RESUMEN
Activity-guided fractionations of Jatropha macrantha Müll. Arg. led to the isolation of pomolic acid (1) and euscaphic acid (2). The potential for inhibition against NF-κB and HIF-1α production of these two compounds was tested in different tumour cell lines. Compounds 1 and 2 showed an inhibitory activity of HIF-1α in the SK-MEL-28 (IC50=3.01 ± 0.02 µM and 3.78 ± 0.02 µM), A549 (IC50=9.97 ± 0.01 µM and 10.25 ± 0.01 µM) and U-373 MG (IC50=6.34 ± 0.02 µM and 8.85 ± 0.02 µM) cell lines. In addition, compounds 1 and 2 showed an inhibitory activity on NF-κB in SK-MEL-28 (IC50=1.05 ± 0.02 µM and 2.71 ± 0.01 µM), A549 (IC50=3.63 ± 0.01 µM and 3.73 ± 0.02 µM) and U-373 MG (IC50=2.55 ± 0.02 µM and 3.39 ± 0.01 µM) cell lines. This is the first report that isolates these compounds from J. macrantha and tests their antitumor potential.
Asunto(s)
Antineoplásicos Fitogénicos/farmacología , Subunidad alfa del Factor 1 Inducible por Hipoxia/antagonistas & inhibidores , Jatropha , FN-kappa B/antagonistas & inhibidores , Triterpenos , Células A549 , Línea Celular Tumoral , Humanos , Jatropha/química , Triterpenos/farmacologíaRESUMEN
ETHNO-PHARMACOLOGICAL RELEVANCE: Tropaeolum tuberosum, commonly known as "Mashua", is one of the plants most frequently used by Andean (Peruvian-Bolivian) people as food and medicine. It is used as a remedy against a wide range of diseases, especially those related with inflammation. OBJECTIVES: This study aims to identify compounds active against inflammatory related conditions. MATERIALS AND METHODS: A bioassay-guided isolation of anti-inflammatory compounds from black and purple tubers of T. tuberosum was performed measuring TNF-α and NF-κB production in THP-1 monocytic cells. RESULTS: The bioassay-guided isolation led to one active compound from purple T. tuberosum, N-oleoyldopamine (1), and another active compound from black T. tuberosum, N-(2-Hydroxyethyl)-7Z,10Z,13Z,16Z-docosatetraenamide (2). Both compounds displayed anti-TNF-α activity with IC50 values of 3.12⯱â¯0.19⯵M and 1.56⯱â¯0.15⯵M, respectively. Also, both compounds suppressed NF-κB with IC50 of 3.54⯱â¯0.02⯵M and 1.77⯱â¯0.07⯵M, respectively. CONCLUSIONS: We identified bioactive compounds from purple and black Tropaeolum tuberosum responsible for their anti-inflammatory activity: N-oleoyldopamine (1) and N-(2-Hydroxyethyl)-7Z,10Z,13Z,16Z-docosatetraenamide (2). This is the first report which isolates these compounds from T. tuberosum and describes their anti-inflammatory activities.