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 ◽  
Mcf 7

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 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.

scholarly journals Anticancer Activity of N-Hexane Extract from Sphagneticola trilobata (L.) J.F Pruski Against MCF-7 Breast Cancer Cell

Elkawnie ◽  
2020 ◽  
Vol 6 (1) ◽  
pp. 48 ◽  
Author(s):  
Vivi Mardina ◽  
Tisna Harmawan ◽  
Halimatussakdiah Halimatussakdiah ◽  
Syafruddin Ilyas ◽  
Masitta Tanjung
Keyword(s):  
Breast Cancer ◽  
Anticancer Activity ◽  
Cancer Cells ◽  
Breast Cancer Cells ◽  
Probit Analysis ◽  
Hexane Extract ◽  
Tetrazolium Salt ◽  
Cytotoxicity Test ◽  
Mcf 7

Abstract : Sphagneticola trilobata (L.) J.F. Pruski is one of the perennial herbs that is widely used by the national and international community to treat various diseases including cancer. The objective of this study was to assessment the anticancer activity of n-hexane extract of S. trilobata leaves for inhibiting the growth of MCF-7 breast cancer cells in vitro by MTT (microculture tetrazolium salt) method. The n-hexane extract of sernai leaves was obtained from the maceration process of samples that were collected from the Langsa city, Aceh. The cytotoxicity test was carried out by incubating MCF-7 cells which had been exposed to several series of sample levels, viz. 1000; 500; 100; 50; 25; 10; 5 and 1 µg/mL. LC50 values are calculated using probit analysis. The results revealed that the n-hexane extract of S. trilobata leaves was cytotoxic against breast cancer cells (MCF-7) with an LC50 value of  0.037 μg /mL.Abstrak : Sphagneticola trilobata (L.) J.F. Pruski merupakan salah satu tanaman herbal yang digunakan secara luas oleh masyarakat nasional dan internasional untuk mengobati berbagai penyakit termasuk kanker. Penelitian ini bertujuan untuk mengetahui aktivitas antikanker ekstrak n-heksana daun S. trilobata dalam menghambat pertumbuhan sel kanker payudara MCF-7 secara in vitro dengan metode MTT (microculture tetrazolium salt). Ekstrak n-heksana daun sernai diperoleh dari proses maserasi sampel yang dikoleksi dari kota Langsa, Aceh. Uji sitotoksisitas dilakukan dengan menginkubasi sel MCF-7 yang telah dipaparkan beberapa seri  kadar sampel yaitu 1000, 500, 100, 50, 25, 10, 5 dan 1 µg/mL. Nilai LC50 dihitung dengan menggunakan analisa probit. Hasil penelitian menunjukkan bahwa ekstrak n-heksana daun S. trilobata bersifat sitotoksik terhadap sel kanker payudara (MCF-7) dengan harga LC50 sebesar 0,037 µg/mL. 

scholarly journals Aptamer-Protamine-siRNA Nanoparticles in Targeted Therapy of ErbB3 Positive Breast Cancer Cells

2020 ◽  
Author(s):  
Xiangshang Xu ◽  
Li Li ◽  
Xiaolan Li ◽  
Deding Tao ◽  
Peng Zhang ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cell Cycle ◽  
Tumor Growth ◽  
Cancer Cells ◽  
Tumor Regression ◽  
Inhibit Tumor Growth ◽  
Mcf 7 ◽  
Positive Breast Cancer

Abstract Background: RNAi-based technology has achieved good results in both in vitro and in vivo applications, and it is expected to become a good genetic treatment for some diseases, especially neoplastic diseases. But there are still many obstacles in the in vivo application, the most important thing is the lack of an efficient and safe carrier.Methods: In this study, we designed and constructed a new siRNA delivery, which was named as aptamer-protamine-siRNA nanoparticle (APR). APR was consisted of ErbB3 aptamer, protamine and siRNA. We used Zeta nanosize to detect the size of APR to verify whether it is a nano-scale compound. We use the FAMRNA to replace the siRNA to detect whether APR could recognize and enter ErbB3 positive MCF-7 cells. The we replaced the siRNA as oncogene suvivin siRNA to detect whether APR could inhibit tumor growth by silence surviving, and replaced siRNA to CDK1 siRNA to detect the cell cycle blocking effect. At last we tested the anticancer effect and safety of APR by carrying survivin siRNA in MCF-7 bearing nude mice. Results: APR was identified as a nanoscale compound. It showed specific targeting for ErbB3-positive MCF-7 cancer cells. APR has demonstrated the characteristics of inhibiting tumor growth by carrying siRNA against oncogene survivin. APR could also block cell cycle of MCF-7 cells by delivering CDK1 siRNAs. In the ErbB3 positive breast cancer xenograft mice model, APR nanoparticles could inhibit tumor growth and cause tumor regression without any toxicity. Conclusions: In both in vivo and in vitro applications, APR nanoparticles could be targeted to recognize and enter ErbB3 positive tumor cells, and play a corresponding role by silencing targeted gene expression. APR nanoparticle is expected to become a good tumor treatment option.

