Predictive hybrid paradigm for cytotoxic activity of 1,3,4-thiadiazole derivatives as CDK6 inhibitors against human (MCF-7) breast cancer cell line and its structural modifications: rational for novel cancer therapeutics

Author(s):  
Prosper Obed Chukwuemeka ◽  
Haruna Isiyaku Umar ◽  
Opeyemi Iwaloye ◽  
Oluwaseyi Matthew Oretade ◽  
Christopher Busayo Olowosoke ◽  
...  
Author(s):  
Farah A Al-marzook ◽  
Rabab Omran

  Objectives: Screening for cytotoxic activity of total alkaloid extracts of Eucalyptus camaldulensis, Aloe vera, and Capparis spinosa against breast cancer cell line Michigan Cancer Foundation-7 (MCF-7) and nontumorigenic fetal hepatic cell line (WRL-68).Methods: The plant powders were extracted separately with 80% methanol and chloroform at pH 2 and 10. Total alkaloids were detected qualitatively by Mayer’s, Dragendorff’s, and Hager‘s reagents and estimated quantitatively by bromocresol green spectrophotometry depending on the atropine calibration curve. The cytotoxic activity was evaluated by 3-[4, 5-dimethylthiazoyl]-2, 5-diphenyltetrazolium bromide assay.Results: The extract of E. camaldulensis had highest total alkaloid content (24.50±1.70 mg/100 g plant dry weight) than the others. The total alkaloids (400 μg/ml) of E. camaldulensis reduced the cell viability of both cell lines MCF-7 and WRL-68 to 45.25±2.20% and 92.00±1.55%, respectively, and the inhibitory concentration 50% of cells were 375.50 μg/ml for MCF-7. The alkaloids of C. spinosa had effect 79.80±7.08% and 89.50±0.09% against MCF-7and WRL-68, respectively. While the total alkaloids of A. vera had slightly effect on both cell lines.Conclusion: Plant alkaloids appeared variable cytotoxic activity against cancer and normal cell lines depending on the alkaloid contents, concentrations, purity, and cell line types.


Author(s):  
Rabab Omran ◽  
Zahraa Mal Taee ◽  
Mohammed Jal Jassani ◽  
Hayder O Hashim

Objective: The objective of the study was to study the antioxidants and cytotoxic activities of phenolic extracts of some plants against breast cancer and normal cell lines.Methods: Phenolics were extracted from different parts of some plants (15) such as seeds, fruits, leaves, and rhizomes using methanol: ethanol: HCl: Distilled water at a ratio 50:29:1:20 (v:v:v:v). The contents of phenolics and flavonoids were estimated using gallic acid and quercetin as standards, respectively. The antioxidant activity was determined by 2,2ˋ-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) radical scavenging assay. Phenolic flavonoids were partially purified by adsorption chromatography using a silica gel column from selected plants and assayed their cytotoxic activity against breast cancer cell line Michigan Cancer Foundation-7 (MCF-7) and a normal cell line of non-tumorigenic fetal hepatic cell line (WRL-68).Results: The Cinnamomum zeylanicum extract had the highest phenolic and flavonoid contents were followed by Lawsonia inermis, Citrullus colocynthis, Syzygium aromaticum, Peganum nigrum, and Phoenix dactylifera. The antioxidant activity of Curcuma longa, P. dactylifera, C. colocynthis, Solanum melongena, and C. zeylanicum extracts had the highest ability to scavenge the free radicals. The acetone fraction of P. dactylifera and C. colocynthis extracts had the minimum inhibition dose that kills 50% of cells inhibitory concentration 50 values 156.91 μg and 1055.06 μg against MCF-7 and 372.86 μg and 153.8 μg against WRL-68, respectively. While the S. melongena extract had less effect on both cell lines.Conclusions: Phenolics as antioxidant substances had moderate or variable effectiveness on normal and cancer cell lines, and the highest concentrations were cancerous poison impact may be on normal cells over than cancer cells.


2015 ◽  
Vol 11 (42) ◽  
pp. 156 ◽  
Author(s):  
Richard Lobo ◽  
Nimmy Kumar ◽  
Rajalekshmi Maheshwari ◽  
CS Shreedhara ◽  
VijayKumar Sodde

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Stefania Nobili ◽  
Antonella Mannini ◽  
Astrid Parenti ◽  
Chiara Raggi ◽  
Andrea Lapucci ◽  
...  

AbstractInvasive ductal carcinoma (IDC) constitutes the most frequent malignant cancer endangering women’s health. In this study, a new spontaneously immortalized breast cancer cell line, DHSF-BR16 cells, was isolated from the primary IDC of a 74-years old female patient, treated with neoadjuvant chemotherapy and disease-free 5-years after adjuvant chemotherapy. Primary breast cancer tissue surgically removed was classified as ER−/PR−/HER2+, and the same phenotype was maintained by DHSF-BR16 cells. We examined DHSF-BR16 cell morphology and relevant biological and molecular markers, as well as their response to anticancer drugs commonly used for breast cancer treatment. MCF-7 cells were used for comparison purposes. The DHSF-BR16 cells showed the ability to form spheroids and migrate. Furthermore, DHSF-BR16 cells showed a mixed stemness phenotype (i.e. CD44+/CD24−/low), high levels of cytokeratin 7, moderate levels of cytokeratin 8 and 18, EpCAM and E-Cadh. Transcriptome analysis showed 2071 differentially expressed genes between DHSF-BR16 and MCF-7 cells (logFC > 2, p-adj < 0.01). Several genes were highly upregulated or downregulated in the new cell line (log2 scale fold change magnitude within − 9.6 to + 12.13). A spontaneous immortalization signature, mainly represented by extracellular exosomes-, plasma membrane- and endoplasmic reticulum membrane pathways (GO database) as well as by metabolic pathways (KEGG database) was observed in DHSF-BR16 cells. Also, these cells were more resistant to anthracyclines compared with MCF-7 cells. Overall, DHSF-BR16 cell line represents a relevant model useful to investigate cancer biology, to identify both novel prognostic and drug response predictive biomarkers as well as to assess new therapeutic strategies.


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