scholarly journals Quantitative Structure-Activity Relationship Study of Curcumin Analogues as Anti-proliferative Agents of Human Prostate Cancer Cell Line (PC-3)

KIMIKA ◽  
2013 ◽  
Vol 24 (1) ◽  
pp. 8-17
Author(s):  
Andrea Marie M. Reyes ◽  
Junie B. Billones

A quantitative structure-activity relationship (QSAR) study has been performed on curcumin analogues in order to establish the effect of variation of structural, electronic and topological properties  on  the  anti-proliferative  activity  against  prostate  cancer  cell  line  PC-3.  The structure-based  properties  were  calculated  by  the  use  of  Hyperchem®  and  Dragon® softwares  and  the  multi-linear  regression  equations  were  generated  by  the  use  of  SPSS® software. Six models of PC-3 activity have been developed according to the types of QSAR descriptors.  All  models  were  cross-validated  using  leave-one-out  (LOO)  method.  The models  indicate  that  a  more  potent  curcumin  derivative  against  PC-3  should  have  smaller surface area, greater volume, lower polarizability, and fewer oxygen and multiple bonds.

2020 ◽  
Vol 45 (4) ◽  
pp. 423-428
Author(s):  
Ali Mert Özgönül ◽  
Aycan Aşık ◽  
Burak Durmaz ◽  
Ramin Aslaminabad ◽  
Cumhur Gündüz ◽  
...  

AbstractObjectivesRecently, phenolic compounds (quercetin, kaempferol, ellagic acid (EA), and myricetin) as natural sources have been suggested to be used for treatment and chemoprevention of prostate cancer. Since rosehip includes the above molecules in high concentration, we set out to investigate possible anti-proliferative effect of rosehip tea on the prostate cancer cell line.MethodsThe flavonol content of rosehip tea prepared at different temperatures and time intervals was determined first and then the antiproliferative effect of tea samples was established by adding tea samples to the prostate cancer cell line (VCaP and LNCaP).ResultsQuercetin was more effective in LNCaP cell than in VCaP cell (IC50 = 20 and 200 μM, respectively). The boiled fruit shredded at minute 7 showed the highest levels of quercetin, EA and kaempferol and the boiled fruit at minute 7 had the highest levels of kaempferol and EA. The tea samples were prepared in concentrations relevant to their IC50 values, added to the VCaP and LNCaP cell lines. The antiproliferative effect of rosehip tea on VCaP cells was slightly greater than that of LNCaP cells.ConclusionEach of the flavonols exhibits an antiproliferative effect. Our data clearly indicated that rosehip as a natural source of all flavonols had an antiproliferative effect on androgen-sensitive prostate cancer. Now that it is important to use natural sources in cancer, rosehip seems to be a promising natural product to be used to treat the prostate illness.


2007 ◽  
Vol 101 (3) ◽  
pp. 631-641 ◽  
Author(s):  
S. Koochekpour ◽  
T.-J. Lee ◽  
R. Wang ◽  
Y. Sun ◽  
N. Delorme ◽  
...  

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