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

Molecules

João Carlos Lima Rodrigues Pita²  Aline Lira Xavier²  Tatyanna Kelvia Gomes de Sousa²  Vivianne Mendes Mangueira²  Josean Fechine Tavares²  Robson José de Oliveira Júnior³  Robson Cavalcante Veras²  Hilzeth de Luna Freire Pessoa²  Marcelo Sobral da Silva²  Sandra Morelli³  Veridiana de Melo Rodrigues Ávila³  Teresinha Gon๺lves da Silva¹  Margareth de Fátima Formiga Melo Diniz² 

[1] Departament of Antibiotics, Federal University of Pernambuco, Recife 50670-901, PE, Brazil;Laboratory of Pharmaceutical Technology, Federal University of Paraíba, P.O. Box 5009, João Pessoa 58051-970, PB, Brazil;Laboratory of Cytogenetic, Institute of Genetics and Biochemistry, Federal University of Uberlandia, P.O. Box 593, Uberlândia 38400-902, MG, Brazil;

关键词: trachylobane-360;    Xylopia langsdorffiana;    antitumor activity;    toxicity;    hemolytic activity;   

DOI  :  10.3390/molecules17089573

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2012 by the authors; licensee MDPI, Basel, Switzerland.