scholarly journals Development of Some Novel Coumarin-Chalcone Compounds as Anti-proliferative Agents

2021 ◽  
pp. 105-111
Author(s):  
Kuldeep Patel ◽  
Jagdish Chandra Rathi ◽  
Neerupma Dhiman
Keyword(s):  
Cell Line ◽  
Proliferative Activity ◽  
Breast Epithelial Cell ◽  
Cancer Breast ◽  
Rational Development ◽  
Anti Cancer ◽  
Different Types ◽  
Cell Cycle Inhibitors ◽  
Tumor Drugs ◽  
Mcf 7

Introduction: Cancer is the world's second leading cause of death and morbidity, behind only heart failure, which claimed the lives of 18.2 million people in 2020. While massive initiatives to establish newer leads and innovative chemotherapeutic methods for combating different types of cancer, continues to be a major concern around the world. As a result, identifying cell-cycle inhibitors and apoptotic triggers to fight cancer cells is an appealing method for finding and developing new anti-tumor drugs. Materials and Methods: The present study involves the rational development and characterization (both physicochemical and spectroscopy) of coumarin-chalcone compounds (A1–A10) and their anti-proliferative potentials against cancer lines of breast cancer origin (MDA-MB468, MDA-MB231, and MCF-7) and non-cancer breast epithelial cell (184B5). Results: The compound A2 exhibited the highest anti-proliferative activity against the cell line MDA-MB-231 as indicated by the GI50 value of 10.06 μM, the compound A6 exhibited the highest anti-proliferative activity against the cell line MDA-MB-468 as indicated by the GI50 value of 17.54 μM, the compound A1 exhibited the highest anti-proliferative activity against the cell line MCF-7 as indicated by the GI50 value of 25.86 μM, and the compound A6 exhibited the highest anti-proliferative activity against the cell line 184B5 as indicated by the GI50 value of 23.26 μM. Conclusion: Furthermore, the research urges medicinal chemists to choose chalcone prototypes with well-defined pathways and SARs while developing more powerful inhibitors. Furthermore, it opens up new pathways for the discovery of anti-cancer derivatives using low molecular weight ligands.

Design, Synthesis and In Vitro Anti-Cancer Evaluation of Novel Derivatives of 2-(2-Methyl-1,5-diaryl-1H-pyrrol-3-yl)-2-oxo-N-(pyridin-3- yl)acetamide

2020 ◽  
Vol 16 (3) ◽  
pp. 340-349
Author(s):  
Ebrahim S. Moghadam ◽  
Farhad Saravani ◽  
Ernest Hamel ◽  
Zahra Shahsavari ◽  
Mohsen Alipour ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Peripheral Neuropathy ◽  
Cell Line ◽  
Normal Cell ◽  
Caspase 3 ◽  
Annexin V ◽  
Normal Cell Line ◽  
Anti Cancer ◽  
Mcf 7

Objective: Several anti-tubulin agents were introduced for the cancer treatment so far. Despite successes in the treatment of cancer, these agents cause toxic side effects, including peripheral neuropathy. Comparing anti-tubulin agents, indibulin seemed to cause minimal peripheral neuropathy, but its poor aqueous solubility and other potential clinical problems have led to its remaining in a preclinical stage. Methods: Herein, indibulin analogues were synthesized and evaluated for their in vitro anti-cancer activity using MTT assay (on the MCF-7, T47-D, MDA-MB231 and NIH-3T3 cell lines), annexin V/PI staining assay, cell cycle analysis, anti-tubulin assay and caspase 3/7 activation assay. Results: One of the compounds, 4a, showed good anti-proliferative activity against MCF-7 cells (IC50: 7.5 μM) and low toxicity on a normal cell line (IC50 > 100 μM). All of the tested compounds showed lower cytotoxicity on normal cell line in comparison to reference compound, indibulin. In the annexin V/PI staining assay, induction of apoptosis in the MCF-7 cell line was observed. Cell cycle analysis illustrated an increasing proportion of cells in the sub-G-1 phase, consistent with an increasing proportion of apoptotic cells. No increase in G2/M cells was observed, consistent with the absence of anti-tubulin activity. A caspase 3/7 assay protocol showed that apoptosis induction by more potent compounds was due to activation of caspase 3. Conclusion: Newly synthesized compounds exerted acceptable anticancer activity and further investigation of current scaffold would be beneficial.

