CYTOTOXIC ACTIVITY AND SELECTIVITY INDEX OF BINAHONG (Anredera cordifolia) EXTRACTS ON MCF-7 BREAST CANCER CELLS AND VERO NORMAL CELLS LINE

Background: Breast cancers occur because of an impaired balance between proliferation, differentiation, and apoptosis of breast glands. Natural products have potency as cytotoxic agents with less side effects than chemotherapy. One of the potential plants is Anredera cordifolia (Ten.) Stennis (binahong), which contains flavonoid 8-glucopyranosyl- 4’,5,7-trihydroxy flavone compounds.Objective: This study aims to determine the potency of binahong leaves extract as an anticancer for breast cancer in vitro and in silico.Methods: Preliminary tests using molecular docking of 8-glucopyranosyl-4’,5,7-trihydroxyflavone compounds on Bcl-2 and HER-2 proteins. The extraction and fractionation were to obtain binahong extract. Thin layer chromatography to identify flavonoid compounds in the extract. DPPH assay was performed to evaluate the antioxidant activity. MTT assay was performed to evaluate cytotoxic activity on MCF-7 breast cancer cells and Vero cells.Results: In silico test showed a stable bond between 8-glucopyranosyl- 4’,5,7-trihydroxylflavone, and Bcl-2 and HER-2 with a docking score of -7.5 kcal/mol and -8.0 kcal/mol, respectively. The binahong extract contain flavonoid compounds that had the retention factor value 0.78; 0.49; 0.35. Antioxidant test resulted IC50 value of 4940 μg/mL. Cytotoxic test resulted in IC50 value of 1073 μg/mL and 486 μg/mL for Vero cells and MCF-7 breast cancer cells, respectively. The comparison between IC50 produced a selectivity index value of 2.149, which shows that binahong extract was selective against MCF-7 breast cancers.Conclusion: This study concluded that binahong extract has weak potency as anticancer agent on MCF-7 cells.

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The Synthesis of Cinchonine Tiglat Ester Compound and Cytotoxic Test Against MCF-7 Breast Cancer Cell

Jurnal Kimia Terapan Indonesia ◽

10.14203/jkti.v19i2.354 ◽

2018 ◽

Vol 19 (2) ◽

pp. 54-61

Author(s):

Ahmad Khanifudin ◽

Gian Primahana ◽

Sylvia Rizky Prima ◽

Puspa Dewi Lotulung ◽

Muhammad Hanafi

Keyword(s):

Breast Cancer ◽

Cancer Cells ◽

Breast Cancer Cells ◽

Cinchona Alkaloid ◽

Alamar Blue ◽

Tiglic Acid ◽

Spectroscopy Instrumentation ◽

Ic50 Value ◽

Pass Through ◽

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Cinchonine is a type of cinchona alkaloid compound commonly found and/or isolated from Cinchona sp. plant. It is commonly used to treat malaria, and can potentially be used against cancer cells. In this particular study, cinchonine ester derivatives were extracted through esterification processs. Synthesized esther is aimed to gain higher lipophilicity of cinchonine so that makes it easier to pass through cell membrane. Esterification was done using DCC activator as well as DMAP catalyst with tiglic acid used to create cinchonine tiglat. Subsequent cinchonine tiglat was obtained in the form of oil with 25,28% yield. The compound obtained from the synthesis was the analyzed using LC-ESI-MS and 1H-NMR spectroscopy instrumentation. Results show that the target compound has been successfully synthesized. Its cytotoxic ability against MCF-7 breast cancer cells was tested using the Alamar Blue method. Results concluded that cinchonine tiglat ester compound has a viable cytotoxic activity with IC50 value of 1.22 ppm.

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Expression of HER-2 in MCF-7 breast cancer cells modulates anti-apoptotic proteins Survivin and Bcl-2 via the extracellular signal-related kinase (ERK) and phosphoinositide-3 kinase (PI3K) signalling pathways

BMC Cancer ◽

10.1186/1471-2407-8-129 ◽

2008 ◽

Vol 8 (1) ◽

Cited By ~ 67

Author(s):

Aisha Siddiqa ◽

Linda M Long ◽

Liuxia Li ◽

Robert A Marciniak ◽

Irene Kazhdan

Keyword(s):

