Prospecção de metabólitos ativos em espécies de Fabaceae recomendadas para o reflorestamento no Estado de São Paulo
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Data
2019-03-15
Autores
Silva, Alene Côrtes de Queiroz
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Universidade Estadual Paulista (Unesp)
Resumo
A família Fabaceae é conhecida pelo seu valor econômico e ecológico, além de possuir reconhecida diversidade de metabolitos secundários. Esta família é amplamente distribuída no Estado de São Paulo, incluindo diversas espécies recomendadas para recuperação de áreas degradadas, sendo muitas delas produzidas em viveiros de mudas. O objetivo deste trabalho foi identificar em espécies de Fabaceae novas fontes de moléculas que já possuem valor significativo no mercado, além de prospectar novas substâncias com potencial citotóxico frente células tumorais e larvicida frente a larvas de Aedes aegypti. A triagem foi iniciada com mudas de 22 espécies. Os extratos aquosos e etanólicos de folhas de mudas destas 22 espécies foram analisados por UPLC-CAD-DAD e por RMN¹H e esses dados indicaram a produção de substância majoritária em Cassia ferruginea. Essa substância foi identificada como (+)-ampelopsina, já com reconhecido valor de mercado por sua ação hepatoprotetora e combate a intoxicação e dependência de álcool. Teores elevados de (+) ampelopsina determinados por RMN de 1H (padrão interno e ERETIC2) foram encontrados em folhas de mudas e matriz (11,6 % e 7,0 %, respectivamente), confirmando a viabilidade de C. ferruginea como nova fonte de (+) ampelopsina. O método de padrão interno foi validado de acordo com RDC n°- 166 da ANVISA Na etapa de prospecção de atividade citotóxica e larvicida dos extratos das 22 espécies de Fabaceae, destacaram-se duas espécies como promissoras para atividade larvicida contra Aedes aegypti: Leucochloron incuriale (Vell.) Benth (angico-rajado) e Enterolobium contortisiliquum (Vell.) Morong (timburi) e três espécies com potencial citotóxico para as linhagens de células tumorais PC3 (próstata humano), HCT-116 (cólon humano) e SF-295/ SNB-19 (glioblastoma humano): Albizia niopoides (Bentham) Burkat (farinha-seca), Enterolobium contortisiliquum (Vell.) Morong (timburi) e Leucochloron incuriale (Vell.) Benth (angico-rajado). Entre elas, os extratos de timburi apresentaram maior atividade citotóxica, além de seletividade, uma vez que foram pouco ativos em células não-tumoral L929 (fibroblasto de pulmão murinho). Assim, este trabalho realça o potencial econômico e terapêutico de espécies de Fabaceae indicadas para o reflorestamento no Estado de São Paulo, as quais constituem uma fonte valiosa de metabolitos com interesse econômico e de novas substâncias bioativas, que podem ser explorados de uma maneira sustentável.
The Fabaceae family is well known for its economic, biological and ecological value, besides the recognized functional and chemical diversity of secondary metabolites. This family is widely distributed in São Paulo state and includes several recommended species for the restoration of degraded areas of the state, many of them being produced in seedlings nurseries. Thus, the aim of this work was to discover new sources of novel bioactive metabolites or known metabolites with commercial value, besides prospecting new compounds with cytotoxic potential against tumor cells and, larvicidal activity against Aedes aegypti. The screening was carried out with seedlings of 22 species. The aqueous and ethanolic extracts from leaves were analyzed by UPLC-CAD-DAD and 1H NMR and these data indicated the production of a major compound in Cassia ferruginea. This compound was identified as (+)-ampelopsin, known for its hepatoprotective action and against alcohol intoxication and dependence. High levels of (+)-ampelopsin were determined by 1H NMR (internal standard and ERETIC2) in leaves of seedlings and the adult plant (11.6% and 7.0%, respectively), confirming the viability of C. ferruginea as a new source of (+)-ampelopsin. The internal standard method was validated based on ANVISA RDC N °166. During the prospection stage of cytotoxic and larvicidal activity of the extracts of the 22 species of Fabaceae, two species were highlighted as promising for larvicidal activity against Aedes aegypti: Leucochloron incuriale(Vell.) Benth (angico-rajado) and Enterolobium contortisiliquum (Vell.) Morong (timburi) and three species with cytotoxic potential against tumor cell lines PC3 (human prostate), HCT-116 (human colon) and SF-295/SNB-19 (human glioblastoma) were also detected: Albizia niopoides (Bentham) Burkat (farinha-seca), Enterolobium contortisiliquum (Vell.) Morong (timburi) and Leucochloron incuriale(Vell.) Benth (angico-rajado). Among them, timburi extracts increased cytotoxic activity in addition to selectivity, since they were little active in non-tumor cells L929 (murine lung fibroblast). Therefore, this work highlights the economic and therapeutic potential of native Fabaceae species indicated for the restoration in São Paulo state, which constitutes a valuable source of metabolites with economic interest and new bioactive substances, that can be exploited in a sustainable manner.
The Fabaceae family is well known for its economic, biological and ecological value, besides the recognized functional and chemical diversity of secondary metabolites. This family is widely distributed in São Paulo state and includes several recommended species for the restoration of degraded areas of the state, many of them being produced in seedlings nurseries. Thus, the aim of this work was to discover new sources of novel bioactive metabolites or known metabolites with commercial value, besides prospecting new compounds with cytotoxic potential against tumor cells and, larvicidal activity against Aedes aegypti. The screening was carried out with seedlings of 22 species. The aqueous and ethanolic extracts from leaves were analyzed by UPLC-CAD-DAD and 1H NMR and these data indicated the production of a major compound in Cassia ferruginea. This compound was identified as (+)-ampelopsin, known for its hepatoprotective action and against alcohol intoxication and dependence. High levels of (+)-ampelopsin were determined by 1H NMR (internal standard and ERETIC2) in leaves of seedlings and the adult plant (11.6% and 7.0%, respectively), confirming the viability of C. ferruginea as a new source of (+)-ampelopsin. The internal standard method was validated based on ANVISA RDC N °166. During the prospection stage of cytotoxic and larvicidal activity of the extracts of the 22 species of Fabaceae, two species were highlighted as promising for larvicidal activity against Aedes aegypti: Leucochloron incuriale(Vell.) Benth (angico-rajado) and Enterolobium contortisiliquum (Vell.) Morong (timburi) and three species with cytotoxic potential against tumor cell lines PC3 (human prostate), HCT-116 (human colon) and SF-295/SNB-19 (human glioblastoma) were also detected: Albizia niopoides (Bentham) Burkat (farinha-seca), Enterolobium contortisiliquum (Vell.) Morong (timburi) and Leucochloron incuriale(Vell.) Benth (angico-rajado). Among them, timburi extracts increased cytotoxic activity in addition to selectivity, since they were little active in non-tumor cells L929 (murine lung fibroblast). Therefore, this work highlights the economic and therapeutic potential of native Fabaceae species indicated for the restoration in São Paulo state, which constitutes a valuable source of metabolites with economic interest and new bioactive substances, that can be exploited in a sustainable manner.
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Cassia ferruginea, (+)-ampelopsina, Enterolobium contortisiliquum, Leucochoron incuriale, Citotóxico