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Full-Text Articles in Natural Products Chemistry and Pharmacognosy
The Effects Of Apigenin On Cell Proliferation And Apoptosis In Glioblastoma Multiforme, Trevor Stump, Brittany Santee, Lauren Williams, Chelsae Heinze, Rachel Kunze, Samson Amos, Denise S. Simpson
The Effects Of Apigenin On Cell Proliferation And Apoptosis In Glioblastoma Multiforme, Trevor Stump, Brittany Santee, Lauren Williams, Chelsae Heinze, Rachel Kunze, Samson Amos, Denise S. Simpson
The Research and Scholarship Symposium (2013-2019)
Glioblastoma multiforme (GBM) is a WHO grade IV brain tumor. These tumors are highly proliferative, infiltrative, necrotic, angiogenic, and resistant to apoptosis. One major characteristic of GBM is the overexpression of epidermal growth factor receptor (EGFR), which leads to cell growth and proliferation when activated. GBM is very difficult to treat due to its location, heterogeneity, and invasiveness; an effective treatment is therefore needed. The use of flavonoids, which are natural compounds found in many fruits and vegetables, has been studied in the treatment of many different tumor types. Apigenin is a specific flavonoid that has previously been shown to …
Piperlongumine (Piplartine) And Analogues: Antiproliferative Microtubule-Destabilising Agents, Mary J. Meegan, Seema M. Nathwani, Brendan Twamley, Daniela M. Zisterer, Niamh O'Boyle
Piperlongumine (Piplartine) And Analogues: Antiproliferative Microtubule-Destabilising Agents, Mary J. Meegan, Seema M. Nathwani, Brendan Twamley, Daniela M. Zisterer, Niamh O'Boyle
Articles
Piperlongumine (piplartine, 1) is a small molecule alkaloid that is receiving intense interest due to its antiproliferative and anticancer activities. We investigated the effects of 1 on tubulin and microtubules. Using both an isolated tubulin assay, and a combination of sedimentation and Western blotting, we demonstrated that 1 is a tubulin-destabilising agent. This result was confirmed by immunofluorescence and confocal microscopy, which showed that microtubules in MCF-7 breast cancer cells were depolymerised when treated with 1. We synthesised a number of analogues of 1 to explore structure-activity relationships. Compound 13 had the best cytotoxic profile of this series, …