Breast Cancer ◽

Cancer Cells ◽

Breast Cancer Cells ◽

Signalling Pathways ◽

Extracellular Signal ◽

Pi3k Signalling ◽

Her 2 ◽

Apoptotic Proteins ◽

Phosphoinositide 3 Kinase ◽

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Structural and In Vitro Biological Studies of Organotin(IV) Precursors; Selective Inhibitory Activity Against Human Breast Cancer Cells, Positive to Estrogen Receptors

Australian Journal of Chemistry ◽

10.1071/ch12448 ◽

2012 ◽

Vol 65 (12) ◽

pp. 1625 ◽

Cited By ~ 25

Author(s):

Vasilis I. Balas ◽

Christina N. Banti ◽

Nikolaos Kourkoumelis ◽

Sotiris K. Hadjikakou ◽

George D. Geromichalos ◽

...

Keyword(s):

Breast Cancer ◽

Cytotoxic Activity ◽

Cancer Cells ◽

Cell Line ◽

Breast Cancer Cells ◽

X Ray ◽

Er Positive ◽

Normal Human ◽

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Crystals of Ph3SnCl (1) were grown from a methanol/acetonitrile solution. Compounds [Ph3SnOH]n (2) and [(Ph2Sn)4Cl2O2(OH)2] (3) were crystallized from diethyl ether/methanol/acetonitrile and hot acetone/water solutions respectively, of the white precipitation, formed by adding KOH to solutions of 1 and [Ph2SnCl2] in 1 : 1 and 1 : 2 molar ratios respectively. Complex 1 was characterized by X-ray crystallography. X-ray structure determination of compounds 2 and 3 confirmed the previously reported identities. The molecular structure of 1, reported here, is a new polymorphic form of the known one for Ph3SnCl. Four independent [Ph3SnCl] molecules constitute the crystal structure of 1. The moieties are packed in two pairs in a tail-to-tail arrangement. Complexes 1–3 were evaluated for their in vitro cytotoxic activity (cell viability) against human cancer cell lines: HeLa (human cervical), MCF-7 (breast, estrogen receptor (ER) positive), MDA-MB-231 (breast, ER negative), A549 (lung), Caki-1 (kidney carcinoma), 786-O (renal adenocarcinoma), K1 (thyroid carcinoma), and the normal human lung cell line MRC-5 (normal human fetal lung fibroblast cells) versus, the normal immortalized human mammary gland epithelial cell line MTSV17 with a sulforhodamine B (SRB) assay. The results show potent cytotoxic activity of the complexes against all cell lines used, which was superior to that of cisplatin (CDDP). Compounds 1–3 showed higher activity against breast cancer cells MCF-7 (ER positive) than against of MDA-MB-231 (ER negative). These findings prompted us to search for possible interaction of these complexes with other cellular elements of fundamental importance in cell proliferation. The influence of these complexes 1–3 upon the catalytic peroxidation of linoleic acid to hydroperoxylinoleic acid by the enzyme lipoxygenase (LOX), as well as their binding affinity towards calf thymus-DNA, were kinetically and theoretically studied.

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Synergistic inhibition of breast cancer cell lines with the combination of a dual inhibitor of EGFR/HER-2/neu and a Bcl-2 inhibitor

Journal of Clinical Oncology ◽

10.1200/jco.2006.24.18_suppl.13100 ◽

2006 ◽

Vol 24 (18_suppl) ◽

pp. 13100-13100

Author(s):

L. Witters ◽

A. Witkoski ◽

M. Planas-Silva ◽

J. Viallet ◽

M. S. Berger ◽

...

Keyword(s):

