Apoptolidin A was first isolated as a secondary metabolite of a Nocardiopsis sp. and is the founding member of a family of potential selective cancer cell toxins. We now report the isolation, production and pharmacological characterization of apoptolidins A and C from an alternate actinomycete p...

Oligomycin A, an inhibitor of mitochondrial ATP synthase, provokes simultaneous and different responses in IPLB-LdFB insect cell line. The oligomycin A treatment causes mitochondrial loss, increase in reactive oxygen species (ROS), destabilization/reorganization of the actin microfilaments and, ...

Recently published X-ray structures of three common forms, A, B and C, of oligomycin, including absolute configurations, are investigated to examine their binding to ATP Synthase. The X-ray studies reveal regions with differences in three-dimensional structure and hydrogen bonding propensity bet...

We investigated the effects of oligomycin, an F1FO-ATPase inhibitor, on ischemic acute kidney injury in male and female rats. Ischemic acute kidney injury was induced by clamping the left renal artery and vein for 45 or 60 min followed by reperfusion, 2 weeks after contralateral nephrectomy. Ren...

The antibiotic oligomycin is known to inhibit mitochondrial F-type ATP synthases. The antibiotic inhibits both ATP synthesis and hydrolysis by blocking the H+ translocation through FO which is coupled to the catalytic activity of F1. The amphiphilic organotin tri-n-butyltin (TBT), a known mitoch...

SummaryAn actinobacterial strain, HG29, with potent activity against pathogenic, toxigenic and phytopathogenic fungi was isolated from a Saharan soil sample of Algeria. On the basis of morphological and chemotaxonomic characteristics, the strain was classified in the genus Streptomyces. Analysis...

A novel way of chemical modification of the macrolide antibiotic oligomycin A (1) at the side chain was developed. Mesylation of 1 with methane sulfonyl chloride in the presence of 4-dimethylaminopyridine produced 33-O-mesyl oligomycin in 56% yield. Reactions of this intermediate with sodium azi...

The mitochondrial F1F0 complex is highly sensitive to macrolide antibiotics and especially targeted by oligomycins. These compounds bind to the membrane-embedded sector F0 and block proton conductance through the inner membrane, thus inhibiting both ATP synthesis and hydrolysis. Oligomycin sensi...

The interaction of nogalamycin (NOM), an anthracycline antitumor drug, with calf thymus DNA has been studied by cyclic voltammetry (CV) and differential pulse voltammetry (DPV). The variations in the cyclic voltammetric behaviour of NOM on addition of DNA have been carried out. The experimental ...

The voltammetric behaviour of nogalamycin (NOG), an important antitumor drug, has been studied at a hanging mercury drop electrode (HMDE). The nature of the process taking place at the HMDE was clarified. A highly sensitive cathodic adsorptive stripping (CAS) voltammetric method for the determin...

This review assimilates up-to-date information on the biochemical pharmacology of nogalamycin and selected derivatives that have shown good biological activities and/or received a relatively detailed investigation. The structure and chemical preparation of these derivatives from nogalamycin is d...

SummaryNogalamycin is an anthracycline polyketide antibiotic that contains two deoxysugars, at positions C-1 and C-7. Previous biosynthetic studies conducted in vivo affiliated snoaL2 with an unusual C-1 hydroxylation reaction, but in vitro activity was not established. Here, we demonstrate that...

A new approach to the total synthesis of anthracycline natural products, nogalamycin and menogaril, was explored. The goal was to enable late-stage introduction of the EF-ring segment. The new synthetic route has been developed through strategic application of a Suzuki-Miyaura reaction as the ke...

The structural changes of DNA, induced by the antitumour antibiotic nogalamycin, have been studied by atomic force microscopy (AFM). The transformation in the tertiary structure of 4361 bp long plasmid pBR322 DNA, after incubation with nogalamycin at 37 °C, has been monitored at the single mole...

A new process has been described for the preparation of coenzyme A of high purity. Pantothenic acid, cysteine and AMP when added to cultures of Brevibacteriumammoniagenes IFO 12071 gave coenzyme A in a high yield. The product was obtained by using Duolite S-30, charcoal and Dowex 1-X2. This meth...

Drugs may be metabolised to reactive electrophilic species that spontaneously react with proteins. The presence of such drug–protein adducts has been associated with drug toxicity. In this study, the reactivity of the major metabolite of naproxen—the 1-β-O-glucuronide (Nap-GlcU)—was compared...

SummaryFluoroacetyl-CoA was synthesized from sodium fluoroacetate via its anhydride. With fluoroacetyl-CoA as the only substrate and a crude mitochondrial extract from Dichapetalum cymosum as enzyme source, CoASH release took place at a rate of 0.0295 μmoles/min/ mg protein, indicating the pres...

Pathogenic Gram-negative bacteria are a major public health concern because they are causative agents of life-threatening hospital-acquired infections. Due to the increasing rates of resistance to available antibiotics, there is an urgent need to develop new drugs. Acetyl-coenzyme A carboxylase ...

α-Methylacyl-coenzyme A racemase (AMACR) catalyzes the epimerization of (2R)- and (2S)-methyl branched fatty acyl-coenzyme A (CoA) thioesters. AMACR is a biomarker for prostate cancer and a putative target for the development of therapeutic agents directed against the disease. To facilitate dev...

Rational approaches for the design of enzyme inhibitors furnish powerful strategies for developing pharmaceutical agents and tools for probing biological mechanisms. A new strategy for the development of gem-disubstituted substrate-product analogues as inhibitors of racemases and epimerases is e...