The peptide antibiotic Bacitracin:
Bacitracin is a cyclic polypeptide antibiotic that was first discovered in 1945 by Johnson et al. and is produced as a mixture of different similar peptides by certain strains of Bacillus subtilis and Bacillus lichenformis. The main compound is bacitracin A and its structure can be seen in Figure X. (Johnson 1945, Strominger 1971, Konz 1997). It is produced nonribosomally by a multienzyme complex composed of the three bacitracin synthetases BA1-3 by a so called thiotemplate mechanism. In this mechanism, adenylated amino acids are activated by hydrolysis of AMP and added to the enzyme, where it is bound as a thioester on the covalently bound 4-phosphopentatheinyl-cofactor. The polypeptide is then produced in a series of transpeptidation reactions (Konz 1997).
Figure X: Sequence and structure of Bacitracin A. The amino acids from L-Lys to L-Asn form the heptapeptide ring and the second cysteine forms the thiazoline ring with the backbone.
The mechanism by which bacitracin inhibits cell growth is by targeting the cell wall synthesis. This is achieved by binding to undecaprenol-pyrophosphate (UPP, C55-PP), which functions as a lipid carrier of peptidoglycan (PG) intermediates during the synthesis of the cell wall, transporting the intermediates from one side of the membrane to the other.
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The cycle starts with UP, which is produced by dephosphorylation of UPP either through recycling or from de novo synthesis. UPP is then coupled to activated MurNAc-pentapeptide by MraY and activated GlcNAc is added by MurG in a second step to form Lipid II. This is transported across the membrane by the flippase FtsW and the GlcNAc-MurNAc-pentapeptide is transferred to the growing peptidoglycan chains. The UPP in the outer leaflet has to be dephosphorylated and transported back to the inner leaflet for the cycle to complete. Bacitracin binds to UPP and inhibits
The most striking aspect of the financial overview of medicine was the limitations of the Affordable Care Act (ACA). Even before the lecture, it was clear to me that from the inception of the law that care accessibility would be prioritized over cost and quality. However, the lecture helped me realize how myopic my understanding of the consequences were for patients.
My coworker had a 40-year-old patient who came to the hospital for alcohol withdrawal. All the nurses on our floor knew him really well because he visits our hospital frequently. At around 7:30 pm, our telemetry showed that the patient was having a heart rate of 180s to190s. We all were still getting report. Charge nurse went to assess the patient, patient started yelling in a loud voice, throwing pillows and a blanket. It turned out that the patient went to the delirium tremens (DT) phase. He was confused, disoriented, hallucinating, agitated, irritated and had muscle tremor. When reviewing the medication administration record (MAR), charge nurse noticed that CIWA scale was not done as ordered and as a result patient did not get enough Lorazepam
In 1995, the FDA approved a miracle drug, which would aid in a person's ability to cope with the severe pain associated with cancer. Purdue Pharma L.P. of Stamford, Connecticut, introduced the wonder drug that would eventually be the demise of many. Oxycotin would, for several, lead to addiction, criminal behaviors, and, for some, their lives. The intent of releasing the drug was solely to treat patients suffering from chronic pain. Since the release of the drug, doctors are now prescribing the medicine for moderate pain as well. Patients have become extremely addicted and have gone to extreme lengths to obtain the "poor man's heroin," which may include criminal activities. Recovering addicts endure an
Enoxaparin is a low molecular weight heparin used to prevent thrombosis, particularly post surgery. Enoxaparin binds to antithrombin III which is responsible for inhibiting coagulation by acting on factor Xa. Enoxaparin accelerates the activity of antithrombin III therefore preventing clot formation (McKenna & Lim, 2014 p766). When a blood vessel is damaged, platelets in circulating blood stick to the site of injury and release chemicals that attract more platelets causing aggregation. There are both intrinsic and extrinsic pathways causing thrombi to form to maintain a closed cardiovascular system (Hollar, 2017). Immobility increases risk of thrombus formation as the blood becomes stagnant with gravity and decreased
In vitro: A non-toxic concentration of enniatin B could strongly inhibit a Pdr5p-mediated efflux of cycloheximide or cerulenin in Pdr5p-overexpressing cells. The mode of Pdr5p inhibition caused by enniatin B was competitive against FK506. However, enniatin B could not inhibit the function of Snq2p, a homologue of Pdr5p [1]. Another study showed that enniatin B was a relatively poor ionophore that could facilitate import of K+ and Na+ across membranes [2]. It was also found that like other enniatins, enniatin B was able to inhibit acyl-CoA: cholesterol acyltransferase [3].