Breast Cancer ◽

Cancer Cells ◽

Cell Lines ◽

Human Breast Cancer ◽

Breast Cancer Cells ◽

Human Breast Cancer Cells ◽

Human Breast ◽

Dual Inhibitor ◽

Her 2 ◽

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13100 Background: The epidermal growth factor receptor (EGFR; ErbB1) and HER-2/neu (ErbB2), members of the ErbB family of receptor tyrosine kinases, are overexpressed in a variety of human tumors and overexpression generally correlates with poor prognosis and decreased survival. Use of inhibitors of these receptors as monotherapies, e.g., trastuzumab, Iressa, and erlotinib, has led to advances in treatment, but many patients do not respond or develop resistance. The anti-apoptotic protein, Bcl-2, is also overexpressed in a number of human tumors. Inhibitors of Bcl-2 induce apoptosis and sensitize cancer cells to other therapies. This study assesses the effects of a combination of a reversible inhibitor of both EGFR and HER-2/neu that is similar to lapatinib (GW2974) and a pan inhibitor of the Bcl-2 family (GX15–070: Gemin X Biotechnologies, Inc.) on the growth of human breast cancer cells. Methods: The MCF-7 human breast cancer cell line transfected with a control vector, MCF/neo, and the HER-2/neu transfected MCF-7 cell line, MCF/18, were treated with various concentrations of GW2974 (0.25–10 μM) and/or the GX15–070 pan Bcl-2 inhibitor (50–500 nM). After a 3 day exposure, cell number was determined using the colorimetric MTT tetrazolium dye assay. Percent of control was normalized to corresponding concentrations of the solvent for both agents (DMSO). Results: Treatment with the GW2974 dual inhibitor or the GX15–070 pan Bcl-2 inhibitor resulted in dose-dependent growth inhibition in both the control and HER-2/neu transfected MCF-7 cell lines. The combination of both agents produced synergistic growth inhibition in both cell lines as confirmed by isobologram analysis. Conclusions: This study has demonstrated synergy with the combination of a dual inhibitor of EGFR and HER-2/neu and an inhibitor of Bcl-2 in control and HER-2/neu overexpressing MCF-7 human breast cancer cells. This finding warrants an evaluation of this combination in clinical trials for the treatment of patients with metastatic breast cancer. [Table: see text]

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Caryophyllene-Type Sesquiterpenoids from the Stembark of Aglalia harmsiana and Their Cytotoxic Activity Against MCF-7 Breast Cancer Cells

Molekul ◽

10.20884/1.jm.2019.14.2.543 ◽

2019 ◽

Vol 14 (2) ◽

pp. 126 ◽

Cited By ~ 1

Author(s):

Hersa Milawati ◽

Desi Harneti ◽

Rani Maharani ◽

Nurlelasari Nurlelasari ◽

Ace Tatang Hidayat ◽

...

Keyword(s):

Breast Cancer ◽

Cytotoxic Activity ◽

Cancer Cells ◽

Breast Cancer Cells ◽

Spectroscopic Methods ◽

Caryophyllene Oxide ◽

Tropical Plants ◽

Chemical Structures ◽

Hexane Extracts ◽

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Sesquiterpenoid is a class of terpenoid compounds that have the most abundant diversity of structures and biological activitiesthat can be found in natural resources. Tropical plants are main source of sesquiterpenoid compounds such as Aglaiagenus belong to Meliaceae family. A. harmsianais a species from Aglaiathat only has few previous researchs. Therefore, the purpose of this study was to isolate and determine the structure of sesquiterpenoid compounds from stem barkA. harmsianaalong withtheir cytotoxic activity against MCF-7 breast cancer cells. The isolation process begins by extracting powder from A. harmsianastembark using n-hexane, ethyl acetate and methanol. All extracts were evaluated for their cytotoxic activity against MCF-7 breast cancer cells, and n-hexane extractsshowed significant cytotoxic activitywith IC50values of 117.86 µg/mL. Therefore, n-hexane extracts were further separated and purified by various chromatographic techniquesto obtain compounds 1and 2. Compounds 1and 2were elucidated their chemical structures by spectroscopic methods includingIR, NMR, and MS as well as bycomparison of data with literatures and identified ascaryophyllene-typesesquiterpenoids, β-caryophylleneoxide (1) and senecrassidiol (2). Compounds 1and 2were submitted for cytotoxic eveluation on MCF-7 breast cancer cells and as a result, β-caryophyllene oxide (1) showed the stronger activity compared to senecrassidiol (2). These finding indicatedthat the cytotoxic activity of caryophyllene-typesesquiterpenoid areinfluenced by the presence of double bonds and configuration of methyl groups.

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CYTOTOXIC EFFECT OF AQUADEST, ETHANOLIC, AND CHLOROFORM EXTRACTS OF Spathoglottis plicata Blume ON BREAST CANCER CELLS LINE (T47D CELLS)

KnE Life Sciences ◽

10.18502/kls.v2i1.118 ◽

2015 ◽

Vol 2 (1) ◽

pp. 64

Author(s):

Mukhlish Jamal Musa Holle ◽

Hestri Dyah Puspitasari ◽

Andaru Satryo ◽

Wahyu Dewi Astuti Ningrum ◽

Digdo Sudigyo ◽

...

