Anti-Mycobacterial Activity of Marine Fungus-Derived 4-Deoxybostrycin and Nigrosporin

Abstract

4-Deoxybostrycin is a natural anthraquinone compound isolated from the Mangrove endophytic fungus Nigrospora sp. collected from the South China Sea. Nigrosporin is the deoxy-derivative of 4-deoxybostrycin. They were tested against mycobacteria, especially Mycobacterium tuberculosis. In the Kirby-Bauer disk diffusion susceptibility test, they both had inhibition zone sizes of over 25 mm. The results of the absolute concentration susceptibility test suggested that they had inhibitory effects against mycobacteria. Moreover, 4-deoxybostrycin exhibited good inhibition which was even better than that of first line anti-tuberculosis (TB) drugs against some clinical multidrug-resistant (MDR) M. tuberculosis strains. The gene expression profile of M. tuberculosis H37Rv after treatment with 4-deoxybostrycin was compared with untreated bacteria. One hundred and nineteen out of 3,875 genes were significantly different in M. tuberculosis exposed to 4-deoxybostrycin from control. There were 46 functionally known genes which are involved in metabolism, information storage and processing and cellular processes. The differential expressions of six genes were further confirmed by quantitative real-time polymerase chain reaction (qRT-PCR). The present study provides a useful experiment basis for exploitation of correlative new drugs against TB and for finding out new targets of anti-mycobacterial therapy.

Anthraquinones and Derivatives from Marine-Derived Fungi: Structural Diversity and Selected Biological Activities

“…As far as bostrycin is concerned, the originally proposed structure [ 119 , 120 , 121 ] was revised by Kelly and his co-workers in 1985 [ 122 ] on the basis of the total synthesis of (+/−)-bostrycin and an X-ray crystal structure of the O -isopropylidene derivative. This revision also concerns its derivative 4-deoxybostrycin found in serveral marine isolates [ 68 , 84 , 86 , 101 , 123 ].…”

“…showed inhibitory effects against mycobacteria. 4-deoxybostrycin also showed significant inhibition of some clinical multidrug-resistant Mycobacterium tuberculosis strains (maximal inhibitory concentration <15.7 μM) [ 123 ].…”

Endophytic fungi: a reservoir of antibacterials

“…of the South China Sea. These compounds are active against M. tuberculosis and clinical multidrug-resistant (MDR) M. tuberculosis strains with MIC values of <5–> 60 μ g/mL (Wang et al, 2013b ).…”

Synthesis and Characterization of New 1‐(4‐Methylpiperazin‐1‐yl)thioureas as Potential Antitubercular Agents

“…The size of the zone of inhibition was related to increasing amounts of the test compound and consistent with a concentration dependence of growth inhibition (see Experimental). Since a larger zone of inhibition corresponds to a more effective test compound , these results were indicative of promising activity and will warrant further investigations of the antimycobacterial character of IIIr and its congeners.…”