scholarly journals Discovery of Nosiheptide, Griseoviridin, and Etamycin as Potent Anti-Mycobacterial Agents against Mycobacterium avium Complex

Molecules ◽  
2019 ◽  
Vol 24 (8) ◽  
pp. 1495
Author(s):  
Hosoda ◽  
Koyama ◽  
Kanamoto ◽  
Tomoda

Mycobacterium avium complex (MAC) is a serious disease mainly caused by M. avium and M. intracellulare. Although the incidence of MAC infection is increasing worldwide, only a few agents are clinically used, and their therapeutic effects are limited. Therefore, new anti-MAC agents are needed. Approximately 6600 microbial samples were screened for new anti-mycobacterial agents that inhibit the growth of both M. avium and M. intracellulare, and two culture broths derived from marine actinomycete strains OPMA1245 and OPMA1730 had strong activity. Nosiheptide (1) was isolated from the culture broth of OPMA1245, and griseoviridin (2) and etamycin (viridogrisein) (3) were isolated from the culture broth of OPMA1730. They had potent anti-mycobacterial activity against M. avium and M. intracellulare with minimum inhibitory concentrations (MICs) between 0.024 and 1.56 μg/mL. In addition, a combination of 2 and 3 markedly enhanced the anti-mycobacterial activity against both M. avium and M. intracellulare. Furthermore, a combination 2 and 3 had a therapeutic effect comparable to that of ethambutol in a silkworm infection assay with M. smegmatis.

1999 ◽  
Vol 43 (12) ◽  
pp. 3001-3004 ◽  
Author(s):  
Haruaki Tomioka ◽  
Katsumasa Sato ◽  
Tatsuya Akaki ◽  
Hiroko Kajitani ◽  
Shin Kawahara ◽  
...  

ABSTRACT We compared the in vitro antimycobacterial activity of a new fluoroquinolone, HSR-903, with strong activity against gram-positive cocci with those of levofloxacin (LVFX), sitafloxacin (STFX), and gatifloxacin (GFLX). The MICs of the quinolones for Mycobacterium tuberculosis and Mycobacterium avium complex were in the order STFX ≈ GFLX < LVFX ≦ HSR-903 and STFX ≦ GFLX ≦ HSR-903 ≦ LVFX, respectively. HSR-903 effectively eliminated intramacrophagial M. tuberculosis, as did LVFX, and exhibited bacteriostatic effects against M. tuberculosis replicating in type II alveolar cells.


CHEST Journal ◽  
2009 ◽  
Vol 136 (6) ◽  
pp. 1569-1575 ◽  
Author(s):  
Naoki Hasegawa ◽  
Tomoyasu Nishimura ◽  
Sumire Ohtani ◽  
Kei Takeshita ◽  
Koichi Fukunaga ◽  
...  

2020 ◽  
Author(s):  
Juliana Rotter ◽  
Christopher S. Graffeo ◽  
Hannah E. Gilder ◽  
Lucas P. Carlstrom ◽  
Avital Perry ◽  
...  

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