Keyword(s):

Breast Cancer ◽

Cytotoxic Activity ◽

Cancer Cells ◽

Mtt Assay ◽

Breast Cancer Cells ◽

Chloroform Extract ◽

Probit Analysis ◽

Antioxidant Compounds ◽

T47d Cells ◽

Ic50 Value

Breast cancer is one of cancer with high mortality. This cancer not only attacks women, but also men. Indonesia has many plants which potential as anticancer, such as orchids. Spathoglottis plicata is one of the orchid species that abundant in Indonesia and has a lot of antioxidant compounds which is guessed have anticancer properties. The objectives of this study were to study the cytotoxic activity and IC50 value of aquadest, ethanolic, and chloroform extracts of S. plicata’s pseudobulbs, leaves, and whole plants on T47D cells (breast cancer cells line) as well as cytotoxic activity of the specific fraction of the most toxic crude extract. S. plicata used in this study was obtained from Bungarinte nursery. Extractions were done by maceration method using aquadest, ethanol, and chloroform as the solvent. Cytotoxic test on T47D cells were done by MTT assay. The cytotoxic data were analyzed using one-way ANOVA followed by Tukey’s HSD test. The IC50 of each extracts were calculate by probit analysis. The lowest IC50 value among all extracts was fractionated and isolated by preparative TLC. The cytotoxic activity and IC50 of this fractions were analyzed. The results showed that only 2 from 9 crude extracts that able to calculate its IC50 because those two extracts have concentration dependent pattern of inhibition concentration. Chloroform extract have the lowest IC50 value (369,837 μg/mL). Then, this extract fractionated by eluen n-hexane : ethyl acetate 4:1. Four fractions were collected. The lowest IC50 value is fraction IV (144,41 μg/mL). Based on the results it could be concluded that S. plicata leaves have moderate potency to develop as anticancet agents, especially on breast cancer. Keywords: S. plicata, T47D cells, cytotoxic, MTT assay, preparative TLC.

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The Enhanced Cytotoxic and Pro-Apoptotic Effects of Optimized Simvastatin-Loaded Emulsomes on MCF-7 Breast Cancer Cells

Pharmaceutics ◽

10.3390/pharmaceutics12070597 ◽

2020 ◽

Vol 12 (7) ◽

pp. 597 ◽

Cited By ~ 1

Author(s):

Zuhier A. Awan ◽

Usama A. Fahmy ◽

Shaimaa M. Badr-Eldin ◽

Tarek S. Ibrahim ◽

Hani Z. Asfour ◽

...

Keyword(s):

Breast Cancer ◽

Cytotoxic Activity ◽

Cancer Cells ◽

Breast Cancer Cells ◽

Spherical Shape ◽

Cytotoxic Activities ◽

Vesicle Size ◽

Apoptotic Activity ◽

The Impact ◽

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Statins, including simvastatin (SMV), are commonly used for the control of hyperlipidaemia and have also proven therapeutic and preventative effects in cardiovascular diseases. Besides that, there is an emerging interest in their use as antineoplastic drugs as demonstrated by different studies showing their cytotoxic activity against different cancer cells. In this study, SMV-loaded emulsomes (SMV-EMLs) were formulated and evaluated for their cytotoxic activity in MCF-7 breast cancer cells. The emulsomes were prepared using a modified thin-film hydration technique. A Box–Behnken model was used to investigate the impact of formulation conditions on vesicle size and drug entrapment. The optimized formulation showed a spherical shape with a vesicle size of 112.42 ± 2.1 nm and an entrapment efficiency of 94.34 ± 1.11%. Assessment of cytotoxic activities indicated that the optimized SMV-EMLs formula exhibited significantly lower half maximal inhibitory concentration (IC50) against MCF-7 cells. Cell cycle analysis indicated the accumulation of cells in the G2-M phase as well as increased cell fraction in the pre-G1 phase, suggesting an enhancement of anti-apoptotic activity of SMV. The staining of cells with Annex V revealed an increase in early and late apoptosis, in line with the increased cellular content of caspase-3 and Bax. In addition, the mitochondrial membrane potential (MMP) was significantly decreased. In conclusion, SMV-EMLs demonstrated superior cell death-inducing activity against MCF-7 cells compared to pure SMV. This is mediated, at least in part, by enhanced pro-apoptotic activity and MMP modulation of SMV.

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