Current Macrolide Antibiotics and Their Mechanisms of Action

Lohsen, Sarah; Stephens, David S.

doi:10.1002/9781119282549.ch5

Cited by 4 publications

(4 citation statements)

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“…The combination with vitamin D greatly enhanced the bacteriocidal potential of Azithromycin. Interestingly, emerging reports from literatures suggests macrolide antibiotics inhibit bacterial protein synthesis by binding to the 50s ribosomal subunit hence disrupting ribosomal RNA molecule and various ribosomal proteins [24]. The vitamin D used in this study may have influenced the binding of azithromycin to the 50s ribosomal subunit which resulted to increased effectiveness of azithromycin against our isolate.…”

Section: Discussionmentioning

confidence: 78%

Activities of Macrolides in Combination with Vitamin D against Bacillus cereus Isolated from Soil of a Lanfill Site in Nsukka South East Nigeria

Ekwebelem

Obinna

2020

IJPR

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Background: The fast moving world of antibiotics resistance is now a big concern, since our antibiotics are in danger of extinction. This is a concern to us because; an empty ‘antibiotic pipeline’ leads to devastating future. Aim: The aim of this study was to isolate Bacillus cereus from soil contaminated with various toxic and domestic wastes and investigate its sensitivity to macrolide antibiotics (erythromycin ERY and azithromycin AZM) in combination with vitamin D supplement. Methodology: Five soil samples were collected from a landfill site and serially diluted up to 10ˉ6. B. cereus was isolated from the soil sample using Mannitol egg Yolk Polymyxin agar medium (MYP), a selective nutrient medium for B. cereus isolation. The sensitivity of B. cereus to erythromycin and azithromycin was screened in Mueller-Hinton agar (MHA) containing varying concentrations (5, 10, 20 mg/ml) of vitamin D. Agar without vitamin D (0.00mg/ml) served as the control. The activities of ERY and AZM in combination with vitamin D were determined by measuring the zones of inhibition. Results: In vitro antibiotic susceptibility tests on our isolate showed maximum sensitivity to ERY and maximum resistance to AZM with 0.00 mg/ml (no combination) of vitamin D. Contrarily, ERY was found to be least active, with the zones of inhibitions decreasing from 28mm to 16mm, with increasing concentration of vitamin D. On the other hand, AZM achieved maximum sensitivity from 12mm to 25mm, with increasing concentration of vitamin D. Conclusion: The activities appeared to be important but dose-dependent. So, the systematic use of Vitamin D in combination with macrolide antibiotics may be efficient in treating food and soil infections caused B. cereus. However, in vivo evaluation of these activities is needed.

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Section: Discussionmentioning

confidence: 78%

Activities of Macrolides in Combination with Vitamin D against Bacillus cereus Isolated from Soil of a Lanfill Site in Nsukka South East Nigeria

Ekwebelem

Obinna

2020

IJPR

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“…(B) Significant chemical structure differences between telithromycin and solithromycin which might combat resistance mechanism of GO (Images modified by the author). (Berg et al, 2002;Carlson-banning & Zechiedrich, 2013;Clarkson, 2018;Donald et al, 2017;Fernandes et al, 2016;Ian & Marilyn, 2001;Lohsen & Stephens, 2019;NCBI, 2020aNCBI, , 2020bNg et al, 2002;Sergeeva et al, 2014;Serio et al, 2017;Tenson et al, 2003).…”

Section: Development Of Solithromycin Research In Vitro Researchmentioning

confidence: 99%

Solithromycin as A Potential Novel Antibiotic Against Neisseria Gonorrhoeae Resistance