scholarly journals Anti-cancer efficacy of ethanolic extracts from various parts of Annona Squamosa on MCF-7 cell line

2016 ◽  
Vol 8 (7) ◽  
pp. 147-154 ◽  
Author(s):  
Veerakumar Sneeha ◽  
Shaikh Dawood Amanulla Safreen ◽  
Ramanathan Kumaresan
Keyword(s):  
Cell Line ◽  
Annona Squamosa ◽  
Anti Cancer ◽  
Ethanolic Extracts ◽  
Mcf 7

scholarly journals Synthesis of Silver-Doxycycline Complex Nanoparticles and Their Biological Evaluation on MCF-7 Cell Line of the Breast Cancer

2021 ◽  
Vol 2021 ◽  
pp. 1-8
Author(s):  
Vahid Mohammadkarimi ◽  
Negar Azarpira ◽  
Zahra Ghanbarinasab ◽  
Pezhman Shiri ◽  
Fatemeh Sadat Dehghani ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Silver Nitrate ◽  
Cell Line ◽  
Biological Evaluation ◽  
Potent Effect ◽  
Different Types ◽  
The Future ◽  
Mcf 7

In the current study, we aim to evaluate the effect of the combination of silver and doxycycline (silver-doxycycline complex) on the viability of the MCF-7 cell line of the breast in comparison with each of them. The Ag-doxycycline NPs were synthesized using silver nitrate and doxycycline solutions. The synthesized Ag-doxycycline NPs were characterized with several analyses. Ag-doxycycline NPs with a concentration of 25 μM is significantly more effective in decreasing the viability of MCF-7 cells than Ag with the same concentration ( P < 0.05 ). Doxycycline with a concentration of 6.25 μM also has a more potent effect on the viability of MCF-7 cells than Ag with the same concentration ( P < 0.05 ). Ag-doxycycline NPs with a 25 μM concentration is more effective than the concentration of 3.125 μM ( P < 0.05 ). Ag-doxycycline NPs were found to be more effective than AgNPs alone in inhibiting the growth of the MCF-7 cells. Also, the increasing utility of nanotechnology in multiple aspects of medicine can lead to using this technology in the treatment of different types of cancer in the future.

scholarly journals Anti cancer activity of Trachyspermum ammi against MCF7 cell lines mediates by p53 and Bcl-2 mRNA levels

2017 ◽  
Vol 6 (2) ◽  
pp. 78-83
Author(s):  
N Ramya ◽  
◽  
Priyadharshini ◽  
R Prakash ◽  
R Dhivya ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cell Line ◽  
Dna Fragmentation ◽  
Cell Lines ◽  
Ethanolic Extract ◽  
Mrna Levels ◽  
Trachyspermum Ammi ◽  
Anti Cancer ◽  
Cancer Activity ◽  
Mcf 7

Breast cancer is second most common in women and accounts for 23% of all occurring cancers in women. Patients with breast cancer have increasingly shown resistance and high toxicity to chemotherapeutic drugs. Plant-derived products have proved to be an important source of anti-cancer drugs. The present study was to investigate the anti cancer activity of ethanolic extract of Trachyspermum ammi against MCF-7 cell lines. The preliminary phytochemical studies of ethanolic extract of Trachyspermum ammi showed the presence of flavanoids, alkaloids, glycosides, steroids, carbohydrates, phenols, tannins and terpenes. The IC50 concentration of ethanolic extract of Trachyspermum ammi was determined by MTT assay. The results showed the greater degree of cytotoxicity at the dose of 25µg/ml of Trachyspermum ammi and it has been taken as IC50 value for our further study. Then, we also evaluated the apoptotic effect by measuring the morphological changes, cell viability rates using light and fluorescent microscopical studies and DNA fragmentation by using gel electrophoresis method. The ethanolic extract of Trachyspermum ammi showed significant signs of apoptosis such as cell shrinkage, membrane blebbing and nuclei DNA fragmentation. Further, we analyze the gene expression mRNA levels by using RT-PCR method, it showed the expression of p53 was significantly (P<0.001) increased when compared with normal MCF-7 cell line. The expression of anti apoptotic gene Bcl-2 was significantly (P<0.01) reduced when compared with MCF-7 cell line. From this study we conclude that ethanolic extract of Trachyspermum ammi having significant anticancer activity against MCF-7 cell lines and it might be good therapeutic value for further investigation to develop natural compounds as a anti tumor agents.

