Curcumin analogues as possible anti-proliferative & anti-inflammatory agents (Journal article)

Katsori, A. M./ Chatzopoulou, M./ Dimas, K./ Kontogiorgis, C./ Patsilinakos, A./ Trangas, T./ Hadjipavlou-Litina, D.

A series of novel curcumin analogues has been designed, synthesized and tested in vitro/in vivo as potential multi-target agents. Their anti-proliferative and anti-inflammatory activities were studied. Compounds 1b and 2b were stronger inhibitors of soybean lipoxygenase (LOX) than curcumin. Analogue 1b was also the most potent aldose reductase (ALR2) inhibitor. Two compounds, (1a and 1f) exhibited in vivo anti-inflammatory activity comparable to that of indomethacin, whereas derivative 1i exhibited even higher activity. The derivatives were also tested for their anti-proliferative activity using three different human cancer cell lines. Compounds 1a, 1b, 1d and 2b exhibited significant growth inhibitory activity as compared to curcumin, against all three cancer cell lines. Lipophilicity was determined as R(M) values using RPTLC and theoretically. The results are discussed in terms of the structural characteristics of the compounds. Docking simulations were performed on LOX and ALR2 inhibitor 1b and curcumin. Compound 1b is well fitted in the active site of ALR2, binding to the ALR2 enzyme in a similar way to curcumin. Allosteric interactions may govern the LOX-inhibitor binding.
Institution and School/Department of submitter: Πανεπιστήμιο Ιωαννίνων. Σχολή Επιστημών και Τεχνολογιών. Τμήμα Βιολογικών Εφαρμογών και Τεχνολογιών
URI: https://olympias.lib.uoi.gr/jspui/handle/123456789/7825
ISSN: 1768-3254
Link: http://www.ncbi.nlm.nih.gov/pubmed/21514701
http://ac.els-cdn.com/S0223523411002777/1-s2.0-S0223523411002777-main.pdf?_tid=6fdaaa63c6a839112d2522e24b01a3dc&acdnat=1337154834_0963cd21408af497e6375c9bbbd1a369
Appears in Collections:Άρθρα σε επιστημονικά περιοδικά ( Ανοικτά)

Files in This Item:
File Description SizeFormat 
Katsori-2011-Curcumin analogues a.pdf1.65 MBAdobe PDFView/Open    Request a copy


 Please use this identifier to cite or link to this item:
https://olympias.lib.uoi.gr/jspui/handle/123456789/7825
  This item is a favorite for 0 people.

Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.