scholarly journals Synthesis of novel potential ROCK inhibitors and their antimigratory effects

2020 ◽  
Vol 13 (4) ◽  
pp. 165-174
Author(s):  
Sümeyye Turanlı ◽  
Azize Gizem Uslu ◽  
Aysun Özdemir
Keyword(s):  
Cell Migration ◽  
Cancer Cell ◽  
Rho Kinase ◽  
Cancer Cell Line ◽  
Cytotoxic Activities ◽  
Design And Synthesis ◽  
Cellular Processes ◽  
Tumor Types ◽  
Rock Inhibition ◽  
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Rho kinase (ROCK), an enzyme belonging to the serine-threonine kinase family, is involved in the regulation of basic cellular processes such as morphology, movement, division, differentiation and apoptosis. On the other hand, excessively activated ROCK can cause to cardiovascular and neurological disorders or cancer. In recent years, overactivation of Rho kinases has been associated with increased metastasis in various tumor types and has been explored as target for the development of new anticancer drugs. We report here the design and synthesis of five urea derivatives in search of novel inhibitors of cancer cell migration. Compounds evaluated for their cytotoxic activities against breast (MCF-7) cancer cell line. After determination of the ineffective concentrations of compounds on the proliferation of MCF-7 cells, wound healing experiments were conducted to investigate the antimigratory effects of compounds. While compounds 4 and 10 had no effect on cell migration, treatment of MCF-7 cells with compounds 5, 8 and 9 resulted in significant reduction in cell motility. Taken together our results suggest that the newly synthesized compounds 5, 8 and 9 had the potential antimigratory activity through possible ROCK inhibition in cancer cells.

scholarly journals Synthesis and Experimental Validation of New Designed Heterocyclic Compounds with Antiproliferative Activity versus Breast Cancer Cell Lines MCF-7 and MDA-MB-231

2017 ◽  
Vol 2017 ◽  
pp. 1-10 ◽  
Author(s):  
Vincenza Barresi ◽  
Carmela Bonaccorso ◽  
Domenico A. Cristaldi ◽  
Maria N. Modica ◽  
Nicolò Musso ◽  
...  
Keyword(s):  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Anticancer Agents ◽  
Cancer Cell Line ◽  
Breast Cancer Cell Lines ◽  
Design And Synthesis ◽  
Human Breast Cell ◽  
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Recent drug discovery efforts are highly focused towards identification, design, and synthesis of small molecules as anticancer agents. With this aim, we recently designed and synthesized novel compounds with high efficacy and specificity for the treatment of breast tumors. Based on the obtained results, we constructed a Volsurf+ (VS+) model using a dataset of 59 compounds able to predict the in vitro antitumor activity against MCF-7 cancer cell line for new derivatives. In the present paper, in order to further verify the robustness of this model, we report the results of the projection of more than 150 known molecules and 9 newly synthesized compounds. We predict their activity versus MCF-7 cell line and experimentally verify the in silico results for some promising chosen molecules in two human breast cell lines, MCF-7 and MDA-MB-231.

Modeling, design and synthesis of new heteroaryl ethylenes active against the MCF-7 breast cancer cell-line

2013 ◽  
Vol 9 (10) ◽  
pp. 2426 ◽  
Author(s):  
Vincenza Barresi ◽  
Carmela Bonaccorso ◽  
Giuseppe Consiglio ◽  
Laura Goracci ◽  
Nicolò Musso ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cell Line ◽  
Cancer Cell ◽  
Breast Cancer Cell ◽  
Breast Cancer Cell Line ◽  
Cancer Cell Line ◽  
Design And Synthesis ◽  
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scholarly journals Cytotoxic activities of Methanolic and Chloroform Extract of Cryptocarya Massoy (Oken) Kosterm. Bark on MCF-7 human breast cancer cell line

