scholarly journals Phloridzin docosahexaenoate, a novel polyphenolic derivative, is cytotoxic to canine osteosarcoma D17 cells

2021 ◽  
Vol 9 (5) ◽  
Author(s):  
Beth Murray ◽  
Niroshaa Arumuggam ◽  
Tess Astatkie ◽  
H.P. Rupasinghe
Keyword(s):  
Bone Cancer ◽  
Preliminary Evidence ◽  
Chemotherapeutic Drugs ◽  
Major Drawback ◽  
Canine Osteosarcoma ◽  
Human Liver Cells ◽  
Normal Human Liver ◽  
Normal Human ◽  
Preliminary Study

Canine osteosarcoma (OSA) is the most common form of bone cancer diagnosticated in dogs and is highly metastatic. There has been limited advancement in discovering an effective treatment for OSA in the last few decades. The major drawback of the currently used chemotherapeutic drugs is their side effects. In this preliminary study, we investigated the efficacy of using a novel food-derived drug, phloridzin docosahexaenoate (PZ-DHA), in the treatment of canine OSA in vitro. PZ-DHA was selectively cytotoxic to canine OSA D17 cells, while normal human liver cells (WRL68) were more resistant. We also found that PZ-DHA had enhanced cellular uptake in D17 cells compared to its precursors and in WRL68 cell line. This study provides preliminary evidence that PZ-DHA needs to be further assessed as a safe and efficacious new drug in the treatment of both canine and human OSA.

Somatomedin activity measured as sulphation factor in culture media from normal human liver and connective tissues explants. Effects of human growth hormone

1981 ◽  
Vol 98 (1) ◽  
pp. 24-28 ◽  
Author(s):  
R. M. Schimpff ◽  
M. Donnadieu ◽  
M. Gautier ◽  
G. Polini ◽  
A. M. Repellin
Keyword(s):  
Growth Hormone ◽  
Human Growth Hormone ◽  
Culture Media ◽  
Human Growth ◽  
Connective Tissues ◽  
Normal Human Liver ◽  
Normal Human ◽  
Higher Doses ◽  
Human Explants

Abstract. Normal human explants from liver and from connective tissues (aponeurosis or skin) incubated in vitro released sulphation activity measurable in chick embryo cartilage. Addition of human Growth Hormone (hGH) at physiological levels (10 ng/ml) increased the sulphation activity after 6 hours incubation time. Higher doses failed to increase the sulphation activity produced by connective tissues and decreased the sulphation activity produced by the liver.

scholarly journals Regulation of Microcystin-LR-Induced DNA Damage by miR-451a in HL7702 Cells

Toxins ◽  
2019 ◽  
Vol 11 (3) ◽  
pp. 164 ◽  
Author(s):  
Lv Chen ◽  
Shu Yang ◽  
Cong Wen ◽  
Shuilin Zheng ◽  
Yue Yang ◽  
...  
Keyword(s):  
Dna Damage ◽  
Human Liver ◽  
Expression Level ◽  
Tail Moment ◽  
Protein Expression Level ◽  
Over Expression ◽  
Human Liver Cells ◽  
Normal Human Liver ◽  
Normal Human ◽  
Cyclic Heptapeptide

Microcystin-LR is a cyclic heptapeptide hepatotoxin produced by harmful cyanobacteria. A panel of microRNAs containing miR-451a were found to be significantly changed in normal human liver cells HL7702 after exposure to microcystin-LR (MC-LR) in our previous study. However, the functions of miR-451a in hepatotoxicity induced by MC-LR remained unclear. The study aimed to investigate the impacts of miR-451a in HL7702 cells following treatment with 5 or 10 μM MC-LR. The comet assay indicated that MC-LR can influence Olive tail moment (OTM) in HL7702 cells. Furthermore, increase of miR-451a significantly repressed DNA damage and the protein expression level of γ-H2AX induced by MC-LR. Moreover, over-expression of miR-451a inhibited the expression level of p-AKT1 protein in cells following treatment by MC-LR. These results showed that miR-451a may protect from MC-LR-induced DNA damage by down-regulating the expression of p-AKT1, which provides new clues for the diagnosis and therapy policies for liver damage induced by MC-LR.

