title: Antitrypanosomal sesquiterpene lactones from Saussurea costus.
abstract: In the course of a larger screen of 1800 plant and fungal extracts, the ethyl acetate extract of Saussurea costus roots potently inhibited the growth of Trypanosoma brucei rhodesiense. Subsequent HPLC based activity profiling led to the identification of the sesquiterpene lactones arbusculin B (1), α-cyclocostunolide (2), costunolide (3), and dehydrocostuslactone (4). They were tested for in vitro antitrypanosomal activities and cytotoxicity alongside the structurally related sesquiterpene lactones parthenolide (5), zaluzanin D (6), and eupatoriopicrin (7), and had IC(50)s between 0.8 and 22 μM. Cytotoxic IC(50)s were from 1.6 to 19 μM, and selectivity indices from 0.5 to 6.5.
authors.affiliation: Division of Pharmaceutical Biology, University of Basel, CH-4056 Basel, Switzerland.
authors.forename: Tasqiah
authors.initials: T
authors.lastname: Julianti
authors.forename: Yoshie
authors.initials: Y
authors.lastname: Hata
authors.forename: Stefanie
authors.initials: S
authors.lastname: Zimmermann
authors.forename: Marcel
authors.initials: M
authors.lastname: Kaiser
authors.forename: Matthias
authors.initials: M
authors.lastname: Hamburger
authors.forename: Michael
authors.initials: M
authors.lastname: Adams
mesh_terms: D000818:Animals; D002851:Chromatography, High Pressure Liquid; D003603:Cytotoxins / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D007783:Lactones / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D032446:Myoblasts / Q000187:drug effects*; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology*; D018517:Plant Roots; D051381:Rats; D030441:Saussurea / Q000737:chemistry*; D012717:Sesquiterpenes / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D014344:Trypanocidal Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D016833:Trypanosoma brucei rhodesiense / Q000187:drug effects
chemical_list: D003603:Cytotoxins; D007783:Lactones; D010936:Plant Extracts; D012717:Sesquiterpenes; D014344:Trypanocidal Agents