ABSTRACT
Trichostatins are potent inhibitors of histone deacetylase (HDAC). In this work, a new trichostatin derivative isotrichostatin RK (1) and five known compounds trichostatin RK (2), JBIR-111 (3), 9179B (4), trichostatic acid (5) and trichostatin A (6) were isolated from marine-derived Streptomyces sp. SCSIO 40028. The biosynthetic gene cluster (tsnB) for trichostatins was identified from Streptomyces sp. SCSIO 40028 and validated by heterologous expression in Streptomyces lividans TK64. N-Methyltransferase TsnB8 was demonstrated to catalyze successive methyltransfer reactions by in vivo gene inactivation and in vitro enzyme assays.
Subject(s)
Hydroxamic Acids/pharmacology , Methyltransferases/antagonists & inhibitors , Hydroxamic Acids/chemistry , Hydroxamic Acids/metabolism , Methyltransferases/metabolism , Molecular Structure , Multigene Family , Streptomyces/enzymologyABSTRACT
The incidence of bacterial disease has increased tremendously in the last decade, because of the emergence of drug resistance strains within the bacterial pathogens. The present study was to investigate the antibacterial compound 2,5-di-tert-butyl-1,4-benzoquinone (DTBBQ) isolated from marine Streptomyces sp. VITVSK1 as a potent antibacterial agent. The antibacterial potential of DTBBQ was investigated against RNA Polymerase (PDB ID-1I6V) by in silico molecular docking tools. Results of our study showed the high affinity interaction between DTBBQ and RNA polymerase and also confirmed the drug likeliness of DTBBQ using ADMET in silico pharmacology tools. Our findings suggest that DTBBQ could be used as antibacterial drug to defend the emerging antibacterial resistance.