Histone demethylase JHDM2A regulates H3K9 dimethylation in response to arsenic‐induced DNA damage and repair in normal human liver cells

2020 ◽  
Vol 40 (12) ◽  
pp. 1661-1672
Author(s):  
An‐liu Zhang ◽  
Shun‐fang Tang ◽  
Yue Yang ◽  
Chang‐zhe Li ◽  
Xue‐jiao Ding ◽  
...  
Keyword(s):  
Dna Damage ◽  
Human Liver ◽  
Liver Cells ◽  
Histone Demethylase ◽  
Dna Damage And Repair ◽  
Human Liver Cells ◽  
Normal Human Liver ◽  
Normal Human ◽  
H3k9 Dimethylation

Ru(III) complexes of pyrazolopyrimidines as anticancer agents: In vitro, in vivo anticancer activity and underlying multi-mechanisms

2022 ◽  
Author(s):  
Yunqiong Gu ◽  
Wen-Ying Shen ◽  
Qi-Yuan Yang ◽  
Zhen-Feng Chen ◽  
Hong Liang
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Anticancer Agents ◽  
Human Liver ◽  
Normal Human Liver ◽  
Normal Human ◽  
Low Toxicity

Three ruthenium(III) complexes with pyrazolopyrimidine [Ru(Ln)(H2O)Cl3] (13, n=13) were prepared and characterized. These Ru(III) compounds show strong cytotoxicity against six cancer cell lines and low toxicity to normal human liver...

Synthesis, cytotoxicity and in silico study of some novel benzocoumarin-chalcone-bearing aryl ester derivatives and benzocoumarin-derived arylamide analogs

2021 ◽  
Vol 76 (3-4) ◽  
pp. 201-210
Author(s):  
Nabeel A. Abdul-Ridha ◽  
Afraah D. Salmaan ◽  
Rita Sabah ◽  
Bahjat Saeed ◽  
Najim A. Al-Masoudi
Keyword(s):  
Prostate Cancer ◽  
Cell Lines ◽  
Human Liver ◽  
Hydrophobic Interactions ◽  
Cytotoxic Agents ◽  
Cytotoxic Activities ◽  
Protein Receptor ◽  
Normal Human Liver ◽  
Normal Human

Abstract The development of new prostate cancer protein receptor cytochrome P450 17A1 inhibitors offers the possibility of generating structures of increased potency. To this end, the chalcone analogs 7 and 8 were prepared from treatment of methyl 3-oxo-3H-benzocoumarin-2-carboxylate (4) with aryl aldehydes. Treatment of 7 and 8 with three anti-inflammatory drugs, flurbiprofen, ketoprofen and ibuprofen, in the presence of POCl3/DMAP gave the ester analogs 9–12. Analogously, treatment of ethyl 3-oxo-3H-benzocoumarin-2-carboxylate (15), prepared previously from 2-hydroxy-1-naphthaldehyde (13) and dimethylmalonate (14), with various arylamines: 4-bromoaniline, 2-amino-6-methylpyridine, amino-antipyrine and 2-amino-5-nitrothiazole, in the presence of potassium tert-butoxide gave the benzocoumarine-3-arylamide analogs. The in vitro cytotoxic activities of 9–12 and 16–19 were evaluated against human prostate cancer cell lines (PC-3) and normal human liver epithelia (WRL-68) by MTT assay. Compounds 10 and 17 were the most active cytotoxic agents among the series against PC-3 cells with IC50 values of 71.35 and 78.25 μg mL–1 with SI values of 3.0 and 4.2, respectively (calculated from the cytotoxicity effects of 10 and 17 on the normal human liver epithelia [WRL-68]). Furthermore, compounds 11 and 12 were tested against breast cancer (HER2 cell lines), prostate cancer (DU-135 cell lines) and MCF-7 but were inactive. Molecular docking studies between the protein receptor CYPP450 17A1 and compounds 10 and 17 revealed that these compounds primarily form hydrophobic interactions with the receptor.

scholarly journals Histone demethylase JHDM2A regulates H3K9 dimethylation in response to arsenic‐induced DNA damage and repair in normal human liver cells