scholarly journals Substituted Thiazole Linked Murrayanine-Schiff�s Base Derivatives as Potential Anti-Breast Cancer Candidates: Future EGFR Kinase Inhibitors

2017 ◽  
Vol 9 (3) ◽  
Author(s):  
Debarshi Kar Mahapatra ◽  
Devashish Das ◽  
Ruchi Shivhare
Keyword(s):  
Breast Cancer ◽  
Cell Line ◽  
Kinase Inhibitors ◽  
Analytical Techniques ◽  
Docking Study ◽  
Breast Cancer Cell Lines ◽  
Synthetic Approach ◽  
Hybrid Molecules ◽  
Anti Cancer ◽  
Mcf 7

Cancer is the second leading causes of mortality across the planet which has had affected millions. In spite of massive efforts in producing new molecules and chemotherapeutic approaches for managing cancer, it continued to be the global threat. Small hybrid molecules have gained popularity in chemotherapy due to their potential and smart characteristics in modulating biological targets. The present research attempts in developing few novel hybridized derivatives of murrayanine (an active carbazole derivative) by the semi-synthetic approach to form substituted thiazole linked murrayanine-Schiffs base derivatives. The protocol involved murrayanine 1 as the template material for constructing a hybridized Schiffs base intermediate 3, which further by Hantzchs cyclization was subsequently converted to various hybridized thiazoles analogs 5a-5f. The purity of the synthesized compounds was ascertained by sophisticated analytical techniques. The anti-cancer potential was screened against breast cancer cell lines; MCF-7 and MDA-MB-231 by Sulforhodamine B (SRB) assay. The compound 5b displayed most potent anti-proliferative activity with IC50 values of 23.41?M against MCF-7 cell line and 32.15?M against MDA-MB-231 cell line. It has been observed that analogs having electron withdrawing substituents exhibited pronounced anticancer activity. The docking study was performed by Autodock Vina where the results were found to be in full agreement with the cytotoxic study, depicting that the probable cytotoxic outcome by EGFR inhibitory mechanism. The study revealed the potential of novel hybridized derivatives as active anti-breast cancer candidates. The research will encourage (medicinal) chemists in rationally designing of semi-synthetic analogs of a heterocyclic prototype having pronounced anti-cancer activity.

Producing the sour cherry pit oil nanoemulsion and evaluation of its anti-cancer effects on both breast cancer murine model and MCF-7 cell line

2019 ◽  
Vol 36 (4) ◽  
pp. 399-409 ◽  
Author(s):  
Atieh Darchini Maragheh ◽  
Masoud Homayouni Tabrizi ◽  
Ehsan Karimi ◽  
Seyed Mohammad Reza Seyedi ◽  
Niloufar Khatamian
Keyword(s):  
Breast Cancer ◽  
Cell Line ◽  
Murine Model ◽  
Sour Cherry ◽  
Anti Cancer ◽  
Mcf 7

Antioxidant and Anti-Proliferative Activity of Calamintha officinalis Extract on Breast Cancer Cell Line MCF-7

2015 ◽  
Vol 15 (4) ◽  
pp. 194-198 ◽  
Author(s):  
Fatemeh Shams Moattar ◽  
Reyhaneh Sariri ◽  
Masoud Giahi ◽  
Prichehr Yaghmaee ◽  
Hosein Ghafoori ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cell Line ◽  
Cancer Cell ◽  
Breast Cancer Cell ◽  
Breast Cancer Cell Line ◽  
Proliferative Activity ◽  
Cancer Cell Line ◽  
Mcf 7

scholarly journals Evaluating the anticancer effects of high-dilution preparations of carcinogens such as HIV virus, Hepatitis C virus, Ethanol and Cancer tissues in in-vitro models

2021 ◽  
Vol 18 (1) ◽  
pp. 11-26
Author(s):  
Rajesh Shah
Keyword(s):  
Hepatitis C ◽  
Anticancer Activity ◽  
Cell Line ◽  
Leukemia Cell Line ◽  
Human Leukemia ◽  
High Dilution ◽  
Anticancer Effects ◽  
Anti Cancer ◽  
Mcf 7

