scholarly journals Synthesis and Antiplasmodial Evaluation of 4-Carboxamido- and 4-Alkoxy-2-Trichloromethyl Quinazolines

Molecules ◽  
2020 ◽  
Vol 25 (17) ◽  
pp. 3929
Author(s):  
Dyhia Amrane ◽  
Armand Gellis ◽  
Sébastien Hutter ◽  
Marion Prieri ◽  
Pierre Verhaeghe ◽  
...  
Keyword(s):  
Cell Line ◽  
Hepg2 Cell ◽  
Alkoxy Group ◽  
Hepg2 Cell Line ◽  
Ccl3 Group ◽  
Falciparum Strain ◽  
Structure Activity ◽  
Trichloromethyl Group ◽  
Sar Study

From three previously identified antiplasmodial hit compounds (A–C) and inactive series (D), all based on a 2-trichloromethylquinazoline scaffold, we conducted a structure-activity relationship (SAR) study at position four of the quinazoline ring by synthesizing 42 novel derivatives bearing either a carboxamido- or an alkoxy-group, to identify antiplasmodial compounds and to enrich the knowledge about the 2-trichloromethylquinazoline antiplasmodial pharmacophore. All compounds were evaluated in vitro for their cytotoxicity towards the HepG2 cell line and their activity against the multiresistant K1 P. falciparum strain, using doxorubicin, chloroquine and doxycycline as reference drugs. Four hit-compounds (EC50 K1 P. falciparum ≤ 2 µM and SI ≥ 20) were identified among 4-carboxamido derivatives (2, 9, 16, and 24) and two among 4-alkoxy derivatives (41 and 44). Regarding the two most potent molecules (16 and 41), five derivatives without a 2-CCl3 group were prepared, evaluated, and appeared totally inactive (EC50 > 50 µM), showing that the 2-trichloromethyl group was mandatory for the antiplasmodial activity.

Evaluation of in vitro antioxidant activities of soyasaponins from soy hypocotyls in human HepG2 cell line

2016 ◽  
Vol 71 (3) ◽  
pp. 653-660 ◽  
Author(s):  
Lijie Zhu ◽  
Minghan Zhang ◽  
Xiuying Liu ◽  
He Liu ◽  
Yutang He ◽  
...  
Keyword(s):  
Cell Line ◽  
Hepg2 Cell ◽  
Antioxidant Activities ◽  
Hepg2 Cell Line

scholarly journals Evaluation of Antioxidant and Antidiabetic Potential of Polyherbal Drug Made with Three Herbs: An In vitro Cell Culture Model

2021 ◽  
Vol 14 (4) ◽  
pp. 1627-1635
Author(s):  
P. Chandrasekaran
Keyword(s):  
Cell Culture ◽  
Cell Line ◽  
Hepg2 Cell ◽  
Plant Extracts ◽  
Antioxidant Properties ◽  
Protein Glycation ◽  
Gas Chromatography Mass Spectrometry ◽  
Individual Plant ◽  
Hepg2 Cell Line

In diabetes, the postprandial phase is characterized by a rapid and large increase in blood glucose levels, and the possibility that the postprandial “hyperglycemic spikes” may be relevant to the onset of cardiovascular complications has recently received much attention. Medicinal use of herbal medicine in the treatment and prevention of diseases including diabetes has a long history compared to conventional medicine. These plants have no side effects and many existing medicines are derived from the plants. Hence, the current investigation was planned to make a poly herbal drug (PHD) through Punica granatum (fruits), Illicium verum (flowers) and Nyctanthes arbor (leaves) and assess their antioxidant and antidiabetic activities in vitro and in HepG2 cell line. The respective plant methanolic extracts and PHD are exposed to phytochemical assessment and to discriminate the bioactive factors by Gas Chromatography–Mass Spectrometry. We evaluated the antioxidant properties 2, 2-diphenyl-1-picrylhydrazyl scavenging, hydrogen peroxide scavenging, thiobarbituric acid reactive substances and total antioxidant activity of individual plant extracts and the PHD. At the same time, In vitro and cell culture approaches were used to assess the anti-diabetic activity. The PHD has a higher concentration of secondary metabolites than individual plant extracts, according to our findings. On the other hand, we also notice that PHD demonstrated higher antioxidant capability and considerable in vitro glucose-lowering effects along with noteworthy inhibition of ɑ-amylase, glucosidase, lipase, dipeptidyl peptidase-IV, collagenase and protein glycation in HepG2 cell line. In conclusion, this study clearly demonstrated the significant antioxidant and antidiabetic activities of the PHD. Hence, PHD may be used as a potential source in the management of diabetes, hyperglycemia and the related state of oxidative stress.