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Uric acid is produced through the breakdown of hypoxanthine and xanthine, and this breakdown is catalyzed by the enzyme xanthine oxidase (XO). High uric acid levels in the human body leads to the formation of gout. Gout is commonly treated with allopurinol, a synthetic chemical drug. However, allopurinol elicits many side effects and induces adverse drug reactions. As such, alternative natural drugs have been introduced to reduce side effects. In this study, the XO inhibitory activity of Morinda citrifolia L. leaves were investigated to evaluate the efficacy of this herb as a substitute for allopurinol. Dried, powdered plant materials were subjected to separate extraction using three solvents, particularly 95% ethanol (EE), methanol (ME), and
Doxycycline, a semi-synthetic derivative of oxytetracycline is a potent antibacterial drug commonly used as doxycycline hyclate (DOX-h) and used for both in humans and animals treatments [8]. The antibacterial mechanism is mainly regarded as time-dependant and DOX-h is a relatively inexpensive antibacterial drug, potent and possesses a broad-spectrum antibacterial action [9]. In this regard, a poloxamer-based matrix was used to produce a long-acting injectable preparation (DOXh-LA) and its serum concentrations vs. time profile was investigated after its s.c. injection to calves. It was found that the DOX-h-LA showed the greatest values for bioavailability (602%); maximum serum concentration (Cmax) of 1.99 lg/mL with a time to reach (Tmax)
The management of Warfarin is complicated because of its intricate pharmacokinetic and pharmacodynamic properties and narrow therapeutic range. Having optimal outcomes as a result of Warfarin therapy depends on maintaining the INR (International Normalized Ratio) in its range. In order to do so, high-quality anticoagulation management (HQACM) is required. HQACM involves reaching efficacy through acts such as appropriate therapy initiation, maintenance of therapeutic anticoagulation measured through TTR, monitoring anticoagulation at the appropriate frequency, managing peri-operative dosing and managing nontherapeutic INRs, as well as measuring safety through bleeding management, patient education and extensive communication. The goals of Warfarin management include obtaining the highest efficacy to prevent thromboembolism and minimizing risk to prevent bleeding. The most known method used for calculating the therapeutic effectiveness of Warfarin over a period of time is TTR. There are many factors such as medications, diet, and concomitant disease states that can alter the pharmacokinetics of Warfarin, therefore,
A prodrug in order to elicit required pharmacological effect, must be converted enzymatically or chemically to the parent drug in vivo. The prodrug approach was widely used to overcome various problems associated with absorption, tumor targeting, distribution, pharmacokinetics, premature metabolism, occurrence of side effects, and patient compliance46-51. The concept of the prodrug was first applied to steroids in ophthalmology to improve the corneal absorption, aqueous solubility and patient compliance 52. The first prodrug dipivefrin (a prodrug of epinephrine) for ophthalmic use was formally introduced in the late 1970s for enhancing ocular bioavailability of epinephrine 53.
Loratadine HCl (LOR) , which is chemically designated as ethyl 4 (8-chloro 5,6 dihydro,11H- benzo[5,6] cyclohepta[1,2 b]pyridin- 11- ylidene) -1- piperidinecarboxylate Hydrochloride is a tricyclic, piperidine derivative of antihistamines [1,2]. It is a second generation antihistamines, so it has non–sedating properties. Loratadine are newer drugs that are much more selective for peripheral H1 receptors as opposed to the central nervous system H1 receptors and cholinergic receptors. H1 antihistamines are applied in the treatment of allergies, they prevent symptoms such as itching, congestion, rhinorrhoea, tearing and sneezing. This selectivity significantly reduces the occurrence of adverse drug reactions, such as sedation, while
The Action Plan synthesizes all the marketing decisions that were made up to this point into an effective plan for activation. New target segments were identified in order to ensure Aleve’s continued growth. For example, younger body pain consumers could be targeted with the same functional and emotional benefits as arthritis sufferers: ease of mobility and freedom to do what they choose. Liquid gel tablets were eventually advertised to these consumers as a modern product with fast pain relief that fulfilled their active lifestyle.
Today, some of the most commonly used and most important antibiotics in modern medicine are derived from a form of chemical synthesis having to do with constructing polyketide chains. Much like fatty acid synthesis, in this mechanism, polyketides are one-by-one added to the end of the polyketide chain by[modular enzymes in an assembly-line fashion. These polyketides are the intermediates of metabolism, metabolites, in fungi, bacteria, plants, and animals. To put the importance of polyketide chain assembly, some of the most important and commonly used antibiotics in modern medicine, such as Avermectin, clarithromycin, and azithromycin, are synthesized through polyketide chain assembly.
The main objective of this experiment is to investigate the effect of different types of antibiotics on bacteria Bacillus subtilis and Escherichia coli. Some of the main methods used in this experiment
Bayan Telecommunications, Inc. (BayanTel) is a telecommunications company serving areas in Metro Manila, Bicol and local exchange service areas in the Visayas and Mindanao regions combined cover a population of over 25 million, nearly 33% of the population of the Philippines.