2021 ◽  
Vol 41 (4) ◽  
pp. 650-650
Author(s):  
An‐liu Zhang ◽  
Shun‐fang Tang ◽  
Yue Yang ◽  
Chang‐zhe Li ◽  
Xue‐jiao Ding ◽  
...  
Keyword(s):  
Dna Damage ◽  
Human Liver ◽  
Liver Cells ◽  
Histone Demethylase ◽  
Dna Damage And Repair ◽  
Human Liver Cells ◽  
Normal Human Liver ◽  
Normal Human ◽  
H3k9 Dimethylation

Effect of l-alanine infusion on 31P nuclear magnetic resonance spectra of normal human liver: towards biochemical pathology in vivo

1992 ◽  
Vol 83 (2) ◽  
pp. 183-190 ◽  
Author(s):  
P. C. Dagnelie ◽  
D. K. Menon ◽  
I. J. Cox ◽  
J. D. Bell ◽  
J. Sargentoni ◽  
...  
Keyword(s):  
Body Weight ◽  
Human Liver ◽  
Pulse Sequence ◽  
Whole Body ◽  
Maximal Increase ◽  
Normal Human Liver ◽  
Normal Human ◽  
Biochemical Pathology

1. 31P n.m.r. spectroscopy in vivo was used to study the effect of l-alanine infusion on the concentrations of gluconeogenic intermediates in normal human liver. Studies were performed in six healthy male subjects (34–44 years, fasted overnight) using a chemical shift imaging pulse sequence on a whole-body n.m.r. system operating at 1.6T. Hepatic 31P n.m.r. spectra were obtained from 10 min before to 70 min after intravenous administration of 0.70 (n = 2), 1.40 (n = 3) or 2.80 (n = 5) nmol of l-alanine/kg body weight over 4.5 min. Concentrations of phosphomonoesters, Pi and phosphodiesters relative to ATP were calculated from peak areas in the n.m.r. spectra, using the β-ATP peak as a reference. 2. Dose-dependent spectral changes were observed for [phosphomonoesters]/[ATP] and [Pi]/[ATP]. At the highest dose given, maximal changes in [phosphomonoesters]/[ATP] (mean ± sem: 98 ± 12%, P<0.005) and [Pi]/[ATP] (−33 ± 3%, P<0.001) were observed approximately 45 min after the l-alanine infusion. [Phosphodiesters]/[ATP] showed a maximal increase of 24 ± 6% (P<0.05), which was independent of the l-alanine dose. Hepatic ATP levels and pH did not change. 3. To identify the metabolites responsible for the changes observed in vivo, male Wistar rats were infused with 11.2 mmol of l-alanine/kg body weight. After 15 min, livers were freeze-clamped and were extracted according to standard procedures. In vitro, 31P n.m.r. spectra obtained at 8.4 or 11.7 T revealed sharp increases in the concentrations of 3-phosphoglycerate and phosphoenolpyruvate after l-alanine infusion. No significant increases in other metabolites contributing to the phosphomonoester or phosphodiester resonances in vivo were observed, suggesting that the rise in [phosphomonoesters] observed in vivo was caused by increasing concentrations of 3-phosphoglycerate, and that phosphoenolpyruvate contributed to the rise in [phosphodiesters]. 5. These results show that l-alanine infusion leads to consistent changes in the 31P n.m.r. spectra of the human liver owing to increased concentrations of gluconeogenic intermediates. The ‘n.m.r.-alanine test’ may constitute a useful tool for studies of gluconeogenesis and hepatic biochemical pathology in vivo.

scholarly journals Effect of fumonisin B1 on the cell cycle of normal human liver cells

2013 ◽  
Vol 7 (6) ◽  
pp. 1970-1976 ◽  
Author(s):  
SHAO-KANG WANG ◽  
SHA LIU ◽  
LI-GANG YANG ◽  
RUO-FU SHI ◽  
GUI-JU SUN
Keyword(s):  
Cell Cycle ◽  
Human Liver ◽  
Fumonisin B1 ◽  
Liver Cells ◽  
Human Liver Cells ◽  
Normal Human Liver ◽  
Normal Human
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