Synthesis, Characterization and Anti-hepatoma Activity of New Hederagenin Derivatives

2020 ◽  
Vol 20 (3) ◽  
pp. 252-257
Author(s):  
Xiao Liu ◽  
Lu Sun ◽  
Qing-Hua Liu ◽  
Bao-Quan Chen ◽  
Yu-Ming Liu
Keyword(s):  
Hepatocellular Carcinoma ◽  
Cell Line ◽  
Hepg2 Cell ◽  
Normal Cell ◽  
Biological Significance ◽  
Cancer Cell Line ◽  
Human Hepatocellular Carcinoma ◽  
Hepg2 Cell Line ◽  
Normal Cell Line

Background: Based on the biological significance of hederagenin-type saponins found in our previous investigation, a series of new hederagenin derivatives were designed and synthesized. Methods : Their in vitro antiproliferative activities were evaluated against the HepG2 liver cancer cell line and normal cell line L929 by MTT assay. Results: The preliminary bioassay results demonstrated that all the tested compounds 1-7 showed potent anti-hepatoma activities, and some compounds exhibited better effects than 5-fluorouracil against human hepatocellular carcinoma HepG2 cell line. Furthermore, compound 5 showed a significant antihepatoma activity against HepG2 cells with an IC50 value of 1.88 µM. Besides, all of the tested compounds showed a low cytotoxic effect against the normal cell line L929. Conclusion: All the compounds 1-7 displayed superior selectivity against human hepatocellular carcinoma HepG2 cell line, and the results suggest that the structural modifications of C ring on the hederagenin backbone are vital for modulating anti-hepatoma activities.

scholarly journals Synthesis of Mixed Ligand Complexes of M(II) Dithiocarbamato Derivative and 2,2'-bipyridyl and Study their Cytotoxic Effect Against HepG2 Cell Line in vitro

2015 ◽  
Vol 12 (1) ◽  
pp. 127-139
Author(s):  
Baghdad Science Journal
Keyword(s):  
Solid State ◽  
Cell Line ◽  
Hepg2 Cell ◽  
Ultra Violet ◽  
Mixed Ligand ◽  
Hepg2 Cell Line ◽  
Standard Drug ◽  
Bidentate Coordination ◽  
Flame Atomic Absorption

Mixed ligand of Co and Ni (II) complexes were prepared from [5-(p-nitrophenyl)-4/-phenyl-1,2,4-triazole-3-dithiocarbamato hydrazide](TRZ.DTC) as primary ligand and 2,2'-bipyridyl (bipy) as a co-ligand with metal salts. These complexes were analytically and spectroscopically characterized in solid state by elemental analyses, flame atomic absorption, magnetic susceptibility and molar conductance measurements, as well as by UV–Vis and FTIR spectroscopy. Infrared, ultra violet spectra reveal a bidentate coordination of the two ligands with metal ions 1:1:1 mole ratio. Room temperature magnetic moments and solid reflectance spectra data indicate paramagnetic complexes with five-coordinate square pyramidal geometry for nickel (II) complex, while six-coordinate octahedral geometry for cobalt (II) complex in solid state. The mixed ligand and its respective complexes were screened for cytotoxicity assay on human HepG2 cell line using cis-Pt drug as a control positive following the cell culture method for 3 days after treatment with the tested compounds using eight different concentrations. The bioassay results showed good inhibition activity of these synthetic compounds especially Ni (II) complex on selected cell lines comparable with standard drug.

