title: Vanillin Analogues o-Vanillin and 2,4,6-Trihydroxybenzaldehyde Inhibit NFĸB Activation and Suppress Growth of A375 Human Melanoma.
abstract: Constitutive activation of nuclear factor kappa-B (NFĸB) is a hallmark of various cancer types, including melanoma. Chemotherapy may further increase tumour NFĸB activity, a phenomenon that, in turn, exacerbates drug resistance. This study aimed at preliminary screening of a panel of aromatic aldehydes, including vanillin, for cytotoxicity and suppression of tumour cell NFĸB activity.
  
  
  
  The cytotoxic and NFĸB-inhibitory effects of 10 aromatic aldehydes, including vanillin, were investigated in cultured A375 human melanoma cells. Each compound was assayed alone and in combination with the model NFĸB-activating drug doxorubicin. The most promising analogues were then tested alone and in combination with 4-hydroperoxycyclophosphamide in vitro, and with cyclophosphamide in mice bearing A375 xenografts.
  
  
  
  The vanillin analogues o-vanillin and 2,4,6-trihydroxybenzaldehyde exhibited cytotoxicity against cultured A375 cells, and inhibited doxorubicin- and 4-hydroperoxycyclophosphamide-induced NFĸB activation. They also suppressed A375 cell growth in mice.
  
  
  
  o-vanillin and 2,4,6-trihydroxybenzaldehyde deserve further evaluation as potential anticancer drugs.
authors: Hungarian Academy of Sciences, Biological Research Centre, Szeged, Hungary.
authors: Annamária
authors: A
authors: Marton
authors: Hungarian Academy of Sciences, Biological Research Centre, Szeged, Hungary.
authors: Erzsébet
authors: E
authors: Kúsz
authors: Hungarian Academy of Sciences, Biological Research Centre, Szeged, Hungary.
authors: Csongor
authors: C
authors: Kolozsi
authors: Creative Laboratory Ltd, Szeged, Hungary.
authors: Vilmos
authors: V
authors: Tubak
authors: Department of Pharmaceutical and Pharmacological Sciences, University of Padova, Padua, Italy.
authors: Giuseppe
authors: G
authors: Zagotto
authors: Hungarian Academy of Sciences, Biological Research Centre, Szeged, Hungary.
authors: Krisztina
authors: K
authors: Buzás
authors: Department of Pharmaceutical and Pharmacological Sciences, University of Padova, Padua, Italy vizler.csaba@brc.mta.hu luigi.quintieri@unipd.it.
authors: Luigi
authors: L
authors: Quintieri
authors: Hungarian Academy of Sciences, Biological Research Centre, Szeged, Hungary vizler.csaba@brc.mta.hu luigi.quintieri@unipd.it.
authors: Csaba
authors: C
authors: Vizler
mesh_terms: D000818:Animals; D001547:Benzaldehydes / Q000494:pharmacology*; D045744:Cell Line, Tumor; D006801:Humans; D008545:Melanoma / Q000473:pathology*; D051379:Mice; D016328:NF-kappa B / Q000037:antagonists & inhibitors* / Q000378:metabolism; D015398:Signal Transduction; D023041:Xenograft Model Antitumor Assays
chemical_list: D001547:Benzaldehydes; D016328:NF-kappa B; C060843:2-vanillin; C535196:2,4,6-trihydroxybenzaldehyde
keywords: Melanomas; NFϰB; chemotherapy; vanillin