goniothalamin has been researched along with Carcinoma--Ehrlich-Tumor* in 2 studies
2 other study(ies) available for goniothalamin and Carcinoma--Ehrlich-Tumor
| Article | Year |
|---|---|
Design and synthesis of N-acylated aza-goniothalamin derivatives and evaluation of their in vitro and in vivo antitumor activity.
Herein we describe the synthesis of a focused library of compounds based on the structure of goniothalamin (1) and the evaluation of the potential antitumor activity of the compounds. N-Acylation of aza-goniothalamin (2) restored the in vitro antiproliferative activity of this family of compounds. 1-(E)-But-2-enoyl-6-styryl-5,6-dihydropyridin-2(1H)-one (18) displayed enhanced antiproliferative activity. Both goniothalamin (1) and derivative 18 led to reactive oxygen species generation in PC-3 cells, which was probably a signal for caspase-dependent apoptosis. Treatment with derivative 18 promoted Annexin V/7-aminoactinomycin D double staining, which indicated apoptosis, and also led to G2 /M cell-cycle arrest. In vivo studies in Ehrlich ascitic and solid tumor models confirmed the antitumor activity of goniothalamin (1), without signs of toxicity. However, derivative 18 exhibited an unexpectedly lower in vivo antitumor activity, despite the treatments being administered at the same site of inoculation. Contrary to its in vitro profile, aza-goniothalamin (2) inhibited Ehrlich tumor growth, both on the ascitic and solid forms. Our findings highlight the importance of in vivo studies in the search for new candidates for cancer treatment. Topics: Acylation; Animals; Antineoplastic Agents; Apoptosis; Aza Compounds; Carcinoma, Ehrlich Tumor; Cell Line, Tumor; Cell Proliferation; Drug Screening Assays, Antitumor; Female; G2 Phase Cell Cycle Checkpoints; Humans; M Phase Cell Cycle Checkpoints; Mice; Mice, Inbred BALB C; Pyrones; Reactive Oxygen Species; Structure-Activity Relationship; Transplantation, Heterologous | 2014 |
Effect of goniothalamin on the development of Ehrlich solid tumor in mice.
In this work the antiproliferative activity of goniothalamin (1), both in racemic and in its enantiomeric pure forms, in a solid tumor experimental model using laboratory animals is described. The antiedematogenic activity displayed by racemic 1 in the carrageenan edema model in mice together with the reduction of Ehrlich solid tumor model suggest a relationship between anticancer and antiinflammatory activities with the antiinflammatory activity favoring the antiproliferative activity itself. Topics: Animals; Anti-Inflammatory Agents; Antineoplastic Agents; Carcinoma, Ehrlich Tumor; Carrageenan; Cell Line, Tumor; Disease Models, Animal; Edema; Humans; Mice; Pyrones; Stereoisomerism | 2010 |