Isolamento de um diterpeno bioactivo a partir de plectranthus ornatus codd.
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Data
2019
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A Tuberculose, infeta milhares de pessoas todos os anos sendo um problema
grave de saúde pública mundial. O agente causador, Mycobacterium tuberculosis, é
uma bactéria detentora de mecanismos de sobrevivência elaborados no hospedeiro.
A descoberta de novos antibióticos é essencial para reduzir as mortes por TB
e os produtos naturais oferecem um excelente ponto de partida para a descoberta
destes compostos devido à sua diversidade estrutural e funcional.
O género Plectranthus pertencente à família Lamiaceae, como a menta e a
sálvia, e exibe uma ampla gama de usos etnobotânicos. A espécie P.ornatus tem
propriedades: diurética, antipirética, analgésica, antibiótica e anti-inflamatória e é
utilizada no alívio de perturbações estomacais e hepáticas.
O diterpeno de esqueleto de halimano (ácido 11R*-acetoxi-halima-5,13E-dien-
15-óico) foi isolado pela primeira vez a partir de um extrato acetónico do P.ornatus. Este
composto está descrito quanto à sua actividade antimicrobiana, nomeadamente antibacilar.
Deste modo, neste trabalho foi-se isolar o composto em grande escala. Assim,
foi realizada uma extração acetónica por ultra-sons (rendimento de extração de 7,082%
(m/m)). Também foi realizado o isolamento cromatográfico de 5,3 mg de diterpeno puro,
identificado por HPLC-DAD, por comparação com uma amostra autêntica. No futuro
será possível o isolamento total do composto neste extrato permitindo novos estudos
biológicos com potencial para o desenvolvimento de novos fármacos tuberculostáticos.
Tuberculosis infects thousands of people every year and is a serious public health problem worldwide. The causative agent, Mycobacterium tuberculosis, is a bacterium that has elaborated survival mechanisms in the host. The discovery of new antibiotics is essential for reducing TB deaths and natural products offer an excellent starting point for the discovery of these compounds due to their structural and functional diversity. The genus Plectranthus belonging to the Lamiaceae family, such as mint and sage, exhibit a wide range of ethnobotanical uses. The P.ornatus species has diuretic, antipyretic, analgesic, antibiotic and anti-inflammatory properties and is used to relieve stomach and liver disorders. Haliman's backbone diterpene (11R*-acetoxy halima-5,13E-dien-15-oic acid) was isolated for the first time from an acetone extract of P.ornatus. This compound is described due to its antimicrobial, namely antitubercular activity. Thus, in this work the large-scale compound was isolated. Thus, acetonic ultrasound extraction was performed (extraction yield 7.082% (w / w)). Chromatographic isolation of 5.3 mg of pure diterpene, identified by HPLC-DAD, was also performed by comparison with an authentic sample. In the future it will be possible the total isolation of the compound in this extract allowing new biological studies with potential for the development of new tuberculostatic drugs.
Tuberculosis infects thousands of people every year and is a serious public health problem worldwide. The causative agent, Mycobacterium tuberculosis, is a bacterium that has elaborated survival mechanisms in the host. The discovery of new antibiotics is essential for reducing TB deaths and natural products offer an excellent starting point for the discovery of these compounds due to their structural and functional diversity. The genus Plectranthus belonging to the Lamiaceae family, such as mint and sage, exhibit a wide range of ethnobotanical uses. The P.ornatus species has diuretic, antipyretic, analgesic, antibiotic and anti-inflammatory properties and is used to relieve stomach and liver disorders. Haliman's backbone diterpene (11R*-acetoxy halima-5,13E-dien-15-oic acid) was isolated for the first time from an acetone extract of P.ornatus. This compound is described due to its antimicrobial, namely antitubercular activity. Thus, in this work the large-scale compound was isolated. Thus, acetonic ultrasound extraction was performed (extraction yield 7.082% (w / w)). Chromatographic isolation of 5.3 mg of pure diterpene, identified by HPLC-DAD, was also performed by comparison with an authentic sample. In the future it will be possible the total isolation of the compound in this extract allowing new biological studies with potential for the development of new tuberculostatic drugs.
Descrição
Orientação: Patrícia Rijo
Palavras-chave
MESTRADO INTEGRADO EM CIÊNCIAS FARMACÊUTICAS, CIÊNCIAS FARMACÊUTICAS, PLANTAS MEDICINAIS, DITERPENOS, TUBERCULOSE, CROMATOGRAFIA, PHARMACEUTICAL SCIENCES, MEDICINAL PLANTS, DITERPENES, TUBERCULOSIS, CHROMATOGRAPHY