IS p-AMINOBENZENESULPHONAMIDE THE ACTIVE AGENT IN PRONTOSIL THERAPY ?

Fuller, A. T.

doi:10.1016/s0140-6736(00)97447-6

Cited by 158 publications

(41 citation statements)

References 2 publications

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“…concurrently, this conversion was the first known prodrug activation by gut bacteria, as metabolite sulfanilamide was found to have antibacterial effect. azoreductases produced by the large intestinal microbiota are responsible for the reduction of the azo bond 54 . prontosil is metabolized to sulfanilamide also in the liver and kidney (Fig.…”

Section: Azo Reductionmentioning

confidence: 99%

Human gut microbiota plays a role in the metabolism of drugs

Jourová¹,

Anzenbacher²,

Anzenbacherová³

2016

Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub

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a Background and Aims. The gut microbiome, an aggregate genome of trillions of microorganisms residing in the human gastrointestinal tract, is now known to play a critical role in human health and predisposition to disease. It is also involved in the biotransformation of xenobiotics and several recent studies have shown that the gut microbiota can affect the pharmacokinetics of orally taken drugs with implications for their oral bioavailability. Methods. Review of Pubmed, Web of Science and Science Direct databases for the years 1957-2016. Results and Conclusions. Recent studies make it clear that the human gut microbiota can play a major role in the metabolism of xenobiotics and, the stability and oral bioavailability of drugs. Over the past 50 years, more than 30 drugs have been identified as a substrate for intestinal bacteria. Questions concerning the impact of the gut microbiota on drug metabolism, remain unanswered or only partially answered, namely (i) what are the molecular mechanisms and which bacterial species are involved? (ii) What is the impact of host genotype and environmental factors on the composition and function of the gut microbiota, (iii) To what extent is the composition of the intestinal microbiome stable, transmissible, and resilient to perturbation? (iv) Has past exposure to a given drug any impact on future microbial response, and, if so, for how long? Answering such questions should be an integral part of pharmaceutical research and personalised health care.

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Section: Azo Reductionmentioning

confidence: 99%

Human gut microbiota plays a role in the metabolism of drugs

Jourová¹,

Anzenbacher²,

Anzenbacherová³

2016

Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub

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“…The ability of the gut microbiome to contribute to the metabolism of drugs has been recognized for over 80 years (Fuller, 1937). While inactive in vitro against most bacteria, the first ever antibiotic prontosil was effective in animals.…”

Section: Mastering Microbial Metabolismmentioning

confidence: 99%

“…While inactive in vitro against most bacteria, the first ever antibiotic prontosil was effective in animals. Subsequent studies would reveal that microbial cleavage of the azo bond yields the antibiotic sulphanilamide (Fuller, 1937). Not all microbial drug metabolism is beneficial.…”

Section: Mastering Microbial Metabolismmentioning

confidence: 99%

How to Determine the Role of the Microbiome in Drug Disposition

et al. 2018

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With a paradigm shift occurring in health care towards personalized and precision medicine, understanding the numerous environmental factors that impact drug disposition is of paramount importance. The highly diverse and variant nature of the human microbiome is now recognized as a factor driving inter-individual variation in therapeutic outcomes. The purpose of this review is to provide a practical guide on methodology that can be applied to study the effects of microbes on the absorption, distribution, metabolism, and excretion of drugs. We also highlight recent examples of how these methods have been successfully applied to help build the basis for researching the intersection of microbiome and pharmacology. While in vitro and in vivo preclinical models are highlighted, these methods are also relevant in late-phase drug development or even as a part of routine after-market surveillance. These approaches will aid in filling major knowledge gaps for both current and upcoming therapeutics with the long-term goal of achieving a new type of knowledge-based medicine that integrates data on the host and the microbiome.

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“…The biological reduction of azo compounds to release aromatic amines had been previously demonstrated by a number of investigators (6)(7)(8) prior to the NTP studies of benzidine and related dyes. Further, the metabolism of four benzidinebased dyes by rhesus monkeys to benzidine was described in a brief report by Rinde and Troll (9) Table 1).…”

Section: Metabolism/disposition Ofdyesmentioning

confidence: 99%

Summary of the National Toxicology Program Benzidine Dye Initiative

Morgan¹,

Dunnick²,

Goehl³

et al. 1994

Environmental Health Perspectives

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The benzidine dye initiative is a research program established by the National Toxicology Program to generate an integrated body of scientific information regarding the potential health risks associated with exposure to benzidine-and benzidine-congener-derived dyes. Because an indepth evaluation of each of the hundreds of benzidine-congener-derived dyes was considered impractical, the research program was designed to study the metabolism and disposition, genetic toxicity, and in vivo toxicity and carcinogenicity of two primary benzidine congeners, 3,3'-dimethylbenzidine and 3,3'-dimethoxybenzidine, and a select group of prototypical dyes derived from those amines. It was anticipated that by applying the basic information generated in these extensive studies, it would be possible to make regulatory decisions about other dyes after conducting only a minimal number of experiments such as studies of disposition and metabolism, and in vitro mutagenicity. This paper summarizes the results of studies conducted to evaluate the metabolism, disposition, mutagenicity, toxicity, and carcinogenicity of representative benzidine congeners and derived dyes. -Environ Health Perspect 102(Suppl 2): 63-78 (1994).

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IS p-AMINOBENZENESULPHONAMIDE THE ACTIVE AGENT IN PRONTOSIL THERAPY ?

Cited by 158 publications

References 2 publications

Human gut microbiota plays a role in the metabolism of drugs

Human gut microbiota plays a role in the metabolism of drugs

How to Determine the Role of the Microbiome in Drug Disposition

Summary of the National Toxicology Program Benzidine Dye Initiative

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