scholarly journals CYTOTOXIC ACTIVITY OF BRAZILEIN ISOLATED FROM SECANG (CAESALPINIA SAPPAN L.) AGAINST MCF7/DOX CELLS BY INHIBITION OF P-GLYCOPROTEIN

2017 ◽  
Vol 9 (12) ◽  
pp. 124 ◽  
Author(s):  
N. P. Linda Laksmiani ◽  
E. D. Y. Meiyanto ◽  
R. Asmah Susidarti
Keyword(s):  
Cell Proliferation ◽  
Ethyl Acetate ◽  
Cytotoxic Activity ◽  
Mtt Assay ◽  
In Silico ◽  
Cancer Resistance ◽  
Caesalpinia Sappan ◽  
P Glycoprotein ◽  
13C Nuclear Magnetic Resonance ◽  
Mcf 7

Objective: This study was focused on isolation of brazilein from the dried heartwood of Secang (Caesalpinia sappan L.) followed by its characterization using Infrared (IR) spectroscopy, liquid chromatography-mass spectrometry (LC-MS) with electrospray ionization (ESI), proton (1H), carbon-13 (13C) nuclear magnetic resonance (NMR) and two dimensional (2D)-NMR, evaluation the cytotoxic activity of brazilein in MCF-7 resistant doxorubicin (MCF-7/DOX) cells and evaluate the interaction between brazilein and ATP with P-glycoprotein (Pgp) in silico using molecular docking.Methods: Brazilein was isolated and purified from ethyl acetate fraction by flash silica gel column chromatography, eluting with chloroform, ethyl acetate and methanol in gradient concentration. In the cytotoxicity assay, MCF-7/DOX cells were cultured in the presence of brazilein for 24 hour (h) and cell viability was evaluated by using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay. Interactions between brazilein and the target proteins were evaluated and calculated in silico by molecular docking using PLANTS.Results: The infrared, mass spectra with a molecular weight of 284 and NMR signal confirmed that was brazilein. MTT assay showed a dose-dependent inhibition of MCF-7/DOX cell proliferation with brazilein IC50 value of 43 µM. The docking score of brazilein was-71,45 kcal/mol and ATP value-96,23 kcal/mol.Conclusion: Brazilein has a potent cytotoxic value on MCF-7/DOX and high affinity in Pgp protein target. Brazilein can be developed as anticancer especially in cancer resistance incidence. Further study must be established to evaluate the molecular mechanism of brazilein inhibit MCF-7/DOX cell proliferation in vitro.

scholarly journals Cytotoxic and Antimetastasis Effect of Ethyl Acetate Fraction from Caesalpinia sappan L. on MCF-7/HER2 Cells

2017 ◽  
Vol 8 (1) ◽  
pp. 42 ◽  
Author(s):  
Riris Istighfari Jenie ◽  
Sri Handayani ◽  
Ratna Asmah Susidarti ◽  
Zalinar Udin ◽  
Edy Meiyanto
Keyword(s):  
Breast Cancer ◽  
Ethyl Acetate ◽  
Cytotoxic Activity ◽  
Cancer Cells ◽  
Cytotoxic Effect ◽  
Ethyl Acetate Fraction ◽  
Migration And Invasion ◽  
Her2 Overexpression ◽  
Caesalpinia Sappan ◽  
Mcf 7

Overexpression of HER2 in breast cancer cell is found on invasive breast cancer and correlated with worse prognosis. Caesalpinia sappan L shows cytotoxic activity on various cancer cells. The goal of this research is to determine the cytotoxic activity and inhibition of migration and invasion of ethyl acetate fraction of Caesalpinia sappan L. (FEA) on HER2 overexpression-breast cancer cells (MCF-7/HER2). The MTT and flow cytometry assay showed that FEA revealed cytotoxic effect in a dose-dependent manner (IC50= 34 ± 3.1 µg/ml) and induced apoptosis, S and G2/M phase accumulation. Wound healing assay, gelatin zymography and immunoblotting assay showed that FEA inhibited migration and suppressed MMP2, MMP9, HER2 and Rac1 protein level. Thus, ethyl acetate fraction of Caesalpinia sappan L. is potential to be developed on future research especially to treat metastatic breast cancer with HER2 overexpression.Keywords: Ethyl acetate fraction of Caesalpinia sappan L, cytotoxic effect, migration and invasion, MCF-7/HER2 cells

scholarly journals In Vitro Cytotoxic Effects of Secondary Metabolites Present in Sarcopoterium Spinosum L.