Habiburrahman¹,

Soetikno²,

Sirait³

et al. 2020

Indonesian J Pharm

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Gonorrhea is one of the most often sexually transmitted infection in the world. In 2016, WHO stated the Southeast Asia region as the fourth-highest incidence rate and prevalence of gonorrhea. One of the current problems with gonorrhea is related to its emerging resistance to first-line drugs such as cephalosporins, macrolides, and fluoroquinolones. This resistance has an impact on the difficulty of finding effective antibiotics to eradicate the infection, thus risking financial loss and infertility in sexually active age patients. This literature review will discuss solithromycin, the first fluoroketolide in phase III clinical trial, and show its potential as a new antibiotic against infection with resistant Neisseria gonorrhoeae. Literatures are searched using Pubmed and Google Scholar search engines with keywords: antibiotics, CEM-101, clinical trial, Neisseria gonorrhoeae, new treatment, pharmacology, pharmacokinetics, resistance, safety, and solithromycin. This semisynthetic antibiotic is supported by a different chemical structure from previous macrolides; improving solithromycin becomes more stable and able to bind easier with bacterial ribosomes. Pharmacologically, solithromycin provides an advantage in its high bioavailability, easy oral administration route, wide distribution, metabolism mainly in the liver, but not required dosage adjustments due to hepatic impairment, and a single dosage preparation that can increase patient compliance in healing gonorrhea infections. Also, its lower MIC50 than previous antibiotics makes it well-tolerated, therefore making this antibiotic as a potential recommendation for the management of multi-drug resistant gonorrhea in the future. Solithromycin is not inferior to the standard therapy (ceftriaxone and azithromycin), with 80% vs. 84% gonorrhea eradication rates. Per the anatomic site, the eradication rate is 92% in genital, 94% in the pharynx, and 83% in the rectum. However, special attention needs to be paid to the side effects of the gastrointestinal tract of solithromycin, as observed in phase III clinical trials at a dose of 1000 mg in the form of diarrhea (24%) and nausea (21%).

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“…γ-lactones are estimated to be present in nearly “10% of all-natural compounds” [ 1 ], δ-lactones appear in a lower percentage, especially as fragrant components in fruits and essential oils, while macrocyclic lactones show up in a small amount, but in numerous active compounds. Lactones are present in pheromones, macrolide antibiotics [ 6 ], and numerous naturally occurring lactones that are also extensively studied for their cytotoxic activity against cancers, and for their anti-bacterial and anti-fungal activity [ 7 ]. Though prostaglandins were found in numerous marine organisms in the 1970s and reviewed recently [ 8 ], prostaglandin lactones were discovered only in the molluscs [ 9 ] nearly 14 years after the synthesis of the first prostaglandin lactones, PGF 2α -1,9-lactone 1 and PGF 2α -1,15-lactone 2 ( Figure 1 ) [ 10 ].…”

Section: Introductionmentioning

confidence: 99%

Lactones in the Synthesis of Prostaglandins and Prostaglandin Analogs

Tănase

Pintilie

Tănase

2021

IJMS

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In the total stereo-controlled synthesis of natural prostaglandins (PGs) and their structural analogs, a vast class of compounds and drugs, known as the lactones, are encountered in a few key steps to build the final molecule, as: δ-lactones, γ-lactones, and 1,9-, 1,11-, and 1,15-macrolactones. After the synthesis of 1,9-PGF2α and 1,15-PGF2α lactones, many 1,15-lactones of E2, E3, F2, F3, A2, and A3 were found in the marine mollusc Tethys fimbria and the quest for understanding their biological role stimulated the research on their synthesis. Then 1,9-, 1,11-, and 1,15-PG lactones of the drugs were synthesized as an alternative to the corresponding esters, and the first part of the paper describes the methods used for their synthesis. The efficient Corey procedure for the synthesis of prostaglandins uses the key δ-lactone and γ-lactone intermediates with three or four stereocenters on the cyclopentane fragment to link the PG side chains. The paper describes the most used procedures for the synthesis of the milestone δ-Corey-lactones and γ-Corey-lactones, their improvements, and some new promising methods, such as interesting, new stereo-controlled and catalyzed enantioselective reactions, and methods based on the chemical/enzymatic resolution of the compounds in different steps of the sequences. The many uses of δ-lactones not only for the synthesis of γ-lactones, but also for obtaining 9β-halogen-PGs and halogen-substituted cyclopentane intermediates, as synthons for new 9β-PG analogs and future applications, are also discussed.

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Current Macrolide Antibiotics and Their Mechanisms of Action

Cited by 4 publications

References 99 publications

Activities of Macrolides in Combination with Vitamin D against Bacillus cereus Isolated from Soil of a Lanfill Site in Nsukka South East Nigeria

Activities of Macrolides in Combination with Vitamin D against Bacillus cereus Isolated from Soil of a Lanfill Site in Nsukka South East Nigeria

Solithromycin as A Potential Novel Antibiotic Against Neisseria Gonorrhoeae Resistance

Lactones in the Synthesis of Prostaglandins and Prostaglandin Analogs

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