Anti-tumour and pharmacokinetics study of 2-Formyl-8-hydroxy-quinolinium chloride as Galipea longiflora alkaloid analogue

2-Formyl-8-hydroxy-quinolinium chloride was prepared as Galipea longiflora alkaloid analogue and its anticancer activity was evaluated. Representative histopathological sections showed (a) significant tumour necrosis could be identified in 2-Formyl-8-hydroxy-quinolinium chloride-treated group while (b) good cellular integrity could be observed in vehicle treated group on day 23 (10 days after stopping the treatment). The quinolinium chloride salt of 8-hydroxyqinolinecarbaldehyde (2-Formyl-8-hydroxy-quinolinium chloride) was prepared as Galipea longiflora alkaloid analogue and its anticancer activity was evaluated both in vitro and in vivo. This chloride salt was found to show certain degree of selectivity between hepatoma cells and normal hepatocytes in vitro. Athymic nude mice Hep3B xenograft model further demonstrated that this 2-Formyl-8-hydroxy-quinolinium chloride could execute strong anti-tumour activity with the identification of extensive necrotic feature from the tumour xenograft and limited adverse toxicological effect.