2021 ◽  
Vol 11 (11) ◽  
pp. 5300
Author(s):  
Jozef Hudec ◽  
Jan Mojzis ◽  
Marta Habanova ◽  
Jorge A. Saraiva ◽  
Pavel Hradil ◽  
...  
Keyword(s):  
Mammary Gland ◽  
Ethyl Acetate ◽  
Cytotoxic Activity ◽  
Cell Lines ◽  
Benzalkonium Chloride ◽  
Ethanol Extract ◽  
Cytotoxic Activities ◽  
Sarcopoterium Spinosum ◽  
Mcf 7

Sarcopoterium spinosum (L.) is a medicinal plant traditionally used for the treatment of various diseases including cancer in the Near- and Middle East. The fractions and constituents of the ethanol extract of S. spinosum were screened for in vitro cytotoxic activities on Jurkat (acute T-lymphoblastic leukemia), HeLa (cervical adenocarcinoma), MCF-7 (mammary gland adenocarcinoma), Caco-2 (human colorectal adenocarcinoma), and MDA-MB-231 (mammary gland adenocarcinoma) cell lines using the MTT (3-(dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay. The ethanol extract was subsequently re-extracted with ethyl acetate and in its sub-fraction obtained by column chromatography three compounds (stachydrine, benzalkonium chloride and rutine) were the first time identified by nuclear magnetic resonance (NMR) analyses. The most active subfraction showed cytotoxic activity against HeLa, MCF-7, and Caco-2 cell lines. The three compounds mentioned, as standards of high-performance liquid chromatography (HPLC) quality, were studied individually and in combination. Cytotoxic activity observed might be due to the presence of benzalkonium chloride and rutin. Benzalkonium chloride showed the strongest growth suppression effect against HeLa cells (IC50 8.10−7 M) and MCF-7 cells (IC50 5.10−6 M). The mixture of stachydrine and benzalkonium chloride allowed a synergistic cytotoxic effect against all tested cancer and normal cells to be obtained. Anti-cancer activity of the plant extract of S. spinosum remains under-investigated, so this research describes how the three major compounds identified in the ethyl acetate extract can exert a significant dose dependent in vitro cytotoxicity.

Biological Effects of p53 Mutation W248 and H175 on MCF-7 Cells

2013 ◽  
Vol 790 ◽  
pp. 550-554
Author(s):  
Xiang Yu Zhou ◽  
Ya Jun Liu ◽  
Dan Li
Keyword(s):  
Flow Cytometry ◽  
Cell Proliferation ◽  
Cell Migration ◽  
Tumor Cell ◽  
Mtt Assay ◽  
Biological Effects ◽  
Scratch Test ◽  
Control Group ◽  
Tumor Cell Migration ◽  
Mcf 7

Objective: p53, a tumor suppressor gene, is one of the hotspots in the world of the biomedical field. Mutation of p53 gene, which is found in approximately 50% of human cancers, is a key event in carcinogenesis. This project aims to investigate the new characteristics of two p53 mutants, p53-W248 and p53-H175, in MCF-7 cells, so as to provide the experimental basis for understanding the functional alternations of mutant p53. Methods: In this study, MCF-7 cells transfected with p53-H175 or p53-W248 plasmids were used as experimental group and the MCF-7 cells transfected wild type p53 plasmid were used as control group. Then the biological effects at the cellular level were investigated using 3-(4.5-dimethylthiazol-2-yl)-2, 5-diphenyl tetrazolium bromide (MTT) assay, flow cytometry analysis and cell scratch test. Results: MTT assay showed that p53-W248 might promote cell proliferation in MCF-7 cells. The results of flow cytometry indicated that no significant effect on cell cycle progression and cell apoptosis by p53-H175 or p53-W248 in cells. The cell scratch test showed that p53-H175 could increase the ability of cell migration. Conclusion: p53-H175 could lead to the promotion of tumor cell migration, while p53-W248 may promote tumor cell proliferation. p53-H175 and p53-W248 might have acquired some new characteristics of oncogenes.

