.38 ?M against H292 and H460, respectively with 10 and 8 folds more potent than that of renieramycin M, mother compound. Besides, 22-O-(4'-pyridinecarbonyl) renieramycin T showed IC50�at 1.27 ? 0.20 ?M and 1.83 ? 0.83 ?M against H292 and H460, respectively with 2 and 3 folds more potent than that of Cisplatin, a first-line chemotherapeutic drug. Hence, these new renieramycins derivatives are the promising candidates for further development an anti-lung cancer agent.�

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Ionizing radiation induces epithelial–mesenchymal transition in human bronchial epithelial cells

Cited by 3 publications

References 37 publications

Synthesis and anticancer activity of ethyl 5‐amino‐1‐N‐substituted‐imidazole‐4‐carboxylate building blocks

Synthesis and anticancer activity of ethyl 5‐amino‐1‐N‐substituted‐imidazole‐4‐carboxylate building blocks

Magnetic resonance imaging and ultrasound elastography in the context of preclinical pharmacological research: significance for the 3R principles

Photochemical reaction of renieramycins and evaluation of cytotoxicity against lung cancer cells

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