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.
Silva
Márcio Luís A
ML
Universidade de Franca, Av. Dr. Armando Salles de Oliveira, 201, CEP 14404-600--Franca, SP, Brazil. mlasilva@unifran.br
Martins
Carlos H G
CH
Lucarini
Rodrigo
R
Sato
Daisy N
DN
Pavanb
Fernando R
FR
Freitas
Nayara H A
NH
Andrade
Leonardo N
LN
Pereira
Ana C
AC
Bianco
Thais N C
TN
Vinholis
Adriana H C
AH
Cunha
Wilson R
WR
Bastos
Jairo K
JK
Silva
Rosangela
R
Da Silva Filho
Ademar A
AA
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