Chenopodium album metabolites act as dual topoisomerase inhibitors and induce apoptosis in the MCF7 cell line

MedChemComm ◽  
2016 ◽  
Vol 7 (5) ◽  
pp. 837-844 ◽  
Author(s):  
Debanjana Chakraborty ◽  
Chetan Kumar Jain ◽  
Arindam Maity ◽  
Shekhar Ghosh ◽  
Susanta Roy Choudhury ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cell Line ◽  
Cell Lines ◽  
Oleanolic Acid ◽  
Cancer Cell ◽  
Mcf7 Cell ◽  
Chenopodium Album ◽  
Topoisomerase Inhibitors ◽  
Mcf7 Cell Line ◽  
Line P

Desgalactotigonin and oleanolic acid 3-O-β-d-glucuronide were isolated from Chenopodium album and were evaluated for cytotoxic activity against various cancer cell lines.

scholarly journals Cytotoxic effect of Spirulina platensis extract and Ulva compressa Linn. on cancer cell lines

Food Research ◽  
2020 ◽  
Vol 4 (4) ◽  
pp. 1018-1023
Author(s):  
M. Maryati ◽  
A. Saifudin ◽  
S. Wahyuni ◽  
J. Rahmawati ◽  
A. Arrum ◽  
...  
Keyword(s):  
Cell Growth ◽  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Spirulina Platensis ◽  
Cytotoxic Effect ◽  
Mcf7 Cell ◽  
Ethanol Extract ◽  
Cancer Cell Lines ◽  
Ulva Compressa

Studies have shown that algae and seaweed have cytotoxic activity. This study was aimed to determine the cytotoxic activity of Spirulina platensis and Ulva compressa Linn. extracts against cancer cell lines. The cytotoxic activity of the extract was carried out using the MTT ((3-(4,5-dimetylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) method. Results showed that the ethanol extract and methanol extract of Spirulina platensis have no cytotoxic effect against HeLa, WiDr, MCF7 and T47D cells. Water extract of Spirulina platensis had no cytotoxic activity on T47D and Vero cells. Water extracts of Spirulina platensis increase MCF7 cell growth. Phycocyanin powder also stimulates MCF7 cell growth. Ethanol extract of Ulva compressa Linn. exhibited potentially cytotoxic activity against MCF7 and moderate cytotoxic against WiDR cells with IC50 values are 31.86 μg/ mL and 104.93 μg/mL, respectively. It can be concluded that extract of Spirulina platensis has no potential to be developed for cancer therapy. Ulva compressa Linn has the potential to be developed as an anti-cancer. Further research for study the mechanism of anticancer of Ulva compressa Linn on MCF7 was needed.

Synthesis of artemisinic acid derived glycoconjugates and their anticancer studies

2020 ◽  
Vol 18 (12) ◽  
pp. 2252-2263
Author(s):  
Tharun K. Kotammagari ◽  
Sayantan Paul ◽  
Ganesh K. Barik ◽  
Manas K. Santra ◽  
Asish K. Bhattacharya
Keyword(s):  
Cell Line ◽  
Mcf7 Cell ◽  
Click Reaction ◽  
Anticancer Activities ◽  
Artemisinic Acid ◽  
Mcf7 Cell Line ◽  
Line P

Twenty-four artemisinic acid glycoconjugate hybrids were synthesized using click reaction and evaluated for their anticancer activities against the MCF7 cell line.

Induction of breast cancer progression and metastasis by HOXB9 gene’s activation by sequence specific binding factors.

2013 ◽  
Vol 31 (26_suppl) ◽  
pp. 26-26
Author(s):  
Aisulu Zhussupova ◽  
Tetsu Hayashida ◽  
Maiko Takahashi ◽  
Hiromitsu Jinno ◽  
Yuko Kitagawa
Keyword(s):  
Breast Cancer ◽  
Cell Line ◽  
Cell Lines ◽  
Cancer Progression ◽  
Promoter Region ◽  
Mcf7 Cell ◽  
Luciferase Activity ◽  
Luciferase Assay ◽  
Chip Assay ◽  
Mcf7 Cell Line

