Chlorambucil-Chitosan Nano-conjugate: An efficient Agent against Breast Cancer Targeted Therapy

2020 ◽  
Vol 17 ◽  
Author(s):  
Azadeh Shayegh ◽  
Farinaz Khalatbari ◽  
Niloofar Zonoubi ◽  
Farjad Zarazvand ◽  
Fatemeh Monavvari ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Side Effects ◽  
Biological Effects ◽  
Rt Pcr ◽  
Chemotherapy Drugs ◽  
Anti Cancer ◽  
Afm Analysis ◽  
Cancer Targeted Therapy ◽  
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Background: Discovering new chemotherapy drugs and techniques with the least side effects is one of the most important and challenging world issues in recent years. Chlorambucil is an anticancer drug that is still commonly used as a primary treatmentin at treatment of some cancers, but it can cause side effects. Objective: In this study, we decided to use chitosan as a carrier for enhance the uptake of chlorambucil and reduce the toxicity of this drug. Method: After producing this nanoconjugate compound and analysing its structure by FTIR, DLS and AFM analysis, we investigated the therapeutic and biological effects of this nanoconjugate compound on the MCF-7 cell line (breast cancer). Results: The results of the MTT assay showed that this nanoconjugate compound not only retained its anti-cancer effect against chlorambucil but also showed less abnormal toxicity. Also, In vitro cellular uptake by flow cytometry indicated the better uptake final product into the MCF-7 cells. The detection of apoptosis induced cell death was confirmed by RT-PCR. Conclusion: This study has created a prospective pathway for targeting cancer cells using chitosan.

Evaluation of Anti-Tumor Potential of Lactobacillus acidophilus ATCC4356 Culture Supernatants in MCF-7 Breast Cancer

2020 ◽  
Vol 21 ◽  
Author(s):  
Ramazan Behzadi ◽  
Ahmad Hormati ◽  
Karim Eivaziatashbeik ◽  
Sajjad Ahmadpour ◽  
Fatemeh Khodadust ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Nude Mice ◽  
Control Group ◽  
Bacterial Strains ◽  
Anti Cancer ◽  
99Mtc Mibi ◽  
Culture Supernatants ◽  
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Background: Anti-cancer activity of some lactic acid bacterial strains is well documented in several literatures. Lactobacillus strains have received considerable attention as a beneficial microbiota. The aim of this study is to evaluate the effects of anti-tumor activities of L. acidophilus ATCC4356 culture supernatants on the MCF-7 human breast cancer cells. Materials and methods: Anti-cancer effect of 24h and 48h culture supernatants at various concentrations (1.25, 2.5, 5, 10 and 20 µg/ml) were determined by various in vitro and in vivo assays including MTT, tumor volume measurement as well as 99mTc-MIBI biodistribution in MCF-7 tumor bearing nude mice and histopathology test. For evaluation of the related mechanism of action, quantitative PCR was conducted. Results: The 48h culture supernatants at 10 and 20 µg/ml exhibited significant in vitro inhibition of MCF-7 cell proliferation. However, this inhibition was not observed for HUVEC human endothelial normal cells. Q-PCR indicated that treatment by the supernatant led to a significant downregulation of VEGFR ( ̴ 0.009 fold) and Bcl-2 ( ̴ 0.5 fold) and upregulation of p53 ( ̴ 1.3 fold). In vivo study using MCF-7 xenograft mouse models demonstrated reduction in tumor weight and volume by both 24h and 48h supernatants (10 µg/ml and 20 µg/ml) after 15 days. According to the 99mTc-MIBI biodistribution result, treatment of MCF-7 bearing nude mice with both 24h and 48h supernatant (20 µg/ml) led to significant decrease in tumor uptake compared with the control group. Conclusion: These results suggest that the culture supernatants of L. acidophilus ATCC4356 at suitable concentrations can be considered as a good alternative nutraceutical with promising therapeutic indexes for breast cancer.

