Cytotoxic evaluation of sarcodifurines A and B, two novel dihydrofuroquinolines from Sarcomelicope follicularis (Rutaceae).
Sarcodifurines A and B are two original dihydrofuroquinolines isolated from Sarcomelicope follicularis, a New Caledonian tree. The cytotoxicity and antiproliferative activity of these two alkaloids were investigated against 8 distinct cell lines representative of the most frequent solid tumors developing in human. Cytotoxicity of sarcodifurines was low on the 8 cell lines, with, for example, less than 10% of the total cells killed after 24 h exposure at 10 microM and IC(50) approximately 7.10(-5) M (MCF-7 and MDA MB 231 cell lines). Proliferation studies confirmed that sarcodifurines had a weak effect on cancer cells growth, with less than 5% growth inhibition at 10 microM. Sarcodifurine A activity was comparable to that of Sarcodifurine B, in term of cytotoxicity and antiproliferative activity on all cell lines. In spite of the weak activity of sarcodifurines and furoquinolines, rationalized pharmacomodulations to obtain planar analogs could lead to efficient topoisomerases inhibitors and DNA intercalants.
Chosson
Elizabeth
E
Université de Rouen, CNRS UMR 6014, C.O.B.R.A. - I.R.C.O.F., UFR Méédecine-Pharmacie, Rouen Cedex 1, France. elizabeth.chosson@univ-rouen.fr
Guguen-Guillouzo
Christiane
C
Glaise
Denise
D
Picot
Laurent
L
Seguin
Elisabeth
E
Besson
Thierry
T
D016923:Cell Death / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D005663:Furans / Q000302:isolation & purification / Q000494:pharmacology*; D006801:Humans; D007364:Intercalating Agents; D011804:Quinolines / Q000302:isolation & purification / Q000494:pharmacology*; D027821:Rutaceae / Q000737:chemistry*; D059003:Topoisomerase Inhibitors
D005663:Furans; D007364:Intercalating Agents; D011804:Quinolines; D059003:Topoisomerase Inhibitors; C534056:sarcodifurine A; C534057:sarcodifurine B