Prenylated flavonoids from the fruits of Sinopodophyllum emodi and their cytotoxic activities

RSC Advances ◽  
2015 ◽  
Vol 5 (101) ◽  
pp. 82736-82742 ◽  
Author(s):  
Yan-Jun Sun ◽  
Zhi-You Hao ◽  
Jin-Guang Si ◽  
Yu Wang ◽  
Yan-Li Zhang ◽  
...  
Keyword(s):  
Hepg2 Cell ◽  
Cell Lines ◽  
Cytotoxic Activities ◽  
Prenylated Flavonoids ◽  
Hepg2 Cell Lines ◽  
Mcf 7

Thirteen new prenylated flavonoids were isolated from Sinopodophyllum emodi together with eleven known analogues. Compound 22 exhibited the most potent cytotoxicity against MCF-7 and HepG2 cell lines.

scholarly journals Sixteen New Prenylated Flavonoids from the Fruit of Sinopodophyllum hexandrum

Molecules ◽  
2019 ◽  
Vol 24 (17) ◽  
pp. 3196 ◽  
Author(s):  
Yanjun Sun ◽  
Haojie Chen ◽  
Junmin Wang ◽  
Meiling Gao ◽  
Chen Zhao ◽  
...  
Keyword(s):  
Hepg2 Cell ◽  
Mtt Assay ◽  
13C Nmr ◽  
Spectroscopic Data ◽  
Cytotoxic Activities ◽  
Prenylated Flavonoids ◽  
Ic50 Values ◽  
Sinopodophyllum Hexandrum ◽  
Hepg2 Cell Lines ◽  
Mcf 7

Sixteen new prenylated flavonoids, sinoflavonoids P–Z (1–11) and sinoflavonoids NA–NE (12–16), were isolated from the fruit of Sinopodophyllum hexandrum, along with eight known analogues (17–24). Their structures were elucidated on the basis of extensive spectroscopic data (HR-ESI-MS, 1H-NMR, 13C-NMR, HSQC, HMBC). The cytotoxic activities of compounds 1–18, 20, and 22 were evaluated by MTT assay. Compound 6 showed the most potent cytotoxicity in MCF-7, and HepG2 cell lines, with IC50 values of 6.25 and 3.83 μM, respectively.

Tadpole-shaped β-cyclodextrin-tagged poly(N-vinylpyrrolidone): synthesis, characterization and studies of its complexation with phenolphthalein and anti tumor activities

RSC Advances ◽  
2015 ◽  
Vol 5 (20) ◽  
pp. 15547-15558 ◽  
Author(s):  
Niraj Kumar Vishwakarma ◽  
Vijay Kumar Patel ◽  
Sumit Kumar Hira ◽  
K. Ramesh ◽  
Prateek Srivastava ◽  
...  
Keyword(s):  
Hepg2 Cell ◽  
Cell Lines ◽  
Effective Delivery ◽  
Hepg2 Cell Lines ◽  
Mcf 7

DOX-loaded β-CD-PNVP shows more effective delivery of DOX compared to free DOX towards the U2-OS, MCF-7 and HEPG2 cell lines.

Synthesis and Evaluation of a Series of 1,3,4-Thiadiazole Derivatives as Potential Anticancer Agents

2019 ◽  
Vol 18 (11) ◽  
pp. 1606-1616 ◽  
Author(s):  
Mehlika D. Altıntop ◽  
Belgin Sever ◽  
Ahmet Özdemir ◽  
Sinem Ilgın ◽  
Özlem Atlı ◽  
...  
Keyword(s):  
Dna Synthesis ◽  
Cell Line ◽  
Hepg2 Cell ◽  
Cell Lines ◽  
Anticancer Agents ◽  
In Vitro Assays ◽  
Breast Adenocarcinoma ◽  
Dependent Manner ◽  
Hepg2 Cell Lines ◽  
Mcf 7

