Antimycobacterial activity of natural and semi-synthetic lignans.
The antimycobacterial activity of (-)-cubebin (1), hinokinin (2), and some of their semisynthetic derivatives, namely (-)-O-acetyl-cubebin (3), (-)-O-methyl-cubebin (4), (-)-O-(N,N-dimethylamine-ethyl)-cubebin (5) and (-)-6,6'-dinitrohinokinin (6), was evaluated against Mycobacterium tuberculosis (ATCC 27294), M. kansasii (ATCC 12478), and M. avium (ATCC 15769). The MIC values ranged from 31.25 to 2000 microg/mL. Among the evaluated compounds, 2 displayed a MIC value of 62.5 microg/mL against M. tuberculosis, while 3 and 4 displayed MIC values of 62.5 and 31.25 microg/mL, respectively, against M. avium. All compounds were inactive against M. kansasii. These are promising results concerning the search for biologically active natural products, highlighting that new approaches to the prevention, treatment, and cure of tuberculosis are extremely important.
Universidade de Franca, Av. Dr. Armando Salles de Oliveira, 201, CEP 14404-600--Franca, SP, Brazil. mlasilva@unifran.br
Márcio Luís A
ML
Silva
Carlos H G
CH
Martins
Rodrigo
R
Lucarini
Daisy N
DN
Sato
Fernando R
FR
Pavanb
Nayara H A
NH
Freitas
Leonardo N
LN
Andrade
Ana C
AC
Pereira
Thais N C
TN
Bianco
Adriana H C
AH
Vinholis
Wilson R
WR
Cunha
Jairo K
JK
Bastos
Rosangela
R
Silva
Ademar A
AA
Da Silva Filho
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D017705:Lignans / Q000138:chemical synthesis / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D008958:Models, Molecular; D009162:Mycobacterium avium / Q000187:drug effects*; D009163:Mycobacterium bovis / Q000187:drug effects*; D019909:Mycobacterium kansasii / Q000187:drug effects*; D009169:Mycobacterium tuberculosis / Q000187:drug effects*
D000900:Anti-Bacterial Agents; D017705:Lignans; C433065:cubebin