Institute of Pharmaceutical Sciences, Pharmacognosy, University of Graz, Graz, Austria.
Department of Laboratory Diagnostics and Clinical Immunology of Developmental Age, Medical University of Warsaw, Warsaw, Poland.
Pharm Biol. 2024 Dec;62(1):563-576. doi: 10.1080/13880209.2024.2374801. Epub 2024 Jul 17.
Virtually all parts of L. (Salvadoraceae) are used in traditional medicine. The twigs and leaves are used for oral health, but leaves are far less investigated.
This study assesses the oral health-promoting potential of leaves with emphasis on anti-inflammatory and antiproliferative effects and provides an in depth-characterization of their metabolite profile.
Hot-water and methanolic leaf extracts (1, 10, and 100 µg/mL) and their major constituents (5, 10, and 50 µM), were subjected to cellular assays on IL-8 and TNFα release in LPS-stimulated human neutrophils, NO-release in LPS/IFNγ stimulated mouse macrophages, and proliferation of HNO97 human tongue carcinoma cells. Metabolite profiling was performed by UHPLC-HRMS analysis. Major constituents were isolated and structurally elucidated.
Both extracts showed pronounced anti-inflammatory activity in LPS-stimulated neutrophils. Major identified compound classes were flavonoid glycosides, the glucosinolate glucotropaeolin, phenyl- and benzylglycoside sulfates, and megastigmane glycosylsulfates, the latter ones identified for the first time in . Glucotropaeolin strongly inhibited the release of IL-8 and TNF-α (13.3 ± 2.0 and 22.7 ± 2.6% of the release of stimulated control cells at 50 µM), while some flavonoids and 3-(3'--sulfo-β-d-glucopyranosyloxy)-7,8-dihydro-β-ionone, a newly isolated megastigmane glycosylsulfate, were moderately active. Benzylisothiocyanate, which is likely formed from glucotropaeolin during traditional application of showed considerable antiproliferative activity (IC in HNO97 cells: 10.19 ± 0.72 µM) besides strongly inhibiting IL-8 and TNFα release.
Glucotropaeolin and benzylisothiocyanate are likely implicated in the oral health-promoting effects of leaves. The chemistry and pharmacology of the newly identified megastigmane glycosylsulfates should be further evaluated.
几乎所有的 L.（Salvadoraceae）部分都被用于传统医学。嫩枝和叶子被用于口腔健康，但叶子的研究要少得多。
本研究评估了 叶子的口腔保健潜力，重点是抗炎和抗增殖作用，并对其代谢物谱进行了深入表征。
热水和甲醇 叶提取物（1、10 和 100μg/mL）及其主要成分（5、10 和 50μM），在 LPS 刺激的人中性粒细胞中进行细胞试验，检测 IL-8 和 TNFα的释放、LPS/IFNγ 刺激的小鼠巨噬细胞中 NO 的释放以及 HNO97 人舌癌细胞的增殖。通过 UHPLC-HRMS 分析进行代谢物谱分析。主要成分被分离并结构阐明。
两种提取物在 LPS 刺激的中性粒细胞中均表现出明显的抗炎活性。鉴定出的主要化合物类为类黄酮糖苷、硫代葡萄糖苷葡萄糖硫苷、苯和苄基糖苷硫酸盐以及megastigmane 糖苷硫酸盐，后者首次在 中被发现。葡萄糖硫苷强烈抑制 IL-8 和 TNF-α的释放（在 50μM 时，分别为刺激对照细胞释放的 13.3±2.0%和 22.7±2.6%），而一些类黄酮和 3-（3'--磺基-β-d-吡喃葡萄糖苷氧基）-7,8-二氢-β-紫罗兰酮，一种新分离的 megastigmane 糖苷硫酸盐，具有中等活性。苯异硫氰酸酯，很可能是在 的传统应用中从葡萄糖硫苷形成的，表现出相当的抗增殖活性（在 HNO97 细胞中的 IC：10.19±0.72μM），除了强烈抑制 IL-8 和 TNFα的释放。
葡萄糖硫苷和苯异硫氰酸酯可能与 叶子的口腔保健作用有关。新鉴定的 megastigmane 糖苷硫酸盐的化学和药理学应进一步评估。
