scholarly journals An Approach to Modify 14-Membered Lactone Macrolide Antibiotic Scaffolds

2022 ◽  
Author(s):  
Anna Janas ◽  
Krystian Pyta ◽  
Maria Gdaniec ◽  
Piotr Przybylski
Keyword(s):  
Macrolide Antibiotic

Ultrastructural autoradiography of L6 skeletal-muscle cells exposed to a tritiated macrolide antibiotic (LY237216) in vitro

1992 ◽  
Vol 50 (1) ◽  
pp. 612-613
Author(s):  
S.L. White ◽  
C.B. Jensen ◽  
D.D. Giera ◽  
D.A. Laska ◽  
M.N. Novilla ◽  
...  
Keyword(s):  
Skeletal Muscle ◽  
Quantitative Analysis ◽  
Macrolide Antibiotic ◽  
Circle Method ◽  
Apical Surface ◽  
Polycarbonate Membrane ◽  
L6 Cells ◽  
Low Viscosity ◽  
Erythromycin A

In vitro exposure to LY237216 (9-Deoxo-11-deoxy-9,11-{imino[2-(2-methoxyethoxy)ethylidene]-oxy}-(9S)-erythromycin), a macrolide antibiotic, was found to induce cytoplasmic vacuolation in L6 skeletal muscle myoblast cultures (White, S.L., unpubl). The present study was done to determine, by autoradiographic quantitative analysis, the subcellular distribution of 3H-LY237216 in L6 cells.L6 cells (ATCC, CRL 1458) were cultured to confluency on polycarbonate membrane filters (Millipore Corp., Bedford, MA) in M-199 medium (GIBCO® Labs) with 10% fetal bovine serum. The cells were exposed from the apical surface for 1-hour to unlabelled-compound (0 μCi/ml) or 50 (μCi/ml of 3H-LY237216 at a compound concentration of 0.25 mg/ml. Following a rapid rinse in compound-free growth medium, the cells were slam-frozen against a liquid nitrogen cooled, polished copper block in a CF-100 cryofixation unit (LifeCell Corp., The Woodlands, TX). Specimens were dried in the MDD-C Molecular Distillation Drier (LifeCell Corp.), vapor osmicated and embedded in Spurrs low viscosity resin. Ultrathin sections collected on formvar coated stainless steel grids were counter-stained, then individually mounted on corks. A monolayer of Ilford L4 nuclear emulsion (Polysciences, Inc., Warrington, PA) was placed on the sections, utilizing a modified “loop method”. The emulsions were exposed for 7-weeks in a light-tight box at 4°C. Autoradiographs were developed in Microdol-X developer and examined on a Philips EM410LS transmission electron microscope. Quantitative analysis of compound localization employed the point and circle approach of Williams; incorporating the probability circle method of Salpeter and McHenry.

A Review: Effects of Macrolides on CYP450 Enzymes

2020 ◽  
Vol 21 (12) ◽  
pp. 928-937
Author(s):  
Liyun Zhang ◽  
Xiaoqing Xu ◽  
Sara Badawy ◽  
Awais Ihsan ◽  
Zhenli Liu ◽  
...  
Keyword(s):  
Drug Interactions ◽  
Prescription Drugs ◽  
Macrolide Antibiotic ◽  
Animal Origin ◽  
Macrolide Antibiotics ◽  
Cytochrome P450 Enzymes ◽  
Rational Use ◽  
Animal Origin Food ◽  
Endogenous Substances ◽  
Exogenous Substances

: As a kind of haemoglobin, cytochrome P450 enzymes (CYP450) participate in the metabolism of many substances, including endogenous substances, exogenous substances and drugs. It is estimated that 60% of common prescription drugs require bioconversion through CYP450. The influence of macrolides on CYP450 contributes to the metabolism and drug-drug interactions (DDIs) of macrolides. At present, most studies on the effects of macrolides on CYP450 are focused on CYP3A, but a few exist on other enzymes and drug combinations, such as telithromycin, which can decrease the activity of hepatic CYP1A2 and CYP3A2. This article summarizes some published applications of the influence of macrolides on CYP450 and the DDIs of macrolides caused by CYP450. And the article may subsequently guide the rational use of drugs in clinical trials. To a certain extent, poisoning caused by adverse drug interactions can be avoided. Unreasonable use of macrolide antibiotics may enable the presence of residue of macrolide antibiotics in animal-origin food. It is unhealthy for people to eat food with macrolide antibiotic residues. So it is of great significance to guarantee food safety and protect the health of consumers by the rational use of macrolides. This review gives a detailed description of the influence of macrolides on CYP450 and the DDIs of macrolides caused by CYP450. Moreover, it offers a perspective for researchers to further explore in this area.

scholarly journals The effects of the new macrolide antibiotic clarithromycin on hepatic drug- $$$metabolizing enzyme in rats

1992 ◽  
Vol 58 ◽  
pp. 331
Author(s):  
Reiji Kitashiro ◽  
Norimitsu Kurata ◽  
Shinichi Kobayashi ◽  
Yuki Nishimura ◽  
Eiji Uchida ◽  
...  
Keyword(s):  
Macrolide Antibiotic ◽  
Hepatic Drug ◽  
Drug Metabolizing Enzyme ◽  
Metabolizing Enzyme

Inhibition of tumor angiogenesis by roxithromycin, a 14-membered ring macrolide antibiotic

1998 ◽  
Vol 131 (2) ◽  
pp. 137-143 ◽  
Author(s):  
Jun Yatsunami ◽  
Nobuko Tsuruta ◽  
Nobuyuki Hara ◽  
Shin-ichiro Hayashi
Keyword(s):  
Tumor Angiogenesis ◽  
Macrolide Antibiotic ◽  
Membered Ring

scholarly journals Biosynthesis of the Novel Macrolide Antibiotic Anthracimycin

2015 ◽  
Vol 10 (11) ◽  
pp. 2468-2479 ◽  
Author(s):  
Silke Alt ◽  
Barrie Wilkinson
Keyword(s):  
Macrolide Antibiotic ◽  
The Novel

Total synthesis of the macrolide antibiotic (±)-A26771B

1980 ◽  
Vol 21 (48) ◽  
pp. 4611-4614 ◽  
Author(s):  
Morio Asaoka ◽  
Noboru Yanagida ◽  
Hisashi Takei
Keyword(s):  
Total Synthesis ◽  
Macrolide Antibiotic
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