龙胆草喷雾干燥提取物的解痉、抗菌和抗氧化活性及硅学药代动力学分析

Plants Pub Date : 2024-05-23 DOI:10.3390/plants13111445
M. Jovanović, Milica Milutinović, Suzana Branković, Tatjana Mihajilov-Krstev, Milica Randjelović, Bojana Miladinović, Nada Ćujić Nikolić, Katarina Šavikin, Dušanka Kitić
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引用次数: 0

摘要

本研究旨在评价龙胆科植物龙胆(Gentiana asclepiadea L.)地下部分提取物的解痉活性,评估其抗氧化和抗菌活性,并探讨提取物封装对上述生物活性的影响。比较测试了通过喷雾干燥与乳清蛋白封装的提取物、纯提取物和纯乳清蛋白。对通过 HPLC-DAD 分析确定的主要化合物进行了默克 ADME 评估。在大鼠回肠自发收缩模型上测试了其解痉作用,并在乙酰胆碱、KCl、CaCl2-、BaCl2-、组胺、N(ω)-硝基-L-精氨酸甲酯和格列本脲修饰收缩模型上进一步评估了其作用机制。最丰富的化合物是仲呋喃类化合物(主要是龙胆内酯),其次是 C-糖基化黄酮类化合物和黄酮类化合物。尽管纯乳清蛋白具有致痉挛活性,但纯提取物和封装提取物都具有显著的解痉作用。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 Ca2+ 通道和打开 K+ 通道,而一氧化氮途径似乎没有参与其中。纯提取物的抗菌和抗氧化活性适中。通过封装稳定的提取物保留了未封装提取物的所有测试生物活性。研究结果表明,G. asclepiadea 具有治疗某些胃肠道疾病的潜力,封装提取物可以成为药品和食品中的重要功能成分。
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Spasmolytic, Antimicrobial, and Antioxidant Activities of Spray-Dried Extracts of Gentiana asclepiadea L. with In Silico Pharmacokinetic Analysis
This study aimed to evaluate the spasmolytic activity of an underground parts extract of Gentiana asclepiadea 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-, CaCl2-, BaCl2-, histamine-, N(ω)-nitro-L-arginine methyl ester-, and glibenclamide-modified contractions. The most abundant compounds were secoiridoids (dominantly gentiopicroside), followed by C-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 Ca2+ 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 G. asclepiadea 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.
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