Synthetic NRG-1 functionalized DNA nanospindels towards HER2/neu targets for in vitro anti-cancer activity assessment against breast cancer MCF-7 cells

2020 ◽  
Vol 182 ◽  
pp. 113133 ◽  
Author(s):  
Mirza Muhammad Faran Ashraf Baig ◽  
Wing-Fu Lai ◽  
Reyaj Mikrani ◽  
Mehreen Jabeen ◽  
Muhammad Naveed ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Activity Assessment ◽  
Anti Cancer ◽  
Cancer Activity ◽  
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scholarly journals Scorpion Venom-Functionalized Quercetin Phytosomes for Breast Cancer Management: In Vitro Response Surface Optimization and Anticancer Activity against MCF-7 Cells

Polymers ◽  
2021 ◽  
Vol 14 (1) ◽  
pp. 93
Author(s):  
Nabil A. Alhakamy ◽  
Usama A. Fahmy ◽  
Shaimaa M. Badr Eldin ◽  
Osama A. A. Ahmed ◽  
Hibah M. Aldawsari ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cell Cycle ◽  
Anticancer Activity ◽  
Cancer Cells ◽  
Biological Effects ◽  
Scorpion Venom ◽  
Cancer Management ◽  
Promising Therapeutic Approach ◽  
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Breast cancer is a dangerous type of cancer in women. Quercetin (QRT), a naturally occurring flavonoid, has wide biological effects including antioxidant, anticarcinogenic, anti-inflammatory, antiallergic, and antiviral activities. The anticancer activity is considered the most valuable effect of QRT against several types of cancer, including prostate, liver, lung, colon, and breast cancer. Scorpion venom peptides (SV) has been found to induce apoptosis and aggravate cancer cells, making it a promising anticancer agent. QRT, SV, and Phospholipon® 90H (PL) were incorporated in a nano-based delivery platform to assess QRT’s cellular uptake and antiproliferative efficacy against a lung cancer cell line derived from human breast cancer cells MCF-7. Several nanovesicles were prepared and optimized, using four-factor Box–Behnken, in an experimental design. The optimized phytosomes showed vesicle size and zeta potential values of 116.9 nm and 31.5 mV, respectively. The IC50 values revealed that MCF-7 cells were significantly more sensitive to the optimized QRT formula than the plain formula and raw QRT. Cell cycle analysis revealed that optimized QRT formula treatment resulted in significant cell cycle arrest at the S phase. The results also indicated that treatment with QRT formula significantly increased caspase-9, Bax, Bcl-2, and p53 mRNA expression, compared with the plain formula and QRT. In terms of the inflammatory markers, the QRT formula significantly reduced the activity of TNF-α and NF-κB, in comparison with the plain formula and QRT only. Overall, the findings from the study proved that a QRT formulation could be a promising therapeutic approach for the treatment of breast cancer.

scholarly journals INSILICO DESIGN, SYNTHESIS AND CHARACTERIZATION OF SOME NOVEL BENZOTHIAZOLE DERIVATIVES AS ANTI-CANCER AGENTS

2017 ◽  
Vol 10 (4) ◽  
pp. 150
Author(s):  
Leena K Pappachen ◽  
Subin Mary Zachariah ◽  
Deepthy Chandran
Keyword(s):  
Breast Cancer ◽  
Cell Lines ◽  
Docking Studies ◽  
Design Synthesis ◽  
Standard Drug ◽  
Mass Spectral ◽  
Benzothiazole Derivatives ◽  
Anti Cancer ◽  
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Objectives: Cancer is a disease characterized by uncontrollable, irreversible, independent, autonomous, uncoordinated and relatively unlimited and abnormal over growth of tissues. Breast cancer is the second most common type of cancer after lung cancer. The aim of the study is to carry out the docking studies, synthesis and anti-tumour activities  of Benzothiazole derivatives containing oxadiazole groups or amino groups.Methods: The docking studies of benzothiazole derivatives were done with known anti-cancer targets like oestrogen receptor by using argus lab and auto dock programmes with the standard drug tamoxifen. Based upon  the results obtained from the molecular modeling, the derivatives were selected for the synthesis. The synthesized compounds were characterized by melting point, TLC, IR, 1H NMR, 13CNMR, MASS spectral data and screened for their in- vitro anti-cancer activities.Results: The docking scores obtained for benzothiazole derivatives (BT1,BT2,BT3,BT4) and std.tamoxifen  from the preliminary docking program by using  argusLab  were- 9.68,-9.4,-9.59, -11.1988,-9.71 and  by using autodock program were -6.29, -5.25,-7.19,-7.48,-3.86 respectively. All the four derivatives were synthesized, characterized and subjected to in vitro anticancer screening by MTT assay in breast cancer (MCF-7) cell lines. Compounds DBT1, DBT2, DBT3 were the most active compounds against MCF-7 cell lines with IC50 of 70.0, 64.0 and 65.0, respectively.Conclusion: All the four  derivatives show  good docking scores when compared to standard drug and can be concluded that all the synthesized benzothiazole  ligands show good anti-cancer property.Keywords: Benzothiazole, Oxadiazole, Estrogen receptor, Anticancer targets.

