In:
Tropical Journal of Pharmaceutical Research, African Journals Online (AJOL), Vol. 19, No. 12 ( 2021-03-12), p. 2483-2489
Abstract:
Purpose: To investigate the effect of excisanin A on human hepatocellular carcinoma cells as well as to elucidate its mechanism of action. Methods: Molecular docking was used to determine the binding characteristics of excisanin A to HIF-1α protein. The transcriptional activation and viability of excisanin A were assessed using Luciferase reporter and MTT assay. The HIF-1α protein in the nucleus was assayed using western blot and immunofluorescence. HIF-1α and VEGF mRNA levels were evaluated using reverse-transcription polymerase chain reaction (RT-PCR). Cell proliferation was determined by flow cytometry, as well as by EdU and clonogenic assays. In vivo tumor growth was assessed in a murine xenograft model of SKHep1 cells. Results: Excisanin A inhibited HIF-1α transcriptional activation, as well as HIF-1α protein synthesis (p 〈 0.001). Excisanin A also reduced VEGF protein and mRNA expressions (p 〈 0.001). In addition, the compound inhibited the proliferation of hepatocellular carcinoma cells. and tumor growth in the xenograft tumor model. Conclusion: Excisanin A is a potent HIF-1α inhibitor, supporting its potential development for human hepatoma therapy. Keywords: Excisanin A, HIF-1α, Protein synthesis, Hepatoma therapy
Type of Medium:
Online Resource
ISSN:
1596-9827
,
1596-5996
DOI:
10.4314/tjpr.v19i12.1
Language:
Unknown
Publisher:
African Journals Online (AJOL)
Publication Date:
2021
detail.hit.zdb_id:
2125881-8
SSG:
15,3
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