26 Background: HOXB9 is a member of class I HOX genes and is known to be overexpressed in human breast cancer and related to EMT, tumor angiogenesis, and radio-resistance (PNAS 2010), being significant prognostic factor in breast cancer patients. (Ann Surg Oncol 2012). Methods: We analyzed the upstream promoter region to determine the critical sequence for HOXB9 transcription. The multiple lengths of HOXB9 promoter region were cloned into pGL3 luciferase vector and each of them were checked by luciferase assay. Then made E2F1 overexpressed cell-lines: MCF7, MCF10A and MDA-MB231 to check HOXB9 gene expression. ChIP assay performed using E2F1 induced MCF7 cell-line model and EMSA made with T47D cells and E2F1 antibody. Results: We demonstrated luciferase activity of MDA-MB231 cells and overexpressed HOXB9 was determined at the region from -404 to -392 bps, showing that the mentioned region plays the critical role for the transcription of HOXB9. Computer prediction system for the binding ability to critical sequence raised several candidate: E2F1, PAX-5, P53, ETS-1, NFY-A, Sp-1, which are known to be related with cancer progression and we confirmed these genes could induce HOXB9. E2F1 overexpressed breast cancer cell-lines indicate high expression of HOXB9 show the correlation between E2F1 and HOXB9 expression. Luciferase assay method done by constructing pGL3 with HOXB9 critical sequence and analyzed using wild-type MCF7 and E2F1 induced MCF7 cells showed high luciferase activity of HOXB9 critical sequence plasmid in E2F1 induced MCF7 cell-line by compare to WT. ChIP assay and EMSA assay methods performed using E2F1 overexpressed MCF7 and T47D cell-lines model revealed high precipitation rate with E2F1 antibody and HOXB9 expression than negative control. Conclusions: HOXB9 is plays the role as the accelerator of breast cancer progression and discovering the properties of the gene and related factors will help to understand new signaling pathways of breast cancer development. E2F1 is a strong candidate direct binds to HOXB9 critical sequence and correlates with HOXB9 expression. Manipulating of E2F1 expression may regulate HOXB9 and reduce cancer progression and metastasis.

Synthesis of imidazothiadiazole–benzimidazole conjugates as mitochondrial apoptosis inducers

MedChemComm ◽  
2014 ◽  
Vol 5 (11) ◽  
pp. 1644-1650 ◽  
Author(s):  
Ahmed Kamal ◽  
Swapna Ponnampalli ◽  
M. V. P. S. Vishnuvardhan ◽  
M. P. Narasimha Rao ◽  
Kishore Mullagiri ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cell Line ◽  
Cell Lines ◽  
Antiproliferative Activity ◽  
Human Cancer ◽  
Mitochondrial Apoptosis ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Cervical Cell ◽  
Line P

A series of imidazothiadiazole–benzimidazole conjugates (3a–z) were synthesized and evaluated for their cytotoxic activity against a set of four selected human cancer cell lines. Compounds3band3yexhibited significant antiproliferative activity against the ME-180 (cervical) cell line.

scholarly journals Synthesis of MeON-Glycoside Derivatives of Oleanolic Acid by Neoglycosylation and Evaluation of Their Cytotoxicity against Selected Cancer Cell Lines

Molecules ◽  
2021 ◽  
Vol 26 (3) ◽  
pp. 772
Author(s):  
Zhichao Du ◽  
Guolong Li ◽  
Xiaoyang Zhou ◽  
Jian Zhang
Keyword(s):  
Cell Line ◽  
Cell Lines ◽  
Oleanolic Acid ◽  
Cancer Cell ◽  
Hepg2 Cells ◽  
Cancer Cell Line ◽  
Cancer Cell Lines ◽  
Cell Counting ◽  
Antiproliferative Agents ◽  
Antiproliferative Activities

