title: Antitrypanosomal quinoline alkaloids from the roots of Waltheria indica.
abstract: Chemical investigation of the dichloromethane root extract of Waltheria indica led to the isolation and characterization of 10 quinoline alkaloids, namely, 8-deoxoantidesmone (1), waltheriones E-L (2-9), and antidesmone (10). Among these, compounds 2-9 have not yet been described in the literature. Their chemical structures were established by means of spectroscopic data interpretation including (1)H and (13)C NMR, HSQC, HMBC, COSY, and NOESY experiments and UV, IR, and HRESIMS. The absolute configurations of the compounds were established by comparison of experimental and TDDFT-calculated ECD spectra. In addition, the isolated constituents were evaluated for their in vitro antitrypanosomal activity. Compounds 4, 5, and 8 showed potent and selective growth inhibition toward Trypanosoma cruzi with IC50 values between 0.02 and 0.04 μM. Cytotoxicity for mouse skeletal L-6 cells was also determined for these compounds.
authors.affiliation: School of Pharmaceutical Sciences, University of Geneva, University of Lausanne , Quai Ernest-Ansermet 30, 1211 Geneva 4, Switzerland.
authors.forename: Sylvian
authors.initials: S
authors.lastname: Cretton
authors.forename: Lise
authors.initials: L
authors.lastname: Breant
authors.forename: Lucie
authors.initials: L
authors.lastname: Pourrez
authors.forename: Chiara
authors.initials: C
authors.lastname: Ambuehl
authors.forename: Laurence
authors.initials: L
authors.lastname: Marcourt
authors.forename: Samad Nejad
authors.initials: SN
authors.lastname: Ebrahimi
authors.forename: Matthias
authors.initials: M
authors.lastname: Hamburger
authors.forename: Remo
authors.initials: R
authors.lastname: Perozzo
authors.forename: Soumana
authors.initials: S
authors.lastname: Karimou
authors.forename: Marcel
authors.initials: M
authors.lastname: Kaiser
authors.forename: Muriel
authors.initials: M
authors.lastname: Cuendet
authors.forename: Philippe
authors.initials: P
authors.lastname: Christen
mesh_terms: D000470:Alkaloids / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D000818:Animals; D020128:Inhibitory Concentration 50; D019660:Malvaceae / Q000737:chemistry*; D051379:Mice; D015394:Molecular Structure; D009548:Niger; D019906:Nuclear Magnetic Resonance, Biomolecular; D018517:Plant Roots / Q000737:chemistry; D011804:Quinolines / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D014344:Trypanocidal Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D014345:Trypanosoma / Q000187:drug effects*
chemical_list: D000470:Alkaloids; D011804:Quinolines; D014344:Trypanocidal Agents