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In Vitro and in Vivo Antitumor Effect of Trachylobane-360, a Diterpene from Xylopia langsdorffiana
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
Departament of Antibiotics, Federal University of Pernambuco, Recife 50670-901, PE, Brazil
* Author to whom correspondence should be addressed.
Received: 4 June 2012; in revised form: 31 July 2012 / Accepted: 2 August 2012 / Published: 10 August 2012
Abstract: 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.
Keywords: trachylobane-360; Xylopia langsdorffiana; antitumor activity; toxicity; hemolytic activity
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Pita, J.C.L.R.; Xavier, A.L.; Sousa, T.K.G.; Mangueira, V.M.; Tavares, J.F.; Júnior, R.J.O.; Veras, R.C.; Pessoa, H.L.F.; Silva, M.S.; Morelli, S.; Ávila, V.M.R.; Silva, T.G.; Diniz, M.F.F.M.; Castello-Branco, M.V.S. In Vitro and in Vivo Antitumor Effect of Trachylobane-360, a Diterpene from Xylopia langsdorffiana. Molecules 2012, 17, 9573-9589.
Pita JCLR, Xavier AL, Sousa TKG, Mangueira VM, Tavares JF, Júnior RJO, Veras RC, Pessoa HLF, Silva MS, Morelli S, Ávila VMR, Silva TG, Diniz MFFM, Castello-Branco MVS. In Vitro and in Vivo Antitumor Effect of Trachylobane-360, a Diterpene from Xylopia langsdorffiana. Molecules. 2012; 17(8):9573-9589.
Pita, João Carlos Lima Rodrigues; Xavier, Aline Lira; Sousa, Tatyanna Kelvia Gomes de; Mangueira, Vivianne Mendes; Tavares, Josean Fechine; Júnior, Robson José de Oliveira; Veras, Robson Cavalcante; Pessoa, Hilzeth de Luna Freire; Silva, Marcelo Sobral da; Morelli, Sandra; Ávila, Veridiana de Melo Rodrigues; Silva, Teresinha Gonçalves da; Diniz, Margareth de Fátima Formiga Melo; Castello-Branco, Marianna Vieira Sobral. 2012. "In Vitro and in Vivo Antitumor Effect of Trachylobane-360, a Diterpene from Xylopia langsdorffiana." Molecules 17, no. 8: 9573-9589.