Pharmacological Studies With Kanamycin

Abstract

Male Swiss-Webster mice weighing 18 to 22 gm. were employed.All animals were observed through 72 hours.Rats.

Biosynthetic Studies of Telomycin Reveal New Lipopeptides with Enhanced Activity

“…Compounds 9 and 10 are ringopened telomycins with different degrees of hydroxylation; they are probably intermediates released spontaneously or by catalysis of the TE domain. Compound 11 is a shunt product representing a prematurely released intermediate while compound 12 is a macrolactone formed between 2 Ser and 11 Pro instead of lactonization between 3 Thr and 11 Pro. The implications of the identification of these shunt products with different length and hydroxylation during the biosynthesis of 1 will be discussed below.…”

“…Telomycin ( 1 ) is a peptide antibiotic produced by Streptomyces canus C159, which was described as an effective antibiotic against Gram-positive pathogens when initially isolated at the Bristol-Myers Company (New York, USA) in the 1950s. − It was demonstrated to inhibit Staphylococcus aureus (SA) with a minimal inhibitory concentration (MIC) of 8 μg/mL and even penicillin-resistant SA with a slightly higher MIC . In the 1960s, a first partial structure of telomycin containing a permutation of three amino acids was published. , Two nuclear magnetic resonance (NMR) based studies on telomycin in 1973 provided the correct structure of the complex molecule. , Telomycin ( 1 , Chart ) is a cyclic depsipeptide which is composed of 11 amino acids including five non-proteinogenic ones.…”

Structural diversity, biosynthesis, and biological functions of lipopeptides fromStreptomyces

“…Telomycin (TEM) is a cyclic depsipeptide initially isolated from an unidentified Streptomyces , and later was found to be produced by S. canus ATCC 12646 and Micromonospora schwarzwaldensis HKI0641. 99–103 Whilst not isolated in acylated form, the biosynthesis of telomycin involves N-terminal acylation that is removed as a part of the maturation process (hence its inclusion in this section, vide infra ). Telomycin displays activity against Gram-positive bacteria but less so towards Gram-negative bacteria.…”

Revision of the full stereochemistry of telomycin

“…9 The antibiotic telomycin, a non-ribosomal cyclic depsipeptide originally isolated from an unidentified Streptomyces strain by scientists at Bristol-Myers at the end of the 1950sduring the 'golden era' of antibiotic discovery -, belongs to this last category. [10][11][12] Telomycin displays potent bactericidal activity against a wide range of Gram-positive bacteria. 11,13 In 2016, within the context of an assembly and clustering study of antibacterial natural products to guide target identification based on a novel retrobiosynthetic algorithm, Magarvey and co-workers identified telomycin from S. canus ATCC 12647 14 as an under-represented chemical scaffold with potential to possess an uncharacterized molecular target.…”

“…This phospholipid dimer is present in the membranes of nearly all bacteria and archaea. [17][18][19][20] Interestingly, telomycin is not hemolytic and does not possess significant toxicity neither to mammals nor towards mammalian cell lines, 12 in which the target phospholipid cardiolipin is only present in the inner mitochondrial membrane. [17][18][19][20] On the other hand, the oral bioavailability of some members of the telomycin family has been reported.…”