The aim of the study was to assess changes in the activity of anti-inflammatory terpenes from Chilean medicinal plants after the formation of derivatives incorporating synthetic anti-inflammatory agents. Ten new hybrid molecules were synthesized combining terpenes (ferruginol (1), imbricatolic acid (2) and oleanolic acid (3)) with ibuprofen (4) or naproxen (5). The topical anti-inflammatory activity of the compounds was assessed in mice by the arachidonic acid (AA) and 12-O-tetradecanoyl phorbol 13-acetate (TPA) induced ear edema assays. Basal cytotoxicity was determined towards human lung fibroblasts, gastric epithelial cells and hepatocytes. At 1.4 µmol/mouse, a strong anti-inflammatory effect in the TPA assay was observed for oleanoyl ibuprofenate 12 (79.9%) and oleanoyl ibuprofenate methyl ester 15 (80.0%). In the AA assay, the best activity was observed for 12 at 3.2 µmol/mouse, with 56.8% reduction of inflammation, in the same range as nimesulide (48.9%). All the terpenyl-synthetic anti-inflammatory hybrids showed better effects in the TPA assay, with best activity for 6, 12 and 15. The cytotoxicity of the compounds 8 and 10 with a free COOH, was higher than that of 2. The derivatives from 3 were less toxic than the triterpene. Several of the new compounds presented better anti-inflammatory effect and lower cytotoxicity than the parent terpenes.

Background: Since the 1980s, cancer research has focused primarily on developing new therapeutic agents targeting DNA alterations rather than understanding cancer as an integrated system composed of several modules. In this sense, G-quadruplex (G4) nucleic acids are a promising target for drug development for cancer therapy since they exist in the chromosomal telomeric sequences and the promoter regions of numerous genes. The G4 structures within telomeric DNA can inhibit telomerase activity and prevent the proliferation and immortalization of cancer cells. Furthermore, such G4 systems within the promoter regions of oncogenes can inhibit the transcription and expression of the oncogene. Objective: The rational design of small molecules such as organic ligands and their metal- organic derivative compounds can stabilize G4 structures through different binding modes on several G4 DNA topologies. Metal-based compounds have demonstrated their competitiveness compared to organic molecules to distinguish G4 over the DNA duplex owing to their convenient coordination features, positive charge, and electron density promoted by organic ligand. Results: This article is a comprehensive review of metal compounds G4-binders and their structural features that confer them the ability to recognize G-quartets and stabilize several DNA G4s. Conclusion: This stabilization can be achieved through extended square aromatic surfaces, increased hydrophobicity, different auxiliary ligands, axially coordinated ligands, and the nature of the metal center.

Objetivos: determinar la composición fitoquímica y evaluar la actividad antioxidante de los extractos hidroalcohólicos de S. haematospermum; P. niruri; P. tenellus; E. serpens. Metodología: la composición fitoquímica se analizó por cromatografía en capa fina y la actividad antioxidante se observó de modo cualitativo por ensayo autográfico. Los fenoles totales se cuantificaron con el método de Folin-Ciocalteu y flavonoides totales con la reacción de complejación de aluminio. Para determinar la actividad antioxidante se utilizaron las técnicas de decoloración del radical libre DPPH• (2,2- difenil-1-picrilhidracilo) y del radical catión ABTS°+ (ácido 2,2´-azino-bis (3-etilbenzotiazolin)-6-sulfónico) y del poder reductor del catión hierro (III). Resultados: el estudio fitoquímico evidenció en todas las especies la presencia de metabolitos bioactivos. El contenido de fenoles totales osciló entre: 627,71 ± 1,45 y 369,8±52,6 mg EAG/g muestra y de flavonoides totales fue de 12,2 ± 0,1 hasta 4,5 ± 0,3 mg Q/g muestra. Las especies S. haematospermum y P. tenellus presentaron mayor contenido de polifenoles. Los ensayos de actividad antioxidante permitieron reconocer que S. haematospermum y P. tenellus tienen capacidad de mayor inhibición de los radicales libres probados y mostraron mayor poder reductor los extractos hidroalcohólicos S. haematospermum y P. niruri. Objectives: To determine the phytochemical composition and evaluate the antioxidant activity of the hydroalcoholic extracts of S. haematospermum; P. niruri; P. tenellus; E. serpens. Methodology: The phytochemical composition was analyzed by thin layer chromatography and the antioxidant activity was observed qualitatively by autographic assay. Total phenols were quantified with the Folin-Ciocalteu method and total flavonoids with the aluminum complexation reaction.To determine the antioxidant activity, the discoloration techniques of the free radical DPPH• (2,2 diphenyl-1-picrilhydracil) and of the cation radical ABTS•+(2,2-Azino-bis-3-ethylbenzothiazolin-6-sulfonic acid) and the reducing power of the iron (III) cation. Results: The phytochemical study showed the presence of bioactive metabolites in all species. The total phenol content ranged from: 627.71 ± 1.45 to 369.8 ± 52.6 mg EAG / g sample and total flavonoids was 12.2 ± 0.1 to 4.5 ± 0.3 mg Q / g sample. The species S. haematospermum and P. tenellus presented higher content of polyphenols. The antioxidant activity tests allowed recognizing that S. haematospermum and P. tenellus have a capacity for greater inhibition of the tested free radicals and the hydroalcoholic extracts S. haematospermum and P. niruri showed greater reducing power. Objetivos: determinar a composição fitoquímica e avaliar a atividade antioxidante dos extratos hidroalcoólicos de S. haematospermum; P. niruri; P. tenellus; E. serpens. Metodologia: a composição fitoquímica foi analisada por cromatografia em camada delgada e a atividade antioxidante foi observada qualitativamente por ensaio autográfico. Fenóis totais foram quantificados pelo método de Folin-Ciocalteu e flavonóides totais pela reação de complexação de alumínio. Para determinar a atividade antioxidante, as técnicas de descoloração do radical livre DPPH• (2,2-difenil-1-picrilhidracil) e do radical catiônico ABTS•+ (2,2-azino-bis-3-etilbenzotiazolin-6-sulfônico ácido) e o poder redutor do cátion ferro (III). Resultados: o estudo fitoquímico mostrou a presença de metabólitos bioativos em todas as espécies. O conteúdo total de fenol variou de: 627,71 ± 1,45 a 369,8 ± 52,6 mg EAG / g amostra e flavonóides totais foi de 12,2 ± 0,1 a 4,5 ± 0,3 mg Q / g amostra. As espécies S. haematospermum e P. tenellus apresentaram maior teor de polifenóis. Os testes de atividade antioxidante permitiram reconhecer que S. haematospermum e P. tenellus apresentam maior capacidade de inibição dos radicais livres testados e os extratos hidroalcoólicos S. haematospermum e P. niruri apresentaram maior poder redutor.