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In Vitro and in Vivo Antitumor Effect of Trachylobane-360, a Diterpene from Xylopia langsdorffiana

2012; Multidisciplinary Digital Publishing Institute; Volume: 17; Issue: 8 Linguagem: Inglês

10.3390/molecules17089573

1433-1373

João Carlos Lima Rodrigues Pita, Aline Lira Xavier, Tatyanna Kélvia Gomes de Sousa, Vivianne Mendes Mangueira, Josean Fechine Tavares, Robson José de Oliveira Júnior, Robson Cavalcante Veras, Hilzeth de Luna Freire Pessôa, Marcelo Sobral da Silva, Sandra Morelli, Veridiana de Melo Rodrigues, Teresinha Gonçalves da Silva, Margareth de Fátima Formiga Melo Diniz, Marianna Vieira S. Castello-Branco,

Alkaloids: synthesis and pharmacology

Trachylobane-360 (ent-7α-acetoxytrachyloban-18-oic acid) was isolated from Xylopia langsdorffiana. Studies have shown that it has weak cytotoxic activity against tumor and non-tumor cells. This study investigated the in vitro and in vivo antitumor effects of trachylobane-360, as well as its cytotoxicity in mouse erythrocytes. In order to evaluate the in vivo toxicological aspects related to trachylobane-360 administration, hematological, biochemical and histopathological analyses of the treated animals were performed. The compound exhibited a concentration-dependent effect in inducing hemolysis with HC50 of 273.6 µM, and a moderate in vitro concentration-dependent inhibitory effect on the proliferation of sarcoma 180 cells with IC50 values of 150.8 µM and 150.4 µM, evaluated by the trypan blue exclusion test and MTT reduction assay, respectively. The in vivo inhibition rates of sarcoma 180 tumor development were 45.60, 71.99 and 80.06% at doses of 12.5 and 25 mg/kg of trachylobane-360 and 25 mg/kg of 5-FU, respectively. Biochemical parameters were not altered. Leukopenia was observed after 5-FU treatment, but this effect was not seen with trachylobane-360 treatment. The histopathological analysis of liver and kidney showed that both organs were mildly affected by trachylobane-360 treatment. Trachylobane-360 showed no immunosuppressive effect. In conclusion, these data reinforce the anticancer potential of this natural diterpene.