scholarly journals Cytotoxic Effect of Two Novel Platinum (II) Complexes on Breast Cancer: An in Vitro Study

2018 ◽  
Vol 3 (2) ◽  
pp. 47-50
Author(s):  
Samad Akbarzadeh ◽  
Fatemeh Ebrahimi ◽  
Zeinab Faghih ◽  
Ali Movahed ◽  
Zahra Faghih
Keyword(s):  
Breast Cancer ◽  
Side Effects ◽  
Cell Lines ◽  
Cytotoxic Effect ◽  
Acquired Resistance ◽  
In Vitro Study ◽  
Cytotoxic Activities ◽  
Breast Cancer Patients ◽  
Chemotherapy Drugs

Background: With 1.36 million new cases in worldwide each year, breast cancer (BC) is the most common malignancy in the female. Among numerous chemotherapy drugs which are widely used for cancer therapy, platinum compounds are the most persuasive ones although challenges remain with the clinical use of them due to their side effects as well as intrinsic and acquired resistance. In the attempt to combat drug resistance, reduce cytotoxic side effects or find the drug for particular forms of cancer, over the years, thousands of other platinum (Pt) compounds i.e. carboplatin and oxaliplatin have been developed.Material and Methods: In this regard, we previously described the synthesis of some new platinum (II) derivatives with potential anti-cancer activities against BC. Here, we chose two of the best platinum(II) compounds, 3b and 2a, to further evaluate their cytotoxic activities against human BC cell lines, SKBR3, MCF-7, MDA-MB-231, and MBA-MB-468, with different molecular subtypes using a colorimetric MTT cytotoxic assay. Their cytotoxic activities were compared to cis-platin as a positive control. Results: Our result showed that both compounds had better cytotoxic effect against BC cell lines than cis-platin in particular in the case of triple-negative subtype.Conclusion: These results suggest these compounds as potentially valuable agents for the treatment of breast cancer patients.

scholarly journals WISP2/CCN5 gene knockdown in vitro and in vivo exhibits proliferation promotion of breast cancer through targeting Skp2 and p27Kip1