scholarly journals Profil Fraksi Sitotoksik terhadap Sel Murine Leukemia P-388 dari Ekstrak Biji Honje (Etlingera elatior)

2017 ◽  
Vol 3 (1) ◽  
pp. 79-87
Author(s):  
Alfindah Rusanti ◽  
Dede Sukandar ◽  
Tarso Rudiana ◽  
Adawiah Adawiah
Keyword(s):  
Ethyl Acetate ◽  
Cytotoxic Activity ◽  
Mtt Assay ◽  
Chemical Structure ◽  
Ethyl Acetate Extract ◽  
Artemia Salina ◽  
Cytotoxic Compounds ◽  
Murine Leukemia ◽  
Etlingera Elatior

The research characterization of cytotoxic fraction against P-388 leukemia murine cells from the extract honje (Etlingera elatior) seed have been reported. This research lead to isolated and characterization of cytotoxic compounds against P-388 leukemia murine cells from the extract E. elantior seed. The extract of E. elantior seed was maserated by methanol, n-hexane, and ethyl acetate, respectively and estimated their cytotoxic activity against P-388 leukemia murine cell with 3- (4, 5-dimetiltiazol-2-yl) -2,5-difeniltetrazolium bromide (MTT) assay guided toxicity test against of shrimp Artemia salina Leach. Brine shirmp Lethality Test (BSLT) method. The active extracts will be separated by fractionation using column chromatography, radial chromatography, and for analyzing the purity of isolate will estimate by HPLC. The chemical structure of pure isolate will be identified by spectroscopies data UV Vis, FTIR, NMR and MS. The ethyl acetate extract from honje seed have cytotoxic activity by leukemia P-388 cell  with IC50 19.21 µg/mL. The compound toxic as cytotoxicagainst P-388 leukemia murine cells is flavonoid compouds their is resveratrol, lapachol, apigenin, methylated chrysin, 6,2’-dihydroxyflavanone, 3-hydroxy-3,4’-dymethoxyflavone and 4’-hydroxy-5,7-dimethoxyflavanone.DOI: http://dx.doi.org/10.15408/jkv.v0i0.3640

scholarly journals Autophagic Cell Death Is Induced by Acetone and Ethyl Acetate Extracts fromEupatorium odoratum In Vitro: Effects on MCF-7 and Vero Cell Lines

2012 ◽  
Vol 2012 ◽  
pp. 1-9 ◽  
Author(s):  
Faizah Bt. Harun ◽  
Syed Mohsin Syed Sahil Jamalullail ◽  
Khoo Boon Yin ◽  
Zulkhairi Othman ◽  
Anita Tilwari ◽  
...  
Keyword(s):  
Cell Death ◽  
Ethyl Acetate ◽  
Cytotoxic Activity ◽  
Vero Cell ◽  
Cell Lines ◽  
Autophagic Cell Death ◽  
Biologically Active ◽  
Vero Cell Lines ◽  
Mcf 7 ◽  
Ethyl Acetate Extracts

Eupatorium odoratum (EO)contains many biologically active compounds, the anticancer effects of which are not well documented. This study evaluates the cytotoxic effects and mechanism of action ofEOextracts on MCF-7 and Vero cell lines. Evaluation of the cytotoxic activity using MTT assay, morphological alterations, and apoptosis were carried out. Autophagy was evaluated by LC3-A protein expression. Cytotoxic activity, membrane blebbing and ballooning at 24 hours, replacement by mass vacuolation, and double membrane vesicles mimicking autophagy and cell death were observed in the cancer cells. No apoptosis was observed by DNA fragmentation assay. Overexpression of LC3-A protein indicated autophagic cell death. Cell cycle analysis showed G0 and G2/M arrest. The Vero cells did not show significant cell death at concentrations <100 μg/mL. These results thus suggest that acetone and ethyl acetate extracts ofEOinduce cell death through induction of autophagy and hold potential for development as potential anticancer drugs.

In Vitro Tracing of Cytotoxic Compounds in Jarak Cina Stem Bark (Jatropha Multifida Linn.)