In Vitro Assessment of Homeopathic Potencies of Hydrastis canadensis on Hormone-Dependent and Independent Breast Cancer

Homeopathy ◽  
2020 ◽  
Vol 109 (04) ◽  
pp. 198-206
Author(s):  
Sabiha Khan ◽  
Debadatta Nayak ◽  
Anil Khurana ◽  
Raj Kumar Manchanda ◽  
Chanderdeep Tandon ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cell Cycle ◽  
Cancer Cells ◽  
Breast Cancer Cells ◽  
Cytotoxic Effect ◽  
Caspase 3 ◽  
Hydrastis Canadensis ◽  
Induction Of Apoptosis ◽  
Mcf 7

Abstract Background Breast cancer is the second leading cause of cancer-related deaths in women. Conventional treatment such as chemotherapy, hormonal therapy and radiotherapy has decreased the mortality rate among cancer patients but has also revealed long-term side effects. Drug resistance and toxicity to normal cells compound the problems associated with the use of modern medicines. Hence, complementary or alternative treatment options are being explored. The current study, using different homeopathic potencies of Hydrastis canadensis, was conducted to distinguish between any effects they might have on hormone-dependent and independent breast cancer. Materials and Methods The cytotoxic effect of homeopathic medicine Hydrastis on hormone-dependent (MCF 7) and hormone-independent (MDA-MB-468) breast cancer cells was assessed using viability and colony-forming assays after 48 or 72 hours of treatment. Flow cytometry-based Annexin V-PI (propidium iodide), caspase 3 and cell cycle analysis was performed following treatment of cells with mother tincture or various potencies of Hydrastis (1C, 2C, 30C, 200C). Results Different potencies of Hydrastis displayed selective cytotoxic effects against MCF 7 cells, but only marginal effects against MDA-MB-468. The maximum cytotoxicity was established in the case of 1C following 72 hours of treatment. Treatment of breast cancer cells revealed an increase in the G0/G1 cell population, along with an increase in the caspase 3 levels and induction of apoptosis. Conclusion Hydrastis may have a selective cytotoxic effect against hormone-dependent breast cancer MCF 7 cells, leading to cell cycle arrest in the G0/G1 phase, which could be the plausible reason for the induction of apoptosis. The results need to be validated in vivo.

scholarly journals Ursolic Acid Enhances Doxorubicin Cytotoxicity on MCF-7 Cells Mediated by G2/M Arrest

2012 ◽  
Vol 3 (3) ◽  
pp. 410
Author(s):  
Ibrahim Arifin ◽  
Adam Hermawan ◽  
Muthi' Ikawati ◽  
Sari Haryanti ◽  
Anindyajati Anindyajati ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cell Cycle ◽  
Cancer Cells ◽  
Ursolic Acid ◽  
Breast Cancer Cells ◽  
Chemotherapeutic Agent ◽  
Ic50 Value ◽  
Combinational Treatment ◽  
Mcf 7

Ursolic acid has been widely known to possess biological activity against numerous tumor cell lines. Previous studies revealed its cytotoxicity on several cancer cells in vitro by either inducing apoptosis or cell cycle modulation. This study was conducted to investigate ursolic acid’s cytotoxicity solely and in combination with a chemotherapeutic agent, doxorubicin, on MCF-7 breast cancer cells, followed by observation on its mechanism. Cytotoxicity of single and combinational treatment of ursolic acid and doxorubicin on MCF-7 breast cancer cells were conducted by using MTT assay. Single treatment was then evaluated by determining IC50 value, while combinational treatment was evaluated by analyzing cell viability and evaluating combination index (CI). To explore the mechanism underlying cytotoxic effect on respected cells, further analysis on cell cycle profile of single and combinational treatment was conducted by flow cytometry. Twenty four hours treatment of ursolic acid inhibited MCF-7 cells’ growth with IC50 value of 37 µM, while combinational treatment showed that several concentration combinations of ursolic acid and doxorubicin exhibited synergism of cytotoxic activity on MCF-7 cells, giving optimum CI value of 0.54. Flow cytometric analysis showed that combinational treatment induced G2/M arrest in MCF-7 cells. These results show that ursolic acid is promising to be developed as either single chemopreventive agent, or as doxorubicin’s co-chemotherapeutic agent in breast cancer treatment. Observation on the selectivity as part of safety aspect together with in silico, in vitro, and in vivo study on its molecular mechanism should be conducted.Keywords: ursolic acid, doxorubicin,co-chemotherapeutic agent, breast cancer, cell cycle

scholarly journals Induction of Apoptosis and Regulation of MicroRNA Expression by (2E,6E)-2,6-bis-(4-hydroxy-3-methoxybenzylidene)-cyclohexanone (BHMC) Treatment on MCF-7 Breast Cancer Cells

