高效液相色谱法测定枸杞种子中潜在的抗幽门螺杆菌碱的分子对接研究

A. Haddad, W. Al-Shareef, S. Eid
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引用次数: 4

摘要

背景:已知世界上近50%的居民感染幽门螺杆菌,幽门螺杆菌是导致消化性溃疡和胃癌的主要原因。由于目前使用的治疗方法存在耐药性,因此应尝试其他替代方法,如与天然产品结合使用。目的:建立高效液相色谱-紫外分光光度法定量测定枸杞种子各种提取物和粗提物中枸杞碱的含量。通过分子对接研究,比较了韭素对幽门螺杆菌的抑菌活性。方法:采用不同溶剂提取麻风碱,采用高效液相色谱-紫外分光光度法测定其含量。用琼脂扩散法和稀释法检测抗幽门螺杆菌活性。对幽门螺杆菌磷酸核糖基转移酶进行了分子对接研究。结果:正己烷提取物中麻风碱含量最高,为316.91µg mL-1;Lepidine对幽门螺杆菌临床分离株具有抗菌作用(MIC = 6.25µg mL-1)。lepidine与磷酸核糖基转移酶结合位点的氨基酸相互作用的能力可能使其观察到的活性合理化。结论:本研究首次证实了槲皮素具有抗幽门螺杆菌的活性,可作为一种可行的营养保健剂开发。需要进一步的研究,以制定合适的药物,以对抗幽门螺杆菌感染的临床理由。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Validated HPLC Determination of the Potential Anti-Helicobacter pylori, Lepidine, in Lepidium sativum Seeds Assessed by Molecular Docking Study
Background: Nearly 50 % of the world residents are known to be infected with Helicobacter pylori which is the main cause of peptic ulcer and gastric cancer. Since resistance to the currently used treatments, other alternative approaches such as combination with natural products should be tried. Objectives: In this work, validated HPLC-UV method was developed for quantification of lepidine content in various extracts and crude oil of Lepidium sativum seeds. Furthermore, antibacterial activity of lepidine against H. pylori was compared with standard antibiotics supported by molecular docking study. Methods: Different solvents were used to extract lepidine as well as the contents were determined using HPLC-UV method. Anti-Helicobacter pylori activity was examined using agar diffusion and dilution methods. Molecular docking study was done on H. pylori phosphoribosyltransferase enzyme. Results: The highest content of lepidine (316.91 µg mL-1) was found in n-hexane extract. Lepidine exhibit antibacterialeffect (MIC = 6.25 µg mL-1) against H. pylori clinical isolates. The ability of lepidine to interact with amino acids in the phosphoribosyl transferase binding site might rationalize its observed activity. Conclusion: Our results demonstrate for the first time the anti-Helicobacter pylori activity of lepidine, which could therefore be developed as viable nutraceutical agent. Further investigations are required to formulate suitable pharmaceuticals to combat with the H. pylori infections on clinical grounds.
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