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Ethnopharmacological relevance: Fabiana imbricata (Solanaceae) is a Patagonian medicinal plant with a long tradition of use. The aim of this review is to provide an integrative overview of the traditional uses, chemistry, bioactivity and chemical profiling of the crude drug. Materials and methods: The information was collected from scientific databases searching with the keywords Fabiana imbricata, Fabiana species, Fabiana (Solanaceae) and includes local literature and books. Results: The indications of use reported in literature show little variation from the data published as early as 1889. The chemical studies showed a rich diversity in metabolites including phenolics, coumarins, flavonoids, phenylpropanoids, terpenes, alkaloids and sugars. Bioactivity studies supported the traditional use as diuretic and also the potential of the crude drug as a gastroprotective agent. The plant can be used as a source of compounds with effect on gastric ulcers and shows enzyme inhibitory activity. While the germination rate of the plant is very low, protocols were developed for the rapid in vitro propagation of the species. The toxicity of the crude drug extracts was low and did not show clastogenic effect in human lymphocytes. Further research is needed to disclose the potential of the F. imbricata sesquiterpenes on other relevant biological targets.

Starting from the diterpene (4S, 9R, 10R) methyl 18-carboxy-labda-8,13(E)-dien-15-oate (PMD) and its 8(9)-en isomer [PMD 8(9)-en], 11 amides were prepared and assessed for a gastroprotective effect in the ethanol/HCl-induced gastric lesions model in mice. Basal cytotoxicity of the compounds was determined on the following human cell lines: normal lung fibroblasts (MRC-5), gastric epithelial adenocarcinoma (AGS), and hepatocellular carcinoma (Hep G2). All compounds are described for the first time. At the single oral dose of 0.1mg/kg, compounds 1, 10, and 11 presented a strong gastroprotective effect, at least comparable with that of the reference compound lansoprazole at 1mg/kg, reducing gastric lesions by 76.7, 67.7, and 77.2%, respectively. The leucyl amide methyl ester 3, tryptophanyl amide methyl ester 5, and benzyl amide 6 of PMD presented a selective basal cytotoxicity on Hep G2 cells with IC50 values of 136.8, 105.3, and 94.2 mu M, respectively, while the IC50 values towards AGS cells were 439.5, 928.0, and 937.3 mu M, respectively. The three compounds did not affect fibroblast viability with IC50 values > 1000 mu M. Compounds 7, 8, 10, and 11 showed no toxic effect against the three selected cell lines. FONDECYTComision Nacional de Investigacion Cientifica y Tecnologica (CONICYT)CONICYT FONDECYT [1085306]; Programa de Investigacion en Productos Bioactivos, Universidad de Talca; Programa Bicentenario de Ciencia y Tecnologia This work was supported by FONDECYT, Project No. 1085306 and Programa de Investigacion en Productos Bioactivos, Universidad de Talca. VRO thanks the Universidad de Talca for a Doctoral grant, and MWP thanks the Programa Bicentenario de Ciencia y Tecnologia PSD-50 for a postdoctoral fellowship. The skilful technical work of Irene Manriquez is gratefully acknowledged.

New diterpenylquinones, combining a diterpene diacid and a naphthoquinone, were prepared from junicedric acid and lapachol. The new derivatives were assessed as gastroprotective agents by the HCl-EtOH-induced gastric lesions model in mice as well as for basal cytotoxicity on the following human cell lines: Normal lung fibroblasts (MRC-5), gastric epithelial adenocarcinoma (AGS), and hepatocellular carcinoma (Hep G2). Several of the new compounds were significantly active as antiulcer agents and showed selective cytotoxicity against AGS cells.

We report the preparation of a series of indolylquinone and pyridine derivatives in order to evaluate structure-activity relationships in human gastric (AGS), lung (SK-MES-1), bladder (J82) cancer cell lines and human normal lung fibroblasts (MCR-5). Two correlations tendency between half-wave redox potentials against their antineoplasic activity were found making it possible to establish that for epithelial human gastric cancer (AGS) cell lines and human normal lung fibroblasts (MCR-5). The quinone bioreduction should correspond to a one electron process under normomix conditions, whilst for all other lines this process should correspond to a two electron attachment via a hypoxic process.