Molecules ◽  
2021 ◽  
Vol 26 (5) ◽  
pp. 1277
Author(s):  
Swee Keong Yeap ◽  
Norlaily Mohd Ali ◽  
Muhammad Nadeem Akhtar ◽  
Nursyamirah Abd Razak ◽  
Zhi Xiong Chong ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cell Cycle ◽  
Cancer Cells ◽  
Breast Cancer Cells ◽  
Quantitative Polymerase Chain Reaction ◽  
M Cell ◽  
Cytotoxic Effects ◽  
Er Positive ◽  
Mcf 7

(2E,6E)-2,6-bis-(4-hydroxy-3-methoxybenzylidene)-cyclohexanone (BHMC) is a synthetic curcumin analogue, which has been reported to possess anti-tumor, anti-metastatic, and anti-invasion properties on estrogen receptor (ER) negative breast cancer cells in vitro and in vivo. However, the cytotoxic effects of BHMC on ER positive breast cancer cells were not widely reported. This study was aimed to investigate the cytotoxic potential of BHMC on MCF-7 cells using cell viability, cell cycle, and apoptotic assays. Besides, microarray and quantitative polymerase chain reaction (qPCR) were performed to identify the list of miRNAs and genes, which could be dysregulated following BHMC treatment. The current study discovered that BHMC exhibits selective cytotoxic effects on ER positive MCF-7 cells as compared to ER negative MDA-MB-231 cells and normal breast cells, MCF-10A. BHMC was shown to promote G2/M cell cycle arrest and apoptosis in MCF-7 cells. Microarray and qPCR analysis demonstrated that BHMC treatment would upregulate several miRNAs like miR-3195 and miR-30a-3p and downregulate miRNAs such as miR-6813-5p and miR-6132 in MCF-7 cells. Besides, BHMC administration was also found to downregulate few tumor-promoting genes like VEGF and SNAIL in MCF-7. In conclusion, BHMC induced apoptosis in the MCF-7 cells by altering the expressions of apoptotic-regulating miRNAs and associated genes.

Anticancer Potential of Calli Versus Seedling Extracts Derived from Rosmarinus officinalis and Coleus hybridus

2020 ◽  
Vol 21 (14) ◽  
pp. 1528-1538
Author(s):  
Sarah Albogami ◽  
Hadeer Darwish ◽  
Hala M. Abdelmigid ◽  
Saqer Alotaibi ◽  
Ahmed Nour El-Deen ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cancer Cells ◽  
Breast Cancer Cells ◽  
Transcriptional Profiling ◽  
Significant Inhibition ◽  
Rosmarinus Officinalis ◽  
Crude Extracts ◽  
Incidence And Mortality ◽  
Mcf 7

Background: In Saudi Arabia, the incidence and mortality rates of breast cancer are high. Although current treatments are effective, breast cancer cells develop resistance to these treatments. Numerous studies have demonstrated that active compounds in plant extracts, such as the phenolic compound Rosmarinic Acid (RA), exert anti-cancer effects. Objective: We investigated the anticancer properties of methanolic crude extracts of seedlings and calli of Rosmarinus officinalis and Coleus hybridus, two Lamiaceae species. Methods: MCF-7 human breast cancer cells were treated with methanolic crude extracts obtained from plant calli and seedlings generated in vitro, and cell proliferation was evaluated. Transcriptional profiling of the seedling and callus tissues was also conducted. Results: The mRNA expression levels of RA genes were higher in C. hybridus seedlings than in R. officinalis seedlings, as well as in C. hybridus calli than in R. officinalis calli, except for TAT and C4H. In addition, seedling and callus extracts of both R. officinalis and C. hybridus showed anti-proliferative effects against MCF-7 cells after 24 or 48 h of treatment. Discussion: At a low concentration of 10 μg/mL, C. hybridus calli and seedling extracts showed the most significant anti-proliferative effects after 24 and 48 h of exposure (p < 0.01); controls (doxorubicin) also showed significant inhibition, but lesser than that observed with C. hybridus (p < 0.05). Results with R. officinalis callus and seedling extracts did not significantly differ from those with untreated cells. Conclusion: Methanolic extracts of R. officinalis and C. hybridus are potentially valuable options for breast cancer treatment.