Background Cancer is one of the leading causes of mortality. The recent experiments with high-diluted preparations have shown anticancer effects in in-vitro and vivo models. The fundamental principle of homeopathy suggests that the substances capable of producing certain diseases may have a capacity to alter the same disease if used in the ultra-dilute-potentized form. This hypothesis led certain carcinogens for examining their potential anti-cancer efficacy. Method Sulforhodamine B assay is useful in determining the cytotoxicity in cell-based studies in evaluating anticancer agents. The protocol involved preparation of homeopathy dilutions, incubation of cells with homeopathy dilutions, SRB binding, and measurement of absorbance. Cells were treated with 30 potencies of HIV nosode, Hepatitis C nosode, Carcinosin, Cancer nosode, and Ethanol along with positive control (Adriamycin). The preparations were tested in HeLa, HepG2, A549, MCF 7, T 24, Jurkat, SCC 40, and HL-60 cell-lines. Results The homeopathic preparations have shown the anticancer activity measured as percentage growth inhibition. All the homeopathy preparations studied, exhibited anticancer activity on HeLa, HepG2, A 549, T 24, and HL-60 cells. Carcinosin showed the anticancer activity on the SCC 40 cells. Hepatitis C nosode, Carcinosin, and Cancer nosode have shown the anticancer activity on breast cancer cell line MCF-7. None of the preparations exhibited anticancer activity on Human Leukemia Cell Line. Conclusion High-dilution, potentized preparations of certain carcinogens have demonstrated anti-cancer, cytotoxic effects in the cell-line model, supporting the rationale of the fundamental homeopathic principle the Law of Similars, opening windows to its wider applications in healthcare.

scholarly journals Niclosamide loaded biodegradable chitosan nanocargoes: an in vitro study for potential application in cancer therapy

2017 ◽  
Vol 4 (11) ◽  
pp. 170611 ◽  
Author(s):  
Saba Naqvi ◽  
Shanid Mohiyuddin ◽  
P. Gopinath
Keyword(s):  
Breast Cancer ◽  
Cancer Therapy ◽  
Cell Line ◽  
Cancer Cell ◽  
Breast Cancer Cell ◽  
Chitosan Nanoparticles ◽  
Cancer Cell Line ◽  
Human Lung Cancer ◽  
Anti Cancer ◽  
Mcf 7

Chitosan nanoparticles can advance the pharmacological and therapeutic properties of chemotherapeutic agents by controlling release rates and targeted delivery process, which eliminates the limitations of conventional anti-cancer therapies and they are also safe as well as cost-effective. The aim of present study is to explore the anti-tumour effect of niclosamide in lung and breast cancer cell lines using biocompatible and biodegradable carrier where nanoparticles loaded with hydrophobic drug (niclosamide) were synthesized, characterized and applied as a stable anti-cancer agent. Niclosamide loaded chitosan nanoparticles (Nic-Chi Np's) of size approximately 100–120 nm in diameter containing hydrophobic anti-cancer drug, i.e. niclosamide, were prepared. Physico-chemical characterization confirms that the prepared nanoparticles are spherical, monodispersed and stable in aqueous systems. The therapeutic efficacy of Nic-Chi Np's was evaluated against breast cancer cell line (MCF-7) and human lung cancer cell line (A549). MTT assay reveals the cell viability of the prepared Nic-Chi Np's against A549 and MCF-7 cells and obtained an IC 50 value of 8.75 µM and 7.5 µM, respectively. Acridine orange/ethidium bromide dual staining results verified the loss of the majority of the cells by apoptosis. Flow cytometer analysis quantified the generation of intracellular reactive oxygen species (ROS) and signified that exposure to a higher concentration (2 × IC 50 ) of Nic-Chi Np's resulted in elevated ROS generation. Notably, Nic-Chi Np treatment showed more apoptosis and cell death in MCF-7 as compared to A549. Further, the remarkable induction of apoptosis by Nic-Chi Np's was confirmed by semi-quantitative reverse transcription polymerase chain reaction, scanning electron microscopy and cell-cycle analysis. Thus, Nic-Chi Np's may have a great potential even at low concentration for anti-cancer therapy and may replace or substitute more toxic anti-mitotic drugs in the near future.

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