A series of C-3 and C-28 MeON-neoglycosides of oleanolic acid were designed and synthesized by neoglycosylation as potential antiproliferative agents. Their cytotoxicity was evaluated in vitro against five human cancer cell lines: human non-small cell lung cancer cell line (A549), human melanoma cell line (A375), human colon cancer cell line (HCT116), human liver carcinoma cell line (HepG2), human breast adenocarcinoma cell line (MCF-7) by the Cell Counting Kit-8 (CCK-8) assay. Most of C-3 and C-28 MeON-neoglycosides of oleanolic acid exhibited notably inhibitory effects against the tested cancer cells and more sensitive to HepG2 cells than 5-Fluorouracil (5-FU). Structure-activities relationship (SAR) analysis revealed that sugar types and the d/l configuration of sugars would significantly affect their antiproliferative activities of neoglycosides. Among them, compound 8a (28-N-methoxyaminooleanane-β-d-glucoside) exhibited the most potent antiproliferative activities against HepG2 cells with IC50 values of 2.1 µM. Further pharmacological experiments revealed that compound 8a could cause morphological changes and cell cycle arrest at G0/G1 phase and induce apoptosis in HepG2 cells. These results suggested that neoglycosylation could provide a rapid strategy for the discovery of potential antiproliferative agents and their possible pharmacological mechanisms need more further research.

scholarly journals Novel Oleanolic Acid-Tryptamine and -Fluorotryptamine Amides: From Adaptogens to Agents Targeting In Vitro Cell Apoptosis

Plants ◽  
2021 ◽  
Vol 10 (10) ◽  
pp. 2082
Author(s):  
Uladzimir Bildziukevich ◽  
Marie Kvasnicová ◽  
David Šaman ◽  
Lucie Rárová ◽  
Zdeněk Wimmer
Keyword(s):  
Cell Line ◽  
Cell Lines ◽  
Oleanolic Acid ◽  
Cancer Cell ◽  
Self Assembly ◽  
Cell Apoptosis ◽  
Cancer Cell Line ◽  
Cancer Cell Lines ◽  
Screening Tests ◽  
Human Malignant Melanoma

Background: Oleanolic acid is a natural plant adaptogen, and tryptamine is a natural psychoactive drug. To compare their effects of with the effect of their derivatives, tryptamine and fluorotryptamine amides of oleanolic acid were designed and synthesized. Methods: The target amides were investigated for their pharmacological effect, and basic supramolecular self-assembly characteristics. Four human cancer cell lines were involved in the screening tests performed by standard methods. Results: The ability to display cytotoxicity and to cause selective cell apoptosis in human cervical carcinoma and in human malignant melanoma was seen with the three most active compounds of the prepared series of compounds. Tryptamine amide of (3β)-3-(acetyloxy)olean-12-en-28-oic acid (3a) exhibited cytotoxicity in HeLa cancer cell lines (IC50 = 8.7 ± 0.4 µM) and in G-361 cancer cell lines (IC50 = 9.0 ± 0.4 µM). Fluorotryptamine amides of (3β)-3-(acetyloxy)olean-12-en-28-oic acid (compounds 3b and 3c) showed cytotoxicity in the HeLa cancer cell line (IC50 = 6.7 ± 0.4 µM and 12.2 ± 4.7 µM, respectively). The fluorotryptamine amide of oleanolic acid (compound 4c) displayed cytotoxicity in the MCF7 cancer cell line (IC50 = 13.5 ± 3.3 µM). Based on the preliminary UV spectra measured in methanol/water mixtures, the compounds 3a–3c were also found to self-assemble into supramolecular systems. Conclusions: An effect of the fluorine atom present in the molecules on self-assembly was observed with 3b. Enhanced cytotoxicity has been achieved in 3a–4c in comparison with the effect of the parent oleanolic acid (1) and tryptamine. The compounds 3a–3c showed a strong induction of apoptosis in HeLa and G-361 cells after 24 h.

Biological Activity, Apoptotic Induction and Cell Cycle Arrest of New Hydrazonoyl Halides Derivatives

2019 ◽  
Vol 19 (9) ◽  
pp. 1141-1149 ◽  
Author(s):  
Magda F. Mohamed ◽  
Hamdi M. Hassaneen ◽  
Emad M. Elzayat ◽  
Salwa M. El-Hallouty ◽  
May El-Manawaty ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Cytotoxic Activity ◽  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Biological Activities ◽  
Breast Epithelial Cell ◽  
Human Cancer Cell ◽  
Hydrazonoyl Halides

