Tetracycline: Classification, Structure Activity Relationship and Mechanism of Action as a Theranostic Agent for Infectious Lesions-A Mini Review
Journal Title: Biomedical Journal of Scientific & Technical Research (BJSTR) - Year 2018, Vol 7, Issue 2
Abstract
Infectious diseases are a major cause of threat throughout the world which may have concern with microorganisms, specifically bacteria. Various antibiotics are synthesized and used against infectious diseases to mimic the death rate. The tetracyclines are a broad spectrum antibiotics discovered as natural products with exclusive biological and chemical properties against both gram-positive/negative bacteria. Many of members of this family also possess some non-antibacterial properties such as anti-inflammatory, immunosuppressant and inhibition of lipase. Various studies reveals structure activity relationship of the tetracycline family, which shows the bioactivity, strength and selectivity to biological target, specifically depends upon modification of lower and upper peripheral zones of tetracycline skeleton. The broad spectrum antibacterial activities of tetracyclines drag the attention toward labeling of tetracycline with radioisotopes for imaging of infectious lesions. For labeling purposes, optimization conditions, characterization, in-vivo and in-vitro studies are essential parameters to be studied. In clinical practice, tetracycline and three of its analogs were labeled with technetium-99m (Tc-99m) used as diagnostic agents for renal and myocardial abnormalities as well as for inflammatory disorders Graphical Abstract. Infection is a complex mechanism caused by the entrance of living microbes (bacteria, fungi and viruses) and other factors such as traumatism, physical and chemical agents which cause infection. Large number of infectious diseases causes worldwide death, so early stage diagnosis may help to reduce morbidity and mortality. Diagnosis of infectious disease involves the identification of the root cause of infectious disorders. In spite of having many advanced techniques to identify and treat infectious lesions, the world is facing a great threat of infectious diseases which is deleterious. The attention of worldwide scientists in search of antibiotic drugs was diverted after the announcement of Alexander Fleming’s discovery regarding penicillin. Various families of antibiotics have been discovered up till now and categorized based on their mechanism of action, chemical structure, or spectrum of activity. Some antibiotics have bactericidal activities to attack on the bacterial cell wall and bacterial cell membrane such as penicillins, vancomycin, isoniazid and cephalosporins polymyxins, while some antibiotics do their work by inhibiting DNA and RNA synthesis such as actinomycin, nucleotide analogs or hold up the essential bacterial enzymes like rifamycins, lipiamycins, quinolones and sulfonamides. Target specificity is another way of classification, according to which antibiotics are classified into two main groups, narrow spectrum and broad spectrum. Narrow spectrum antibiotics target specific type of bacteria such as gram positive/negative bacteria, whereas broad spectrum antibiotics act against a wide range of disease causing bacteria such as ampicillin, which is used to prevent and treat number of bacterial infections including respiratory and urinary tract infections, meningitis, salmonella infection and endocarditis [1]. Government sponsored research and development program to promote the growth of antibiotic’s research. In order to contribute toward this research in mid of 1940s a 71 years old Benjamin Minge Duggar head of the soil engineering department identified tetracycline as a therapeutic substance produced by soil microorganisms. At early stages, tetracycline was first originated as a fermentation product of golden colored soil bacterium named Streptomyces aureofacians [2]. This discovery led to many natural and semi-synthetic derivatives that expanded the spectrum of activity. Tetracycline is a class of antibiotics biologically effective and commercially available for the treatment and prevention of growth of gram positive/negative bacteria and intercellular chlamydiae, mycoplasmas and rickettsiae. It has bactericidal (destroy the bacteria) or bacteriostatic (hinder the reproduction and growth of bacteria) potential, extensively used as antibiotics for human and veterinary use [3]. They possess exclusive biological and chemical characteristics to work equally against prokaryotes and eukaryotes bacteria by interacting with different cellular targets and receptors [4]. They are very vibrant molecules because of their use in the field of neurology, oncology and virology [2]. Tetracycline is one of the cheapest classes of antibiotics, abundantly used in developing countries with limited health care budgets and have a number of non-antibacterial effects, including anti-inflammatory, immunosuppression, inhibition of lipase and collagenase activity and wound healing [5-7].
Authors and Affiliations
Saleha Tariq, Syed Faheem Askari Rizvi, Ummar Anwar
Keywords
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- EP ID EP592740
- DOI 10.26717/BJSTR.2018.07.001475
- Views 193
- Downloads 0
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