New Molecular Complexes of Glycyrrhizic Acid Monoammonium Salt (Glycyram) with Fluoroquinolone Antibiotics

Q2 Pharmacology, Toxicology and Pharmaceutics
Leonid A. Yakovishin, Sergey V. Bukharov, Vasily M. Babaev, Elena V. Nikitina, Elena S. Bulatova
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引用次数: 0

Abstract

Aims: The study aimed to search of new molecular complexes of licorice saponin with fluoroquinolone antibiotics and to explore their pharmaceutical potential. Background: Molecular complexation of triterpene glycosides with pharmaceutical substances reduces side effects and therapeutic doses, increases bioavailability and stability, and expands the spectrum of biological activity of drugs. Glycyrrhizic acid is the major triterpene glycoside of licorice. Molecular complexes of monoammonium salt of glycyrrhizic acid (glycyram, GC) with fluoroquinolone antibiotics have not been described. Objectives: This study is devoted to the preparation and analysis of molecular complexes of GC with fluoroquinolones, and investigation of their antimicrobial activity. Methods: Complexation was studied via FT-IR spectroscopy, UV-Vis spectroscopy and mass spectrometry methods. Results: Molecular complexes of GC with fluoroquinolone antibiotics, along with their benzylated derivatives, were obtained for the first time. Conclusion: The complexes composition was defined as 1:1. Intermolecular hydrogen bonds are formed during complexation. In addition, stability constants of 105 М–1 order were calculated. Some complexes are comparable in antimicrobial activity with individual antibiotics ciprofloxacin (CP) and moxifloxacin (Moc) or surpass them in relation to a number of bacteria. These molecular complexes could be potential low-dose drugs with antimicrobial activity.
甘草酸单铵盐与氟喹诺酮类抗生素的新型分子配合物
目的:寻找新的甘草皂苷与氟喹诺酮类抗生素的分子配合物,探索其药用潜力。背景:三萜苷与原料药的分子络合减少了副作用和治疗剂量,提高了生物利用度和稳定性,扩大了药物的生物活性谱。甘草酸是甘草中主要的三萜苷。甘草酸单铵盐(glycyram, GC)与氟喹诺酮类抗生素的分子配合物尚未见报道。目的:研究气相色谱与氟喹诺酮类药物的分子配合物的制备和分析,并对其抗菌活性进行研究。方法:采用红外光谱、紫外-可见光谱、质谱等方法研究络合作用。结果:首次获得了GC与氟喹诺酮类抗生素及其苯基化衍生物的分子配合物。结论:配合物的组成为1:1。分子间氢键在络合过程中形成。此外,还计算了105 М-1阶的稳定常数。一些配合物的抗菌活性与单个抗生素环丙沙星(CP)和莫西沙星(Moc)相当,或在许多细菌中超过它们。这些分子复合物可能是潜在的具有抗菌活性的低剂量药物。
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来源期刊
Current Bioactive Compounds
Current Bioactive Compounds Pharmacology, Toxicology and Pharmaceutics-Pharmacology, Toxicology and Pharmaceutics (all)
CiteScore
1.90
自引率
0.00%
发文量
112
期刊介绍: The journal aims to provide comprehensive review articles on new bioactive compounds with proven activities in various biological screenings and pharmacological models with a special emphasis on stereoeselective synthesis. The aim is to provide a valuable information source of bioactive compounds synthesized or isolated, which can be used for further development of pharmaceuticals by industry and academia. The journal should prove to be essential reading for pharmacologists, natural product chemists and medicinal chemists who wish to be kept informed and up-to-date with the most important developments on new bioactive compounds of natural or synthetic origin, including their stereoeselective synthesis.
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