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

Abstract

Trachylobane-360 (<em>ent</em>-7α-acetoxytrachyloban-18-oic acid) was isolated from <em>Xylopia langsdorffiana</em>. Studies have shown that it has weak cytotoxic activity against tumor and non-tumor cells. This study investigated the <em>in vitro</em><em> </em>and <em>in vivo</em> antitumor effects of trachylobane-360, as well as its cytotoxicity in mouse erythrocytes. In order to evaluate the <em>in vivo</em> 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 <em>in vitro</em><em> </em>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 <em>in vivo</em> 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
• &lt;em&gt;Xylopia langsdorffiana&lt;/em&gt;
• antitumor activity
• toxicity
• hemolytic activity