Mechanistic studies of cytotoxic activity of the mesoionic compound MIH 2.4Bl in MCF‑7 breast cancer cells

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

Acta Biochimica Indonesiana ◽

10.32889/actabioina.v3i2.57 ◽

2021 ◽

Vol 3 (2) ◽

pp. 72-80

Author(s):

Dita Sozianty ◽

Rifki Febriansah

Keyword(s):

Breast Cancer ◽

Cytotoxic Activity ◽

Cancer Cells ◽

Breast Cancer Cells ◽

Selectivity Index ◽

Cytotoxic Agents ◽

Flavonoid Compounds ◽

Ic50 Value ◽

Her 2 ◽

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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 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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Probing the interaction of thionine with human serum albumin by multispectroscopic studies and its in vitro cytotoxic activity toward MCF-7 breast cancer cells

Journal of Biomolecular Structure and Dynamics ◽

10.1080/07391102.2016.1235513 ◽

2016 ◽

Vol 35 (14) ◽

pp. 3012-3031 ◽

Cited By ~ 5

Author(s):

Perumal Manivel ◽

Manickam Paulpandi ◽

Kadarkarai Murugan ◽

Giovanni Benelli ◽

Malaichamy Ilanchelian

Keyword(s):

Breast Cancer ◽

Human Serum Albumin ◽

Serum Albumin ◽

Human Serum ◽

Cytotoxic Activity ◽

Cancer Cells ◽

Breast Cancer Cells ◽

Mcf 7

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Evaluation of the Cytotoxic Activity of Anthriscus nemorosa on Breast Cancer Cells

Journal of Contemporary Medical Sciences ◽

10.22317/jcms.v7i2.940 ◽

2021 ◽

Vol 7 (2) ◽

Author(s):

Mahtab Zarchini ◽

Haleh Forouhandeh ◽

Elham Safarzadeh ◽

Omoleila Molavi ◽

Vahideh Tarhriz ◽

...

Keyword(s):

Breast Cancer ◽

Flow Cytometry ◽

Cell Death ◽

Cytotoxic Activity ◽

Cancer Cells ◽

Cell Lines ◽

Breast Cancer Cells ◽

Hexane Extract ◽

Volatile Components ◽

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Objective: The genus Anthriscus from the Umbelliferae family has valuable compounds and pharmacological properties. Terpenoids, phenolics, anthocyanins, podophyllotoxins, and others have been identified in Anthriscus genus which has effects like analgesic, antiviral, anti-inflammatory, hepatoprotective, and anti-platelet aggregation. The present study concerns the cytotoxic activity of A. nemorosa different extracts on breast cancer cells (MCF-7) and normal cell lines (HFFF). Methods: Different extracts of aerial parts of A. nemorosa were prepared using Soxhlet apparatus. The cytotoxicity of samples was assessed by MTT assay on breast cancer cells (MCF-7) and noncancerous cells (HFFF) with different concentrations of extracts in 24 and 48 hours. The most potent extract was fractioned and cytotoxic activity of fractions was considered, As well. A flow cytometry (annexin V/PI) assay has been used for detecting the mechanism of cell death in sample treated cell lines. Moreover, for clarifying volatile components of n-Hexane extract and its 80% and 100% VLC fractions were subjected to GC-MS apparatus. Results: Results indicated that n-Hexane extract and its 80% and 100% VLC fractions exhibited a significant (p<0.001) inhibitory effect on the growth of the MCF-7 cell line compared to the control group. Meanwhile, flow cytometry analysis revealed that potent extract caused cell death through necrosis and 80% and 100% fractions showed different mechanisms (such as autophagy). The major compounds, which maybe were in charge of showing cytotoxic activity were non-terpenoids. Conclusion: This study provides the evidence that in vitro cytotoxic activity of n-Hexane extract and 80% and 100% VLC fractions of A. nemorosa inhibited the proliferation of breast cancer cells (MCF7) via a different mechanism.

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Thermoresponsive dendrimers based on oligoethylene glycols: Design, synthesis and cytotoxic activity against MCF-7 breast cancer cells

European Journal of Medicinal Chemistry ◽

10.1016/j.ejmech.2013.09.019 ◽

2013 ◽

Vol 69 ◽

pp. 848-854 ◽

Cited By ~ 9

Author(s):

Mona A. Abdel-Rahman ◽

Ahmed M. Al-Abd

Keyword(s):

Breast Cancer ◽

Cytotoxic Activity ◽

Cancer Cells ◽

Breast Cancer Cells ◽

Design Synthesis ◽

Oligoethylene Glycols ◽

Mcf 7

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Antioxidant and cytotoxic activity of isoindole compounds in breast cancer cells (MCF-7)

Journal of Molecular Structure ◽

10.1016/j.molstruc.2020.128366 ◽

2020 ◽

Vol 1217 ◽

pp. 128366

Author(s):

Seda Mesci ◽

Melek Gül ◽

Serpil Eryılmaz ◽

Tadeusz Lis ◽

Sławomir Szafert ◽

...

