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Molecules 2012, 17(8), 9573-9589; doi:10.3390/molecules17089573
Article

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

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1 Laboratory of Pharmaceutical Technology, Federal University of Paraíba, P.O. Box 5009, João Pessoa 58051-970, PB, Brazil 2 Laboratory of Cytogenetic, Institute of Genetics and Biochemistry, Federal University of Uberlandia, P.O. Box 593, Uberlândia 38400-902, MG, Brazil 3 Departament of Antibiotics, Federal University of Pernambuco, Recife 50670-901, PE, Brazil
* Author to whom correspondence should be addressed.
Received: 4 June 2012 / Revised: 31 July 2012 / Accepted: 2 August 2012 / Published: 10 August 2012
(This article belongs to the Section Metabolites)
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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 trachylobane-360; Xylopia langsdorffiana; antitumor activity; toxicity; hemolytic activity
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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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.

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