Background:The hydrazonoyl halides are presently an important target in the field of medicinal chemistry. The interest in the chemistry of hydrazonoyl halides is a consequence of the fact that they undergo a wide variety of reactions which provide routes to a myriad of both heterocyclic and acyclic compounds. In addition, they have diverse biological activities such as antiviral, anthelmintic, antiarthropodal, fungicidal, herbicidal, insecticidal, pesticidal, acaricidal and miticidal Activity correlated to the presence of hydrazonoyl halides. Moreover, many applications in both industrial and pharmaceutical fields have been found to be associated with these halides. Depending on the above facts and continuation to our work, we herein report on the evaluation of the anticancer activity of these two halides prepared according to the published work and trying to know their molecular mechanism that they proceed to stop proliferation and metastasis of tumor cells by molecular tools such as real time PCR using different apoptotic genes, and cell cycle assay.Objective:The goal of this present study is to bring attention to the biological activities of hydrazonoyl halides and the molecular pathway they follow to exert their role in apoptotic death of cancer cell.Methods:Synthesis of hydrazonoyl halides 2c and 2f. The cytotoxic effect against different human cancer cell lines PC3, HepG-2, HCT-116, MCF-7 and also on normal human cell lines as MCF-10 and MCF-12 in a monolayer culture model was evaluated. Their mechanism of action inside cancer cell was evaluated using different molecular tools.Conclusion:Strong and promising chemotherapeutic hydrazonoyl halides (2a-2f) were evaluated for their different biological activities. As antimicrobial agents, results indicated that three compounds 2a, 2e and 2f exhibited high activity against two tested gram positive bacteria Staphylococcus aureus, Bacillus subtilis, and gram negative ones Escherichia coli, and Pseudomonas aeruginosa, the rest of the compounds were found to be moderately active against the tested microorganisms. Regarding their antifungal effect, compound 2c exhibited potent and promising effect against Candida albicans, while 2b was the most potent toward Aspergillus flavus Link. The compound 2f has repellent effect. With respect to the in vitro antitumor screening, this was done on different human cancer cell lines; namely PC3, HepG-2, HCT-116, MCF-7 and also on normal human cell lines; as MCF-10 and MCF-12 (normal breast epithelial cell and non-tumorigenic breast epithelial cell line) in a monolayer culture model where screening has been conducted at 100μg/ml (single dose test). Single dose test (100μg/ml) showed that, in case of PC3, all compounds have cytotoxic activity over 90% inhibition, 4 compounds have cytotoxic activity with 100% inhibition with Human colon cancer cell line, 4 compounds showed over 90% inhibition with MCF7 cell line and 4 compounds showed cytotoxic activity over 90% inhibition with HepG-2. Results of IC50 values for most promising compounds showed compounds with values lower than 20μM for all tested human cancer cell line. The promising hydrazonoyl halide 2c and 2f were selected for molecular study to know how they could act inside cancer cell causing death. Two biochemical tests were performed using the two halides 2c and 2f to predict their mechanism of action against breast carcinoma. Real time PCR analysis indicates that the two compounds induced the apoptosis of MCF7 cells through the up regulation of caspase-3, BAX mediated P53 mechanism but unfortunately, they promote the expression of anti-apoptotic protein BCL2. Also, cell cycle assay was performed using two different cell lines MCF7 and HCT116 and data revealed that the two compounds 2c and 2f induced apoptotic cells death of both lines via cell growth arrest at G2/M phase. In addition, it was noted that 2c induced arrest in the two lines more efficiently than 2f at G2/M phase.

scholarly journals Determination of Cytisine and N-Methylcytisine from Selected Plant Extracts by High-Performance Liquid Chromatography and Comparison of Their Cytotoxic Activity

Toxins ◽  
2020 ◽  
Vol 12 (9) ◽  
pp. 557
Author(s):  
Anna Petruczynik ◽  
Karol Wróblewski ◽  
Justyna Misiurek ◽  
Tomasz Plech ◽  
Karolina Szalast ◽  
...  
Keyword(s):  
High Performance Liquid Chromatography ◽  
Liquid Chromatography ◽  
Cytotoxic Activity ◽  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Plant Extracts ◽  
High Performance ◽  
Cancer Cell Lines ◽  
Breast Adenocarcinoma

