Antiproliferative Potential of Gloriosine: A Lead for Anticancer Drug Development.
Bharat GoelBiswajit DeyEssha ChatterjeeNancy TripathiNivedita BhardwajSanjay KumarSantosh Kumar GuruShreyans K JainPublished in: ACS omega (2022)
Gloriosine, a colchicine-like natural product, is widely obtained from Gloriosa superba roots. Despite having remarkable anticancer potential, colchicine could not pave its way to the clinic, while gloriosine is yet to be investigated for its pharmacological effects. In the present work, 14 compounds, including gloriosine, were isolated from the G. superba roots and were characterized by NMR spectroscopy. Gloriosine ( 11 ) was evaluated for its antiproliferative activity against a panel of 15 human cancer cell lines of different tissues and normal breast cells. Gloroisine ( 11 ) displayed significant antiproliferative activity against various cancer cell lines selectively, with IC 50 values ranging from 32.61 to 100.28 nM. Further, gloriosine ( 11 ) was investigated for its apoptosis-inducing ability and found to form apoptotic bodies. It also inhibited A549 cell migration in the wound healing assay. Finally, molecular docking studies were performed to explore the possible binding modes of gloriosine with the colchicine-binding site of tubulin protein. Our findings suggested that gloriosine might be a potential lead for anticancer drug discovery.
Keyphrases
- molecular docking
- cell migration
- papillary thyroid
- drug discovery
- cell cycle arrest
- cell death
- induced apoptosis
- squamous cell
- endothelial cells
- oxidative stress
- endoplasmic reticulum stress
- molecular dynamics simulations
- gene expression
- primary care
- human health
- cell proliferation
- lymph node metastasis
- small molecule
- mass spectrometry
- childhood cancer
- young adults
- protein protein
- single molecule
- pluripotent stem cells
- cell wall