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SUMMARY:Bismuth-NSAIDs as colorectal cancer chemopreventives
DTSTART;VALUE=DATE-TIME:20181120T005000Z
DTEND;VALUE=DATE-TIME:20181120T011000Z
DTSTAMP;VALUE=DATE-TIME:20260711T055708Z
UID:indico-contribution-2588@events01.synchrotron.org.au
DESCRIPTION:Speakers: Tara Brown (University of Wolloongong)\nTo date\, ep
 idemiological studies\, animal studies and clinical trials have indicated 
 the potential of non-steroidal anti-inflammatory drugs (NSAIDs) for the ch
 emoprevention of colorectal cancer (CRC) [1]. Unfortunately\, the use of N
 SAIDs for CRC chemoprevention is significantly limited due to the severe g
 astrointestinal (GI) side effects that have been associated with their lon
 g term use [1]. It is hypothesised that the coordination of NSAIDs to bism
 uth\, a heavy metal with proven gastrointestinal sparing properties [2]\, 
 may allow the use of NSAIDs as chemopreventives for CRC while also combati
 ng their associated GI side effects. The present study investigates the in
 teractions of bismuth-coordinated NSAIDs (BiNSAIDs) with eukaryotic membra
 ne mimics with the aim of establishing the possible uptake mechanisms of t
 hese compounds. This knowledge will be extended by investigating the behav
 iour of BiNSAIDs in more complex systems\, including CRC cells and a CRC a
 nimal model.\n\nQCM-D studies involving biological membrane mimics compose
 d of POPC or POPC/cholesterol demonstrated that BiNSAIDs and their parent 
 NSAIDs interact with biological membranes [3]. Neutron reflectometry was a
 lso used to study the membrane interactions of BiNSAIDs and provided furth
 er evidence of the membrane interactions of BiNSAIDs\, suggesting that pas
 sive diffusion is a likely method of uptake of these compounds [3]. These 
 strength of these membrane interactions was an indicator of BiNSAID cytoto
 xicity against CRC cells.3 A CRC animal study has recently been completed 
 with aspirin\, which has promising preliminary results. In conclusion\, th
 e aforementioned studies continue to highlight the potential of BiNSAIDs a
 s candidates for further investigations into their potential for the chemo
 prevention of CRC. \n\nReferences\n1. M. J. Thun\, S. J. Henley\, C. Patro
 no\, “Nonsteroidal Anti-inflammatory Drugs as Anticancer Agents: Mechani
 stic\, Pharmacologic\, and Clinical Issues”\, J. Natl. Cancer Inst.\, 94
 \, 252-266 (2002)\n2. P. J. Sadler\, H. Li\, H. Sun\, “Coordination chem
 istry of metals in medicine: target sites for bismuth”\, Coord. Chem. Re
 v.\, 185-186\, 689-709 (1999)\n3. T. Brown\, “Bismuth-NSAIDs as colorect
 al cancer chemopreventives: Insights into their membrane interactions and 
 uptake mechanisms”\, Bachelor of Medicinal Chemistry Advanced (Honours) 
 Dissertation\, University of Wollongong\, (2016)\n\nhttps://events01.synch
 rotron.org.au/event/84/contributions/2588/
LOCATION:AINSE Conference Centre New Illawarra Road Lucas Heights NSW 2234
  Australia
URL:https://events01.synchrotron.org.au/event/84/contributions/2588/
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