title: Further in vitro evaluation of cytotoxicity of the marine natural product derivative 4'-leucine-avarone.
abstract: The cytotoxicity of 4'-leucine-avarone, amino derivative of the sponge Dysidea avara secondary metabolite avarone, was evaluated by 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyl tetrazolium bromide assay in vitro against seven human solid tumours for the first time. The compound tested induced dose-dependent cytotoxic response in all cancer cells showing better activity towards the lung A-549 and colon HT-29 cell lines (IC50 7.40 μM and 9.62 μM, respectively) than towards the breast adenocarcinoma ER positive MCF-7 and ER negative MDA-MB-231 cells (IC50 11.64 μM and 17.31 μM, respectively), the prostate adenocarcinoma PC-3 and epiteloid cervix carcinoma HeLa cells (IC50 14.24 μM and 15.54 μM, respectively). No toxicity was found towards the foetal lung fibroblast MRC-5 cell line at the concentrations used. According to experimental data obtained, the sesquiterpenoid quinone structure of avarone may inspire development of new drug-like substances with improved cytotoxicity on lung cancer in humans.
authors.affiliation: a National Research Council of Italy, Institute of Biomolecular Chemistry, CNR-ICB , Pozzuoli-Naples , Italy.
authors.forename: Boris
authors.initials: B
authors.lastname: Pejin
authors.forename: Carmine
authors.initials: C
authors.lastname: Iodice
authors.forename: Giuseppina
authors.initials: G
authors.lastname: Tommonaro
authors.forename: Gordana
authors.initials: G
authors.lastname: Bogdanovic
authors.forename: Vesna
authors.initials: V
authors.lastname: Kojic
authors.forename: Salvatore
authors.initials: S
authors.lastname: De Rosa
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D001688:Biological Products / Q000737:chemistry / Q000494:pharmacology*; D053138:Cyclohexenes / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D005260:Female; D019073:HT29 Cells; D006367:HeLa Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D007930:Leucine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology*; D008175:Lung Neoplasms / Q000188:drug therapy; D008297:Male; D015394:Molecular Structure; D011161:Porifera / Q000737:chemistry*; D011809:Quinones / Q000737:chemistry / Q000494:pharmacology*; D012717:Sesquiterpenes / Q000737:chemistry / Q000494:pharmacology*
chemical_list: C000591438:4'-leucine-avarone; D000970:Antineoplastic Agents; D001688:Biological Products; D053138:Cyclohexenes; D011809:Quinones; D012717:Sesquiterpenes; C046374:avarone; D007930:Leucine