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.

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.

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.

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 Transcriptomic analysis of marine endophytic fungi extract identifies highly enriched anti-fungal fractions targeting cancer pathways in HepG2 cell lines

BMC Genomics ◽  
2020 ◽  
Vol 21 (1) ◽  
Author(s):  
Ethel Juliet Blessie ◽  
Wasco Wruck ◽  
Benaiah Annertey Abbey ◽  
Audrey Ncube ◽  
Nina Graffmann ◽  
...  
Keyword(s):  
Hepg2 Cell ◽  
Cell Lines ◽  
Endophytic Fungi ◽  
Transcriptomic Analysis ◽  
Cancer Pathways ◽  
Hepg2 Cell Lines ◽  
Anti Fungal

Green Synthesis of Silver Nanocomposites of Nigella sativa Seeds Extract for Hepatocellular Carcinoma

2019 ◽  
Vol 4 (3) ◽  
pp. 191-200 ◽  
Author(s):  
Afreen Usmani ◽  
Anuradha Mishra ◽  
Asif Jafri ◽  
Md Arshad ◽  
Mohd Aftab Siddiqui
Keyword(s):  
Hepatocellular Carcinoma ◽  
Green Synthesis ◽  
Hepg2 Cell ◽  
Cell Lines ◽  
Nigella Sativa ◽  
Uv Spectroscopy ◽  
Silver Nanocomposites ◽  
Natural Drugs ◽  
Hepg2 Cell Lines

Background: Silver nanoparticles play a significant role in bioavailability and refining the compatibility of natural drugs in the treatment of various chronic diseases including different types of cancer. Objective: Green synthesis of silver nanocomposites of Nigella sativa seeds extract to evaluate the anticancer effects against hepatocellular carcinoma using HepG2 cell lines. Methods: The AgNCs were developed by treating aqueous extract of N. sativa seeds treated with silver nitrate (1mM) solution and were used to test its efficacy against hepatocellular carcinoma using HepG2 cell lines. Results and Discussion: The Surface Plasmon Resonance (SPR) of prepared AgNCs showed a peak at 432 nm via UV spectroscopy. The selected N. sativa AgNCs were characterized for polydispersity, surface charge and size and the results showed 0.215±0.093 polydispersity index (PDI), zeta potential 18.8±0.372 mV and size range 10-20 nm, respectively. The Fourier transform infrared spectroscopy (FTIR) also showed various peak of functional groups that are possibly involved in the reduction of silver ion and synthesized the N. sativa silver nanocomposites, respectively. N. sativa AgNCs showed 89.954% drug release while in the case of extract release, it was only 33.821% in 24 hrs. Further, in vitro studies of N. sativa AgNCs against hepatocellular carcinoma showed good cytotoxic effect p<0.05 with 7.16 µg/ml IC50 value. Conclusion: Thus, the present results revealed that green synthesis of N. sativa AgNCs can be an alternative tool for clinical application in cancer therapy; however, there is a need to find the mechanism and role of AgNCs inside the individual.

scholarly journals Fast Detection of Two Smenamide Family Members Using Molecular Networking

Marine Drugs ◽  
2019 ◽  
Vol 17 (11) ◽  
pp. 618 ◽  
Author(s):  
Alessia Caso ◽  
Germana Esposito ◽  
Gerardo Della Sala ◽  
Joseph R. Pawlik ◽  
Roberta Teta ◽  
...  
Keyword(s):  
Secondary Metabolites ◽  
Cell Lines ◽  
Absolute Configuration ◽  
Antiproliferative Activity ◽  
Spectroscopic Analysis ◽  
Alkyl Chain ◽  
Molecular Networking ◽  
New Members ◽  
Fast Detection ◽  
Mcf 7

Caribbean sponges of the genus Smenospongia are a prolific source of chlorinated secondary metabolites. The use of molecular networking as a powerful dereplication tool revealed in the metabolome of S. aurea two new members of the smenamide family, namely smenamide F (1) and G (2). The structure of smenamide F (1) and G (2) was determined by spectroscopic analysis (NMR, MS, ECD). The relative and the absolute configuration at C-13, C-15, and C-16 was determined on the basis of the conformational rigidity of a 1,3-disubstituted alkyl chain system (i.e., the C-12/C-18 segment of compound (1). Smenamide F (1) and G (2) were shown to exert a selective moderate antiproliferative activity against cancer cell lines MCF-7 and MDA-MB-231, while being inactive against MG-63.

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