Topic
Boromycin
About: Boromycin is a research topic. Over the lifetime, 45 publications have been published within this topic receiving 1260 citations.
Papers
TL;DR: In this article, it was shown that boromycin at a concentration of 0.05 μg/ml inhibits the synthesis of protein, RNA and DNA in whole cells of Bacillus subtilis.
Abstract: Boromycin, at a concentration of 0.05 μg/ml inhibits the synthesis of protein, RNA and DNA in whole cells of Bacillus subtilis. It is being antagonised by surface active compounds and is being bound to lipoprotein. Binding of the boromycin within the cell especially takes place at the cytoplasmic membrane. The inhibitory effect to Bacillus subtilis is being reversed by high concentration of potassium salts (e.g. 0.2 m KCl). The reversion is specific of potassium salts. After the adding of boromycin a discharge of potassium ions from the cells can be observed. The K+-Na+-activated ATP-ase of the cytoplasmic membrane is not influenced by boromycin. On an artificial membrane of carbon tetrachloride boromycin shows a low selectivity for potassium ions compared with sodium and lithium ions. The degradation of boromycin through alkaline and acid hydrolysis leads to a loss of antibiotic activity, due to the splitting off the boric acid from the molecule.
283 citations
TL;DR: Semi-metals (boron, silicon, arsenic and selenium) form organo-metal compounds, some of which are found in nature and affect the physiology of living organisms, and are often used as analogues of important pharmacological sulfur compounds.
121 citations
TL;DR: The structure II of boromycin C45H74BNO15 (cf. [2]) has been established by combination of chemical evidence with X-ray analysis.
Abstract: The structure II of boromycin C45H74BNO15 (cf. [2]) has been established by combination of chemical evidence with X-ray analysis. The antibiotic is a D-valine ester of a Boeseken-complex of boric acid with a macrodiolide of a new type.
114 citations
TL;DR: New antibiotics were isolated from the culture broth of the myxobacterium, Sorangium cellulosum, strain So ce 678, and named tartrolon A and B, which were active against Gram-positive bacteria and mammalian cells.
Abstract: New antibiotics were isolated from the culture broth of the myxobacterium, Sorangium cellulosum, strain So ce 678. The antibiotics were active against Gram-positive bacteria and mammalian cells. They were named tartrolon A and B. Tartrolon B contains a boron atom. The boron binding region of tartrolon is identical with that of boromycin and aplasmomycin.
93 citations
TL;DR: The results suggest that targeting mycobacterial transmembrane ion gradients may be an attractive chemotherapeutic intervention level to kill otherwise drug tolerant persister bacilli, and to slow down the development of genetic antibiotic resistance.
Abstract: Boromycin is a boron-containing polyether macrolide antibiotic isolated from Streptomyces antibioticus. It was shown to be active against Gram positive bacteria and to act as an ionophore for potassium ions. The antibiotic is ineffective against Gram negative bacteria where the outer membrane appears to block access of the molecule to the cytoplasmic membrane. Here we asked whether boromycin is active against Mycobacterium tuberculosis which, similar to Gram negative bacteria, possesses an outer membrane. The results show that boromycin is a potent inhibitor of mycobacterial growth (MIC50 = 80 nM) with strong bactericidal activity against growing and non-growing drug tolerant persister bacilli. Exposure to boromycin resulted in a rapid loss of membrane potential, reduction of the intracellular ATP level and leakage of cytoplasmic protein. Consistent with boromycin acting as a potassium ionophore, addition of KCl to the medium blocked its antimycobacterial activity. In contrast to the potent antimycobacterial activities of the polyether macrolide, its cytotoxicity and haemolytic activity were low (CC50 = 30 μM, HC50 = 40 μM) with a selectivity index of more than 300. Spontaneous resistant mutants could not be isolated suggesting a mutation frequency of less than 10(-9)/CFU. Taken together, the results suggests that targeting mycobacterial transmembrane ion gradients may be an attractive chemotherapeutic intervention level to kill otherwise drug tolerant persister bacilli, and to slow down the development of genetic antibiotic resistance.
74 citations
Related Topics (5)
Performance Metrics
| Year | Papers |
|---|---|
| 2021 | 1 |
| 2018 | 1 |
| 2016 | 1 |
| 2014 | 1 |
| 2012 | 1 |
| 2010 | 1 |