Background and Methods: In an attempt to develop potent antitumor agents, the synthesis of a series of N-(6-substituted benzothiazol-2-yl)-2-[(5-(arylamino)-1,3,4-thiadiazol-2-yl)thio]acetamides (1-14) was described and their cytotoxic effects on A549 human lung adenocarcinoma, MCF-7 human breast adenocarcinoma, HepG2 human hepatocellular carcinoma and NIH/3T3 mouse embryonic fibroblast cell lines were investigated using MTT assay. <p> Results: Phenyl-substituted compounds (8-14) were found to be more effective than naphthyl-substituted compounds (1-7) on cancer cells. Compounds 8, 9, 10, 12, 13 and 14 were identified as the most potent anticancer agents on MCF-7 and HepG2 cell lines and therefore their effects on DNA synthesis and apoptosis/necrosis in MCF-7 cell line were evaluated. Among these compounds, N-(6-methoxybenzothiazol-2-yl)-2-[(5- (phenylamino)-1,3,4-thiadiazol-2-yl)thio]acetamide (13) was the most selective anticancer agent against MCF-7 and HepG2 cell lines with a SI value of 100. On the other hand, compounds 8, 9, 10, 12, 13 and 14 inhibited DNA synthesis in MCF-7 cell line in a dose-dependent manner. Flow cytometric analyses clearly indicated that the compounds showed significant anticancer activity against MCF-7 cell line via the induction of apoptosis dose dependently. <p> Conclusion: According to in vitro assays, compounds 8, 9, 10, 12, 13 and 14 stand out as promising candidates for further studies.

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.

One-Pot Synthesis of 5-(Het)Aryl 8-Aminoquinoline Amide Derivatives as Potential Antibacterial / Cytotoxic Agents

2020 ◽  
Vol 16 (2) ◽  
pp. 142-151
Author(s):  
Zanjam Spandana ◽  
Tadigiri M. Rekha ◽  
Mandava V.B. Rao ◽  
Manojit Pal
Keyword(s):  
Hepg2 Cell ◽  
Cell Lines ◽  
Antibacterial Activities ◽  
Cytotoxic Agents ◽  
Hek293 Cells ◽  
Cytotoxic Activities ◽  
Quinoline Derivatives ◽  
One Pot ◽  
Hepg2 Cell Lines

Background: The 8-Aminoquinoline (8-AQ) framework has attracted particular attention in the discovery and development of antimalarial and anti-bacterial agents or drugs. However, the clinical uses of 8-AQ based drugs are often associated with toxic side effects such as methemoglobinemia and hemolytic anemia with deficiency in Glucose-6-Phosphate Dehydrogenase (G6PD) Activity. The 4-aryl- 8-amino(acetamido)quinoline derivatives, on the other hand, have shown antiproliferative activities against cancer cell lines. These reports prompted us to assess the antibacterial and cytotoxic activities of a series of compounds based on 5-aryl 8-aminoquinoline amide scaffold. Methods: A series of compounds based on 5-(het)aryl 8-aminoquinoline amide scaffold was synthesized via a one-pot ultrasound-assisted method using a C-5 selective halogenation of quinoline derivatives followed by Pd/C-catalyzed Suzuki-Miyaura coupling with (het)aryl boronic acids. All these compounds were evaluated for their in vitro antibacterial activities against representative Gram-(+) and Gram-(-) strains including Escherichia coli, Pseudomonas aeruginosa, Klebsiella species and Staphylococcus aureus. Three compounds were further tested for cytotoxicities in vitro against breast adenocarcinoma (MCF7) and Hepatocellular Carcinoma (HepG2) along with non-cancerous human embryonic kidney (HEK293) cell lines. Results: All these compounds demonstrated moderate to good antibacterial activities against the four organisms used. In vitro assay results revealed that three compounds showed good activities against Gram-(+) strains and Gram-(-) strains and one was comparable to ciprofloxacin and pefloxacin. These three compounds were further tested for their cytotoxic properties against MCF7 and HepG2 cell lines. One of them showed IC50 value comparable to doxorubicin when tested against HepG2 cell lines. However, none of these compounds showed any significant effects when tested against HEK293 cells indicating their selectivity towards the growth inhibition of cancer cells. Conclusion: A series of compounds based on 5-(het)aryl 8-aminoquinoline amide scaffold was synthesized and evaluated for antibacterial and cytotoxic activities. Several of these compounds showed promising antibacterial and cytotoxic activities when tested in vitro suggesting that the present class of compounds may be of interest for the identification of new and potential antibacterial / cytotoxic agents.

