PDF(Pubmed)
Abstract：
Black locust flower extract contains various polyphenols and their glucosides contribute to the potential health benefits. After intake of these bioactive compounds and passage through the gastrointestinal tract, their degradation can occur and lead to a loss of biological activity. To overcome this problem, the bioactive compounds should be protected from environmental conditions. This study aimed to encapsulate the black flower extract in the microparticles based on biodegradable polysaccharides, alginate, and chitosan. In the extract, the total antioxidant content was found to be 3.18 ± 0.01 g gallic acid equivalent per 100 g of dry weight. Also, the presence of lipids (16), phenolics (27), organic acids (4), L-aspartic acid derivative, questinol, gibberellic acid, sterol, and saponins (2) was confirmed using the UHPLC-ESI-MS analysis. In vitro assays showed that the extract has weak anti-α-glucosidase activity and moderate antioxidant and cytotoxic activity against the HeLa cell line. The extrusion method with secondary air flow enabled the preparation of microparticles (about 270 μm) encapsulated with extract. An encapsulation efficiency of over 92% was achieved in the alginate and alginate-chitosan microparticles. The swelling study confirmed a lower permeability of alginate-chitosan microparticles compared with alginate microparticles. For both types of microparticles, the release profile of antioxidants in the simulated gastrointestinal fluids at 37 °C followed the Korsmeyer-Peppas model. A lower diffusion coefficient than 0.5 indicated the simple Fick diffusion of antioxidants. The alginate-chitosan microparticles enabled a more sustained release of antioxidants from extract compared to the alginate microparticles. The obtained results indicated an improvement in the antioxidant activity of bioactive compounds from the extract and their protection from degradation in the simulated gastric conditions via encapsulation in the polymer matrixes. Alginate-chitosan showed slightly slower cumulative antioxidant release from microparticles and better antioxidant activity of the extract compared to the alginate system. According to these results, alginate-chitosan microparticles are more suitable for further application in the encapsulation of black locust flower extract. Also, the proposed polymer matrix as a drug delivery system is safe for human use due to its biodegradability and non-toxicity.
摘要：
刺槐花提取物含有各种多酚，它们的葡糖苷有助于潜在的健康益处。摄入这些生物活性化合物并通过胃肠道后，它们的降解可能发生并导致生物活性的丧失。为了克服这个问题，生物活性化合物应该被保护免受环境条件的影响。本研究旨在将黑花提取物封装在基于可生物降解多糖的微粒中，海藻酸盐,和壳聚糖。在摘录中，发现总抗氧化剂含量为每100克干重3.18±0.01克没食子酸当量。此外，脂质的存在（16），酚类物质（27），有机酸(4)，L-天冬氨酸衍生物,Questinol,赤霉素,甾醇,和皂苷(2)使用UHPLC-ESI-MS分析确认。体外实验表明，该提取物对HeLa细胞系具有弱的抗α-葡萄糖苷酶活性和中等的抗氧化和细胞毒活性。使用二次气流的挤出方法能够制备用提取物包封的微粒(约270μm)。在藻酸盐和藻酸盐-壳聚糖微粒中实现了超过92%的包封效率。溶胀研究证实,与藻酸盐微粒相比,藻酸盐-壳聚糖微粒的渗透性较低。对于这两种类型的微粒，在37°C下模拟胃肠液中抗氧化剂的释放曲线遵循Korsmeyer-Peppas模型。低于0.5的扩散系数表明抗氧化剂的简单Fick扩散。与藻酸盐微粒相比,藻酸盐-壳聚糖微粒能够更持续地从提取物释放抗氧化剂。获得的结果表明，通过包封在聚合物基质中，提取物中的生物活性化合物的抗氧化活性得到了改善，并且在模拟的胃条件下保护它们免受降解。与藻酸盐系统相比，藻酸盐-壳聚糖显示出从微粒中累积抗氧化剂释放的速度稍慢，并且提取物的抗氧化活性更好。根据这些结果,海藻酸盐-壳聚糖微粒更适合进一步应用于刺槐花提取物的包封。此外，所提出的作为药物递送系统的聚合物基质由于其可生物降解性和无毒性而对人类使用是安全的。