2020 ◽  
Vol 20 (1) ◽  
Author(s):  
Sista Werdyani ◽  
Annisa Fitria ◽  
Sari Rakhmawati
Keyword(s):  
Ethyl Acetate ◽  
Cytotoxic Activity ◽  
Cancer Cells ◽  
Cancer Cell ◽  
Ethyl Acetate Extract ◽  
Soxhlet Extraction ◽  
Ethanol Extract ◽  
Jatropha Multifida ◽  
Mcf 7

Cancer remains one of the diseases with increasing number of sufferers, but research on compounds that act as anti-cancer is also ongoing. Terpenoids have been known as a compound that can inhibit the proliferation of cancer cells. One of the medical plants that produce terpenoids is Jarak cina (Jatropha multifida Linn.). Therefore, the possibility of Jarak cina (Jatropha multifida Linn.) to have an cytotoxic activity on cancer cell proliferation is reasonably high. This study was conducted to determine the cytotoxic activity of Jarak cina (Jatropha multifida Linn.) bark extracts against cancer cell MCF-7. Jarak cina bark was extracted using the multilevel soxhlet extraction method with n-hexane, ethyl acetate, and ethanol as the solvents. All the three extracts were then tested against MCF-7 cancer cells using MTT (3-(4,5-dimethylthiazol-2-yl) - 2,5-diphenyltetrazolium bromide) method. Data analysis was performed for IC50 (ppm) parameter. The results showed that the IC50 of n-hexane extract was 313.21 ppm, while the ethyl acetate extract reached 258.38 ppm of IC50, and the IC50 of ethanol extract was 418.51 ppm. The highest potential of cytotoxicity was found in the ethyl acetate extract, so further testing would be required to optimize the proliferation inhibitory activity.

Synthesis and In Vitro Evaluation of Tetrahydroquinoline Derivatives as Antiproliferative Compounds of Breast Cancer via Targeting the GPER

2019 ◽  
Vol 19 (6) ◽  
pp. 760-771 ◽  
Author(s):  
Oscar J. Zacarías-Lara ◽  
David Méndez-Luna ◽  
Gustavo Martínez-Ruíz ◽  
José R. García-Sanchéz ◽  
Manuel J. Fragoso-Vázquez ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cell Proliferation ◽  
Cancer Cells ◽  
Cell Lines ◽  
In Silico ◽  
Breast Cancer Cells ◽  
Breast Cancer Cell Lines ◽  
In Silico Studies ◽  
Mcf 7

Background: Some reports have demonstrated the role of the G Protein-coupled Estrogen Receptor (GPER) in growth and proliferation of breast cancer cells. Objective: In an effort to develop new therapeutic strategies against breast cancer, we employed an in silico study to explore the binding modes of tetrahydroquinoline 2 and 4 to be compared with the reported ligands G1 and G1PABA. Methods: This study aimed to design and filter ligands by in silico studies determining their Lipinski's rule, toxicity and binding properties with GPER to achieve experimental assays as anti-proliferative compounds of breast cancer cell lines. Results: In silico studies suggest as promissory two tetrahydroquinoline 2 and 4 which contain a carboxyl group instead of the acetyl group (as is needed for G1 synthesis), which add low (2) and high hindrance (4) chemical moieties to explore the polar, hydrophobic and hindrance effects. Docking and molecular dynamics simulations of the target compounds were performed with GPER to explore their binding mode and free energy values. In addition, the target small molecules were synthesized and assayed in vitro using breast cancer cells (MCF-7 and MDA-MB-231). Experimental assays showed that compound 2 decreased cell proliferation, showing IC50 values of 50µM and 25µM after 72h of treatment of MCF-7 and MDA-MB-231 cell lines, respectively. Importantly, compound 2 showed a similar inhibitory effect on proliferation as G1 compound in MDA-MB-231 cells, suggesting that both ligands reach the GPER-binding site in a similar way, as was demonstrated through in silico studies. Conclusion: A concentration-dependent inhibition of cell proliferation occurred with compound 2 in the two cell lines regardless of GPER.

Isolation of Lupeol and Gallic acid with cytotoxic activity of two different extracts from the leaves of Iraqi Conocarpus erectus L.