Quinolizidine alkaloids exhibit various forms of biological activity. A lot of them were found in the Leguminosae family, including Laburnum and Genista. The aim of the study was the optimization of a chromatographic system for the analysis of cytisine and N-methylcytisine in various plant extracts as well as an investigation of the cytotoxic activities of selected alkaloids and plant extracts obtained from Laburnum anagyroides, Laburnum anagyroides L. quercifolium, Laburnum alpinum, Laburnum watereri, Genista germanica, and Genista tinctoria against various cancer cell lines. The determination of investigated compounds was performed by High Performance Liquid Chromatography with Diode Array Detection (HPLC-DAD), while High Performance Liquid Chromatography coupled with Quadrupole Time-of-Flight–Mass Spectrometry (HPLC-QTOF-MS) was applied for the qualitative analysis of plant extracts. The retention, separation selectivity, peaks shape, and systems efficiency obtained for cytisine and N-methylcytisine in different chromatographic systems were compared. The application of columns with alkylbonded and phenyl stationary phases led to a very weak retention of cytisine and N-methylcytisine, even when the mobile phases containing only 5% of organic modifiers were used. The strongest retention was observed when hydrophilic interaction chromatography (HILIC) or especially when ion exchange chromatography (IEC) were applied. The most optimal system in terms of alkaloid retention, peak shape, and system efficiency containing an strong cation exchange (SCX) stationary phase and a mobile phase consisted of 25% acetonitrile and formic buffer at pH 4.0 was applied for investigating alkaloids analysis in plant extracts. Cytotoxic properties of the investigated plant extracts as well as cytisine and N-methylcytisine were examined using human tongue squamous carcinoma cells (SCC-25), human pharyngeal squamous carcinoma cells (FaDu), human triple-negative breast adenocarcinoma cell line (MDA-MB-231), and human breast adenocarcinoma cell line (MCF-7). The highest cytotoxic activity against FaDu, MCF-7, and MDA-MB cancer cell lines was observed after applying the Genista germanica leaves extract. In contrast, the highest cytotoxic activity against SCC-25 cell line was obtained after treating with the seed extract of Laburnum watereri. The investigated plant extracts exhibit significant cytotoxicity against the tested human cancer cell lines and seem to be promising for further research on its anticancer activity.

scholarly journals In vitro Cytotoxic Activity of Sesamin Isolated from Vismia baccifera var. dealbata Triana & Planch (Guttiferae) Collected from Venezuela

2008 ◽  
Vol 3 (10) ◽  
pp. 1934578X0800301 ◽  
Author(s):  
Fabiola Salas ◽  
Janne Rojas ◽  
Antonio Morales ◽  
Maria E. Ramos-Nino ◽  
Nelida G. Colmenares
Keyword(s):  
Lung Cancer ◽  
Cytotoxic Activity ◽  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
Lung Cancer Cell Line ◽  
Cytostatic Activity ◽  
Lung Cancer Cell

Sesamin extracted from Vismia baccifera var. dealbata was demonstrated to have cytostatic activity on the cancer cell lines tested, particularly the lung cancer cell line, with an IC50 of 1 g/L.

scholarly journals Anatolicin, a Highly Potent and Selective Cytotoxic Sesquiterpene Coumarin from the Root Extract of Heptaptera anatolica

Molecules ◽  
2019 ◽  
Vol 24 (6) ◽  
pp. 1153 ◽  
Author(s):  
Fatma Tosun ◽  
John Beutler ◽  
Tanya Ransom ◽  
Mahmut Miski
Keyword(s):  
Cytotoxic Activity ◽  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Kidney Cancer ◽  
Spectral Properties ◽  
Cancer Cell Line ◽  
Cancer Cell Lines ◽  
Root Extract ◽  
Selective Cytotoxicity

Seven known sesquiterpene coumarins and a new sesquiterpene coumarin, anatolicin (8), were isolated from the dichloromethane extract of the roots of Heptaptera anatolica. Structures of these compounds were elucidated based on their spectral properties. While some of these sesquiterpene coumarins showed modest cytotoxic activity against COLO205, KM12, A498, UO31, and TC32 cancer cell lines, selective cytotoxicity of anatolicin (8) and 14′-acetoxybadrakemin (7) were observed at nanomolar level against the UO31 kidney cancer cell line.

Sign in / Sign up

Export Citation Format

Share Document