2018 ◽  
Vol 9 (1) ◽  
pp. 57-62
Author(s):  
Yuli Widiyastuti ◽  
Ika Yanti M. Sholikhah ◽  
Sari Haryanti
Keyword(s):  
Breast Cancer ◽  
Cell Line ◽  
Cancer Cell ◽  
Mtt Assay ◽  
Cancer Cell Line ◽  
Chloroform Extract ◽  
Cytotoxic Activities ◽  
Litsea Cubeba ◽  
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Abstrak Latar Belakang. Krangean [Litsea cubeba (Lour.) Pers.] Adalah salah satu tanaman aromatik purba di Indonesia. Tanaman ini adalah anggota keluarga Lauraceae, tumbuh liar di dataran tinggi Sumatera, Kalimantan, dan pulau Jawa. Aktivitas antikanker tanaman ini belum banyak dieksplorasi. Penelitian ini bertujuan untuk mengetahui kandungan fitokimia dan aktivitas sitotoksik ekstrak buah krangean pada sel kanker manusia secara in vitro. Metode. Kloroform dan metanol digunakan untuk mempererat bubuk buah kering selama 3x24 jam. Senyawa fitokimia utama ditandai dengan KLT (kromatografi lapis tipis). Uji MTT dilakukan untuk mengamati morfologi dan viabilitas kanker serviks HeLa, kanker payudara MCF-7, dan sel HEPG2 hepar. Hasil. Hasil penelitian menunjukkan bahwa karakterisasi KLT ekstrak kloroform dan metanol Litsea cubeba menunjukkan profil yang sama, dengan senyawa utama yang ditemukan adalah terpenoid dan alkaloid. Uji MTT menemukan bahwa kedua ekstrak memiliki penghambatan kuat pada sel HeLa. Ekstrak kloroform menunjukkan aktivitas sitotoksik yang lebih kuat dibandingkan dengan metanol, dengan nilai IC50 masing-masing 33,7 dan 64,8 μg / mL. Kesimpulan. Esktrak kloroform dan ekstrak metanol dari Litsea cubeba memiliki aktivitas yang kuat terhadap sel HeLa dan aktivitas sedang terhadap sel HEPG2 dan MCF-7.  Selanjutnya disarankan untuk dilakukan penelitian lebih lanjut untuk mengathui senyawa aktif L. cubeba (Lour.) Pers. yang memiliki aktivitas antikanker potensial. Kata kunci: Litsea cubeba (Lour.) Pers., sitotoksik, HeLa, MCF-7, HebG2, MTT assay   Abstract Background. Krangean [Litsea cubeba (Lour.) Pers.] is one of ancient aromatic plants in Indonesia. This plant is the member of Lauraceae family, growing wild on the highlands of Sumatera, Kalimantan, and Java island. The anticancer activity of this plant haven’t been explored extensively.This research aimed to investigate phytochemical content and cytotoxic activity of krangean fruits extract on human cancer cell line in vitro. Method. Chloroform and methanol were used to macerate dried fruits powder for 3x24 hours. Major phytochemical compounds was characterized by TLC (thin layer chromatography). MTT assay was done to observe morphology and viability of HeLa cervical cancer, MCF-7 breast cancer, and HepG2 hepar cancer cell line. Result. The results showed that TLC characterization of chloroform and methanolic extracts of Litsea cubeba revealed similar profile, with the major compound found are terpenoid and alkaloid. The MTT assay found that both extracts have strong inhibition on HeLa cell line. Chloroform extract exhibited stronger cytotoxic activities compared to methanol, with the IC50 values of 33,7 and 64,8 μg/mL respectively. While, the both extract have moderate cytotoxic activities to HEPG2 and MCF-7 cancer cell line indicated by IC50value more than 100 mg/mL. Conclusion. Chloroform and methanolic extract of Litsea cubeba have a strong activity againts HeLa cancer cell lines and moderate activity to HEPG2 and MCF-7, thought chloroform extract of Litsea cubeba has stronger effect on cancer cell line viability. It is well recommended for further studies to investigate the active compound of L. cubeba (Lour.) Pers. for potential anticancer activity.   Key words: Litsea cubeba (Lour.) Pers., cytotoxic, HeLa, MCF-7, HebG2, MTT assay

Cytotoxic activity and anti-cancer potential of Ontario grown onion extracts against breast cancer cell lines

2018 ◽  
Vol 8 (3) ◽  
pp. 159 ◽  
Author(s):  
Meghan Fragis ◽  
Abdulmonem I. Murayyan ◽  
Suresh Neethirajan
Keyword(s):  
Breast Cancer ◽  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Breast Cancer Cell ◽  
Cancer Cell Lines ◽  
Breast Cancer Cell Lines ◽  
Cytotoxic Activities ◽  
Cancer Line ◽  
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Background: Breast cancer is the most commonly diagnosed cancer and the second leading cause of cancer deaths among Canadian women. Cancer management through changes in lifestyle, such as increased intake of foods rich in dietary flavonoids, have been shown to decrease the risk associated with breast, liver, colorectal, and upper-digestive cancers in epidemiologic studies. Onions are high in flavonoid content and one of the most common vegetables. Additionally, onions are used in most Canadian cuisines.Methods: We investigated the effect of five prominent Ontario grown onion (Stanley, Ruby Ring, LaSalle, Fortress, and Safrane) extracts on two subtypes of breast cancer cell lines: a triple negative breast cancer line MDA-MB-231 and an ER+ breast cancer line MCF-7.Results: These onion extracts elicited strong anti-proliferative, anti-migratory, and cytotoxic activities on both the cancer cell lines. Flavonoids present in these onion extracts induced apoptosis, cell cycle arrest in the G2/M phase, and a reduction in mitochondrial membrane potential at dose-dependent concentrations. Onion extracts were more effective against MDA-MB-231 compared to the MCF-7 cell line. Conclusion: In this study, we investigated the extracts synthesized from Ontario-grown onion varieties in inducing anti-migratory, cytostatic, and cytotoxic activities in two sub-types of human breast cancer cell lines. Anti-tumor activity of these extracts depends upon the varietal and can be formulated into nutraceuticals and functional foods for the wellbeing of cancer patients. Overall, the results suggest that onion extracts are a good source of flavonoids with anti-cancerous properties.Keywords: onion extracts; flavonoids; anti-proliferative; breast cancer; cytotoxic activity

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