The activity of flavones and oleanolic acid from Lippia lacunosa against susceptible and resistant Mycobacterium tuberculosis strains

Revista Brasileira de Farmacognosia

Silva, Pedro E. A.¹  Universidade Federal do Rio de Janeiro, Brazil¹  Fundação Universidade Federal do Rio Grande, Brazil¹  Coelho, Tatiane S.¹  Julião, Lisieux S.¹  Lage, Celso L. S.¹  Leitão, Suzana G.¹  Barbosa, Ymira G.¹  Ramos, Daniela F.¹  Castellar, Aline¹  Fundação Oswaldo Cruz, Brazil¹  Lourenço, Maria Cristina S.¹ 

关键词: Lippia lacunosa;    Verbenaceae;    flavonoids;    antimycobacterial activity;    Mycobacterium tuberculosis;    methoxyflavones;    oleanolic acid.;   

DOI  :  10.1590/S0102-695X2011005000076

来源: Sociedade Brasileira de Farmacognosia

【 摘 要 】

Tuberculosis (TB), caused by Mycobacterium tuberculosis, is the world's number one killer among infectious diseases. The search for new naturalproducts that can act as drugs against TB has received increased attention duringthe last years. In this work we describe the isolation and identification of the active antimycobacterial principles of the dichloromethane extract from Lippia lacunosa Mart. & Schauer, Verbenaceae. Compounds were evaluated for their in vitro activity against Mycobacterium tuberculosis (susceptible and rifampicin resistantstrain) using a redox bioassay. From the dichloromethane extract of L. lacunosa leaves, seven methoxy-flavones named cirsimaritin (1), eupatilin (2), eupatorin (3), salvigenin (4), 3'-O-methyl-eupatorin (5), 3',7-dimethoxy-5,6,4'- trihydroxyflavone (6), and 7'-O-methylapigenin (7), and one triterpene, named oleanolic acid (8), were isolated. All compounds were found to display antimycobacterial activity against susceptible strain, with MIC ranging from 25 to 200 µg/mL. None of them was active against rifampicin resistant strain. This is the first report in the antimycobacterial activity of 6-substituted flavones, as well as the first report of the occurrence of these substances in L. lacunosa.

【 授权许可】

Unknown