Arsenical antibiotics

Of historical interest, arsenical antibiotics (8.107) were once used to treat syphilis and mercurial diuretics (8.108) were once used to treat edema and to promote water excretion. Due to their high toxicity, neither is currently used. 

Before antibiotics were available, infections were often treated with moderate levels of poisons like strychnine or arsenic. Antibiotics target the disease without harming the patient, and they have saved millions of lives. Unfortunately, some bacteria in antibiotic resistant strains have developed defenses against these chemicals since they first became available over 60 years ago. New antibiotics are developed every year in an effort to continue the suppression of bacterial diseases. 

One type of fatty liver that has been smdied extensively in rats is due to a deficiency of choline, which has therefore been called a lipotropic factor. The antibiotic puromycin, ethionine (a-amino-y-mercaptobu-tyric acid), carbon tetrachloride, chloroform, phosphorus, lead, and arsenic all cause fatty liver and a marked reduction in concentration of VLDL in rats. Choline will not protect the organism against these agents but appears to aid in recovery. The action of carbon tetrachloride probably involves formation of free radicals... 

At the present time we are faced with the real and frightening threat of a post-antibiotic era in years to come, where our existing antibiotic arsenal will become largely ineffective against bacterial infections. 

At the beginning of the twentieth century, arsenic compounds were used to kill spirochete bacteria, which cause the sexually transmitted disease syphilis. After this amphetamine compound was used to treat syphilis in Europe, the disease rate was reduced by more than half. The antibiotic penicillin has replaced arsenic for most medical purposes... 

Those siderophores with low molecular weight, nonpeptidal structures are anticipated to be stable to proteolytic enzymatic degradation, and less likely to evoke an immune response. The antibiotic can be selected from commercial sources or from a large arsenal of potential antibiotics with low solubility that were overlooked, or never underwent extensive clinical investigations. 

People long ago recognized that, depending on the dose, arsenic could either treat an illness or be used as a poison to cause death. Its medicinal use to treat syphilis and amebic dysentery ended with the introduction of penicillin and other antibiotics in the twentieth century. Arsenic-based compounds are currently used to treat some forms of cancer. As a poison, arsenic trioxide (As20 ) has several desirable qualities it looks like sugar, it is tasteless, and it only takes about a tenth of gram to kill some-... 

The most important tool in the arsenal of the product innovators is the ability to make predictions on which structure would lead to what properties, as well as what structure modifications would lead to what property modifications. The reverse research from a given set of properties to material that has these properties is even more important in creating new products and in modifying existing products. In most cases of molecular properties, it is more realistic to depend on empirical correlations between structure and properties. Forward and reverse searches are currently only available for simple physical-chemical properties, such as boiling points and densities such a facility is still not available for biological properties, such as narcotic and antibiotic activities. The development of such search engines would have a tremendous impact on the productivity of product innovators. 

Buquinolate is used at a level of 82-110 ppm in the feed, often in association with arsenicals or antibiotics, for prevention of coccidiosis in chickens. Their minimal absorption by the host probably accounts for the remarkable freedom... 

Since many of the above-mentioned compounds possess major anti-infec-tious activity in addition to their role as growth promoters, their application in animal farming has already been discussed in previous chapters. Hence, this chapter concentrates on the remaining compounds within this group, namely the organic arsenicals, peptide antibiotics, quinoxaline-l,4-dioxides, and miscellaneous substances. 

Penicillin [1406-05-9] - [EXTRACTION - LIQUm-LIQUID] (Vol 10) - [ANTIPARASITIC AGENTS - ANTIPROTOZOALS] (Vol 3) - [ARSENIC COMPOUNDS] (Vol 3) - [ANTIBIOTICS- TETRACYCLINES] (Vol 3) -detection of [BIOPOLYMERS - ANALYTICAL TECHNIQUES] (Vol 4)... 

It is of historical interest that Fowler s solution, which contains 1% potassium arsenite, was widely used as a medicine for many conditions from the eighteenth century through the mid twentieth century. Organic arsenicals were the first pharmaceutical antibiotics and were widely used for the first half of the twentieth century until supplanted by penicillin and other more effective and less toxic agents. 

---