A Novel Triazole Derivative Drug Presenting In Vitro and In Vivo Anticancer Properties

2018 ◽  
Vol 18 (17) ◽  
pp. 1483-1493
Author(s):  
Ricardo Imbroisi Filho ◽  
Daniel T.G. Gonzaga ◽  
Thainá M. Demaria ◽  
João G.B. Leandro ◽  
Dora C.S. Costa ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cancer Cells ◽  
Cell Line ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
Hepatic Function ◽  
Anticancer Properties ◽  
Mcf 7

Background: Cancer is a major cause of death worldwide, despite many different drugs available to treat the disease. This high mortality rate is largely due to the complexity of the disease, which results from several genetic and epigenetic changes. Therefore, researchers are constantly searching for novel drugs that can target different and multiple aspects of cancer. Experimental: After a screening, we selected one novel molecule, out of ninety-four triazole derivatives, that strongly affects the viability and proliferation of the human breast cancer cell line MCF-7, with minimal effects on non-cancer cells. The drug, named DAN94, induced a dose-dependent decrease in MCF-7 cells viability, with an IC50 of 3.2 ± 0.2 µM. Additionally, DAN94 interfered with mitochondria metabolism promoting reactive oxygen species production, triggering apoptosis and arresting the cancer cells on G1/G0 phase of cell cycle, inhibiting cell proliferation. These effects are not observed when the drug was tested in the non-cancer cell line MCF10A. Using a mouse model with xenograft tumor implants, the drug preventing tumor growth presented no toxicity for the animal and without altering biochemical markers of hepatic function. Results and Conclusion: The novel drug DAN94 is selective for cancer cells, targeting the mitochondrial metabolism, which culminates in the cancer cell death. In the end, DAN94 has been shown to be a promising drug for controlling breast cancer with minimal undesirable effects.

scholarly journals Mutant p53L194F Harboring Luminal-A Breast Cancer Cells Are Refractory to Apoptosis and Cell Cycle Arrest in Response to MortaparibPlus, a Multimodal Small Molecule Inhibitor

Cancers ◽  
2021 ◽  
Vol 13 (12) ◽  
pp. 3043
Author(s):  
Ahmed Elwakeel ◽  
Anissa Nofita Sari ◽  
Jaspreet Kaur Dhanjal ◽  
Hazna Noor Meidinna ◽  
Durai Sundar ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cell Cycle ◽  
Cell Cycle Arrest ◽  
Cancer Cells ◽  
Small Molecule ◽  
Breast Cancer Cells ◽  
Luminal A ◽  
Molecular Analyses ◽  
Cycle Arrest ◽  
Mcf 7

We previously performed a drug screening to identify a potential inhibitor of mortalin–p53 interaction. In four rounds of screenings based on the shift in mortalin immunostaining pattern from perinuclear to pan-cytoplasmic and nuclear enrichment of p53, we had identified MortaparibPlus (4-[(1E)-2-(2-phenylindol-3-yl)-1-azavinyl]-1,2,4-triazole) as a novel synthetic small molecule. In order to validate its activity and mechanism of action, we recruited Luminal-A breast cancer cells, MCF-7 (p53wild type) and T47D (p53L194F) and performed extensive biochemical and immunocytochemical analyses. Molecular analyses revealed that MortaparibPlus is capable of abrogating mortalin–p53 interaction in both MCF-7 and T47D cells. Intriguingly, upregulation of transcriptional activation function of p53 (as marked by upregulation of the p53 effector gene—p21WAF1—responsible for cell cycle arrest and apoptosis) was recorded only in MortaparibPlus-treated MCF-7 cells. On the other hand, MortaparibPlus-treated T47D cells exhibited hyperactivation of PARP1 (accumulation of PAR polymer and decrease in ATP levels) as a possible non-p53 tumor suppression program. However, these cells did not show full signs of either apoptosis or PAR-Thanatos. Molecular analyses attributed such a response to the inability of MortaparibPlus to disrupt the AIF–mortalin complexes; hence, AIF did not translocate to the nucleus to induce chromatinolysis and DNA degradation. These data suggested that the cancer cells possessing enriched levels of such complexes may not respond to MortaparibPlus. Taken together, we report the multimodal anticancer potential of MortaparibPlus that warrants further attention in laboratory and clinical studies.

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