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L.喷雾干燥提取物的解痉、抗菌和抗氧化活性及计算机模拟药代动力学分析

Spasmolytic, Antimicrobial, and Antioxidant Activities of Spray-Dried Extracts of L. with In Silico Pharmacokinetic Analysis.

作者信息

Jovanović Miloš S, Milutinović Milica, Branković Suzana, Mihajilov-Krstev Tatjana, Randjelović Milica, Miladinović Bojana, Ćujić Nikolić Nada, Šavikin Katarina, Kitić Dušanka

机构信息

Department of Pharmacy, Faculty of Medicine, University of Niš, Boulevard Dr. Zorana Đinđića 81, 18000 Niš, Serbia.

Department of Physiology, Faculty of Medicine, University of Niš, Boulevard Dr. Zorana Đinđića 81, 18000 Niš, Serbia.

出版信息

Plants (Basel). 2024 May 23;13(11):1445. doi: 10.3390/plants13111445.

Abstract

This study aimed to evaluate the spasmolytic activity of an underground parts extract of L. (Gentianaceae), assess its antioxidant and antimicrobial activities, and explore the impact of extract encapsulation on the aforementioned bioactivities. An extract encapsulated by spray drying with whey protein, pure extract, and pure whey protein were comparatively tested. The main compounds identified via HPLC-DAD analysis underwent in silico ADME assessment. The spasmolytic effect was tested on a model of spontaneous rat ileum contractions, and the mechanism of action was further evaluated on acetylcholine-, KCl-, CaCl-, BaCl-, histamine-, N()-nitro-L-arginine methyl ester-, and glibenclamide-modified contractions. The most abundant compounds were secoiridoids (dominantly gentiopicroside), followed by -glycosylated flavonoids and xanthones. Both pure and encapsulated extracts achieved significant spasmolytic effects, despite the spasmogenic activity of pure whey protein. The extract may exert its spasmolytic effect through multiple pathways, predominantly by antagonizing the Ca channel and opening the K channel, while the nitric oxide pathway appears not to be involved. The antimicrobial and antioxidant activities of the pure extract were moderate. The extract stabilized by encapsulation retained all of the tested bioactivities of the unencapsulated extract. The obtained results suggest that has potential for use in the treatment of some gastrointestinal complaints and that the encapsulated extract could be a valuable functional ingredient in pharmaceutical and food products.

摘要

本研究旨在评估龙胆科植物地下部分提取物的解痉活性,评估其抗氧化和抗菌活性,并探讨提取物包封对上述生物活性的影响。对经喷雾干燥用乳清蛋白包封的提取物、纯提取物和纯乳清蛋白进行了对比测试。通过高效液相色谱-二极管阵列检测(HPLC-DAD)分析鉴定出的主要化合物进行了计算机辅助的药物代谢动力学(ADME)评估。在大鼠离体回肠自发收缩模型上测试解痉效果,并在乙酰胆碱、氯化钾、氯化钙、氯化钡、组胺、N-硝基-L-精氨酸甲酯和格列本脲诱导的收缩模型上进一步评估其作用机制。含量最丰富的化合物是裂环环烯醚萜类(主要是龙胆苦苷),其次是β-糖基化黄酮类和氧杂蒽酮类。尽管纯乳清蛋白有致痉活性,但纯提取物和包封提取物均产生了显著的解痉效果。该提取物可能通过多种途径发挥其解痉作用,主要是通过拮抗钙通道和开放钾通道,而一氧化氮途径似乎未参与其中。纯提取物的抗菌和抗氧化活性中等。通过包封稳定的提取物保留了未包封提取物的所有测试生物活性。所得结果表明,该植物在治疗某些胃肠道疾病方面具有应用潜力,且包封提取物可能是制药和食品产品中有价值的功能性成分。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9270/11174654/386fbadd537f/plants-13-01445-g001.jpg

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