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Teicoplanin
Teicoplanin is an antibiotic used in the prophylaxis and treatment of serious infections caused by Gram-positive bacteria, including methicillin-resistant ''Staphylococcus aureus'' and '' Enterococcus faecalis''. It is a semisynthetic glycopeptide antibiotic with a spectrum of activity similar to vancomycin. Its mechanism of action is to inhibit bacterial cell wall synthesis. Teicoplanin is marketed by Sanofi-Aventis under the trade name Targocid. Other trade names include Ticocin marketed by Cipla(India). Oral teicoplanin has been demonstrated to be effective in the treatment of pseudomembranous colitis and ''Clostridium difficile''-associated diarrhoea, with comparable efficacy with vancomycin. Its strength is considered to be due to the length of the hydrocarbon chain. Teicoplanin is produced by so-called "rare" actinobacterium ''Actinoplanes teichomyceticus'' ATCC 31121, belonging to the ''Micromonosporaceae'' family. Biosynthetic pathway leading to teicoplanin, as we ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Teicoplanin P450 Oxidations
Teicoplanin is an antibiotic used in the prophylaxis and treatment of serious infections caused by Gram-positive bacteria, including methicillin-resistant ''Staphylococcus aureus'' and ''Enterococcus faecalis''. It is a semisynthetic glycopeptide antibiotic with a spectrum of activity similar to vancomycin. Its mechanism of action is to inhibit bacterial cell wall synthesis. Teicoplanin is marketed by Sanofi-Aventis under the trade name Targocid. Other trade names include Ticocin marketed by Cipla(India). Oral teicoplanin has been demonstrated to be effective in the treatment of pseudomembranous colitis and '' Clostridium difficile''-associated diarrhoea, with comparable efficacy with vancomycin. Its strength is considered to be due to the length of the hydrocarbon chain. Teicoplanin is produced by so-called "rare" actinobacterium ''Actinoplanes teichomyceticus'' ATCC 31121, belonging to the ''Micromonosporaceae'' family. Biosynthetic pathway leading to teicoplanin, as well as ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Methicillin-resistant Staphylococcus Aureus
Methicillin-resistant ''Staphylococcus aureus'' (MRSA) is a group of Gram-positive bacteria that are genetically distinct from other strains of ''Staphylococcus aureus''. MRSA is responsible for several difficult-to-treat infections in humans. It caused more than 100,000 deaths attributable to antimicrobial resistance in 2019. MRSA is any strain of ''S. aureus'' that has developed (through natural selection) or acquired (through horizontal gene transfer) a multiple drug resistance to beta-lactam antibiotics. Beta-lactam (β-lactam) antibiotics are a broad-spectrum group that include some penams (penicillin derivatives such as methicillin and oxacillin) and cephems such as the cephalosporins. Strains unable to resist these antibiotics are classified as methicillin-susceptible ''S. aureus'', or MSSA. MRSA is common in hospitals, prisons, and nursing homes, where people with open wounds, invasive devices such as catheters, and weakened immune systems are at greater risk of ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Glycopeptide Antibiotics
Glycopeptide antibiotics are a class of drugs of microbial origin that are composed of glycosylated cyclic or polycyclic nonribosomal peptides. Significant glycopeptide antibiotics include the anti-infective antibiotics vancomycin, teicoplanin, telavancin, ramoplanin and decaplanin, corbomycin, complestatin and the antitumor antibiotic bleomycin. Vancomycin is used if infection with methicillin-resistant ''Staphylococcus aureus'' (MRSA) is suspected. Mechanism and classification Some members of this class of drugs inhibit the synthesis of cell walls in susceptible microbes by inhibiting peptidoglycan synthesis. The core class (including vancomycin) binds to acyl-D-alanyl-D-alanine in lipid II, preventing the addition of new units to the peptidoglycan. Of this core class, one may distinguish multiple generations: the first generation includes vancomycin and teicoplanin, while the semisynthetic second generation includes lipoglycopeptides like telavancin, oritavancin an ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Vancomycin
Vancomycin is a glycopeptide antibiotic medication used to treat a number of bacterial infections. It is recommended intravenously as a treatment for complicated skin infections, bloodstream infections, endocarditis, bone and joint infections, and meningitis caused by methicillin-resistant ''Staphylococcus aureus''. Blood levels may be measured to determine the correct dose. Vancomycin is also taken by mouth as a treatment for severe ''Clostridium difficile'' colitis. When taken by mouth it is poorly absorbed. Common side effects include pain in the area of injection and allergic reactions. Occasionally, hearing loss, low blood pressure, or bone marrow suppression occur. Safety in pregnancy is not clear, but no evidence of harm has been found, and it is likely safe for use when breastfeeding. It is a type of glycopeptide antibiotic and works by blocking the construction of a cell wall. Vancomycin was approved for medical use in the United States in 1958. It is on the Wo ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Actinoplanes Teichomyceticus
