Method for obtaining supramolecular complex based on 3-ohypyridine derivatives and its application for correction of osteoporosis

Q3 Pharmacology, Toxicology and Pharmaceutics
K. S. Trunov
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Abstract

Introduction: Currently, there are no safe and ideal medicines for the prevention and treatment of oophorectomy-induced osteoporosis. The development of an effective pharmacotherapy for hypoestrogen-induced osteoporosis is an important task of pharmacology. Materials and Methods: A new supramolecular complex (composition №1) was obtained on the basis of 3-hydroxypyridine derivatives: 2-ethyl-6-methyl-3-hydroxypyridinium 3-pyridinocarbonoate and 2-ethyl-6-methyl-3-hydroxypyridinium N-acetyl-6-aminohexanoate in a ratio of 1:3 by topochemical synthesis. The study of the osteoprotective activity of the supramolecular complex at a dose of 50 mg/kg was performed on 60 white female rats of the Wistar line on a model of hypoestrogen-induced osteoporosis. The effectiveness of the osteoprotective activity of the complex was evaluated on the 57th day of the experiment. Results and Discussion: The new supramolecular complex (composition №1) has osteoprotective activity, which is expressed in improving the indicators of X-ray and histomorphological samples. Oral administration of composition №1 at a dose of 50 mg/kg led to an increase in bone density to values of 2.55±0.02 g/cm3, which is 1.3 times higher than in the control group 1.92±0.01 g/cm3 (p≤0.05) and reduce bone resorption by improving cortical and trabecular bone structures. Conclusion: The obtained data characterize the prospects of studying composition №1 for the correction and prevention of hypoestrogen-induced osteoporosis. Graphical Abstract
基于3-羟基苯胺衍生物的超分子络合物的制备方法及其在骨质疏松症中的应用
导读:目前,还没有安全、理想的预防和治疗卵巢切除术所致骨质疏松症的药物。开发一种有效的药物治疗低雌激素性骨质疏松症是药理学的一项重要任务。材料与方法:以3-羟吡啶衍生物2-乙基-6-甲基-3-羟吡啶-3-吡啶碳酸酯和2-乙基-6-甲基-3-羟吡啶- n -乙酰-6-氨基己酸酯为原料,以1:3的拓扑化学比例合成了一种新的超分子配合物(组合物№1)。采用低雌激素致骨质疏松症Wistar系白种雌性大鼠60只,研究了50 mg/kg剂量下该超分子复合物的骨保护活性。在实验第57天评估复合物的骨保护活性的有效性。结果与讨论:新型超分子复合物(组合物№1)具有骨保护活性,其表现为改善x射线和组织形态学样品的指标。口服剂量为50 mg/kg的组合物№1导致骨密度增加至2.55±0.02 g/cm3,比对照组(1.92±0.01 g/cm3)高1.3倍(p≤0.05),并通过改善骨皮质和骨小梁结构减少骨吸收。结论:所获得的数据表征了研究组合物№1用于纠正和预防低雌激素性骨质疏松症的前景。图形抽象
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来源期刊
Research Results in Pharmacology
Research Results in Pharmacology Medicine-Pharmacology (medical)
CiteScore
1.50
自引率
0.00%
发文量
32
审稿时长
12 weeks
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