In vitro expression of hepatitis C virus non-structure 5 antigen in the HepG2 cell line

2000 ◽  
Vol 20 (4) ◽  
pp. 277-279
Author(s):  
Ye Jin ◽  
Zeng Linglan ◽  
Yang Mulan ◽  
Luo Duande ◽  
Guo Jinsong
Keyword(s):  
Hepatitis C Virus ◽  
Hepatitis C ◽  
Cell Line ◽  
Hepg2 Cell ◽  
Hepg2 Cell Line ◽  
In Vitro Expression

In vitro challenge using thymoquinone on (HepG2) cell line

2009 ◽  
Vol 189 ◽  
pp. S266
Author(s):  
Sohair Hassan ◽  
Wafaa A. Ahmed ◽  
Fayek M. Galeb ◽  
Maha A. El-Taweel
Keyword(s):  
Cell Line ◽  
Hepg2 Cell ◽  
Hepg2 Cell Line

scholarly journals The Curious Case of the HepG2 Cell Line: 40 Years of Expertise

2021 ◽  
Vol 22 (23) ◽  
pp. 13135
Author(s):  
Viktoriia A. Arzumanian ◽  
Olga I. Kiseleva ◽  
Ekaterina V. Poverennaya
Keyword(s):  
Liver Cancer ◽  
Cell Line ◽  
Hepg2 Cell ◽  
Cell Lines ◽  
Molecular Mechanisms ◽  
Basic Research ◽  
Health Concern ◽  
Hepg2 Cell Line ◽  
Wide Range

Liver cancer is the third leading cause of cancer death worldwide. Representing such a dramatic impact on our lives, liver cancer is a significant public health concern. Sustainable and reliable methods for preventing and treating liver cancer require fundamental research on its molecular mechanisms. Cell lines are treated as in vitro equivalents of tumor tissues, making them a must-have for basic research on the nature of cancer. According to recent discoveries, certified cell lines retain most genetic properties of the original tumor and mimic its microenvironment. On the other hand, modern technologies allowing the deepest level of detail in omics landscapes have shown significant differences even between samples of the same cell line due to cross- and mycoplasma infection. This and other observations suggest that, in some cases, cell cultures are not suitable as cancer models, with limited predictive value for the effectiveness of new treatments. HepG2 is a popular hepatic cell line. It is used in a wide range of studies, from the oncogenesis to the cytotoxicity of substances on the liver. In this regard, we set out to collect up-to-date information on the HepG2 cell line to assess whether the level of heterogeneity of the cell line allows in vitro biomedical studies as a model with guaranteed production and quality.

scholarly journals IN VITRO EVALUATION OF ANTIDIABETIC AND CYTOTOXICITY POTENTIALS OF THE RHIZOME EXTRACT OF DRYNARIA QUERCIFOLIA (L.) J. SMITH

2019 ◽  
pp. 72-76
Author(s):  
PRASANNA G ◽  
DEVI R ◽  
ISHWARYA G
Keyword(s):  
Liver Cancer ◽  
Glucose Uptake ◽  
Cell Line ◽  
Hepg2 Cell ◽  
Plant Extract ◽  
Mtt Assay ◽  
Hepg2 Cell Line ◽  
Uptake Assay ◽  
Glucose Uptake Assay

Objective: In the present study, an attempt has been made to evaluate the in vitro antidiabetic and cytotoxic potentials of the rhizome extract of Drynaria quercifolia (L.) J. Smith. Methods: In vitro antidiabetic activity was determined by two different assays such as alpha-amylase inhibition assay and glucose uptake assay. The plant extract with three different concentrations was used for this assay. L6 rat myogenic cells were selected and subjected to glucose uptake assay. The cytotoxic activity of the different concentrations of the plant extract on HepG2 cell line was also investigated in vitro through 3-(4,5, dimethythiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay. Results: The findings of the study provide evidence that the rhizome extract of D. quercifolia possesses significant anti-diabetic activity. In MTT assay, the significant cytotoxic effect of plant extract was observed by measuring the percentage of cell viability on the HepG2 cell line. Conclusion: The findings indicated that rhizome extracts of D. quercifolia have potential as a medicinal drug against diabetes mellitus (DM) and liver cancer. Further, studies with in vivo and clinical trials need to be conducted to establish rhizome extract as a safe agent for DM and liver cancer therapy.

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