In Vitro Measures Used to Predict Anticancer Activity of Apple Cultivars and Their Comparison to Outcomes From a Rat Model of Experimentally Induced Breast Cancer

2009 ◽  
Vol 61 (4) ◽  
pp. 510-517 ◽  
Author(s):  
Matthew D. Thompson ◽  
Cecil Stushnoff ◽  
John N. McGinley ◽  
Henry J. Thompson
Keyword(s):  
Breast Cancer ◽  
Anticancer Activity ◽  
Rat Model ◽  
Apple Cultivars ◽  
Experimentally Induced

scholarly journals A Nitrocarbazole as a New Microtubule-Targeting Agent in Breast Cancer Treatment

2021 ◽  
Vol 11 (19) ◽  
pp. 9139
Author(s):  
Maria Stefania Sinicropi ◽  
Cinzia Tavani ◽  
Camillo Rosano ◽  
Jessica Ceramella ◽  
Domenico Iacopetta ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Anticancer Activity ◽  
Breast Cancer Cell Lines ◽  
Cellular Functions ◽  
Anticancer Properties ◽  
Cycle Arrest ◽  
In Silico Studies ◽  
Ic50 Values ◽  
Mcf 7

Breast cancer is still considered a high-incidence disease, and numerous are the research efforts for the development of new useful and effective therapies. Among anticancer drugs, carbazole compounds are largely studied for their anticancer properties and their ability to interfere with specific targets, such as microtubule components. The latter are involved in vital cellular functions, and the perturbation of their dynamics leads to cell cycle arrest and subsequent apoptosis. In this context, we report the anticancer activity of a series of carbazole analogues 1–8. Among them, 2-nitrocarbazole 1 exhibited the best cytotoxic profile, showing good anticancer activity against two breast cancer cell lines, namely MCF-7 and MDA-MB-231, with IC50 values of 7 ± 1.0 and 11.6 ± 0.8 μM, respectively. Furthermore, compound 1 did not interfere with the growth of the normal cell line MCF-10A, contrarily to Ellipticine, a well-known carbazole derivative used as a reference molecule. Finally, in vitro immunofluorescence analysis and in silico studies allowed us to demonstrate the ability of compound 1 to interfere with tubulin organization, similarly to vinblastine: a feature that results in triggering MCF-7 cell death by apoptosis, as demonstrated using a TUNEL assay.

scholarly journals Enhanced Anticancer Activity of Nanoformulation of Dasatinib against Triple-Negative Breast Cancer by Reduced Metabolic Degradation

2021 ◽  
Author(s):  
Fatemah Bahman ◽  
Valeria Pittalà ◽  
Mohamed Haider ◽  
Khaled Greish
Keyword(s):  
Breast Cancer ◽  
Anticancer Activity ◽  
Triple Negative Breast Cancer ◽  
Tyrosine Kinases ◽  
Triple Negative ◽  
Growth Factor Receptor ◽  
Initial Response ◽  
Response To Chemotherapy

Triple negative breast cancer (TNBC) is the most aggressive breast cancer accounting for around 15% of identified breast cancer cases. TNBC, by lacking estrogen receptor (ER), progesterone receptor (PR), and human epidermal growth factor receptor 2 (HER2), is unresponsive to current targeted therapies. Existing treatment relies on chemotherapeutic treatment but, despite an initial response to chemotherapy, the inception of resistance and relapse is unfortunately common. Dasatinib is an approved second-generation inhibitor of multiple tyrosine kinases and literature data strongly support its use in the management of TNBC. However, dasatinib binds to plasma proteins and undergoes extensive metabolism through oxidation and conjugation. To protect dasatinib from fast pharmacokinetic degradation and to prolong its activity, it was encapsulated on poly(styrene-co-maleic acid) (SMA) micelles. The obtained SMA-dasatinib nanoparticles (NPs) were evaluated for their physicochemical properties, in vitro antiproliferative activity in different TNBC cell lines, and in vivo anticancer activity in a syngeneic model of breast cancer. Obtained results showed that SMA-dasatinib is more potent against 4T1 TNBC tumor growth in vivo compared to free drug. This enhanced effect was ascribed to the encapsulation of the drug protecting it from a rapid metabolism. Our finding highlights the often-overlooked value of nanoformulations in protecting its cargo from degradation. Overall, results may provide an alternative therapeutic strategy for TNBC management.

Thymic Immunosuppressive Pentapeptide (TIPP) Showed Anticancer Activity in Breast Cancer and Chronic Myeloid Leukemia Both In Vitro and In Vivo

2021 ◽  
Vol 28 ◽  
Author(s):  
Muhammad Ijaz ◽  
Muhammad Shahbaz ◽  
Wenjie Jiang ◽  
Yikang Shi ◽  
Xiuli Guo ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Chronic Myeloid Leukemia ◽  
Anticancer Activity ◽  
Myeloid Leukemia ◽  
Map Kinases ◽  
Inflammatory Responses ◽  
Tumor Xenograft ◽  
Immunohistochemistry Analysis

