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1.
J Oleo Sci ; 71(7): 959-974, 2022 Jul 01.
Article de Anglais | MEDLINE | ID: mdl-35691838

RÉSUMÉ

Pulsed electric field (PEF) is a nonthermal technology resulting in the rupture of cell membranes and increasing the electrical conductivity and the permeability of intracellular material. There was little work about the safety of food treated by PEF. The acute, subacute oral, and genetic toxicities were investigated to explore the safety of canola oil extracted by aid of PEF treatment (PTCO). The results showed that no negative consequences were caused by PEF. PTCO was regarded as practically non-toxic with a LD50 higher than 40 g/kg bw. No oil intake-related mortality, clinical, weight gain and organ coefficient abnormalities were observed. The histopathological symptoms indicated a mild load but not obvious toxicities on liver and kidney. The 28-day subacute toxicity test confirmed that less than 10 g/kg·d bw of oil intake did not exhibit any intake-related changes in physical, physiological, biochemical, hematological, and histopathological signs. The less than 4 of atherosclerosis index suggested that no risk of cardiovascular disease caused by PTCO intake. It was speculated that the PEF treatment would not cause any safety issues to food products.


Sujet(s)
Électricité , Foie , Conductivité électrique , Rein , Huile de colza
2.
Eur J Med Chem ; 145: 498-510, 2018 Feb 10.
Article de Anglais | MEDLINE | ID: mdl-29335211

RÉSUMÉ

Novel topoisomerase II (Topo II) inhibitors have gained considerable interest for the development of anticancer agents. In this study, a series of carbazole derivatives containing chalcone analogs (CDCAs) were synthesized and investigated for their Topo II inhibition and cytotoxic activities. The results from Topo II mediated DNA relaxation assay showed that CDCAs could significantly inhibit the activity of Topo II, and the structure-activity relationship indicated the halogen substituent in phenyl ring play an important role in the activity. Further mechanism studies revealed that CDCAs function as non-intercalative Topo II catalytic inhibitors. Moreover, some CDCAs showed micromolar cytotoxic activities. The most potent compound 3h exhibited notable growth inhibition against four human cancer cell lines. Flow cytometric analysis revealed that compounds 3d and 3h arrested the HL-60 cells in sub G1 phase by induction of apoptosis. It was further confirmed by Annexin-V-FITC binding assay. Western blot analysis revealed that compound 3h induces apoptosis likely through the activation of caspase proteins.


Sujet(s)
Antinéoplasiques/pharmacologie , Apoptose/effets des médicaments et des substances chimiques , Carbazoles/pharmacologie , Chalcone/pharmacologie , ADN topoisomérases de type II/métabolisme , Inhibiteurs de la topoisomérase-II/pharmacologie , Antinéoplasiques/synthèse chimique , Antinéoplasiques/composition chimique , Biocatalyse , Carbazoles/synthèse chimique , Carbazoles/composition chimique , Points de contrôle du cycle cellulaire/effets des médicaments et des substances chimiques , Prolifération cellulaire/effets des médicaments et des substances chimiques , Chalcone/composition chimique , Clivage de l'ADN/effets des médicaments et des substances chimiques , Relation dose-effet des médicaments , Tests de criblage d'agents antitumoraux , Cellules HL-60 , Humains , Structure moléculaire , Plasmides , Relation structure-activité , Inhibiteurs de la topoisomérase-II/synthèse chimique , Inhibiteurs de la topoisomérase-II/composition chimique
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