2021 ◽  
pp. 3495-3503
Author(s):  
Tahany Amir Tawfeeq ◽  
Ghaith Ali Jasim ◽  
Abdulmutalib A. Nasser ◽  
Basma Talib Al-Sudani
Keyword(s):  
Ethyl Acetate ◽  
Cytotoxic Activity ◽  
Gallic Acid ◽  
Cell Line ◽  
Ethyl Acetate Fraction ◽  
Hexane Fraction ◽  
High Concentration ◽  
Conocarpus Erectus ◽  
Mcf 7 ◽  
Ethyl Acetate Extracts

Conocarpus erectus L. is a perennial, evergreen shrub belonging to Combretaceae family. Conocarpus plant reported to contain phenolic acid, flavonoids, lignan, terpenes and tannins. Aim of study was to isolate lupeol from hexane fraction and gallic acid from ethyl acetate fraction and investigate the effects of (hexane and ethyl acetate) fractions on viability of pancreatic AsPC-1 and breast MCF-7 cell lines by MTT assay. The presence of lupeol in the hexane and gallic acid in the ethyl acetate extracts was detected by TLC. The identification of isolated lupeol and gallic acid by HPTLC and HPLC comparing with standard lupeol and gallic acid. Structural elucidation of isolated compounds done by FTIR and UV spectrophotometer. The cytotoxic activity showed more at high concentration (30µg/ml) in both ethyl acetate and hexane fractions against MCF-7 cell line, the percentage of cellular inhibition for ethyl acetate at 30mg/ml was (73% and 79%) more than the hexane fraction in which the inhibition was (60% and 76%) at 48hr and 72 hr respectively. Furthermore, the cytotoxic activity more at high concentration (30µg/ml) in both fractions against AsPC-1 cell line with cellular inhibition (58% and 70%) for ethyl acetate fraction and (50% and 66%) for hexane fraction in compared with Cisplatin.

scholarly journals Diltiazem potentiation of doxorubicin cytotoxicity and cellular uptake in human breast cancer cells

2019 ◽  
Vol 8 (4) ◽  
pp. BMT31
Author(s):  
Hamdan S Al-malky ◽  
Zoheir A Damanhouri ◽  
Jumana Y Al Aama ◽  
Ali A Al Qahtani ◽  
Wafaa S Ramadan ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Multidrug Resistance ◽  
Cytotoxic Activity ◽  
Cellular Uptake ◽  
Breast Cancer Cells ◽  
Limiting Factors ◽  
Human Breast ◽  
Common Cancer ◽  
P Glycoprotein ◽  
Mcf 7

Aim: Breast cancer is the most common cancer among Arab women and also around the world. Chronic cardiotoxicity and multidrug resistance are potential limiting factors of doxorubicin (DOX), a known anthracycline antibiotic. Materials & methods: DOX cytotoxicity was evaluated by the sulforhodamine method. DOX cellular uptake, detection of P-glycoprotein activity and the photomicrograph of MCF-7 cells were also determined. Results: Diltiazem (DIL) treatment improved DOX cytotoxic activity and increased the cellular uptake of DOX significantly and aggregation of rhodamine 123, reflecting inhibition of P-glycoprotein pump. Cytopathological investigation of MCF-7 cells revealed marked cytotoxic activity of DOX in the presence of DIL. Conclusion: DIL treatment enhanced DOX cytotoxic effect and reduced multidrug resistance, which increased the drug accumulation intracellularly.

scholarly journals Six New Coumarin Glycosides from the Aerial Parts of Gendarussa vulgaris

Molecules ◽  
2019 ◽  
Vol 24 (8) ◽  
pp. 1456 ◽  
Author(s):  
Yanjun Sun ◽  
Meiling Gao ◽  
Haojie Chen ◽  
Ruijie Han ◽  
Hui Chen ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Hepg2 Cell ◽  
Mtt Assay ◽  
Spectroscopic Data ◽  
Hplc Analysis ◽  
Cytotoxic Activities ◽  
Aerial Parts ◽  
Structure Activity ◽  
Hepg2 Cell Lines ◽  
Mcf 7

Six new coumarin glycosides, genglycoside A–F (1–6), were isolated from the aerial parts of Gendarussa vulgaris, along with ten known analogues (7–16). Their structures were unambiguously established on the basis of extensive spectroscopic data and HPLC analysis. The cytotoxic activities of all isolated compounds were evaluated by MTT assay. Compound 12 showed the most potent cytotoxicity in Eca-109, MCF-7, and HepG2 cell lines. By the preliminary structure–activity relationships, it was firstly discovered that the glycosylation or esterification at 7,8-dihydroxy or 7-hydroxy drastically reduced the cytotoxic activity of the parent coumarin.

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