2020 ◽  
Author(s):  
Yan Lv ◽  
Chang Zhang ◽  
Xiao Jiang Li ◽  
Shan Gao ◽  
Xu Zheng ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cancer Cells ◽  
Breast Cancer Cells ◽  
Gene Knockdown ◽  
Control Group ◽  
Rt Pcr ◽  
Protein Levels ◽  
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AbstractBackgroundEmerging evidence has demonstrated that WISP2/CCN5 is critically involved in tumorigenesis. However, the function of WISP2/CCN5 in breast cancer carcinogenesis is largely unclear.Methodswe aim to explore the effects and potential mechanisms of WISP2/CCN5 on proliferation of breast cancer cells and carcinogenesis of breast cancer xenograft. Lentivirus vector with WISP2/CCN5shRNA was transfected into MCF-7, and breast cancer cells and xenograft were conducted. Effect of WISP2/CCN5 on growth and carcinogenesis of breast cancer cells and xenografts was evaluated by MTT assay and tumor volume. The relationship between WISP2/CCN5, Skp2 and p27Kip1 was detected in vitro and in vivo by RT-PCR at mRNA level and Western blotting at protein level.ResultsThe result of MTT assay indicated that MCF-7 cell growth viability in WISP2/CCN5 gene knockdown group was significantly higher than negative vector group(P<0.05) or control group (P<0.05). It suggested that knockdown of WISP2/CCN5 gene by shRNA lentivirus plasmid promoted proliferation of MCF-7 cells. The growth curves of breast cancer xenograft showed that xenografts in WISP2/CCN5 knockdown group grew more quickly than negative vector group(P< 0.05) or control group (P< 0.05). Subsequently, the results of RT-PCR and Western blotting revealed that WISP2/CCN5 gene knockdown led to increased Skp2 and decreased p27Kip1 at mRNA and protein levels. WISP2/CCN5 exerts its inhibition on proliferation of MCF-7 cell line and suppressive functions on growth of breast carcinoma via regulation of Skp2 and p27Kip1at mRNA and protein levels. However, WISP2/CCN5 gene knockdown resulted in loss of inhibition effect on MCF-7 and breast cancer.ConclusionsOur findings suggest that WISP2/CCN5 could be a useful therapeutic strategy for the treatment of breast cancer through targeting Skp2 and p27Kip1.

scholarly journals Evaluation of Anticancer Activity of Neolamarckia Cadamba Leaves and Its Metabolite Profile

2021 ◽  
Author(s):  
Shakirah Razali ◽  
Al’aina Firus Khan ◽  
Alfi Khatib ◽  
Qamar Uddin Ahmed ◽  
Habibah Hassan ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Gene Expression ◽  
Cell Cycle ◽  
Cell Cycle Arrest ◽  
Traditional Use ◽  
Chromatography Analysis ◽  
Cycle Arrest ◽  
Anti Cancer ◽  
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Abstract Neolamarckia cadamba (NC) leaf is traditionally used for the treatment of breast cancer, however this claim is unverified. This study aimed to evaluate the anti-cancer activities of NC leaf ethanol extract on breast cancer cell line (MCF-7 cells) using in vitro cell viability, cytotoxicity and gene expression assays followed by gas chromatography analysis. Results revealed inhibition concentration (IC50) against MCF-7 at 0.2 mg/mL. The extract exerted a dose and time dependent inhibitory effect against MCF-7 cells. The cell cycle assay showed that the extract arrested MCF-7 cells in G0/G1 phase, and apoptosis were observed after 72 hours by Annexin-V assay. The gene expression assay revealed that the cell cycle arrest was associated with the down-regulation of CDK2 and subsequent up-regulation of p21 and cyclin E. The extract induced apoptosis via mediation of the mitochondrial cell death pathways. Chromatography analysis revealed the contribution of d-pinitol and myo-inositol to the activity observed as the two major bioactive compounds. Overall, the study demonstrated that NC exerts anti-cancer effect on MCF-7 human breast cancer cells through induction of apoptosis and cell cycle arrest thus justifying its traditional use for breast cancer treatment in Malaysia.

scholarly journals Selinexor Improves the Anti-Cancer Effect of Tucidinostat on TP53 Wild-type Breast Cancer