Aim: Being the common cause and major burden of deaths globally, timely management of cancer is crucial. Background: Thymic immunosuppressive pentapeptide (TIPP) is a novel pentapeptide originally obtained from calf thymic immunosuppressive extract. Previously, TIPP has been proved to suppress the allergic and inflammatory responses in allergic mice via blocking MAP kinases/NF-κB signaling pathways. Objective: In this study, in vitro anticancer activity of TIPP was tested on two different types of cancers using MCF-7 and K562 cell lines. Methods: Tumor xenograft models for breast cancer and chronic myeloid leukemia were designed. In vivo anticancer activity of TIPP was investigated on both cancer types. The liver and tumor tissues of the mice were preserved for immunohistochemistry analysis. Results: In vitro anticancer activity of TIPP showed significant inhibition on cell viability of both breast cancer and chronic myeloid leukemia. In vivo anticancer effect of TIPP in both types of cancer models further proved the potent anticancer nature of TIPP. Immunohistochemistry analysis assured that TIPP is a safe drug for normal organs such as the liver. Conclusion: Our present study revealed that TIPP is a potent anticancer drug and an important treatment option for various diseases. Further work is needed to test the flexible and proficient activity of the novel peptide.

scholarly journals SYNTHESIS AND CHARACTERIZATION OF CYCLOHEXANE-1,3-DIONE DERIVATIVES AND THEIR IN SILICO AND IN VITRO STUDIES ON ANTIMICROBIAL AND BREAST CANCER ACTIVITY

2019 ◽  
pp. 311-320 ◽  
Author(s):  
RAJA CHINNAMANAYAKAR ◽  
EZHILARASI MR ◽  
PRABHA B ◽  
KULANDHAIVEL M
Keyword(s):  
Breast Cancer ◽  
Antimicrobial Activity ◽  
Anticancer Activity ◽  
Mtt Assay ◽  
In Silico ◽  
Biologically Active ◽  
Diffusion Method ◽  
Breast Adenocarcinoma ◽  
In Silico Docking

Objective: The objective of this study was to evaluate in silico and in vitro anticancer activity for synthesized cyclohexane-1,3-dione derivatives. Methods: The new series of cyclohexane-1,3-dione derivatives were synthesized based on the Michael addition reaction. Further, the structures of the synthesized compounds were confirmed by Fourier-transform infrared spectroscopy, 1H nuclear magnetic resonance (NMR), and 13C NMR spectral data. Then, the in silico molecular docking studies were carried out using AutoDock tool version 1.5.6 and AutoDock version 4.2.5.1 docking program. The antimicrobial activity was carried out using the agar disk diffusion method, and the in vitro anticancer activity was performed by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay for the synthesized compound. Results: In silico docking study, compound 5c showed good binding score and binding interactions with selected bacterial proteins and breast cancer protein. Further, compound (5a-5h) was tested for their antimicrobial activity and compound 5c was only tested for anticancer activity (human breast adenocarcinoma 3,4-methylenedioxyamphetamine-MB-231 cell line). Compound 5c was found to be the most active one of all the tested compounds. In the MTT assay compound, 5c showed the LC50 value of 10.31±0.003 μg/ml. In antimicrobial activity, the minimum inhibitory concentration of compound 5c is 2.5 mg/ml. Conclusion: An efficient synthesis of biologically active cyclohexane-1, 3-dione derivatives has been developed.

scholarly journals Activity Anticancer n-hexane Fraction of Cyperus Rotundus l. Rhizome to Breast Cancer MCF-7 Cell Line

2019 ◽  
Vol 7 (22) ◽  
pp. 3904-3906
Author(s):  
Delisma Simorangkir ◽  
Masfria Masfria ◽  
Urip Harahap ◽  
Denny Satria
Keyword(s):  
Breast Cancer ◽  
Cell Cycle ◽  
Anticancer Activity ◽  
Cell Line ◽  
Vero Cells ◽  
Cyperus Rotundus ◽  
Hexane Fraction ◽  
Synthetic Drugs ◽  
Mcf 7

BACKGROUND: Cancer is one of the causes of morbidity and mortality worldwide. Breast cancer is one of the most common types of cancer in Indonesia. Failures that often occur in the treatment of cancer primarily through chemotherapy, synthetic drugs that have side effects include anemia, alopecia, cardiotoxic and hepatotoxic due to low anti-cancer selectivity and unclear carcinogenesis process. Cyperus rotundus L. rhizome is one of the medicinal plants that potential enough to be developed as an anticancer agent. AIM: The aim of this study was to anticancer activity n-hexane fraction Cyperus rotundus L. rhizomes to breast cancer MCF-7 cell line in vitro. METHODS: Cyperus rutundus L. rhizomes powder was extracted ethanol by percolation then fractionated with n-hexane. Phytochemical screening was then carried out. The cytotoxic activity of the n-hexane fraction was determined by observing this extract on MCF-7 cells using the (3- (4,5-dimethylimidazole-2-il) -2,5-diphenyl tetrazolium bromide) (MTT). Selectivity index (IS) of normal cells (Vero cells). Cell cycle and apoptosis induction were analyzed by flow cytometry. RESULTS: The result showed that the fraction n-hexane Cyperus rutundus L. rhizome has anticancer activity against breast cancer MCF-7 cells with accumulation cell cycle in the G0-G1 phase and through induction of apoptosis. CONCLUSION: The n-hexane fraction Cyperus rotundus L. rhizome has potent anticancer activity.

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