title: Cytotoxic evaluation of sarcodifurines A and B, two novel dihydrofuroquinolines from Sarcomelicope follicularis (Rutaceae).
abstract: 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.
authors.affiliation: 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
authors.forename: Elizabeth
authors.initials: E
authors.lastname: Chosson
authors.forename: Christiane
authors.initials: C
authors.lastname: Guguen-Guillouzo
authors.forename: Denise
authors.initials: D
authors.lastname: Glaise
authors.forename: Laurent
authors.initials: L
authors.lastname: Picot
authors.forename: Elisabeth
authors.initials: E
authors.lastname: Seguin
authors.forename: Thierry
authors.initials: T
authors.lastname: Besson
mesh_terms: 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
chemical_list: D005663:Furans; D007364:Intercalating Agents; D011804:Quinolines; D059003:Topoisomerase Inhibitors; C534056:sarcodifurine A; C534057:sarcodifurine B