Keyword(s):

Breast Cancer ◽

Cytotoxic Activity ◽

Cancer Cells ◽

Breast Cancer Cells ◽

Mcf 7

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Flavone constituents of Phlomis bruguieri Desf. with cytotoxic activity against MCF-7 breast cancer cells

Research in Pharmaceutical Sciences ◽

10.4103/1735-5362.236835 ◽

2018 ◽

Vol 13 (5) ◽

pp. 422 ◽

Cited By ~ 6

Author(s):

Mustafa Ghannadian ◽

SeyedEbrahim Sajjadi ◽

Zeinab Delazari ◽

Mahmoud Aghaei

Keyword(s):

Breast Cancer ◽

Cytotoxic Activity ◽

Cancer Cells ◽

Breast Cancer Cells ◽

Mcf 7

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PERBANDINGAN AKTIVITAS SITOTOKSIK EKSTRAK DAN MINYAK ATSIRI RIMPANG Curcuma mangga Val. TERHADAP SEL MCF-7

Jurnal Penelitian Saintek ◽

10.21831/jps.v26i1.39977 ◽

2021 ◽

Vol 26 (1) ◽

pp. 85-94

Author(s):

Purwanto Purwanto ◽

Putri Khaerani Cahyaningrum ◽

Retno Sunarminingsih Sudibyo

Keyword(s):

Breast Cancer ◽

Essential Oil ◽

Essential Oils ◽

Cytotoxic Activity ◽

Cancer Cells ◽

Mtt Assay ◽

Breast Cancer Cells ◽

Steam Distillation ◽

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Rimpang Curcuma mangga Val. banyak digunakan sebagai obat herbal antikanker payudara. Penelitian aktivitas sitotoksik terhadap sel kanker payudara banyak dilakukan utamanya untuk minyak atsiri rimpang, dan hanya sedikit penelitian terhadap ekstraknya. Walaupun demikian belum ada yang membandingkan aktivitas sitotoksik dari ekstrak dan minyak atsiri tersebut terhadap sel kanker payudara; meskipun kandungan senyawa keduanya berbeda. Oleh karena itu penelitian ini bertujuan membandingkan aktivitas sitotoksik dari ekstrak dan minyak atsiri rimpang C. mangga Val. secara in vitro terhadap sel kanker payudara MCF7. Ekstrak rimpang dibuat secara maserasi menggunakan pelarut n-heksana; sedangkan minyak atsiri dibuat melalui destilasi uap irisan rimpang selama 5 jam. Uji aktivitas sitotoksik in vitro dilakukan menggunakan metoda MTT Assay. Rendemen minyak dari ekstrak n-heksana rimpang C. mangga Val. adalah 1,15 x 10-2 % sedangkan rendemen minyak atsiri adalah 6,3 x 10-2 %. Hasil uji sitotoksik menghasilkan IC50 ekstrak 106,414 µg/ml (R2=0,9677) dan minyak atsiri 198,557 µg/ml (R2=0,8037). Hal ini menunjukkan bahwa ekstrak rimpang C. mangga Val. lebih sitotoksik terhadap sel kanker payudara MCF-7 daripada minyak atsirinya, karena kandungan ekstrak mayoritas diterpenoid (53,18%) sedangkan minyak atsiri mayoritas monoterpenoid (51,34%).THE COMPARISON BETWEEN THE ACTIVITIES OF CYTOTOXIC EXTRACTS AND ESSENTIAL OILS OF RHIZOME Curcuma mango Val. TOWARD MCF-7 CELLSCurcuma mangga Val. rhizome has been used as herbal anti breast cancer. Researches on cytotoxic activity towards breast cancer cells have been done especially to the rhizome’s essential oil; and only few researches done to the extract. However there is no cytotoxic activity comparation of the extract and essential oil towards breast cancer cells; even tough their substance contents are different. Therefore, this study aimed to compare the cytotoxic activity in vitro of the extract and essential oil of C. mangga Val. rhizomes towards breast cancer cells of MCF-7. The rhizome extract was prepared by maceration using N-hexane; while the essential oil was prepared by steam distillation for 5 hours of the sliced rhizomes. The in vitro cytotoxic test was carried out using MTT Assay. The yield of oil from rhizome extract was 1.15 x 10-2 %; while the yield of essential oil was 6.3 x 10-2 %. The IC50 of extract oil was 106.414 µg/ml (R2=0.9677) and the IC50 of essential oil was 198.557 µg/ml (R2=0.8037). It shows that rhizome extract of C. mangga Val. was more cytotoxic towards MCF-7 than the oil because the majority content of extract were diterpenoids (53.18%) while the oil were monoterpenoids (51.34%).

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