Selenium Nanoparticles Induce Cytotoxicity and Apoptosis in Human Breast Cancer (MCF-7) and Liver (HepG2) Cell Lines

2020 ◽  
Vol 12 (3) ◽  
pp. 324-330
Author(s):  
Abdulsalam A. Alkhudhayri ◽  
Rizwan Wahab ◽  
Maqsood A. Siddiqui ◽  
Javed Ahmad
Keyword(s):  
Hepg2 Cell ◽  
Cell Lines ◽  
Selenium Nanoparticles ◽  
Model Systems ◽  
Mrna Levels ◽  
Hepg2 Cell Lines ◽  
Apoptotic Effects ◽  
Relative Differences ◽  
Mcf 7

This investigation was designed to assess the cytotoxic and apoptotic effects of selenium nanoparticles. It explored the cytotoxic effects of selenium nanoparticles in MCF-7 and HepG2 cell lines. The morphology of selenium nanoparticles was analyzed by transmission electron microscopy (TEM) to verify their size and crystalline properties. The selenium nanoparticles were almost spherical and cubic in shape and in size (∼20 nm). Selenium nanoparticles were tested for their cytotoxic activity in MCF-7 and HepG2 cell lines using MTT and NRU assays. We found relative differences in the vulnerability of both cell lines in their response to selenium nanoparticle-induced cytotoxicity. Specifically, MCF-7 cells exhibited greater vulnerability to exposure to selenium nanoparticles than HepG2 cells. Selenium nanoparticles exposure also induced higher mRNA levels of apoptosis related genes and caspase-3 enzyme activity. Overall, the present study provided the evidence of cytotoxicity induced by SeNPs via apoptotic gene expression in human cell lines. These results warrant further investigation into more precise mechanism(s) of selenium nanoparticles-induced cell death in in vivo model systems.

scholarly journals Genetic Profile Evaluation of Human Cell Lines Treated with Anastatica hierochuntica Using Forensic DNA Fingerprinting Markers

2021 ◽  
Vol 3 (2) ◽  
pp. 231-244
Author(s):  
Saranya Rameshbabu ◽  
Mohammed S. Ali ◽  
Abrar B. Alsaleh ◽  
Anuradha Venkatraman ◽  
Safia A. Messaoudi
Keyword(s):  
Cell Line ◽  
Hepg2 Cell ◽  
Cell Lines ◽  
Tandem Repeats ◽  
Dna Analysis ◽  
Genetic Profile ◽  
Forensic Dna ◽  
Cell Line Authentication ◽  
Hepg2 Cell Lines ◽  
Mcf 7

Cell line authentication using Short Tandem Repeats (STRs) is necessary to ensure the integrity of the cell for its continuous culture and to identify misidentification and cross-contamination issues. This study investigates the changes in the genetic profile of MCF-7 and HepG2 cell lines caused by the methanolic leaf extract of Anastatica hierochuntica (AH) using human identification based STR markers. MCF-7 and HepG2 cell lines were treated with various concentrations of AH extracts for three different periods. The treated and control cells' DNA was extracted using a QIAamp® DNA Micro Kit, quantified using a Quantifiler Duo DNA Quantification Kit, and amplified using an AmpFlSTR Identifiler plus PCR Amplification Kit. The concentrations of the DNA extracted from control and MCF-7 and HepG2 cell lines treated with AH extract at 300 to 2400 µg/ml for 24hr and 150 to 2400 µg/ml for 48 and 72hrs were statistically significant (p<0.05). Microsatellite instability (MSI), loss of heterozygosity (LOH), insertion/deletions changes in the STRs profile were observed in treated cell lines at 1200 and 2400 µg/ml in MCF-7 cells for 48 and 72hrs and HepG2 cells for 24, 48, and 72hrs. We conclude that the highest concentration of AH extracts affected the genotype of the cell lines leading to misidentification. Therefore, cell line authentication by forensic DNA analysis techniques plays a decisive role for cells tested with a high concentration of chemical compounds and gives the forensic investigator an insight into these changes in the STR genotype of a victim/suspect who has been been under long term chemotherapeutic treatment.