2021 ◽  
Author(s):  
Shengxi Xu ◽  
Yingfang Shi ◽  
Sen Li
Keyword(s):  
Breast Cancer ◽  
Cyclin D1 ◽  
Effective Strategy ◽  
Wild Type ◽  
Expression Levels ◽  
Anti Cancer ◽  
Protein Expressions ◽  
Proliferation And Invasion ◽  
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Abstract Background: Histone deacetylase (HDAC) is closely related to the occurrence and development of breast cancer (BC). Its inhibitor (HDACi) has been used to treat BC, while the efficacy of clinical trials was not reached expectations. HDACi combined with other drugs may be an effective strategy. This study explored the effect of HDACitucidinostat combined with selinexor, anexportin 1 (XPO1) inhibitor, on BC cellsin vitro. Methods: BC cell lines of MCF-7 (wt-TP53), MDA-MB-175 (wt-TP53), MDA-MB-134 (mut-TP53), T47D (mut-TP53) were cultured. The IC50 values of tucidinostat and selinexor on BC cells were calculated. The effects of tucidinostat and selinexor on proliferation, invasion and apoptosis of BC cells were observed accordingly. Western blotting was used to detect the protein expressions of p53, p21, Cyclin D1, Bcl-2 and Bax.Results:Compared with mut-TP53 BC, both tucidinostat and selinexor showed better inhibitory activitiesonwt-TP53 BC including MCF-7 and MDA-MB-175. Tucidinostat combined with selinexor significantly improved the effects of tucidinostat alone on the proliferation and invasion inhibitions and apoptosis promotionsof MCF-7 and MDA-MB-175 cells in vitro. It also significantly enhanced the effects of tucidinostat on up-regulating the expression levels of acetyl-p53, nuclear p53, total p53, p21 and Bax, and down-regulating the expression levels of Cyclin D1 and Bcl-2 in MCF-7 or MDA-MB-175 cells. Conclusion: Taken together, we believe that tucidinostat and selinexor are potentially effective drug combinations for the treatment of wt-TP53 BC, and the molecular mechanism may be throughenhancing the activity of p53 in the nucleus of BC cells to suppress proliferation and invasion and promote apoptosis of BC cells.

scholarly journals In vitro Anti-oxidant and Anti-cancer Activity of Tetradesmus acuminatus Microalgae Extract on MCF-7 Human Breast Cancer Cell Line

2019 ◽  
Vol 16 (1) ◽  
pp. 1-9 ◽  
Author(s):  
Mohammed Abdul Mujeeb ◽  
Ankalabasappa Vedamurthy ◽  
Arun Kashivishwanath Shettar ◽  
Sridevi Indrajeet Puranik ◽  
Shridhar Ghagane ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Human Breast Cancer ◽  
Cancer Cell Line ◽  
Human Breast Cancer Cell ◽  
Human Breast ◽  
Anti Cancer ◽  
Anti Oxidant ◽  
Cancer Activity ◽  
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scholarly journals Sea Cucumber Intestinal Peptide Induces the Apoptosis of MCF-7 Cells by Inhibiting PI3K/AKT Pathway

2021 ◽  
Vol 8 ◽  
Author(s):  
Wei Wei ◽  
Xiao-Man Fan ◽  
Shao-Hui Jia ◽  
Xi-Ping Zhang ◽  
Zhao Zhang ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Amino Acids ◽  
Sea Cucumber ◽  
Bioactive Substances ◽  
Sea Cucumbers ◽  
Anti Cancer ◽  
Active Substances ◽  
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Sea cucumbers are one of many marine echinoderm animals that contain valuable nutrients and medicinal compounds. The bioactive substances in sea cucumbers make them have promising biological and pharmacological properties, including antioxidant, anti-bacterial, and anti-tumor effects. In this study, sea cucumber intestinal peptide (SCIP) is a small molecular oligopeptide (&lt;1,000 Da) extracted from sea cucumber intestines hydrolyzed by alkaline protease. The analysis of amino acid composition showed that hydrophobic amino acids and branched-chain amino acids were rich in SCIP. Nowadays, although increasing studies have revealed the biological functions of the sea cucumber active substances, there are few studies on the function of SCIP. Furthermore, due to the anti-cancer activity being an essential characteristic of sea cucumber active substances, we also investigated the anti-cancer potential and the underlying mechanism of SCIP in vivo and in vitro. The results indicate that SCIP inhibits the growth of MCF-7 tumor cells in zebrafish and increases the apoptosis of human breast cancer MCF-7 cells. Further mechanism studies confirm that SCIP promotes the expression of apoptosis-related proteins and thus promotes the breast cancer cells (MCF-7) apoptosis via inhibition of PI3K/AKT signal transduction pathway.

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