Antiproliferative activity of long chain acylated esters of quercetin-3-O-glucoside in hepatocellular carcinoma HepG2 cells
| Autor: | H.P. Vasantha Rupasinghe, Sudhanshu Sudan |
|---|---|
| Jazyk: | angličtina |
| Rok vydání: | 2015 |
| Předmět: |
Sorafenib
Niacinamide Carcinoma Hepatocellular Antineoplastic Agents Apoptosis DNA Fragmentation General Biochemistry Genetics and Molecular Biology chemistry.chemical_compound Glucosides medicine Humans Original Research Cell Proliferation chemistry.chemical_classification Cisplatin Flavonoids Caspase 3 Phenylurea Compounds Cell Cycle Fatty Acids Liver Neoplasms Fatty acid Esters Hep G2 Cells Cell cycle Oleic acid DNA Topoisomerases Type II Biochemistry chemistry Microscopy Fluorescence DNA fragmentation Quercetin Long chain fatty acid Drug Screening Assays Antitumor medicine.drug |
| Popis: | Despite their strong role in human health, poor bioavailability of flavonoids limits their biological effects in vivo. Enzymatically catalyzed acylation of fatty acids to flavonoids is one of the approaches of increasing cellular permeability and hence, biological activities. In this study, six long chain fatty acid esters of quercetin-3- O-glucoside (Q3G) acylated enzymatically and were used for determining their antiproliferative action in hepatocellular carcinoma cells (HepG2) in comparison to precursor compounds and two chemotherapy drugs (Sorafenib and Cisplatin). Fatty acid esters of Q3G showed significant inhibition of HepG2 cell proliferation by 85 to 90% after 6 h and 24 h of treatment, respectively. The cell death due to these novel compounds was associated with cell-cycle arrest in S-phase and apoptosis observed by DNA fragmentation, fluorescent microscopy and elevated caspase-3 activity and strong DNA topoisomerase II inhibition. Interestingly, Q3G esters showed significantly low toxicity to normal liver cells than Sorafenib ( P |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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