SYNTHESIS AND ANTIPROLIFERATIVE ACTIVITY OF FLAVONOID DERIVATIVES: EFFECT OF B-RING SUBSTITUTION

INDIAN DRUGS ◽  
2018 ◽  
Vol 55 (09) ◽  
pp. 7-14
Author(s):  
U Joshi ◽  
◽  
A Anantram ◽  
A Joshi ◽  
K Gokhale ◽  
...  
Keyword(s):  
Hepg2 Cell ◽  
Cell Lines ◽  
Antiproliferative Activity ◽  
Anticancer Therapy ◽  
Good Activity ◽  
Naturally Occurring ◽  
Hepg2 Cell Lines ◽  
Mcf 7

Flavones, flavonols, flavanones and isoflavones constitute four important categories of naturally occurring flavonoids. These compounds possess good antiproliferative activity and can act as adjuvants to existing anticancer therapy. We have synthesized twenty synthetic flavonoids including flavones, flavonols, flavanones and isoflavones using Claisen-Schmidt condensation, Baker-Venkataraman rearrangement and related reactions. The synthesized compounds were evaluated for antiproliferative activity against MCF-7, K562 and HepG2 cell lines. Flavanones showed good activity against HepG2 cell lines whereas some flavones and isoflavones were active in inhibiting the growth of K562 and MCF-7 cell lines. The study underlines the importance of electron rich substituents on the B-ring of synthetic flavonoids.

Cytotoxic activity and anti-cancer potential of Ontario grown onion extracts against breast cancer cell lines

2018 ◽  
Vol 8 (3) ◽  
pp. 159 ◽  
Author(s):  
Meghan Fragis ◽  
Abdulmonem I. Murayyan ◽  
Suresh Neethirajan
Keyword(s):  
Breast Cancer ◽  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Breast Cancer Cell ◽  
Cancer Cell Lines ◽  
Breast Cancer Cell Lines ◽  
Cytotoxic Activities ◽  
Cancer Line ◽  
Mcf 7

Background: Breast cancer is the most commonly diagnosed cancer and the second leading cause of cancer deaths among Canadian women. Cancer management through changes in lifestyle, such as increased intake of foods rich in dietary flavonoids, have been shown to decrease the risk associated with breast, liver, colorectal, and upper-digestive cancers in epidemiologic studies. Onions are high in flavonoid content and one of the most common vegetables. Additionally, onions are used in most Canadian cuisines.Methods: We investigated the effect of five prominent Ontario grown onion (Stanley, Ruby Ring, LaSalle, Fortress, and Safrane) extracts on two subtypes of breast cancer cell lines: a triple negative breast cancer line MDA-MB-231 and an ER+ breast cancer line MCF-7.Results: These onion extracts elicited strong anti-proliferative, anti-migratory, and cytotoxic activities on both the cancer cell lines. Flavonoids present in these onion extracts induced apoptosis, cell cycle arrest in the G2/M phase, and a reduction in mitochondrial membrane potential at dose-dependent concentrations. Onion extracts were more effective against MDA-MB-231 compared to the MCF-7 cell line. Conclusion: In this study, we investigated the extracts synthesized from Ontario-grown onion varieties in inducing anti-migratory, cytostatic, and cytotoxic activities in two sub-types of human breast cancer cell lines. Anti-tumor activity of these extracts depends upon the varietal and can be formulated into nutraceuticals and functional foods for the wellbeing of cancer patients. Overall, the results suggest that onion extracts are a good source of flavonoids with anti-cancerous properties.Keywords: onion extracts; flavonoids; anti-proliferative; breast cancer; cytotoxic activity

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.

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