''Actinoplanes'' is a genus in the family Micromonosporaceae. They have aerial mycelia and spherical, motile spores. ''Actinoplanes'' species produce the pharmaceutically important compounds valienamine (a precursor to the antidiabetic drug acarbose and to the antibiotic validamycin), teicoplanin, and ramoplanin Ramoplanin ( INN) is a glycolipodepsipeptide antibiotic drug derived from strain ATCC 33076 of '' Actinoplanes''. It is effective against Gram-positive bacteria. Mechanism It exerts its bacteriocidal effect by inhibiting cell wall biosynthes .... Species ''Actinoplanes'' comprises the following species: * '' A. abujensis'' Sazak et al. 2012 * "'' A. arizonaensis''" Karwowski et al. 1988 * '' A. atraurantiacus'' Zhang et al. 2012 * '' A. auranticolor'' (Couch 1963) Stackebrandt and Kroppenstedt 1988 * "'' A. aureus''" Song et al. 2021 * '' A. bogorensis'' corrig. Nurkanto et al. 2016 * '' A. brasiliensis'' Thiemann et al. 1969 (Approved Lists 1980) * '' A. camp ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Intravenous Therapy
Intravenous therapy (abbreviated as IV therapy) is a medical technique that administers fluids, medications and nutrients directly into a person's vein. The intravenous route of administration is commonly used for rehydration or to provide nutrients for those who cannot, or will not—due to reduced mental states or otherwise—consume food or water by mouth. It may also be used to administer medications or other medical therapy such as blood products or electrolytes to correct electrolyte imbalances. Attempts at providing intravenous therapy have been recorded as early as the 1400s, but the practice did not become widespread until the 1900s after the development of techniques for safe, effective use. The intravenous route is the fastest way to deliver medications and fluid replacement throughout the body as they are introduced directly into the circulatory system and thus quickly distributed. For this reason, the intravenous route of administration is also used for the cons ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Mannose
Mannose is a sugar monomer of the aldohexose series of carbohydrates. It is a C-2 epimer of glucose. Mannose is important in human metabolism, especially in the glycosylation of certain proteins. Several congenital disorders of glycosylation are associated with mutations in enzymes involved in mannose metabolism. Mannose is not an essential nutrient; it can be produced in the human body from glucose, or converted into glucose. Mannose provides 2–5 kcal/g. It is partially excreted in the urine. Etymology The root of both "mannose" and "mannitol" is manna, which the Bible describes as the food supplied to the Israelites during their journey in the region of Sinai. Several trees and shrubs can produce a substance called manna, such as the "manna tree" ('' Fraxinus ornus'') from whose secretions mannitol was originally isolated. Structure Mannose commonly exists as two different-sized rings, the pyranose (six-membered) form and the furanose (five-membered) form. Eac ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Atropisomer
Atropisomers are stereoisomers arising because of hindered rotation about a single bond, where energy differences due to steric strain or other contributors create a barrier to rotation that is high enough to allow for isolation of individual conformers. They occur naturally and are important in pharmaceutical design. When the substituents are achiral, these conformers are enantiomers (''atropoenantiomers''), showing axial chirality; otherwise they are diastereomers (''atropodiastereomers''). Etymology and history The word ''atropisomer'' ( el, άτροπος, , meaning "without turn") was coined in application to a theoretical concept by German biochemist Richard Kuhn for Karl Freudenberg's seminal ''Stereochemie'' volume in 1933. Atropisomerism was first experimentally detected in a tetra substituted biphenyl, a diacid, by George Christie and James Kenner in 1922. Michinori Ōki further refined the definition of atropisomers taking into account the temperature-dependence ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
3,5-dihydroxyphenylglycine
(''S'')-3,5-Dihydroxyphenylglycine or DHPG is a potent agonist of group I metabotropic glutamate receptors (mGluRs) mGluR1 and mGluR5. DHPG was the first agonist shown to be selective for group I mGluRs. Agonist activity is found in only the (''S'')-isomer, and (''S'')-DHPG may be a partial agonist of group I mGluRs. (''S'')-DHPG has been investigated for therapeutic effects in the treatment of neuronal injury (such as those associated with ischemia or hypoxia), cognitive enhancement, and Alzheimer's disease. 3,5-Dihydroxyphenylglycine can be isolated from the latex of ''Euphorbia helioscopia''. DHGP is also found in vancomycin and related glycopeptides. Although the (S) stereoisomer is synthesized by the DpgA-D enzymes, it is the (R) stereoisomer that is used in vancomycin and other related compounds. DHPG is enzymatically derived from the polyketide synthase pathway. Biosynthesis When synthesized in bacteria, DHPG requires 5 enzymes, DpgA-D and 4-hydroxyphenylglycine t ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
4-Hydroxyphenylglycine
4-Hydroxyphenylglycine (HPG) is a non-proteogenic amino acid found in vancomycin and related glycopeptides. HPG is synthesized from the shikimic acid pathway and requires four enzymes to synthesize: Both L- and D-HPG are used in the vancomycin class of antibiotics. Tyrosine, a similar amino acid, differs by a methylene group (CH2) between the aromatic ring and the alpha carbon. Biosynthesis : HPG is synthesized from prephenate, an intermediate in the shikimic acid pathway and also a precursor to tyrosine. Prephenate is aromatized by prephenate dehydrogenase (Pdh) using NAD+ as a cofactor to produce 4-hydroxyphenylpyruvate. 4-Hydroxyphenylpyruvate is then oxidized by 4-hydroxymandelate synthase (4HmaS) using oxygen to form 4-hydroxymandelate and hydrogen peroxide. 4HmaS is a non-heme iron-dependent dioxygenase. The reaction mechanism of this unique oxidation was proposed by Choroba ''et al'' in 2000 : 4-Hydroxymandelate is subsequently oxidized by hydroxymandelate oxidase (Hm ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
