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In Vitro and in Vivo Antitumor Effect of Trachylobane-360, a Diterpene from Xylopia langsdorffiana
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 cytotoxi...
Autores principales: | , , , , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2012
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6269042/ https://www.ncbi.nlm.nih.gov/pubmed/22885357 http://dx.doi.org/10.3390/molecules17089573 |
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author | Pita, João Carlos Lima Rodrigues Xavier, Aline Lira de Sousa, Tatyanna Kelvia Gomes Mangueira, Vivianne Mendes Tavares, Josean Fechine Júnior, Robson José de Oliveira Veras, Robson Cavalcante Pessoa, Hilzeth de Luna Freire da Silva, Marcelo Sobral Morelli, Sandra Ávila, Veridiana de Melo Rodrigues da Silva, Teresinha Gonçalves Diniz, Margareth de Fátima Formiga Melo Castello-Branco, Marianna Vieira Sobral |
author_facet | Pita, João Carlos Lima Rodrigues Xavier, Aline Lira de Sousa, Tatyanna Kelvia Gomes Mangueira, Vivianne Mendes Tavares, Josean Fechine Júnior, Robson José de Oliveira Veras, Robson Cavalcante Pessoa, Hilzeth de Luna Freire da Silva, Marcelo Sobral Morelli, Sandra Ávila, Veridiana de Melo Rodrigues da Silva, Teresinha Gonçalves Diniz, Margareth de Fátima Formiga Melo Castello-Branco, Marianna Vieira Sobral |
author_sort | Pita, João Carlos Lima Rodrigues |
collection | PubMed |
description | 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 HC(50) of 273.6 µM, and a moderate in vitro concentration-dependent inhibitory effect on the proliferation of sarcoma 180 cells with IC(50) 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. |
format | Online Article Text |
id | pubmed-6269042 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2012 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-62690422018-12-12 In Vitro and in Vivo Antitumor Effect of Trachylobane-360, a Diterpene from Xylopia langsdorffiana Pita, João Carlos Lima Rodrigues Xavier, Aline Lira de Sousa, Tatyanna Kelvia Gomes Mangueira, Vivianne Mendes Tavares, Josean Fechine Júnior, Robson José de Oliveira Veras, Robson Cavalcante Pessoa, Hilzeth de Luna Freire da Silva, Marcelo Sobral Morelli, Sandra Ávila, Veridiana de Melo Rodrigues da Silva, Teresinha Gonçalves Diniz, Margareth de Fátima Formiga Melo Castello-Branco, Marianna Vieira Sobral Molecules Article 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 HC(50) of 273.6 µM, and a moderate in vitro concentration-dependent inhibitory effect on the proliferation of sarcoma 180 cells with IC(50) 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. MDPI 2012-08-10 /pmc/articles/PMC6269042/ /pubmed/22885357 http://dx.doi.org/10.3390/molecules17089573 Text en © 2012 by the authors; licensee MDPI, Basel, Switzerland. http://creativecommons.org/licenses/by/3.0/ This article is an open-access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/). |
spellingShingle | Article Pita, João Carlos Lima Rodrigues Xavier, Aline Lira de Sousa, Tatyanna Kelvia Gomes Mangueira, Vivianne Mendes Tavares, Josean Fechine Júnior, Robson José de Oliveira Veras, Robson Cavalcante Pessoa, Hilzeth de Luna Freire da Silva, Marcelo Sobral Morelli, Sandra Ávila, Veridiana de Melo Rodrigues da Silva, Teresinha Gonçalves Diniz, Margareth de Fátima Formiga Melo Castello-Branco, Marianna Vieira Sobral In Vitro and in Vivo Antitumor Effect of Trachylobane-360, a Diterpene from Xylopia langsdorffiana |
title | In Vitro and in
Vivo Antitumor Effect of Trachylobane-360, a Diterpene from Xylopia langsdorffiana |
title_full | In Vitro and in
Vivo Antitumor Effect of Trachylobane-360, a Diterpene from Xylopia langsdorffiana |
title_fullStr | In Vitro and in
Vivo Antitumor Effect of Trachylobane-360, a Diterpene from Xylopia langsdorffiana |
title_full_unstemmed | In Vitro and in
Vivo Antitumor Effect of Trachylobane-360, a Diterpene from Xylopia langsdorffiana |
title_short | In Vitro and in
Vivo Antitumor Effect of Trachylobane-360, a Diterpene from Xylopia langsdorffiana |
title_sort | in vitro and in
vivo antitumor effect of trachylobane-360, a diterpene from xylopia langsdorffiana |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6269042/ https://www.ncbi.nlm.nih.gov/pubmed/22885357 http://dx.doi.org/10.3390/molecules17089573 |
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